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BioAssay: AID 504934

Late stage assay provider results from the probe development effort to identify inverse agonists of the liver receptor homolog-1 (LRH-1; NR5A2): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors

Name: Late stage assay provider results from the probe development effort to identify inverse agonists of the liver receptor homolog-1 (LRH-1; NR5A2): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Probe(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Probe(1)
 
 
Active(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 504934
Data Source: The Scripps Research Institute Molecular Screening Center (NUCLEAR-RECEPTOR_MOD_LUMI_0384_1XFOLDCHANGE Round 0 LRH1 IAG)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
Deposit Date: 2011-07-08
Hold-until Date: 2012-07-06
Modify Date: 2012-07-11

Data Table ( Complete ):           Probe    Active    All
BioActive Compound: Chemical Probe: 1    Active: 1
Depositor Specified Assays
AIDNameTypeComment
485348Center Based Initiative to identify novel inverse agonists of the liver receptor homolog-1 (LRH-1; NR5A2): Luminescence-based primary assay to identify LRH1 inhibitors (3X%INH)otherPrimary screen (LRH1 inhibitors in triplicate)
488769Center Based Initiative to identify novel inverse agonists of the liver receptor homolog-1 (LRH-1; NR5A2): fluorescence-based cell-based quantitative PCR assay to identify inhibitors of LRH-1 target gene expressionotherScreen (LRH1 target gene expression inhibitors in triplicate)
488775Center Based Initiative to identify novel inverse agonists of the liver receptor homolog-1 (LRH1; NR5A2): Luminescence-based counterscreen assay to identify inhibitors of the human herpes virus VP16 transcriptional activator protein (VP16)otherCounterscreen (VP16 inhibitors in triplicate)
488779Center Based Initiative to identify novel inverse agonists of the liver receptor homolog-1 (LRH1; NR5A2): Luminescence-based counterscreen assay to identify SF-1 inhibitorsotherCounterscreen (SF-1 inhibitors in triplicate)
488780Center Based Initiative to identify novel inverse agonists of the liver receptor homolog-1 (LRH1; NR5A2): Luminescence-based dose response counterscreen assay to identify SF1 inhibitorsconfirmatoryDose response counterscreen (SF-1 inhibitors in triplicate)
488781Summary of the probe development efforts to identify novel inverse agonists of the liver receptor homolog-1 (LRH1; NR5A2)summarySummary (LRH1 inverse agonists)
488782Center Based Initiative to identify novel inverse agonists of the liver receptor homolog-1 (LRH1; NR5A2): Luminescence-based dose response assay to identify LRH1 inhibitors (Cyp19 aromatase-luciferase reporter)confirmatoryDose response (LRH1 inhibitors in triplicate)
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRISMC)
Center Affiliation: The Scripps Research Institute, TSRI
Assay Provider: Patrick Griffin, TSRI
Network: Molecular Library Probe Production Center Network (MLPCN)
Grant Proposal Number: U54 MH084512
Grant Proposal PI: Patrick Griffin, TSRI
External Assay ID: NUCLEAR-RECEPTOR_MOD_LUMI_0384_1XFOLDCHANGE Round 0 LRH1 IAG

Name: Late stage assay provider results from the probe development effort to identify inverse agonists of the liver receptor homolog-1 (LRH-1; NR5A2): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors.

Description:

NR5A2 or Liver receptor homologue-1 (LRH-1) is a member of the NR5A, or Ftz-F1, subfamily V nuclear receptors for which there are four members (1). Murine LRH-1 was originally identified due to its sequence homology to the Drosophila Fushi tarazu factor-1 but orthologs have been subsequently identified in several other species including rat, chicken, horse, zebrafish and human (2-7). LRH-1, and its closest family member steroidogenic factor-1 (SF-1, NR5A1), bind to identical DNA consensus sequences (response elements or REs) and both have the ability to bind phospholipids in their ligand binding domains (LBDs) (8-10). However, LRH-1 and SF-1 are expressed in different tissues and thus are considered likely to have non-overlapping, non-redundant functions. SF-1 expression is confined to steroidogenic tissues and adrenals where it regulates development, differentiation, steroidogenesis and sexual determination (5, 7, 11]). LRH-1 is highly expressed in tissues of endodermal origin and its expression is essential for normal liver, intestine, and pancreas function. LRH-1 has also been shown to be expressed in the ovary and adipose tissue (12).

In a very recent report, Chand and colleagues investigated the mechanism of action of LRH-1 in invasive breast cancer cells. They found that LRH-1 promotes motility and cell invasiveness in both ER-positive (MCF-7) and ER-negative (MDA-MB-231) breast cancer cells and similar effects were observed in non-tumorigenic mammary epithelial cells. Interestingly, both remodeling of the actin cytoskeleton and E-cadherin processing were observed when LRH-1 was over-expressed. These findings implicate LRH-1 in promotion of migration and invasion in breast cancer independent of estrogen sensitivity. Together these findings provided strong evidence that LRH-1 plays a significant role in tumor formation both in vitro and in vivo. Therefore, the identification of potent and selective LRH-1 inverse agonists may provide new approaches for the treatment of cancer.

References:

1. Fayard, E., J. Auwerx, and K. Schoonjans, LRH-1: an orphan nuclear receptor involved in development, metabolism and steroidogenesis. Trends in Cell Biology, 2004. 14(5): p. 250-260.
2. Galarneau, L., J.F. Pare, D. Allard, D. Hamel, L. Levesque, J.D. Tugwood, S. Green, and L. Belanger, The alpha1-fetoprotein locus is activated by a nuclear receptor of the Drosophila FTZ-F1 family. Mol Cell Biol, 1996. 16(7): p. 3853-65.
3. Kudo, T. and S. Sutou, Molecular cloning of chicken FTZ-F1-related orphan receptors. Gene, 1997. 197(1-2): p. 261-8.
4. Boerboom, D., N. Pilon, R. Behdjani, D.W. Silversides, and J. Sirois, Expression and regulation of transcripts encoding two members of the NR5A nuclear receptor subfamily of orphan nuclear receptors, steroidogenic factor-1 and NR5A2, in equine ovarian cells during the ovulatory process. Endocrinology, 2000. 141(12): p. 4647-56.
5. Broadus, J., J.R. McCabe, B. Endrizzi, C.S. Thummel, and C.T. Woodard, The Drosophila beta FTZ-F1 orphan nuclear receptor provides competence for stage-specific responses to the steroid hormone ecdysone. Mol Cell, 1999. 3(2): p. 143-9.
6. Ellinger-Ziegelbauer, H., A.K. Hihi, V. Laudet, H. Keller, W. Wahli, and C. Dreyer, FTZ-F1-related orphan receptors in Xenopus laevis: transcriptional regulators differentially expressed during early embryogenesis. Mol Cell Biol, 1994. 14(4): p. 2786-97.
7. Lavorgna, G., H. Ueda, J. Clos, and C. Wu, FTZ-F1, a steroid hormone receptor-like protein implicated in the activation of fushi tarazu. Science, 1991. 252(5007): p. 848-51.
8. Li, Y., M. Choi, G. Cavey, J. Daugherty, K. Suino, A. Kovach, N.C. Bingham, S.A. Kliewer, and H.E. Xu, Crystallographic identification and functional characterization of phospholipids as ligands for the orphan nuclear receptor steroidogenic factor-1. Mol Cell, 2005. 17(4): p. 491-502.
9. Solomon, I.H., J.M. Hager, R. Safi, D.P. McDonnell, M.R. Redinbo, and E.A. Ortlund, Crystal structure of the human LRH-1 DBD-DNA complex reveals Ftz-F1 domain positioning is required for receptor activity. J Mol Biol, 2005. 354(5): p. 1091-102.
10. Krylova, I.N., E.P. Sablin, J. Moore, R.X. Xu, G.M. Waitt, J.A. MacKay, D. Juzumiene, J.M. Bynum, K. Madauss, V. Montana, L. Lebedeva, M. Suzawa, J.D. Williams, S.P. Williams, R.K. Guy, J.W. Thornton, R.J. Fletterick, T.M. Willson, and H.A. Ingraham, Structural Analyses Reveal Phosphatidyl Inositols as Ligands for the NR5 Orphan Receptors SF-1 and LRH-1. Cell, 2005. 120(3): p. 343-355.
11. Luo, X., Y. Ikeda, and K.L. Parker, A cell-specific nuclear receptor is essential for adrenal and gonadal development and sexual differentiation. Cell, 1994. 77(4): p. 481-90.
12. Clyne CD, Speed CJ, Zhou J, Simpson ER, Liver receptor homologue-1 (LRH-1) regulates expression of aromatase in preadipocytes. J Biol Chem. 2002 Jun 7;277(23):20591-7. Epub 2002 Apr 1.
13. Kumar N, Solt LA, Conkright JJ, Wang Y, Istrate MA, Busby SA, Garcia-Ordonez R, Burris TP, Griffin PR. The benzenesulfoamide T0901317 is a novel RORalpha/gamma Inverse Agonist. Mol Pharm. 2010 Feb;77(2):228-36.

Keywords:

Late stage, late stage AID, assay provider, purchased, synthesized, counterscreen, Nuclear receptor, NR, profiling, ML180, ML179, absorbance, cytotoxicity, viability, survival, growth, proliferation, spectrophotometer, duplicate, dose response, titration, IC50, CC50, nuclear receptor, library, liver receptor homolog 1; liver receptor homolog-1; nuclear receptor NR5A2; nuclear receptor subfamily 5 group A member 2, LRH1, liver, inhibitor, inverse agonist, IAG, transcriptional assay, assay provider, center based initiative, center-based, luciferase, luminescence, selective, Scripps Florida, The Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN.
Panel Information
Receptors
    Data Table(Active)    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1LXRa1oxysterols receptor LXR-alpha isoform c [Homo sapiens] [gi:194294519]
Taxonomy id: 9606
Gene id: 10062
2LXRb1oxysterols receptor LXR-beta [Homo sapiens] [gi:85362735]
Taxonomy id: 9606
Gene id: 7376
3FXR1unnamed protein product [Homo sapiens] [gi:221041442]
Taxonomy id: 9606
Gene id: 9971
4RORa1nuclear receptor ROR-alpha isoform c [Homo sapiens] [gi:4506577]
Taxonomy id: 9606
Gene id: 6095
5RORb1nuclear receptor ROR-beta [Homo sapiens] [gi:19743907]
Taxonomy id: 9606
Gene id: 6096
6RORg1nuclear receptor ROR-gamma isoform b [Homo sapiens] [gi:48255918]
Taxonomy id: 9606
Gene id: 6097
7PPARa1peroxisome proliferator-activated receptor alpha [Homo sapiens] [gi:50348666]
Taxonomy id: 9606
Gene id: 5465
8PPARd1peroxisome proliferator-activated receptor delta isoform 2 [Homo sapiens] [gi:29171750]
Taxonomy id: 9606
Gene id: 5467
9PPARg1peroxisome proliferator-activated receptor gamma isoform 1 [Homo sapiens] [gi:116284368]
Taxonomy id: 9606
Gene id: 5468
10Rev-erb a1nuclear receptor subfamily 1 group D member 1 [Homo sapiens] [gi:13430848]
Taxonomy id: 9606
Gene id: 9572
11Rev-erb b1nuclear receptor subfamily 1 group D member 2 isoform 1 [Homo sapiens] [gi:224177491]
Taxonomy id: 9606
Gene id: 9975
12LRH11nuclear receptor subfamily 5 group A member 2 isoform 2 [Homo sapiens] [gi:4504343]
Taxonomy id: 9606
Gene id: 2494
13SF11steroidogenic factor 1 [Homo sapiens] [gi:20070193]
Taxonomy id: 9606
Gene id: 2516
14AR1AR protein [Homo sapiens] [gi:124375976]
Taxonomy id: 9606
Gene id: 367
15CAR1nuclear receptor subfamily 1 group I member 3 isoform 12 [Homo sapiens] [gi:117938738]
Taxonomy id: 9606
Gene id: 9970
16ESR1 (ESRA; Era)1estrogen receptor isoform 1 [Homo sapiens] [gi:62821794]
Taxonomy id: 9606
Gene id: 2099
17Erb (ESR2)1estrogen receptor beta isoform 2 [Homo sapiens] [gi:94538325]
Taxonomy id: 9606
Gene id: 2100
18ERRa1steroid hormone receptor ERR1 [Homo sapiens] [gi:18860920]
Taxonomy id: 9606
Gene id: 2101
19ERRb1steroid hormone receptor ERR2 [Homo sapiens] [gi:238550159]
Taxonomy id: 9606
Gene id: 2103
20ERRg1estrogen-related receptor gamma isoform 2 [Homo sapiens] [gi:197209821]
Taxonomy id: 9606
Gene id: 2104
21GCCR1glucocorticoid receptor isoform gamma [Homo sapiens] [gi:66528677]
Taxonomy id: 9606
Gene id: 2908
22MR1mineralocorticoid receptor isoform 2 [Homo sapiens] [gi:260656020]
Taxonomy id: 9606
Gene id: 4306
23PGR1progesterone receptor isoform B [Homo sapiens] [gi:110611914]
Taxonomy id: 9606
Gene id: 5241
24PXR1nuclear receptor subfamily 1 group I member 2 isoform 1 [Homo sapiens] [gi:34398348]
Taxonomy id: 9606
Gene id: 8856
25VDR1vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:4507883]
Taxonomy id: 9606
Gene id: 7421
26Coup-TF11COUP transcription factor 1 [Homo sapiens] [gi:5032173]
Taxonomy id: 9606
Gene id: 7025
27Coup-TF21COUP transcription factor 2 isoform b [Homo sapiens] [gi:223555949]
Taxonomy id: 9606
Gene id: 7026
28DAX1nuclear receptor subfamily 0 group B member 1 [Homo sapiens] [gi:5016090]
Taxonomy id: 9606
Gene id: 190
29HNF4a1hepatocyte nuclear factor 4-alpha isoform e [Homo sapiens] [gi:71725341]
Taxonomy id: 9606
Gene id: 3172
30HNF4g1hepatocyte nuclear factor 4-gamma [Homo sapiens] [gi:115583654]
Taxonomy id: 9606
Gene id: 3174
31PNR1photoreceptor-specific nuclear receptor isoform b [Homo sapiens] [gi:7657395]
Taxonomy id: 9606
Gene id: 10002
32SHP1nuclear receptor subfamily 0 group B member 2 [Homo sapiens] [gi:13259503]
Taxonomy id: 9606
Gene id: 8431
33TLX1nuclear receptor subfamily 2 group E member 1 [Homo sapiens] [gi:4507537]
Taxonomy id: 9606
Gene id: 7101
34TR21nuclear receptor subfamily 2 group C member 1 isoform c [Homo sapiens] [gi:189491766]
Taxonomy id: 9606
Gene id: 7181
35TR41nuclear receptor subfamily 2 group C member 2 [Homo sapiens] [gi:36950991]
Taxonomy id: 9606
Gene id: 7182
36GCNR1nuclear receptor subfamily 6, group A, member 1 [Homo sapiens] [gi:55859655]
Taxonomy id: 9606
Gene id: 2649
37Nur771nuclear receptor subfamily 4 group A member 1 isoform 1 [Homo sapiens] [gi:21361342]
Taxonomy id: 9606
Gene id: 3164
38Nurr11nuclear receptor subfamily 4 group A member 2 [Homo sapiens] [gi:5453822]
Taxonomy id: 9606
Gene id: 4929
39NOR11nuclear receptor subfamily 4 group A member 3 isoform a [Homo sapiens] [gi:27894357]
Taxonomy id: 9606
Gene id: 8013
40RARa1retinoic acid receptor alpha isoform 1 [Homo sapiens] [gi:4506419]
Taxonomy id: 9606
Gene id: 5914
41RARb1retinoic acid receptor beta isoform 1 [Homo sapiens] [gi:14916494]
Taxonomy id: 9606
Gene id: 5915
42RARg1retinoic acid receptor gamma isoform 1 [Homo sapiens] [gi:4506423]
Taxonomy id: 9606
Gene id: 5916
43RXRa1retinoic acid receptor RXR-alpha [Homo sapiens] [gi:4506755]
Taxonomy id: 9606
Gene id: 6256
44RXRb1retinoic acid receptor RXR-alpha [Homo sapiens] [gi:4506755]
Taxonomy id: 9606
Gene id: 6256
45RXRg1retinoic acid receptor RXR-gamma isoform b [Homo sapiens] [gi:58331207]
Taxonomy id: 9606
Gene id: 6258
46THRa1thyroid hormone receptor alpha isoform 1 [Homo sapiens] [gi:40806160]
Taxonomy id: 9606
Gene id: 7067
47THRb1thyroid hormone receptor beta [Homo sapiens] [gi:40806162]
Taxonomy id: 9606
Gene id: 7068
48EAR-2 (COUP-TF3)1nuclear receptor subfamily 2, group F, member 6 [Homo sapiens] [gi:216409732]
Taxonomy id: 9606
Gene id: 2063
49pBIND-11
50VP16 Control Plasmid1transactivating tegument protein VP16 [Human herpesvirus 1] [gi:9629429]
Taxonomy id: 10298
Gene id: 2703416

§ Panel component ID.
Protocol
Assay Overview:

The purpose of this assay is to identify compounds that act as modulators of human nuclear receptors and to demonstrate the utility of the GAL4 nuclear receptor library (13). This assay screens endogenous and synthetic ligands against a GAL4 nuclear receptor library which was built by replacing the endogenous N-terminus and DNA-binding domain (DBD) of all 48 receptors with a GAL4 DBD. The fusion constructs consist of the GAL4 DBD, the hinge domain, ligand binding domain (LBD), and F domain if applicable, of the human receptors. Plasmids coding for full-length receptors were also included for some receptors. In this assay HEK293T cells are co-transfected with a single GAL4 receptor and a luciferase reporter containing an upstream activating sequence (UAS) recognized by the GAL4 DBD, followed by treatment with test compounds. As designed, compounds that modulate activity of a particular nuclear receptor will modulate the binding of the GAL4 DBD to the UAS, thereby modulating luciferase production, resulting in an increase or decrease in well luminescence. Compounds are tested in triplicate at a nominal test concentration of 2 uM.

Protocol Summary:

The nuclear receptor library was plated into 384-well plates. HEK293T cells were reverse transfected with the well-specific construct and the UAS luciferase reporter pGL4.31 using Fugene6 transfection reagent in a final volume of 40 uL. Control wells containing constructs encoding for the GAL4 DBD alone (pBind) or GAL4 fused to VP16 were also analyzed. After 24 hours, optimized compounds (2 uM final concentration) or DMSO was added to the plates and allowed to incubate for 20 hours. Next, 40 uL of BriteLite was added to all wells and luciferase activity was measured on the PerkinElmer Envision 2104. Compounds that attenuate the GAL4-VP16-dependent luciferase activity are considered promiscuous or cytotoxic. To correct for plate-to-plate variance, sample data was normalized to wells containing vector only (69 wells) to determine Normalized Data Values (NDV). For each nuclear receptor, the average of NDV treated with a particular test compound was divided by the average NDV of wells treated with DMSO. This resulted in a fold-activation or fold-inhibition value for each receptor-compound pair. Because the activity of VP16 should not be impacted by these compounds and a change in this value is indicative of cell toxicity or general disruptions in transcription/translation, this fold-change value was then normalized to the VP16 fold-change. Compounds that induced in any receptor an average fold change that was three standard deviations from the VP16 value were considered active for that particular receptor.

The maximal response (inhibition) for each replicate well of each compound was calculated as follows:

Maximal_Response = Cells_treated_with_Test_Compound / Cells_treated_with_Vehicle_(DMSO)

PubChem Activity Outcome and Score:

For selected test compounds, fold inhibition was plotted against compound concentration. The fold change values were calculated from GraphPad Prism software. Compounds with an average fold change within 20% of 1.0 (reported value less than 1.20 or greater than 0.80 were considered inactive. Compounds with an average fold change value over 20% from 1.0 (reported value greater than or equal to 1.20 or less than or equal to 0.80) were considered active.

Active compounds were given a score of 100 and inactive compounds were given a score of 0.

LXRa Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

LXRb Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

FXR Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

RORa Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

RORb Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

RORg Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

PPARa Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

PPARd Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

PPARg Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

Rev-erb a Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

Rev-erb b Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

LRH1 Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

SF1 Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

AR Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

CAR Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

ESR1 (ESRA; Era) Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

Erb (ESR2) Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

ERRa Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

ERRb Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

ERRg Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

GCCR Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

MR Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

PGR Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

PXR Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

VDR Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

Coup-TF1 Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

Coup-TF2 Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

DAX Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

HNF4a Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

HNF4g Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

PNR Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

SHP Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

TLX Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

TR2 Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

TR4 Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

GCNR Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

Nur77 Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

Nurr1 Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

NOR1 Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

RARa Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

RARb Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

RARg Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

RXRa Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

RXRb Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

RXRg Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

THRa Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

THRb Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

EAR-2 (COUP-TF3) Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

pBIND-1 Score: The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

VP16 Control Plasmid: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

Overall Outcome and Score:

Probe compounds were given a score of 100, actives a score of 50 and inactives a score of 0.

The PubChem Activity Score range for active compounds is 100-100. There were no inactive compounds.

List of Reagents:

Fugene6 transfection reagent (Roche Applied Sciences)
BriteLite reagent (Perkin Elmer)
pGL4.31 construct (Promega)
384-well plates (Greiner, part 789176)
Comment
This assay was performed by the assay provider. This assay may have been run as two or more separate campaigns, each campaign testing a unique set of compounds. In this case the results of each separate campaign were assigned "Active/Inactive" status based upon that campaign's specific compound activity cutoff value. All data reported were normalized on a per-plate basis. Possible artifacts of this assay can include, but are not limited to: dust or lint located in or on wells of the microtiter plate, or compounds that modulate well luminescence. All test compound concentrations reported above and below are nominal; the specific test concentration(s) for a particular compound may vary based upon the actual sample provided.
Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1Outcome [LXRa]The BioAssay activity outcome1oxysterols receptor LXR-alpha isoform c [Homo sapiens]Outcome
2Score [LXRa]The BioAssay activity ranking score1Integer
3Fold Change [1] [LXRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.1Floatratio
4Fold Change [2] [LXRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.1Floatratio
5Fold Change [3] [LXRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.1Floatratio
6Average Fold Change [LXRa] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.1Floatratio
7Standard Deviation [LXRa]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.1Float
8Outcome [LXRb]The BioAssay activity outcome2oxysterols receptor LXR-beta [Homo sapiens]Outcome
9Score [LXRb]The BioAssay activity ranking score2Integer
10Fold Change [1] [LXRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.2Floatratio
11Fold Change [2] [LXRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.2Floatratio
12Fold Change [3] [LXRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.2Floatratio
13Average Fold Change [LXRb] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.2Floatratio
14Standard Deviation [LXRb]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.2Float
15Outcome [FXR]The BioAssay activity outcome3unnamed protein product [Homo sapiens]Outcome
16Score [FXR]The BioAssay activity ranking score3Integer
17Fold Change [1] [FXR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.3Floatratio
18Fold Change [2] [FXR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.3Floatratio
19Fold Change [3] [FXR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.3Floatratio
20Average Fold Change [FXR] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.3Floatratio
21Standard Deviation [FXR]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.3Float
22Outcome [RORa]The BioAssay activity outcome4nuclear receptor ROR-alpha isoform c [Homo sapiens]Outcome
23Score [RORa]The BioAssay activity ranking score4Integer
24Fold Change [1] [RORa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.4Floatratio
25Fold Change [2] [RORa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.4Floatratio
26Fold Change [3] [RORa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.4Floatratio
27Average Fold Change [RORa] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.4Floatratio
28Standard Deviation [RORa]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.4Float
29Outcome [RORb]The BioAssay activity outcome5nuclear receptor ROR-beta [Homo sapiens]Outcome
30Score [RORb]The BioAssay activity ranking score5Integer
31Fold Change [1] [RORb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.5Floatratio
32Fold Change [2] [RORb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.5Floatratio
33Fold Change [3] [RORb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.5Floatratio
34Average Fold Change [RORb] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.5Floatratio
35Standard Deviation [RORb]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.5Float
36Outcome [RORg]The BioAssay activity outcome6nuclear receptor ROR-gamma isoform b [Homo sapiens]Outcome
37Score [RORg]The BioAssay activity ranking score6Integer
38Fold Change [1] [RORg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.6Floatratio
39Fold Change [2] [RORg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.6Floatratio
40Fold Change [3] [RORg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.6Floatratio
41Average Fold Change [RORg] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.6Floatratio
42Standard Deviation [RORg]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.6Float
43Outcome [PPARa]The BioAssay activity outcome7peroxisome proliferator-activated receptor alpha [Homo sapiens]Outcome
44Score [PPARa]The BioAssay activity ranking score7Integer
45Fold Change [1] [PPARa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.7Floatratio
46Fold Change [2] [PPARa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.7Floatratio
47Fold Change [3] [PPARa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.7Floatratio
48Average Fold Change [PPARa] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.7Floatratio
49Standard Deviation [PPARa]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.7Float
50Outcome [PPARd]The BioAssay activity outcome8peroxisome proliferator-activated receptor delta isoform 2 [Homo sapiens]Outcome
51Score [PPARd]The BioAssay activity ranking score8Integer
52Fold Change [1] [PPARd] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.8Floatratio
53Fold Change [2] [PPARd] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.8Floatratio
54Fold Change [3] [PPARd] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.8Floatratio
55Average Fold Change [PPARd] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.8Floatratio
56Standard Deviation [PPARd]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.8Float
57Outcome [PPARg]The BioAssay activity outcome9peroxisome proliferator-activated receptor gamma isoform 1 [Homo sapiens]Outcome
58Score [PPARg]The BioAssay activity ranking score9Integer
59Fold Change [1] [PPARg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.9Floatratio
60Fold Change [2] [PPARg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.9Floatratio
61Fold Change [3] [PPARg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.9Floatratio
62Average Fold Change [PPARg] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.9Floatratio
63Standard Deviation [PPARg]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.9Float
64Outcome [Rev-erb a]The BioAssay activity outcome10nuclear receptor subfamily 1 group D member 1 [Homo sapiens]Outcome
65Score [Rev-erb a]The BioAssay activity ranking score10Integer
66Fold Change [1] [Rev-erb a] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.10Floatratio
67Fold Change [2] [Rev-erb a] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.10Floatratio
68Fold Change [3] [Rev-erb a] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.10Floatratio
69Average Fold Change [Rev-erb a] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.10Floatratio
70Standard Deviation [Rev-erb a]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.10Float
71Outcome [Rev-erb b]The BioAssay activity outcome11nuclear receptor subfamily 1 group D member 2 isoform 1 [Homo sapiens]Outcome
72Score [Rev-erb b]The BioAssay activity ranking score11Integer
73Fold Change [1] [Rev-erb b] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.11Floatratio
74Fold Change [2] [Rev-erb b] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.11Floatratio
75Fold Change [3] [Rev-erb b] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.11Floatratio
76Average Fold Change [Rev-erb b] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.11Floatratio
77Standard Deviation [Rev-erb b]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.11Float
78Outcome [LRH1]The BioAssay activity outcome12nuclear receptor subfamily 5 group A member 2 isoform 2 [Homo sapiens]Outcome
79Score [LRH1]The BioAssay activity ranking score12Integer
80Fold Change [1] [LRH1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.12Floatratio
81Fold Change [2] [LRH1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.12Floatratio
82Fold Change [3] [LRH1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.12Floatratio
83Average Fold Change [LRH1] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.12Floatratio
84Standard Deviation [LRH1]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.12Float
85Outcome [SF1]The BioAssay activity outcome13steroidogenic factor 1 [Homo sapiens]Outcome
86Score [SF1]The BioAssay activity ranking score13Integer
87Fold Change [1] [SF1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.13Floatratio
88Fold Change [2] [SF1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.13Floatratio
89Fold Change [3] [SF1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.13Floatratio
90Average Fold Change [SF1] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.13Floatratio
91Standard Deviation [SF1]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.13Float
92Outcome [AR]The BioAssay activity outcome14AR protein [Homo sapiens]Outcome
93Score [AR]The BioAssay activity ranking score14Integer
94Fold Change [1] [AR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.14Floatratio
95Fold Change [2] [AR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.14Floatratio
96Fold Change [3] [AR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.14Floatratio
97Average Fold Change [AR] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.14Floatratio
98Standard Deviation [AR]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.14Float
99Outcome [CAR]The BioAssay activity outcome15nuclear receptor subfamily 1 group I member 3 isoform 12 [Homo sapiens]Outcome
100Score [CAR]The BioAssay activity ranking score15Integer
101Fold Change [1] [CAR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.15Floatratio
102Fold Change [2] [CAR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.15Floatratio
103Fold Change [3] [CAR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.15Floatratio
104Average Fold Change [CAR] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.15Floatratio
105Standard Deviation [CAR]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.15Float
106Outcome [ESR1]The BioAssay activity outcome16estrogen receptor isoform 1 [Homo sapiens]Outcome
107Score [ESR1]The BioAssay activity ranking score16Integer
108Fold Change [1] [ESR1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.16Floatratio
109Fold Change [2] [ESR1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.16Floatratio
110Fold Change [3] [ESR1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.16Floatratio
111Average Fold Change [ESR1] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.16Floatratio
112Standard Deviation [ESR1]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.16Float
113Outcome [Erb]The BioAssay activity outcome17estrogen receptor beta isoform 2 [Homo sapiens]Outcome
114Score [Erb]The BioAssay activity ranking score17Integer
115Fold Change [1] [Erb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.17Floatratio
116Fold Change [2] [Erb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.17Floatratio
117Fold Change [3] [Erb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.17Floatratio
118Average Fold Change [Erb] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.17Floatratio
119Standard Deviation [Erb]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.17Float
120Outcome [ERRa]The BioAssay activity outcome18steroid hormone receptor ERR1 [Homo sapiens]Outcome
121Score [ERRa]The BioAssay activity ranking score18Integer
122Fold Change [1] [ERRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.18Floatratio
123Fold Change [2] [ERRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.18Floatratio
124Fold Change [3] [ERRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.18Floatratio
125Average Fold Change [ERRa] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.18Floatratio
126Standard Deviation [ERRa]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.18Float
127Outcome [ERRb]The BioAssay activity outcome19steroid hormone receptor ERR2 [Homo sapiens]Outcome
128Score [ERRb]The BioAssay activity ranking score19Integer
129Fold Change [1] [ERRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.19Floatratio
130Fold Change [2] [ERRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.19Floatratio
131Fold Change [3] [ERRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.19Floatratio
132Average Fold Change [ERRb] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.19Floatratio
133Standard Deviation [ERRb]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.19Float
134Outcome [ERRg]The BioAssay activity outcome20estrogen-related receptor gamma isoform 2 [Homo sapiens]Outcome
135Score [ERRg]The BioAssay activity ranking score20Integer
136Fold Change [1] [ERRg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.20Floatratio
137Fold Change [2] [ERRg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.20Floatratio
138Fold Change [3] [ERRg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.20Floatratio
139Average Fold Change [ERRg] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.20Floatratio
140Standard Deviation [ERRg]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.20Float
141Outcome [GCCR]The BioAssay activity outcome21glucocorticoid receptor isoform gamma [Homo sapiens]Outcome
142Score [GCCR]The BioAssay activity ranking score21Integer
143Fold Change [1] [GCCR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.21Floatratio
144Fold Change [2] [GCCR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.21Floatratio
145Fold Change [3] [GCCR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.21Floatratio
146Average Fold Change [GCCR] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.21Floatratio
147Standard Deviation [GCCR]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.21Float
148Outcome [MR]The BioAssay activity outcome22mineralocorticoid receptor isoform 2 [Homo sapiens]Outcome
149Score [MR]The BioAssay activity ranking score22Integer
150Fold Change [1] [MR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.22Floatratio
151Fold Change [2] [MR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.22Floatratio
152Fold Change [3] [MR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.22Floatratio
153Average Fold Change [MR] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.22Floatratio
154Standard Deviation [MR]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.22Float
155Outcome [PGR]The BioAssay activity outcome23progesterone receptor isoform B [Homo sapiens]Outcome
156Score [PGR]The BioAssay activity ranking score23Integer
157Fold Change [1] [PGR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.23Floatratio
158Fold Change [2] [PGR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.23Floatratio
159Fold Change [3] [PGR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.23Floatratio
160Average Fold Change [PGR] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.23Floatratio
161Standard Deviation [PGR]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.23Float
162Outcome [PXR]The BioAssay activity outcome24nuclear receptor subfamily 1 group I member 2 isoform 1 [Homo sapiens]Outcome
163Score [PXR]The BioAssay activity ranking score24Integer
164Fold Change [1] [PXR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.24Floatratio
165Fold Change [2] [PXR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.24Floatratio
166Fold Change [3] [PXR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.24Floatratio
167Average Fold Change [PXR] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.24Floatratio
168Standard Deviation [PXR]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.24Float
169Outcome [VDR]The BioAssay activity outcome25vitamin D3 receptor isoform VDRA [Homo sapiens]Outcome
170Score [VDR]The BioAssay activity ranking score25Integer
171Fold Change [1] [VDR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.25Floatratio
172Fold Change [2] [VDR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.25Floatratio
173Fold Change [3] [VDR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.25Floatratio
174Average Fold Change [VDR] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.25Floatratio
175Standard Deviation [VDR]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.25Float
176Outcome [Coup-TF1]The BioAssay activity outcome26COUP transcription factor 1 [Homo sapiens]Outcome
177Score [Coup-TF1]The BioAssay activity ranking score26Integer
178Fold Change [1] [Coup-TF1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.26Floatratio
179Fold Change [2] [Coup-TF1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.26Floatratio
180Fold Change [3] [Coup-TF1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.26Floatratio
181Average Fold Change [Coup-TF1] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.26Floatratio
182Standard Deviation [Coup-TF1]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.26Float
183Outcome [Coup-TF2]The BioAssay activity outcome27COUP transcription factor 2 isoform b [Homo sapiens]Outcome
184Score [Coup-TF2]The BioAssay activity ranking score27Integer
185Fold Change [1] [Coup-TF2] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.27Floatratio
186Fold Change [2] [Coup-TF2] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.27Floatratio
187Fold Change [3] [Coup-TF2] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.27Floatratio
188Average Fold Change [Coup-TF2] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.27Floatratio
189Standard Deviation [Coup-TF2]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.27Float
190Outcome [DAX]The BioAssay activity outcome28nuclear receptor subfamily 0 group B member 1 [Homo sapiens]Outcome
191Score [DAX]The BioAssay activity ranking score28Integer
192Fold Change [1] [DAX] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.28Floatratio
193Fold Change [2] [DAX] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.28Floatratio
194Fold Change [3] [DAX] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.28Floatratio
195Average Fold Change [DAX] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.28Floatratio
196Standard Deviation [DAX]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.28Float
197Outcome [HNF4a]The BioAssay activity outcome29hepatocyte nuclear factor 4-alpha isoform e [Homo sapiens]Outcome
198Score [HNF4a]The BioAssay activity ranking score29Integer
199Fold Change [1] [HNF4a] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.29Floatratio
200Fold Change [2] [HNF4a] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.29Floatratio
201Fold Change [3] [HNF4a] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.29Floatratio
202Average Fold Change [HNF4a] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.29Floatratio
203Standard Deviation [HNF4a]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.29Float
204Outcome [HNF4g]The BioAssay activity outcome30hepatocyte nuclear factor 4-gamma [Homo sapiens]Outcome
205Score [HNF4g]The BioAssay activity ranking score30Integer
206Fold Change [1] [HNF4g] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.30Floatratio
207Fold Change [2] [HNF4g] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.30Floatratio
208Fold Change [3] [HNF4g] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.30Floatratio
209Average Fold Change [HNF4g] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.30Floatratio
210Standard Deviation [HNF4g]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.30Float
211Outcome [PMR]The BioAssay activity outcome31photoreceptor-specific nuclear receptor isoform b [Homo sapiens]Outcome
212Score [PMR]The BioAssay activity ranking score31Integer
213Fold Change [1] [PMR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.31Floatratio
214Fold Change [2] [PMR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.31Floatratio
215Fold Change [3] [PMR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.31Floatratio
216Average Fold Change [PMR] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.31Floatratio
217Standard Deviation [PMR]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.31Float
218Outcome [SHP]The BioAssay activity outcome32nuclear receptor subfamily 0 group B member 2 [Homo sapiens]Outcome
219Score [SHP]The BioAssay activity ranking score32Integer
220Fold Change [1] [SHP] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.32Floatratio
221Fold Change [2] [SHP] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.32Floatratio
222Fold Change [3] [SHP] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.32Floatratio
223Average Fold Change [SHP] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.32Floatratio
224Standard Deviation [SHP]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.32Float
225Outcome [TLX]The BioAssay activity outcome33nuclear receptor subfamily 2 group E member 1 [Homo sapiens]Outcome
226Score [TLX]The BioAssay activity ranking score33Integer
227Fold Change [1] [TLX] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.33Floatratio
228Fold Change [2] [TLX] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.33Floatratio
229Fold Change [3] [TLX] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.33Floatratio
230Average Fold Change [TLX] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.33Floatratio
231Standard Deviation [TLX]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.33Float
232Outcome [TR2]The BioAssay activity outcome34nuclear receptor subfamily 2 group C member 1 isoform c [Homo sapiens]Outcome
233Score [TR2]The BioAssay activity ranking score34Integer
234Fold Change [1] [TR2] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.34Floatratio
235Fold Change [2] [TR2] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.34Floatratio
236Fold Change [3] [TR2] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.34Floatratio
237Average Fold Change [TR2] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.34Floatratio
238Standard Deviation [TR2]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.34Float
239Outcome [TR4]The BioAssay activity outcome35nuclear receptor subfamily 2 group C member 2 [Homo sapiens]Outcome
240Score [TR4]The BioAssay activity ranking score35Integer
241Fold Change [1] [TR4] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.35Floatratio
242Fold Change [2] [TR4] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.35Floatratio
243Fold Change [3] [TR4] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.35Floatratio
244Average Fold Change [TR4] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.35Floatratio
245Standard Deviation [TR4]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.35Float
246Outcome [GCNR]The BioAssay activity outcome36nuclear receptor subfamily 6, group A, member 1 [Homo sapiens]Outcome
247Score [GCNR]The BioAssay activity ranking score36Integer
248Fold Change [1] [GCNR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.36Floatratio
249Fold Change [2] [GCNR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.36Floatratio
250Fold Change [3] [GCNR] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.36Floatratio
251Average Fold Change [GCNR] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.36Floatratio
252Standard Deviation [GCNR]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.36Float
253Outcome [Nur77]The BioAssay activity outcome37nuclear receptor subfamily 4 group A member 1 isoform 1 [Homo sapiens]Outcome
254Score [Nur77]The BioAssay activity ranking score37Integer
255Fold Change [1] [Nur77] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.37Floatratio
256Fold Change [2] [Nur77] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.37Floatratio
257Fold Change [3] [Nur77] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.37Floatratio
258Average Fold Change [Nur77] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.37Floatratio
259Standard Deviation [Nur77]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.37Float
260Outcome [Nurr1]The BioAssay activity outcome38nuclear receptor subfamily 4 group A member 2 [Homo sapiens]Outcome
261Score [Nurr1]The BioAssay activity ranking score38Integer
262Fold Change [1] [Nurr1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.38Floatratio
263Fold Change [2] [Nurr1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.38Floatratio
264Fold Change [3] [Nurr1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.38Floatratio
265Average Fold Change [Nurr1] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.38Floatratio
266Standard Deviation [Nurr1]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.38Float
267Outcome [NOR1]The BioAssay activity outcome39nuclear receptor subfamily 4 group A member 3 isoform a [Homo sapiens]Outcome
268Score [NOR1]The BioAssay activity ranking score39Integer
269Fold Change [1] [NOR1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.39Floatratio
270Fold Change [2] [NOR1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.39Floatratio
271Fold Change [3] [NOR1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.39Floatratio
272Average Fold Change [NOR1] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.39Floatratio
273Standard Deviation [NOR1]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.39Float
274Outcome [RARa]The BioAssay activity outcome40retinoic acid receptor alpha isoform 1 [Homo sapiens]Outcome
275Score [RARa]The BioAssay activity ranking score40Integer
276Fold Change [1] [RARa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.40Floatratio
277Fold Change [2] [RARa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.40Floatratio
278Fold Change [3] [RARa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.40Floatratio
279Average Fold Change [RARa] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.40Floatratio
280Standard Deviation [RARa]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.40Float
281Outcome [RARb]The BioAssay activity outcome41retinoic acid receptor beta isoform 1 [Homo sapiens]Outcome
282Score [RARb]The BioAssay activity ranking score41Integer
283Fold Change [1] [RARb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.41Floatratio
284Fold Change [2] [RARb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.41Floatratio
285Fold Change [3] [RARb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.41Floatratio
286Average Fold Change [RARb] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.41Floatratio
287Standard Deviation [RARb]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.41Float
288Outcome [RARg]The BioAssay activity outcome42retinoic acid receptor gamma isoform 1 [Homo sapiens]Outcome
289Score [RARg]The BioAssay activity ranking score42Integer
290Fold Change [1] [RARg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.42Floatratio
291Fold Change [2] [RARg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.42Floatratio
292Fold Change [3] [RARg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.42Floatratio
293Average Fold Change [RARg] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.42Floatratio
294Standard Deviation [RARg]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.42Float
295Outcome [RXRa]The BioAssay activity outcome43retinoic acid receptor RXR-alpha [Homo sapiens]Outcome
296Score [RXRa]The BioAssay activity ranking score43Integer
297Fold Change [1] [RXRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.43Floatratio
298Fold Change [2] [RXRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.43Floatratio
299Fold Change [3] [RXRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.43Floatratio
300Average Fold Change [RXRa] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.43Floatratio
301Standard Deviation [RXRa]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.43Float
302Outcome [RXRb]The BioAssay activity outcome44retinoic acid receptor RXR-alpha [Homo sapiens]Outcome
303Score [RXRb]The BioAssay activity ranking score44Integer
304Fold Change [1] [RXRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.44Floatratio
305Fold Change [2] [RXRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.44Floatratio
306Fold Change [3] [RXRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.44Floatratio
307Average Fold Change [RXRb] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.44Floatratio
308Standard Deviation [RXRb]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.44Float
309Outcome [RXRg]The BioAssay activity outcome45retinoic acid receptor RXR-gamma isoform b [Homo sapiens]Outcome
310Score [RXRg]The BioAssay activity ranking score45Integer
311Fold Change [1] [RXRg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.45Floatratio
312Fold Change [2] [RXRg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.45Floatratio
313Fold Change [3] [RXRg] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.45Floatratio
314Average Fold Change [RXRg] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.45Floatratio
315Standard Deviation [RXRg]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.45Float
316Outcome [THRa]The BioAssay activity outcome46thyroid hormone receptor alpha isoform 1 [Homo sapiens]Outcome
317Score [THRa]The BioAssay activity ranking score46Integer
318Fold Change [1] [THRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.46Floatratio
319Fold Change [2] [THRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.46Floatratio
320Fold Change [3] [THRa] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.46Floatratio
321Average Fold Change [THRa] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.46Floatratio
322Standard Deviation [THRa]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.46Float
323Outcome [THRb]The BioAssay activity outcome47thyroid hormone receptor beta [Homo sapiens]Outcome
324Score [THRb]The BioAssay activity ranking score47Integer
325Fold Change [1] [THRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.47Floatratio
326Fold Change [2] [THRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.47Floatratio
327Fold Change [3] [THRb] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.47Floatratio
328Average Fold Change [THRb] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.47Floatratio
329Standard Deviation [THRb]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.47Float
330Outcome [EAR-2]The BioAssay activity outcome48nuclear receptor subfamily 2, group F, member 6 [Homo sapiens]Outcome
331Score [EAR-2]The BioAssay activity ranking score48Integer
332Fold Change [1] [EAR-2] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.48Floatratio
333Fold Change [2] [EAR-2] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.48Floatratio
334Fold Change [3] [EAR-2] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.48Floatratio
335Average Fold Change [EAR-2] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.48Floatratio
336Standard Deviation [EAR-2]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.48Float
337Outcome [pBIND-1]The BioAssay activity outcome49Outcome
338Score [pBIND-1]The BioAssay activity ranking score49Integer
339Fold Change [1] [pBIND-1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.49Floatratio
340Fold Change [2] [pBIND-1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.49Floatratio
341Fold Change [3] [pBIND-1] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.49Floatratio
342Average Fold Change [pBIND-1] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.49Floatratio
343Standard Deviation [pBIND-1]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.49Float
344Outcome [VP16]The BioAssay activity outcome50transactivating tegument protein VP16 [Human herpesvirus 1]Outcome
345Score [VP16]The BioAssay activity ranking score50Integer
346Fold Change [1] [VP16] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.50Floatratio
347Fold Change [2] [VP16] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.50Floatratio
348Fold Change [3] [VP16] (10μM**)Normalized fold change at the indicated nominal compound concentration of 10 micromolar.50Floatratio
349Average Fold Change [VP16] (10μM**)Indicates average of 3 replicates of the normalized fold change at the indicated nominal compound concentration of 10 micromolar.50Floatratio
350Standard Deviation [VP16]Standard error of the replicate fold change derived from the normalized fold change of the replicate data for each compound.50Float

** Test Concentration. § Panel component ID.
Additional Information
Grant Number: U54 MH084512

Classification
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