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BioAssay: AID 2277

Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors.

Name: Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. ..more
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 Tested Compounds
 Tested Compounds
All(14)
 
 
Active(14)
 
 
 Tested Substances
 Tested Substances
All(14)
 
 
Active(14)
 
 
AID: 2277
Data Source: The Scripps Research Institute Molecular Screening Center (NUCLEAR-RECEPTOR_MOD_LUMI_384_1XFOLDCHANGE)
BioAssay Type: Panel, Primary, Primary Screening, Single Concentration Activity Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2010-01-21
Hold-until Date: 2010-06-09
Modify Date: 2010-06-08

Data Table ( Complete ):           Active    All
BioActive Compounds: 14
Depositor Specified Assays
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AIDNameTypeProbeComment
2139Summary of probe development efforts to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR).summary2 Summary AID.
2117Late stage results from the probe development effort to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR).screening
463078Late stage assay provider results from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): luminescent-based assay to identify RORA inhibitorsother
463143Late stage assay provider counterscreen from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): luminescence-based cell-based assay to identify activators of the liver X receptor (LXR)screening
463144Late stage assay provider counterscreen from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): luminescence-based cell-based assay to identify inhibitors of glucose-6-phosphatase (G6PC)other
463145Late stage assay provider counterscreen from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): luminescence-based cell-based assay to identify activators of the farnesoid X receptor (FXR)screening
463147Late stage assay provider counterscreen from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): luminescence-based cell-based assay to identify RORG inhibitorsscreening
463148Late stage assay provider counterscreen from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): luminescence-based cell-based assay to identify inhibitors of the human herpes virus VP16 transcriptional activator protein (VP16)screening
463150Late stage assay provider counterscreen from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): luminescence-based dose response assay to identify activators of the liver X receptor (LXR)confirmatory
463151Late stage assay provider counterscreen from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): luminescent-based dose response assay to identify RORG inhibitorsconfirmatory
463152Late stage assay provider results from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): luminescence-based dose response assay to identify RORA inhibitorsconfirmatory
463172Late stage assay provider counterscreen from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): luminescence-based cell-based dose response assay to identify inhibitors of glucose-6-phosphatase (G6PC)confirmatory
504899Late stage assay provider results from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): Diet-Induced obesity (DIO) mouse model studies to assess the effect of probe candidate on hepatic glucose productionother
504906Late stage assay provider results from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): radioligand binding assay for RORa using [3H]25-hydroxycholesterol to determine whether probe candidates bind directly to RORaother
504907Late stage assay provider results from the probe development effort to identify selective inverse agonists of the Retinoic acid receptor-related Orphan Receptors (RORA): fluorescence-based real-time polymerase chain reaction assay to determine the effect of probe candidates on endogenous expression of glucose-6-phosphatase (G6PC)other
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: Hugh Rosen, TSRI
External Assay ID: NUCLEAR-RECEPTOR_MOD_LUMI_384_1XFOLDCHANGE

Name: Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors.

Description:

Nuclear receptors are a family of small molecule and hormone-regulated transcription factors that share conserved DNA-binding and ligand-binding domains. Small pharmacological compounds able to bind to the cleft of the ligand-binding domain could alter its conformation and subsequently modify transcription of target genes. Such ligand agonists and/or antagonists have already been successfully designed for 23 nuclear receptors among the 48 previously identified in the human genome (1-3). RORalpha (RORa; RORA; NR1F1) is one of three related orphan nuclear receptors, including RORbeta (RORβ; RORB; NR1F2) and RORgamma (RORγ; RORC; NR1F3), known as "Retinoic Acid Receptor-related orphan receptors" (4).

RORA has unusual potential as a therapeutic target for the "metabolic syndrome" which results in pathologies such as insulin resistance, dyslipidemia, hypertension, and a pro-inflammatory state, that greatly elevates the risk of diabetes and atherosclerosis (5).The related RORC demonstrates significant expression in metabolic tissues such as liver, adipose, and skeletal muscle (6). These two receptors are implicated in several key aspects of this metabolic pathogenesis. For instance, the staggerer mouse, which carries a homozygous germline inactivation of RORA, shows low body weight, high food consumption (7-9), elevated angiogenesis in response to ischemia (10), susceptibility to atherosclerosis (9), and an abnormal serum lipid profile (11). RORG null mice exhibit normal plasma cholesterol levels, but when bred with the RORA staggerer mice, the resulting RORalpha/gamma knockout exhibits hypoglycemia not found in the single mutant animals. These studies reveal the functional redundancy of RORa and RORg in regulating blood glucose levels and highlight the need for RORalpha/gamma ligands that can bind to these receptors and modulate their transcriptional activity.

References: (1) Evans RM. The nuclear receptor superfamily: a rosetta stone for physiology. Mol Endocrinol 19:1429-1438, 2005.
(2) Kliewer SA, Lehmann JM, and Willson TM. Orphan nuclear receptors: shifting endocrinology into reverse. Science 284: 757-760, 1999.
(3) Li Y, Lambert MH, and Xu HE. Activation of nuclear receptors: a perspective from structural genomics. Structure (Camb) 11: 741-746., 2003.
(4) Jetten AM, Kurebayashi S, and Ueda E. The ROR nuclear orphan receptor subfamily: critical regulators of multiple biological processes. Prog Nucleic Acid Res Mol Biol 69: 205-247, 2001.
(5) Grundy SM, Brewer HB, Jr., Cleeman JI, Smith SC, Jr., and Lenfant C. Definition of metabolic syndrome: report of the National Heart, Lung, and Blood Institute/American Heart Association conference on scientific issues related to definition. Arterioscler Thromb Vasc Biol 24: e13-18, 2004.
(6) Medvedev A, Yan ZH, Hirose T, Giguere V, Jetten AM. Cloning of a cDNA encoding the murine orphan receptor RZR/ROR gamma and characterization of its response element. Gene. 1996 Nov 28;181(1-2):199-206.
(7) Bertin R, Guastavino JM, and Portet R. Effects of cold acclimation on the energetic metabolism of the staggerer mutant mouse. Physiol Behav 47: 377-380, 1990.
(8) Guastavino JM, Bertin R, and Portet R. Effects of the rearing temperature on the temporal feeding pattern of the staggerer mutant mouse. Physiol Behav 49: 405-409, 1991.
(9) Mamontova A, Seguret-Mace S, Esposito B, Chaniale C, Bouly M, Delhaye-Bouchaud N, Luc G, Staels B, Duverger N, Mariani J, and Tedgui A. Severe atherosclerosis and hypoalphalipoproteinemia in the staggerer mouse, a mutant of the nuclear receptor RORalpha. Circulation 98: 2738-2743., 1998.
(10) Besnard S, Silvestre J-S, Duriez M, Bakouche J, Lemaigre-Dubreuil Y, Mariani J, Levy BI, and Tedgui A. Increased ischemia-induced angiogenesis in the staggerer mouse, a mutant of the nuclear receptor RORa. Circ Res 89: 1209-1215, 2001.
(11) Raspe E, Duez H, Gervois P, Fievet C, Fruchart J-C, Besnard S, Mariani J, Tedgui A, and Staels B. Transcriptional regulation of apolipoprotein C-III gene expression by the orphan nuclear receptor RORalpha. J Biol Chem 276: 2865-2871, 2001.
(12) Schultz JR, Tu H, Luk A, Repa JJ, Medina JC, Li L, Schwendner S, Wang S, Thoolen M, Mangelsdorf DJ, Lustig KD, Shan B. Role of LXRs in control of lipogenesis. Genes Dev. 2000 Nov 15;14(22):2831-8.
(13) The benzenesulfoamide T0901317 is a novel RORa/? Inverse Agonist. Kumar N, Solt LA, Conkright JJ, Wang Y, Istrate MA, Busby SA, Garcia-Ordonez R, Burris TP, Griffin PR. Mol Pharm. 2009 Nov 10. [Epub ahead of print].

Keywords:

Nuclear receptor, NR, profiling, primary, Center-based initiative, RAR-related orphan receptor A, ROR alpha, RORa, RORA, library, low throughput assay, RZRA, ROR1, ROR2, ROR3, NR1F1, inhibitor, activator, modulator, transcriptional assay, luciferase, luminescence, ROR gamma, RORg, RORC, RORG, NR1F3, Scripps Florida, assay provider, The Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN.
Panel Information
NUCLEAR-RECEPTOR_MOD_LUMI_384_1XFOLDCHANGE
    Data Table(Active)    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1311AR protein [Homo sapiens] [gi:124375976]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 367
2410estrogen receptor alpha isoform 1 [Homo sapiens] [gi:62821794]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 2099
3113estrogen receptor beta isoform 2 [Homo sapiens] [gi:94538325]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 2100
4113estrogen-related receptor alpha [Homo sapiens] [gi:18860920]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 2101
5113estrogen-related receptor beta [Homo sapiens] [gi:238550159]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 2103
677estrogen-related receptor gamma isoform 2 [Homo sapiens] [gi:197209821]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 2104
768hepatocyte nuclear factor 4 alpha isoform e [Homo sapiens] [gi:71725341]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 3172
8410hepatocyte nuclear factor 4, gamma [Homo sapiens] [gi:115583654]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 3174
9113nuclear receptor subfamily 0, group B, member 1 [Homo sapiens] [gi:5016090]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 190
10113nuclear receptor subfamily 0, group B, member 1 [Homo sapiens] [gi:5016090]
Full LengthTaxonomy id: 9606
Gene id: 190
1114short heterodimer partner [Homo sapiens] [gi:13259503]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 8431
12113nuclear receptor subfamily 1, group D, member 1 [Homo sapiens] [gi:13430848]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 9572
1314nuclear receptor subfamily 1, group D, member 2 isoform 1 [Homo sapiens] [gi:224177491]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 9975
1495nuclear receptor subfamily 1, group H, member 2 [Homo sapiens] [gi:85362735]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 7376
15212nuclear receptor subfamily 1, group H, member 3 isoform c [Homo sapiens] [gi:194294519]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 10062
16113unnamed protein product [Homo sapiens] [gi:221041442]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 9971
17212nuclear receptor subfamily 1, group I, member 2 isoform 1 [Homo sapiens] [gi:34398348]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 8856
18212constitutive androstane receptor isoform 12 [Homo sapiens] [gi:117938738]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 9970
19212nuclear receptor subfamily 2, group C, member 1 isoform c [Homo sapiens] [gi:189491766]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 7181
20113nuclear receptor subfamily 2, group C, member 2 [Homo sapiens] [gi:36950991]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 7182
2114nuclear receptor subfamily 2, group E, member 1 [Homo sapiens] [gi:4507537]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 7101
2214nuclear receptor subfamily 2, group E, member 1 [Homo sapiens] [gi:4507537]
Full LengthTaxonomy id: 9606
Gene id: 7101
2314photoreceptor-specific nuclear receptor isoform b [Homo sapiens] [gi:7657395]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 10002
2468nuclear receptor subfamily 2, group F, member 1 [Homo sapiens] [gi:5032173]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 7025
2514nuclear receptor subfamily 2, group F, member 1 [Homo sapiens] [gi:5032173]
Full LengthTaxonomy id: 9606
Gene id: 7025
26113nuclear receptor subfamily 2, group F, member 2 isoform b [Homo sapiens] [gi:223555949]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 7026
2714nuclear receptor subfamily 2, group F, member 2 isoform b [Homo sapiens] [gi:223555949]
Full LengthTaxonomy id: 9606
Gene id: 7026
28212nuclear receptor subfamily 2, group F, member 6 [Homo sapiens] [gi:216409732]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 2063
29410glucocorticoid receptor isoform gamma [Homo sapiens] [gi:66528677]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 2908
3059nuclear receptor subfamily 3, group C, member 2 isoform 2 [Homo sapiens] [gi:260656020]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 4306
3114nuclear receptor subfamily 4, group A, member 1 [Homo sapiens] [gi:21361342]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 3164
32113nuclear receptor subfamily 4, group A, member 1 [Homo sapiens] [gi:21361342]
Full LengthTaxonomy id: 9606
Gene id: 3164
33410nuclear receptor subfamily 4, group A, member 2 [Homo sapiens] [gi:5453822]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 4929
3468nuclear receptor subfamily 4, group A, member 2 [Homo sapiens] [gi:5453822]
Full LengthTaxonomy id: 9606
Gene id: 4929
3559nuclear receptor subfamily 4, group A, member 3 isoform a [Homo sapiens] [gi:27894357]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 8013
36131nuclear receptor subfamily 5, group A, member 1 [Homo sapiens] [gi:20070193]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 2516
3795nuclear receptor subfamily 5, group A, member 1 [Homo sapiens] [gi:20070193]
Full LengthTaxonomy id: 9606
Gene id: 2516
38113nuclear receptor subfamily 5, group A, member 2 isoform 2 [Homo sapiens] [gi:4504343]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 2494
39113nuclear receptor subfamily 6, group A, member 1 [Homo sapiens] [gi:55859655]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 2649
40311nuclear receptor subfamily 6, group A, member 1 [Homo sapiens] [gi:55859655]
Full LengthTaxonomy id: 9606
Gene id: 2649
41212progesterone receptor isoform B [Homo sapiens] [gi:110611914]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 5241
42113peroxisome proliferative activated receptor, alpha [Homo sapiens] [gi:50348666]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 5465
43311peroxisome proliferative activated receptor, delta isoform 2 [Homo sapiens] [gi:29171750]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 5467
4414peroxisome proliferative activated receptor gamma isoform 1 [Homo sapiens] [gi:116284368]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 5468
4514peroxisome proliferative activated receptor gamma isoform 1 [Homo sapiens] [gi:116284368]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 5468
4668retinoic acid receptor, alpha isoform 1 [Homo sapiens] [gi:4506419]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 5914
4768retinoic acid receptor, alpha isoform 1 [Homo sapiens] [gi:4506419]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 5914
48410retinoic acid receptor, beta isoform 1 [Homo sapiens] [gi:14916494]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 5915
49311retinoic acid receptor, beta isoform 1 [Homo sapiens] [gi:14916494]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 5915
5059retinoic acid receptor, gamma isoform 1 [Homo sapiens] [gi:4506423]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 5916
51212retinoic acid receptor, gamma isoform 1 [Homo sapiens] [gi:4506423]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 5916
5277RAR-related orphan receptor A isoform c [Homo sapiens] [gi:4506577]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 6095
53212RAR-related orphan receptor B [Homo sapiens] [gi:19743907]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 6096
5468RAR-related orphan receptor C isoform b [Homo sapiens] [gi:48255918]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 6097
55410retinoid X receptor, alpha [Homo sapiens] [gi:4506755]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 6256
56410retinoid X receptor, alpha [Homo sapiens] [gi:4506755]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 6256
5777retinoid X receptor, alpha [Homo sapiens] [gi:4506755]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 6256
58410retinoid X receptor, alpha [Homo sapiens] [gi:4506755]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 6256
59311retinoid X receptor, gamma isoform b [Homo sapiens] [gi:58331207]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 6258
6014retinoid X receptor, gamma isoform b [Homo sapiens] [gi:58331207]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 6258
61212thyroid hormone receptor, alpha isoform 1 [Homo sapiens] [gi:40806160]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 7067
62311thyroid hormone receptor, beta [Homo sapiens] [gi:40806162]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 7068
63113vitamin D (1,25-dihydroxyvitamin D3) receptor [Homo sapiens] [gi:4507883]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 7421
64311vitamin D (1,25-dihydroxyvitamin D3) receptor [Homo sapiens] [gi:4507883]
Ligand Binding DomainTaxonomy id: 9606
Gene id: 7421
65311vitamin D (1,25-dihydroxyvitamin D3) receptor [Homo sapiens] [gi:4507883]
Variant 5' UTRTaxonomy id: 9606
Gene id: 7421
6614transactivating tegument protein VP16 [Human herpesvirus 1] [gi:9629429]
Ligand Binding DomainTaxonomy 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. Each compound was evaluated using two plates of the GAL4 NR library for a total of six replicates, at a nominal test concentration of 2 micromolar.

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 microliters. 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 micromolar final concentration) or DMSO was added to the plates and allowed to incubate for 20 hours. Next, 40 microliters 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.

Activity Score:

The PubChem Activity Score is assigned a value of 100 for probe compounds, 50 for actives and 0 for inactives.

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 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, and compounds that modulate well luminescence. All test compound concentrations reported above and below are nominal. The protein sequences encoded by the VDR and VDR-var2 plasmids are identical; there is an alternatively spliced exon in the 5'UTR in VDR-var2.
Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1Fold Change (NR3C4)1AR protein [Homo sapiens]Floatratio
2Outcome (NR3C4)1Outcome
3Fold Change (NR3A1)2estrogen receptor alpha isoform 1 [Homo sapiens]Floatratio
4Outcome (NR3A1)2Outcome
5Fold Change (NR3A2)3estrogen receptor beta isoform 2 [Homo sapiens]Floatratio
6Outcome (NR3A2)3Outcome
7Fold Change (NR3B1)4estrogen-related receptor alpha [Homo sapiens]Floatratio
8Outcome (NR3B1)4Outcome
9Fold Change (NR3B2)5estrogen-related receptor beta [Homo sapiens]Floatratio
10Outcome (NR3B2)5Outcome
11Fold Change (NR3B3)6estrogen-related receptor gamma isoform 2 [Homo sapiens]Floatratio
12Outcome (NR3B3)6Outcome
13Fold Change (NR2A1)7hepatocyte nuclear factor 4 alpha isoform e [Homo sapiens]Floatratio
14Outcome (NR2A1)7Outcome
15Fold Change (NR2A2)8hepatocyte nuclear factor 4, gamma [Homo sapiens]Floatratio
16Outcome (NR2A2)8Outcome
17Fold Change (DAX)9nuclear receptor subfamily 0, group B, member 1 [Homo sapiens]Floatratio
18Outcome (DAX)9Outcome
19Fold Change (DAX FL)10nuclear receptor subfamily 0, group B, member 1 [Homo sapiens]Floatratio
20Outcome (DAX FL)10Outcome
21Fold Change (SHP)11short heterodimer partner [Homo sapiens]Floatratio
22Outcome (SHP)11Outcome
23Fold Change (Rev-ERBa)12nuclear receptor subfamily 1, group D, member 1 [Homo sapiens]Floatratio
24Outcome (Rev-ERBa)12Outcome
25Fold Change (Rev-ERBb)13nuclear receptor subfamily 1, group D, member 2 isoform 1 [Homo sapiens]Floatratio
26Outcome (Rev-ERBb)13Outcome
27Fold Change (LXRb)14nuclear receptor subfamily 1, group H, member 2 [Homo sapiens]Floatratio
28Outcome (LXRb)14Outcome
29Fold Change (LXRa)15nuclear receptor subfamily 1, group H, member 3 isoform c [Homo sapiens]Floatratio
30Outcome (LXRa)15Outcome
31Fold Change (FXR)16unnamed protein product [Homo sapiens]Floatratio
32Outcome (FXR)16Outcome
33Fold Change (PXR)17nuclear receptor subfamily 1, group I, member 2 isoform 1 [Homo sapiens]Floatratio
34Outcome (PXR)17Outcome
35Fold Change (CAR1)18constitutive androstane receptor isoform 12 [Homo sapiens]Floatratio
36Outcome (CAR1)18Outcome
37Fold Change (TR2)19nuclear receptor subfamily 2, group C, member 1 isoform c [Homo sapiens]Floatratio
38Outcome (TR2)19Outcome
39Fold Change (TR4)20nuclear receptor subfamily 2, group C, member 2 [Homo sapiens]Floatratio
40Outcome (TR4)20Outcome
41Fold Change (TLL)21nuclear receptor subfamily 2, group E, member 1 [Homo sapiens]Floatratio
42Outcome (TLL)21Outcome
43Fold Change (TLL FL)22nuclear receptor subfamily 2, group E, member 1 [Homo sapiens]Floatratio
44Outcome (TLL FL)22Outcome
45Fold Change (PNR)23photoreceptor-specific nuclear receptor isoform b [Homo sapiens]Floatratio
46Outcome (PNR)23Outcome
47Fold Change (COUP-TF1)24nuclear receptor subfamily 2, group F, member 1 [Homo sapiens]Floatratio
48Outcome (COUP-TF1)24Outcome
49Fold Change (COUP-TF1 FL)25nuclear receptor subfamily 2, group F, member 1 [Homo sapiens]Floatratio
50Outcome (COUP-TF1 FL)25Outcome
51Fold Change (COUP-TF2)26nuclear receptor subfamily 2, group F, member 2 isoform b [Homo sapiens]Floatratio
52Outcome (COUP-TF2)26Outcome
53Fold Change (COUP-TF2 FL)27nuclear receptor subfamily 2, group F, member 2 isoform b [Homo sapiens]Floatratio
54Outcome (COUP-TF2 FL)27Outcome
55Fold Change (COUP-TF3)28nuclear receptor subfamily 2, group F, member 6 [Homo sapiens]Floatratio
56Outcome (COUP-TF3)28Outcome
57Fold Change (GCCR)29glucocorticoid receptor isoform gamma [Homo sapiens]Floatratio
58Outcome (GCCR)29Outcome
59Fold Change (MR)30nuclear receptor subfamily 3, group C, member 2 isoform 2 [Homo sapiens]Floatratio
60Outcome (MR)30Outcome
61Fold Change (Nur77)31nuclear receptor subfamily 4, group A, member 1 [Homo sapiens]Floatratio
62Outcome (Nur77)31Outcome
63Fold Change (Nur77 FL)32nuclear receptor subfamily 4, group A, member 1 [Homo sapiens]Floatratio
64Outcome (Nur77 FL)32Outcome
65Fold Change (Nurr1)33nuclear receptor subfamily 4, group A, member 2 [Homo sapiens]Floatratio
66Outcome (Nurr1)33Outcome
67Fold Change (Nurr1 FL)34nuclear receptor subfamily 4, group A, member 2 [Homo sapiens]Floatratio
68Outcome (Nurr1 FL)34Outcome
69Fold Change (Nor1)35nuclear receptor subfamily 4, group A, member 3 isoform a [Homo sapiens]Floatratio
70Outcome (Nor1)35Outcome
71Fold Change (SF-1)36nuclear receptor subfamily 5, group A, member 1 [Homo sapiens]Floatratio
72Outcome (SF-1)36Outcome
73Fold Change (SF-1 FL)37nuclear receptor subfamily 5, group A, member 1 [Homo sapiens]Floatratio
74Outcome (SF-1 FL)37Outcome
75Fold Change (LRH-1)38nuclear receptor subfamily 5, group A, member 2 isoform 2 [Homo sapiens]Floatratio
76Outcome (LRH-1)38Outcome
77Fold Change (GCNR)39nuclear receptor subfamily 6, group A, member 1 [Homo sapiens]Floatratio
78Outcome (GCNR)39Outcome
79Fold Change (GCNR FL)40nuclear receptor subfamily 6, group A, member 1 [Homo sapiens]Floatratio
80Outcome (GCNR FL)40Outcome
81Fold Change (PGR)41progesterone receptor isoform B [Homo sapiens]Floatratio
82Outcome (PGR)41Outcome
83Fold Change (PPARA)42peroxisome proliferative activated receptor, alpha [Homo sapiens]Floatratio
84Outcome (PPARA)42Outcome
85Fold Change (PPARD)43peroxisome proliferative activated receptor, delta isoform 2 [Homo sapiens]Floatratio
86Outcome (PPARD)43Outcome
87Fold Change (PPARG)44peroxisome proliferative activated receptor gamma isoform 1 [Homo sapiens]Floatratio
88Outcome (PPARG)44Outcome
89Fold Change (PPARG FL)45peroxisome proliferative activated receptor gamma isoform 1 [Homo sapiens]Floatratio
90Outcome (PPARG FL)45Outcome
91Fold Change (RARA)46retinoic acid receptor, alpha isoform 1 [Homo sapiens]Floatratio
92Outcome (RARA)46Outcome
93Fold Change (RARA FL)47retinoic acid receptor, alpha isoform 1 [Homo sapiens]Floatratio
94Outcome (RARA FL)47Outcome
95Fold Change (RARB)48retinoic acid receptor, beta isoform 1 [Homo sapiens]Floatratio
96Outcome (RARB)48Outcome
97Fold Change (RARB FL)49retinoic acid receptor, beta isoform 1 [Homo sapiens]Floatratio
98Outcome (RARB FL)49Outcome
99Fold Change (RARG)50retinoic acid receptor, gamma isoform 1 [Homo sapiens]Floatratio
100Outcome (RARG)50Outcome
101Fold Change (RARG FL)51retinoic acid receptor, gamma isoform 1 [Homo sapiens]Floatratio
102Outcome (RARG FL)51Outcome
103Fold Change (RORA)52RAR-related orphan receptor A isoform c [Homo sapiens]Floatratio
104Outcome (RORA)52Outcome
105Fold Change (RORB)53RAR-related orphan receptor B [Homo sapiens]Floatratio
106Outcome (RORB)53Outcome
107Fold Change (RORC)54RAR-related orphan receptor C isoform b [Homo sapiens]Floatratio
108Outcome (RORC)54Outcome
109Fold Change (RXRA)55retinoid X receptor, alpha [Homo sapiens]Floatratio
110Outcome (RXRA)55Outcome
111Fold Change (RXRA FL)56retinoid X receptor, alpha [Homo sapiens]Floatratio
112Outcome (RXRA FL)56Outcome
113Fold Change (RXRB)57retinoid X receptor, alpha [Homo sapiens]Floatratio
114Outcome (RXRB)57Outcome
115Fold Change (RXRB FL)58retinoid X receptor, alpha [Homo sapiens]Floatratio
116Outcome (RXRB FL)58Outcome
117Fold Change (RXRG)59retinoid X receptor, gamma isoform b [Homo sapiens]Floatratio
118Outcome (RXRG)59Outcome
119Fold Change (RXRG FL)60retinoid X receptor, gamma isoform b [Homo sapiens]Floatratio
120Outcome (RXRG FL)60Outcome
121Fold Change (THRA)61thyroid hormone receptor, alpha isoform 1 [Homo sapiens]Floatratio
122Outcome (THRA)61Outcome
123Fold Change (THRB)62thyroid hormone receptor, beta [Homo sapiens]Floatratio
124Outcome (THRB)62Outcome
125Fold Change (VDR)63vitamin D (1,25-dihydroxyvitamin D3) receptor [Homo sapiens]Floatratio
126Outcome (VDR)63Outcome
127Fold Change (VDR FL)64vitamin D (1,25-dihydroxyvitamin D3) receptor [Homo sapiens]Floatratio
128Outcome (VDR FL)64Outcome
129Fold Change (VDR variant2)65vitamin D (1,25-dihydroxyvitamin D3) receptor [Homo sapiens]Floatratio
130Outcome (VDR variant2)65Outcome
131Fold Change (VP16)66transactivating tegument protein VP16 [Human herpesvirus 1]Floatratio
132Outcome (VP16)66Outcome
133Probe Molecule OutcomeIndicates if the molecule is identified as a probe or not. One of Probe, Active or Inactive.String
Additional Information
Grant Number: U54 MH084512

Classification
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