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BioAssay: AID 624406

Late stage results from the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs

Name: Late stage results from the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs. ..more
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 Tested Compounds
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Unspecified(1)
 
 
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 Tested Substances
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Unspecified(1)
 
 
AID: 624406
Data Source: The Scripps Research Institute Molecular Screening Center (HCV-CORE_INH_RICERCA_2X%INH CSRUN)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
BioAssay Version:
Deposit Date: 2012-07-24
Hold-until Date: 2013-06-25
Modify Date: 2013-06-25

Data Table ( Complete ):           View All Data
Tested Compound:
Related Experiments
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AIDNameTypeProbeComment
1899TR-FRET-based primary biochemical high-throughput screening assay to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerizationScreening depositor-specified cross reference: Primary screen (HCV dimerization inhibitors in singlicate)
1911Summary of probe development efforts to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerizationSummary depositor-specified cross reference: Summary (HCV dimerization inhibitors)
2152TR-FRET-based biochemical high-throughput confirmation assay for inhibitors of Hepatitis C Virus (HCV) core protein dimerization.Screening depositor-specified cross reference: Confirmation screen (HCV dimerization inhibitors in triplicate)
2159TR-FRET-based biochemical high-throughput dose response assay to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization.Confirmatory depositor-specified cross reference: Dose response (HCV dimerization inhibitors in triplicate)
2488Late stage results for the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: TR-FRET-based biochemical dose response assay for HCV core inhibitorsConfirmatory depositor-specified cross reference: Late stage dose response (HCV core inhibitors in triplicate)
463085Late stage assay provider counterscreen results for the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Luminescence-based biochemical AlphaScreen assay to identify inhibitors of HCV core dimerizationConfirmatory depositor-specified cross reference: Late stage counterscreen (HCV core inhibitors in triplicate)
485271Late stage assay provider counterscreen results for the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: fluorescence-based cell-based quantitative PCR assay to identify inhibitors of HCV infectivityConfirmatory depositor-specified cross reference: Late stage counterscreen (HCV infectivity inhibitors in triplicate)
485280Late stage assay provider counterscreen results for the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Absorbance-based cell-based assay to identify compounds that are cytotoxic to Huh-7.5 cellsConfirmatory depositor-specified cross reference: Late stage counterscreen (Cytotoxicity in triplicate)
651574Late stage assay provider counterscreen results for the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Fluorescence-based cell-based Quantitative Polymerase Chain Reaction (QPCR) assay to identify inhibitors of HCV infectivity (2 timepoints)Other1 depositor-specified cross reference
651575Late stage assay provider counterscreen results for the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Fluorescence-based cell-based Quantitative Polymerase Chain Reaction (QPCR) assay to identify inhibitors of HCV infectivityConfirmatory1 depositor-specified cross reference
651576Late stage assay provider counterscreen results for the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Luminescence-based biochemical AlphaScreen assay to identify inhibitors of HCV core dimerization (%INH 15uM)Other1 depositor-specified cross reference
651577Late stage assay provider counterscreen results for the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Luminescence-based biochemical dose response AlphaScreen assay to identify inhibitors of HCV core dimerizationConfirmatory1 depositor-specified cross reference
651583Late stage assay provider counterscreen results for the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Absorbance-based cell-based assay to identify compounds that are cytotoxic to Huh-7.5 cellsConfirmatory depositor-specified cross reference
Description:
Source (MLSCN Center Name): The Scripps Research Institute Molecular Screening Center
Center Affiliation: The Scripps Research Institute (TSRI)
Assay Provider: A.D. Strosberg, TSRI
Network: Molecular Library Probe Production Center Network (MLPCN)
Grant Proposal Number: 1-X01-MH085709-01
Grant Proposal PI: A.D. Strosberg, TSRI
External Assay ID: HCV-CORE_INH_RICERCA_2X%INH CSRUN

Name: Late stage results from the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs.

Description:

The Hepatitis C Virus (HCV) is a major cause of liver failure and hepatocellular cancer, with about 170 million people infected worldwide (1). The HCV has a small RNA genome that is directly translated by the infected host cell into a single precursor polyprotein that is processed by enzymatic cleavage into 10 proteins of diverse function. The most N-terminal 21kDa protein of this HCV polyprotein is the HCV core (C) protein, which is a highly basic, RNA-binding structural protein essential for assembly and packaging of the viral genome (2). Core protein is cleaved by a host peptidase and anchored to the host cell endoplasmic reticulum, where it undergoes further processing into its mature form (3). The N terminal portion of this mature C protein mediates viral assembly through homodimerization and formation of higher order complexes with viral RNA to form the nucleocapsid, while the hydrophobic C terminal interacts with envelope glycoproteins to form the infectious particle (4). The conserved nature of the HCV protein and absence of a vaccine to prevent HCV infection (5), along with studies demonstrating that C protein contributes to host cell oncogenesis (6), apoptosis inhibition (7), and suppression of host T cell responses (8), support a role for core protein as a major pathogenic component of HCV. The identification of specific inhibitors of HCV core dimerization will provide valuable tools for inhibiting HCV assembly without host cell effects (9).

References:

1. Hoofnagle, J.H., Course and outcome of hepatitis C. Hepatology, 2002. 36(5 Suppl 1): p. s21-s29.
2. Lin, C., Lindenbach, B.D., Pragai, B.M., McCourt, D.W., and Rice, C.M., Processing in the hepatitis C virus E2-NS2 region: identification of p7 and two distinct E2-specific products with different C termini. J Virol, 1994. 68(8): p. 5063-73.
3. Moradpour, D. and Blum, H.E., A primer on the molecular virology of hepatitis C. Liver Int, 2004. 24(6): p. 519-25.
4. Majeau, N., Gagne, V., Boivin, A., Bolduc, M., Majeau, J.A., Ouellet, D., and Leclerc, D., The N-terminal half of the core protein of hepatitis C virus is sufficient for nucleocapsid formation. J Gen Virol, 2004. 85(Pt 4): p. 971-81.
5. Yang, J.P., Zhou, D., and Wong-Staal, F., Screening of small-molecule compounds as inhibitors of HCV entry. Methods Mol Biol, 2009. 510: p. 295-304.
6. Ray, R.B., Lagging, L.M., Meyer, K., and Ray, R., Hepatitis C virus core protein cooperates with ras and transforms primary rat embryo fibroblasts to tumorigenic phenotype. J Virol, 1996. 70(7): p. 4438-43.
7. Marusawa, H., Hijikata, M., Chiba, T., and Shimotohno, K., Hepatitis C virus core protein inhibits Fas- and tumor necrosis factor alpha-mediated apoptosis via NF-kappaB activation. J Virol, 1999. 73(6): p. 4713-20.
8. Large, M.K., Kittlesen, D.J., and Hahn, Y.S., Suppression of host immune response by the core protein of hepatitis C virus: possible implications for hepatitis C virus persistence. J Immunol, 1999. 162(2): p. 931-8.
9. Kota S, Coito C, Mousseau G, Lavergne JP, Strosberg AD. Peptide inhibitors of hepatitis C virus core oligomerization and virus production. J Gen Virol. 2009 Jun;90(Pt 6):1319-28.

Keywords:

Ricerca, counterscreen, purchased, HCV, core protein, core 106, core, hepatitis, hepatitis C, RNA virus, virus, protein-protein interaction, dimerization, inhibitor, inhibition, inhibit, fluorescence, infectivity, Scripps, Scripps Florida, The Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN.
Panel Information
Targets
    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1Adenosine A11adenosine A1 receptor [Homo sapiens] [gi:119611871]
Taxonomy id: 9606
Gene id: 134
2Adenosine A2A1adenosine A2a receptor [Homo sapiens] [gi:119580062]
Taxonomy id: 9606
Gene id: 135
3Adenosine A31adenosine receptor A3 isoform 2 [Homo sapiens] [gi:4501953]
Taxonomy id: 9606
Gene id: 140
4Adrenergic alpha1A1adrenergic receptor, alpha 1a [Rattus norvegicus] [gi:149030335]
Taxonomy id: 10116
Gene id: 29412
5Adrenergic alpha1B1Adrenergic, alpha-1B-, receptor [Homo sapiens] [gi:187953275]
Taxonomy id: 10116
Gene id: 147
6Adrenergic alpha1D1adrenergic, alpha-1D-, receptor [Homo sapiens] [gi:167882784]
Taxonomy id: 9606
Gene id: 146
7Adrenergic alpha2A1alpha-2A adrenergic receptor [Homo sapiens] [gi:194353970]
Taxonomy id: 9606
Gene id: 150
8Adrenergic beta11adrenergic, beta-1-, receptor [Homo sapiens] [gi:166706747]
Taxonomy id: 9606
Gene id: 153
9Adrenergic beta21Adrenergic, beta-2-, receptor, surface [Homo sapiens] [gi:127798637]
Taxonomy id: 9606
Gene id: 154
10Androgen (Testosterone) AR1androgen receptor isoform 1 [Homo sapiens] [gi:21322252]
Taxonomy id: 10116
Gene id: 367
11Bradykinin B11bradykinin receptor B1 [Homo sapiens] [gi:119602038]
Taxonomy id: 9606
Gene id: 623
12Bradykinin B21B2 bradykinin receptor [Homo sapiens] [gi:4557359]
Taxonomy id: 9606
Gene id: 624
13Calcium Channel L-Type, Benzothiazepine1voltage-dependent L-type calcium channel subunit beta-4 [Rattus norvegicus] [gi:157787131]
Taxonomy id: 10116
Gene id: 58942
14Calcium Channel L-Type, Dihydropyridine1voltage-dependent L-type calcium channel subunit alpha-1D [Rattus norvegicus] [gi:8393030]
Taxonomy id: 10116
Gene id: 29716
15Calcium Channel N-Type1voltage-dependent N-type calcium channel subunit alpha-1B isoform 1 [Rattus norvegicus] [gi:304555571]
Taxonomy id: 10116
Gene id: 257648
16Cannabinoid CB11cannabinoid receptor [Homo sapiens] [gi:67550212]
Taxonomy id: 9606
Gene id: 1268
17Dopamine D11Dopamine receptor D1 [Homo sapiens] [gi:67677841]
Taxonomy id: 9606
Gene id: 1812
18Dopamine D2S1dopamine receptor D2 isoform short [Homo sapiens] [gi:197692661]
Taxonomy id: 9606
Gene id: 1813
19Dopamine D31D(3) dopamine receptor isoform a [Homo sapiens] [gi:89191861]
Taxonomy id: 9606
Gene id: 1814
20Dopamine D4.21D(4) dopamine receptor [Homo sapiens] [gi:32483397]
Taxonomy id: 9606
Gene id: 1815
21Endothelin ETA1endothelin-1 receptor isoform b precursor [Homo sapiens] [gi:260593650]
Taxonomy id: 9606
Gene id: 1909
22Endothelin ETB1endothelin B receptor isoform 1 precursor [Homo sapiens] [gi:4557547]
Taxonomy id: 9606
Gene id: 1910
23Epidermal Growth Factor (EGF)1pro-epidermal growth factor isoform 1 preproprotein [Homo sapiens] [gi:166362728]
Taxonomy id: 9606
Gene id: 1950
24Estrogen Eralpha1estrogen receptor [Homo sapiens] [gi:62821794]
Taxonomy id: 9606
Gene id: 2099
25GABAA, Flunitrazepam, Central1gamma-aminobutyric acid A receptor, gamma 2 [Rattus norvegicus] [gi:149052302]
Taxonomy id: 10116
Gene id: 29709
26GABAA, Muscimol, Central1testis gamma-aminobutyric acid receptor subunit beta 3 [Rattus norvegicus] [gi:53765741]
Taxonomy id: 10116
Gene id: 24922
27GABAB1A1gamma-aminobutyric acid type B receptor subunit 1 isoform a precursor [Homo sapiens] [gi:10835015]
Taxonomy id: 9606
Gene id: 2550
28Glucocorticoid1glucocorticoid receptor isoform alpha [Homo sapiens] [gi:4504133]
Taxonomy id: 9606
Gene id: 2908
29Glutamate, Kainate1glutamate receptor, ionotropic kainate 3 isoform 1 precursor [Rattus norvegicus] [gi:163659915]
Taxonomy id: 10116
Gene id: 298521
30Glutamate, NMDA, Agonism1glutamate [NMDA] receptor subunit epsilon-2 precursor [Rattus norvegicus] [gi:6980984]
Taxonomy id: 10116
Gene id: 24410
31Glutamate, NMDA, Glycine1N-methyl-D-Aspartate receptor [Rattus norvegicus] [gi:57848]
Taxonomy id: 10116
Gene id: 24408
32Glutamate, NMDA, Phencyclidine1glutamate receptor, ionotropic, N-methyl D-aspartate 1, isoform CRA_h [Rattus norvegicus] [gi:149039393]
Taxonomy id: 10116
Gene id: 24408
33Histamine H11histamine H1 receptor [Homo sapiens] [gi:149158709]
Taxonomy id: 9606
Gene id: 3269
34Histamine H21histamine H2 receptor isoform 1 [Homo sapiens] [gi:197085610]
Taxonomy id: 9606
Gene id: 3274
35Histamine H31histamine H3 receptor [Homo sapiens] [gi:194018562]
Taxonomy id: 9606
Gene id: 11255
36Imidazoline I2, Central1alpha-2A adrenergic receptor [Rattus norvegicus] [gi:340805866]
Taxonomy id: 10116
Gene id: 25083
37Interleukin IL-11Taxonomy id: 10090
Gene id: 111343
38Leukotriene, Cysteinyl CysLT11cysteinyl leukotriene receptor 1 [Homo sapiens] [gi:5729798]
Taxonomy id: 9606
Gene id: 10800
39Melatonin MT11melatonin receptor type 1A [Homo sapiens] [gi:5174593]
Taxonomy id: 9606
Gene id: 4543
40Muscarinic M11muscarinic acetylcholine receptor M1 [Homo sapiens] [gi:37622910]
Taxonomy id: 9606
Gene id: 1128
41Muscarinic M21cholinergic receptor, muscarinic 2 [Homo sapiens] [gi:119604271]
Taxonomy id: 9606
Gene id: 1129
42Muscarinic M31Cholinergic receptor, muscarinic 3 [Homo sapiens] [gi:111306506]
Taxonomy id: 9606
Gene id: 1131
43Neuropeptide Y Y11neuropeptide Y receptor type 1 [Homo sapiens] [gi:4505445]
Taxonomy id: 9606
Gene id: 4886
44Neuropeptide Y Y21neuropeptide Y receptor type 2 [Homo sapiens] [gi:4505447]
Taxonomy id: 9606
Gene id: 4887
45Nicotinic Acetylcholine1cholinergic receptor, nicotinic, alpha 3, isoform CRA_a [Homo sapiens] [gi:119619563]
Taxonomy id: 9606
Gene id: 1136
46Nicotinic Acetylcholine alpha 1, Bungarotoxin1cholinergic receptor, nicotinic, alpha 1 (muscle), isoform CRA_a [Homo sapiens] [gi:119631533]
Taxonomy id: 9606
Gene id: 1134
47Opiate delat1 (OP1, DOP)1delta-type opioid receptor [Homo sapiens] [gi:63477962]
Taxonomy id: 9606
Gene id: 4985
48Opiate kappa (OP2, KOP)1kappa-type opioid receptor [Homo sapiens] [gi:39725940]
Taxonomy id: 9606
Gene id: 4986
49Opiate mu (OP3, MOP)1mu-type opioid receptor isoform MOR-1B2 [Homo sapiens] [gi:223718719]
Taxonomy id: 9606
Gene id: 4988
50Phorbol Ester1protein kinase C zeta type isoform b [Mus musculus] [gi:84872205]
Taxonomy id: 10090
Gene id: 18762
51Platelet Activating Factor (PAF)1platelet-activating factor acetylhydrolase precursor [Homo sapiens] [gi:270133071]
Taxonomy id: 9606
Gene id: 7941
52Potassium Channel [KATP]1Calcium-activated potassium channel subunit beta-1 [Cricetulus griseus] [gi:344244667]
Taxonomy id: 10036
Gene id: 100765448
53Potassium Channel hERG1voltage-gated potassium channel subfamily H isoform 3.1 [Homo sapiens] [gi:237862038]
Taxonomy id: 9606
Gene id: 3757
54Prostanoid EP41Prostaglandin E receptor 4 (subtype EP4) [Homo sapiens] [gi:109731195]
Taxonomy id: 9606
Gene id: 5734
55Purinergic P2X1PREDICTED: purinergic receptor P2X2 isoform 1 [Oryctolagus cuniculus] [gi:291412549]
Taxonomy id: 9986
Gene id: 100356670
56Purinergic P2Y1P2Y purinoceptor 1 [Rattus norvegicus] [gi:25742733]
Taxonomy id: 10116
Gene id: 25265
57Rolipram1high affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A [Rattus norvegicus] [gi:213972559]
Taxonomy id: 10116
Gene id: 81744
58Serotonin (5-Hydroxytryptamine) 5-HT1A15-hydroxytryptamine receptor 1A [Homo sapiens] [gi:55956923]
Taxonomy id: 9606
Gene id: 3350
59Serotonin (5-Hydroxytryptamine) 5-HT2B15-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] [gi:119591355]
Taxonomy id: 9606
Gene id: 3357
60Serotonin (5-Hydroxytryptamine) 5-HT315-hydroxytryptamine receptor 3A isoform b precursor [Homo sapiens] [gi:253735700]
Taxonomy id: 9606
Gene id: 3359
61Sigma 11opioid receptor, sigma 1 [Homo sapiens] [gi:123231939]
Taxonomy id: 9606
Gene id: 10280
62Tachykinin NK11tachykinin receptor 1, isoform CRA_a [Homo sapiens] [gi:119620001]
Taxonomy id: 9606
Gene id: 6869
63Thyroid Hormone1thyroid hormone receptor alpha isoform TRalpha1 [Rattus norvegicus] [gi:63079705]
Taxonomy id: 10116
Gene id: 81812
64Transporter, Dopamine (DAT)1sodium-dependent dopamine transporter [Homo sapiens] [gi:4507041]
Taxonomy id: 9606
Gene id: 6531
65Transporter, GABA1sodium- and chloride-dependent GABA transporter 1 [Rattus norvegicus] [gi:13242269]
Taxonomy id: 10116
Gene id: 79212
66Transporter, Norepinephrine (NET)1Net [Homo sapiens] [gi:531523]
Taxonomy id: 9606
Gene id: 6530
67Transporter, Serotonin (5-Hydroxytryptamine)1sodium-dependent serotonin transporter [Homo sapiens] [gi:4507043]
Taxonomy id: 9606
Gene id: 6532

§ Panel component ID.
Protocol
Assay Overview:

The purpose of this panel of binding assays performed by Ricerca Biosciences, LLC, is to identify a subset of potential receptors, transporters, ion channels, etc. for which the HCV Core 106 dimerization inhibitor lead candidate compound SID 103771539 displays affinity.

Protocol Summary:

This assay was performed in duplicate by Ricerca, LLC. See website for details. Negative inhibition represents a stimulation of binding. Methods employed in this study have been adapted from the scientific literature to maximize reliability and reproducibility. Reference standards were run as an integral part of each assay to ensure the validity of the results obtained.

PubChem Activity Outcome and Score:

The following applies to each panel:

A response of greater than or equal to 50% inhibition is considered active.

List of Reagents:

Reagents were provided by Ricerca Biosciences, LLC.
Categorized Comment - additional comments and annotations
From PubChem:
Assay Format: Cell-based
Result Definitions
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TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Outcome [Adenosine A1]The assay outcome, one of Inactive or Active.1adenosine A1 receptor [Homo sapiens]Outcome
2Inhibition at 10 uM [Adenosine A1] (10μM**)Value of average % inhibition at 10 uM compound concentration.1Float%
3Outcome [Adenosine A2A]The assay outcome, one of Inactive or Active.2adenosine A2a receptor [Homo sapiens]Outcome
4Inhibition at 10 uM [Adenosine A2A] (10μM**)Value of average % inhibition at 10 uM compound concentration.2Float%
5Outcome [Adenosine A3]The assay outcome, one of Inactive or Active.3adenosine receptor A3 isoform 2 [Homo sapiens]Outcome
6Inhibition at 10 uM [Adenosine A3] (10μM**)Value of average % inhibition at 10 uM compound concentration.3Float%
7Outcome [Adrenergic alpha1A]The assay outcome, one of Inactive or Active.4adrenergic receptor, alpha 1a [Rattus norvegicus]Outcome
8Inhibition at 10 uM [Adrenergic alpha1A] (10μM**)Value of average % inhibition at 10 uM compound concentration.4Float%
9Outcome [Adrenergic alpha1B]The assay outcome, one of Inactive or Active.5Adrenergic, alpha-1B-, receptor [Homo sapiens]Outcome
10Inhibition at 10 uM [Adrenergic alpha1B] (10μM**)Value of average % inhibition at 10 uM compound concentration.5Float%
11Outcome [Adrenergic alpha1D]The assay outcome, one of Inactive or Active.6adrenergic, alpha-1D-, receptor [Homo sapiens]Outcome
12Inhibition at 10 uM [Adrenergic alpha1D] (10μM**)Value of average % inhibition at 10 uM compound concentration.6Float%
13Outcome [Adrenergic alpha2A]The assay outcome, one of Inactive or Active.7alpha-2A adrenergic receptor [Homo sapiens]Outcome
14Inhibition at 10 uM [Adrenergic alpha2A] (10μM**)Value of average % inhibition at 10 uM compound concentration.7Float%
15Outcome [Adrenergic beta1]The assay outcome, one of Inactive or Active.8adrenergic, beta-1-, receptor [Homo sapiens]Outcome
16Inhibition at 10 uM [Adrenergic beta1] (10μM**)Value of average % inhibition at 10 uM compound concentration.8Float%
17Outcome [Adrenergic beta2]The assay outcome, one of Inactive or Active.9Adrenergic, beta-2-, receptor, surface [Homo sapiens]Outcome
18Inhibition at 10 uM [Adrenergic beta2] (10μM**)Value of average % inhibition at 10 uM compound concentration.9Float%
19Outcome [Androgen (Testosterone) AR]The assay outcome, one of Inactive or Active.10androgen receptor isoform 1 [Homo sapiens]Outcome
20Inhibition at 10 uM [Androgen (Testosterone) AR] (10μM**)Value of average % inhibition at 10 uM compound concentration.10Float%
21Outcome [Bradykinin B1 ]The assay outcome, one of Inactive or Active.11bradykinin receptor B1 [Homo sapiens]Outcome
22Inhibition at 10 uM [Bradykinin B1 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.11Float%
23Outcome [Bradykinin B2 ]The assay outcome, one of Inactive or Active.12B2 bradykinin receptor [Homo sapiens]Outcome
24Inhibition at 10 uM [Bradykinin B2 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.12Float%
25Outcome [Calcium Channel L-Type, Benzothiazepine ]The assay outcome, one of Inactive or Active.13voltage-dependent L-type calcium channel subunit beta-4 [Rattus norvegicus]Outcome
26Inhibition at 10 uM [Calcium Channel L-Type, Benzothiazepine ] (10μM**)Value of average % inhibition at 10 uM compound concentration.13Float%
27Outcome [Calcium Channel L-Type, Dihydropyridine]The assay outcome, one of Inactive or Active.14voltage-dependent L-type calcium channel subunit alpha-1D [Rattus norvegicus]Outcome
28Inhibition at 10 uM [Calcium Channel L-Type, Dihydropyridine] (10μM**)Value of average % inhibition at 10 uM compound concentration.14Float%
29Outcome [Calcium Channel N-Type ]The assay outcome, one of Inactive or Active.15voltage-dependent N-type calcium channel subunit alpha-1B isoform 1 [Rattus norvegicus]Outcome
30Inhibition at 10 uM [Calcium Channel N-Type ] (10μM**)Value of average % inhibition at 10 uM compound concentration.15Float%
31Outcome [Cannabinoid CB1]The assay outcome, one of Inactive or Active.16cannabinoid receptor [Homo sapiens]Outcome
32Inhibition at 10 uM [Cannabinoid CB1] (10μM**)Value of average % inhibition at 10 uM compound concentration.16Float%
33Outcome [Dopamine D1]The assay outcome, one of Inactive or Active.17Dopamine receptor D1 [Homo sapiens]Outcome
34Inhibition at 10 uM [Dopamine D1] (10μM**)Value of average % inhibition at 10 uM compound concentration.17Float%
35Outcome [Dopamine D2S]The assay outcome, one of Inactive or Active.18dopamine receptor D2 isoform short [Homo sapiens]Outcome
36Inhibition at 10 uM [Dopamine D2S] (10μM**)Value of average % inhibition at 10 uM compound concentration.18Float%
37Outcome [Dopamine D3 ]The assay outcome, one of Inactive or Active.19D(3) dopamine receptor isoform a [Homo sapiens]Outcome
38Inhibition at 10 uM [Dopamine D3 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.19Float%
39Outcome [Dopamine D4.2 ]The assay outcome, one of Inactive or Active.20D(4) dopamine receptor [Homo sapiens]Outcome
40Inhibition at 10 uM [Dopamine D4.2 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.20Float%
41Outcome [Endothelin ETA ]The assay outcome, one of Inactive or Active.21endothelin-1 receptor isoform b precursor [Homo sapiens]Outcome
42Inhibition at 10 uM [Endothelin ETA ] (10μM**)Value of average % inhibition at 10 uM compound concentration.21Float%
43Outcome [Endothelin ETB ]The assay outcome, one of Inactive or Active.22endothelin B receptor isoform 1 precursor [Homo sapiens]Outcome
44Inhibition at 10 uM [Endothelin ETB ] (10μM**)Value of average % inhibition at 10 uM compound concentration.22Float%
45Outcome [Epidermal Growth Factor (EGF) ]The assay outcome, one of Inactive or Active.23pro-epidermal growth factor isoform 1 preproprotein [Homo sapiens]Outcome
46Inhibition at 10 uM [Epidermal Growth Factor (EGF) ] (10μM**)Value of average % inhibition at 10 uM compound concentration.23Float%
47Outcome [Estrogen Eralpha]The assay outcome, one of Inactive or Active.24estrogen receptor [Homo sapiens]Outcome
48Inhibition at 10 uM [Estrogen Eralpha] (10μM**)Value of average % inhibition at 10 uM compound concentration.24Float%
49Outcome [GABAA, Flunitrazepam, Central]The assay outcome, one of Inactive or Active.25gamma-aminobutyric acid A receptor, gamma 2 [Rattus norvegicus]Outcome
50Inhibition at 10 uM [GABAA, Flunitrazepam, Central] (10μM**)Value of average % inhibition at 10 uM compound concentration.25Float%
51Outcome [GABAA, Muscimol, Central]The assay outcome, one of Inactive or Active.26testis gamma-aminobutyric acid receptor subunit beta 3 [Rattus norvegicus]Outcome
52Inhibition at 10 uM [GABAA, Muscimol, Central] (10μM**)Value of average % inhibition at 10 uM compound concentration.26Float%
53Outcome [GABAB1A ]The assay outcome, one of Inactive or Active.27gamma-aminobutyric acid type B receptor subunit 1 isoform a precursor [Homo sapiens]Outcome
54Inhibition at 10 uM [GABAB1A ] (10μM**)Value of average % inhibition at 10 uM compound concentration.27Float%
55Outcome [Glucocorticoid ]The assay outcome, one of Inactive or Active.28glucocorticoid receptor isoform alpha [Homo sapiens]Outcome
56Inhibition at 10 uM [Glucocorticoid ] (10μM**)Value of average % inhibition at 10 uM compound concentration.28Float%
57Outcome [Glutamate, Kainate ]The assay outcome, one of Inactive or Active.29glutamate receptor, ionotropic kainate 3 isoform 1 precursor [Rattus norvegicus]Outcome
58Inhibition at 10 uM [Glutamate, Kainate ] (10μM**)Value of average % inhibition at 10 uM compound concentration.29Float%
59Outcome [Glutamate, NMDA, Agonism ]The assay outcome, one of Inactive or Active.30glutamate [NMDA] receptor subunit epsilon-2 precursor [Rattus norvegicus]Outcome
60Inhibition at 10 uM [Glutamate, NMDA, Agonism ] (10μM**)Value of average % inhibition at 10 uM compound concentration.30Float%
61Outcome [Glutamate, NMDA, Glycine ]The assay outcome, one of Inactive or Active.31N-methyl-D-Aspartate receptor [Rattus norvegicus]Outcome
62Inhibition at 10 uM [Glutamate, NMDA, Glycine ] (10μM**)Value of average % inhibition at 10 uM compound concentration.31Float%
63Outcome [Glutamate, NMDA, Phencyclidine]The assay outcome, one of Inactive or Active.32glutamate receptor, ionotropic, N-methyl D-aspartate 1, isoform CRA_h [Rattus norvegicus]Outcome
64Inhibition at 10 uM [Glutamate, NMDA, Phencyclidine] (10μM**)Value of average % inhibition at 10 uM compound concentration.32Float%
65Outcome [Histamine H1]The assay outcome, one of Inactive or Active.33histamine H1 receptor [Homo sapiens]Outcome
66Inhibition at 10 uM [Histamine H1] (10μM**)Value of average % inhibition at 10 uM compound concentration.33Float%
67Outcome [Histamine H2 ]The assay outcome, one of Inactive or Active.34histamine H2 receptor isoform 1 [Homo sapiens]Outcome
68Inhibition at 10 uM [Histamine H2 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.34Float%
69Outcome [Histamine H3 ]The assay outcome, one of Inactive or Active.35histamine H3 receptor [Homo sapiens]Outcome
70Inhibition at 10 uM [Histamine H3 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.35Float%
71Outcome [Imidazoline I2, Central]The assay outcome, one of Inactive or Active.36alpha-2A adrenergic receptor [Rattus norvegicus]Outcome
72Inhibition at 10 uM [Imidazoline I2, Central] (10μM**)Value of average % inhibition at 10 uM compound concentration.36Float%
73Outcome [Interleukin IL-1 ]The assay outcome, one of Inactive or Active.37Outcome
74Inhibition at 10 uM [Interleukin IL-1 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.37Float%
75Outcome [Leukotriene, Cysteinyl CysLT1 ]The assay outcome, one of Inactive or Active.38cysteinyl leukotriene receptor 1 [Homo sapiens]Outcome
76Inhibition at 10 uM [Leukotriene, Cysteinyl CysLT1 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.38Float%
77Outcome [Melatonin MT1 ]The assay outcome, one of Inactive or Active.39melatonin receptor type 1A [Homo sapiens]Outcome
78Inhibition at 10 uM [Melatonin MT1 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.39Float%
79Outcome [Muscarinic M1 ]The assay outcome, one of Inactive or Active.40muscarinic acetylcholine receptor M1 [Homo sapiens]Outcome
80Inhibition at 10 uM [Muscarinic M1 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.40Float%
81Outcome [Muscarinic M2]The assay outcome, one of Inactive or Active.41cholinergic receptor, muscarinic 2 [Homo sapiens]Outcome
82Inhibition at 10 uM [Muscarinic M2] (10μM**)Value of average % inhibition at 10 uM compound concentration.41Float%
83Outcome [Muscarinic M3]The assay outcome, one of Inactive or Active.42Cholinergic receptor, muscarinic 3 [Homo sapiens]Outcome
84Inhibition at 10 uM [Muscarinic M3] (10μM**)Value of average % inhibition at 10 uM compound concentration.42Float%
85Outcome [Neuropeptide Y Y1 ]The assay outcome, one of Inactive or Active.43neuropeptide Y receptor type 1 [Homo sapiens]Outcome
86Inhibition at 10 uM [Neuropeptide Y Y1 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.43Float%
87Outcome [Neuropeptide Y Y2 ]The assay outcome, one of Inactive or Active.44neuropeptide Y receptor type 2 [Homo sapiens]Outcome
88Inhibition at 10 uM [Neuropeptide Y Y2 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.44Float%
89Outcome [Nicotinic Acetylcholine]The assay outcome, one of Inactive or Active.45cholinergic receptor, nicotinic, alpha 3, isoform CRA_a [Homo sapiens]Outcome
90Inhibition at 10 uM [Nicotinic Acetylcholine] (10μM**)Value of average % inhibition at 10 uM compound concentration.45Float%
91Outcome [Nicotinic Acetylcholine alpha 1, Bungarotoxin]The assay outcome, one of Inactive or Active.46cholinergic receptor, nicotinic, alpha 1 (muscle), isoform CRA_a [Homo sapiens]Outcome
92Inhibition at 10 uM [Nicotinic Acetylcholine alpha 1, Bungarotoxin] (10μM**)Value of average % inhibition at 10 uM compound concentration.46Float%
93Outcome [Opiate delat1 (OP1, DOP) ]The assay outcome, one of Inactive or Active.47delta-type opioid receptor [Homo sapiens]Outcome
94Inhibition at 10 uM [Opiate delat1 (OP1, DOP) ] (10μM**)Value of average % inhibition at 10 uM compound concentration.47Float%
95Outcome [Opiate kappa (OP2, KOP) ]The assay outcome, one of Inactive or Active.48kappa-type opioid receptor [Homo sapiens]Outcome
96Inhibition at 10 uM [Opiate kappa (OP2, KOP) ] (10μM**)Value of average % inhibition at 10 uM compound concentration.48Float%
97Outcome [Opiate mu (OP3, MOP)]The assay outcome, one of Inactive or Active.49mu-type opioid receptor isoform MOR-1B2 [Homo sapiens]Outcome
98Inhibition at 10 uM [Opiate mu (OP3, MOP)] (10μM**)Value of average % inhibition at 10 uM compound concentration.49Float%
99Outcome [Phorbol Ester]The assay outcome, one of Inactive or Active.50protein kinase C zeta type isoform b [Mus musculus]Outcome
100Inhibition at 10 uM [Phorbol Ester] (10μM**)Value of average % inhibition at 10 uM compound concentration.50Float%
101Outcome [Platelet Activating Factor (PAF) ]The assay outcome, one of Inactive or Active.51platelet-activating factor acetylhydrolase precursor [Homo sapiens]Outcome
102Inhibition at 10 uM [Platelet Activating Factor (PAF) ] (10μM**)Value of average % inhibition at 10 uM compound concentration.51Float%
103Outcome [Potassium Channel [KATP]]The assay outcome, one of Inactive or Active.52Calcium-activated potassium channel subunit beta-1 [Cricetulus griseus]Outcome
104Inhibition at 10 uM [Potassium Channel [KATP]] (10μM**)Value of average % inhibition at 10 uM compound concentration.52Float%
105Outcome [Potassium Channel hERG]The assay outcome, one of Inactive or Active.53voltage-gated potassium channel subfamily H isoform 3.1 [Homo sapiens]Outcome
106Inhibition at 10 uM [Potassium Channel hERG] (10μM**)Value of average % inhibition at 10 uM compound concentration.53Float%
107Outcome [Prostanoid EP4]The assay outcome, one of Inactive or Active.54Prostaglandin E receptor 4 (subtype EP4) [Homo sapiens]Outcome
108Inhibition at 10 uM [Prostanoid EP4] (10μM**)Value of average % inhibition at 10 uM compound concentration.54Float%
109Outcome [Purinergic P2X ]The assay outcome, one of Inactive or Active.55PREDICTED: purinergic receptor P2X2 isoform 1 [Oryctolagus cuniculus]Outcome
110Inhibition at 10 uM [Purinergic P2X ] (10μM**)Value of average % inhibition at 10 uM compound concentration.55Float%
111Outcome [Purinergic P2Y ]The assay outcome, one of Inactive or Active.56P2Y purinoceptor 1 [Rattus norvegicus]Outcome
112Inhibition at 10 uM [Purinergic P2Y ] (10μM**)Value of average % inhibition at 10 uM compound concentration.56Float%
113Outcome [Rolipram]The assay outcome, one of Inactive or Active.57high affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A [Rattus norvegicus]Outcome
114Inhibition at 10 uM [Rolipram] (10μM**)Value of average % inhibition at 10 uM compound concentration.57Float%
115Outcome [Serotonin (5-Hydroxytryptamine) 5-HT1A ]The assay outcome, one of Inactive or Active.585-hydroxytryptamine receptor 1A [Homo sapiens]Outcome
116Inhibition at 10 uM [Serotonin (5-Hydroxytryptamine) 5-HT1A ] (10μM**)Value of average % inhibition at 10 uM compound concentration.58Float%
117Outcome [Serotonin (5-Hydroxytryptamine) 5-HT2B]The assay outcome, one of Inactive or Active.595-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens]Outcome
118Inhibition at 10 uM [Serotonin (5-Hydroxytryptamine) 5-HT2B] (10μM**)Value of average % inhibition at 10 uM compound concentration.59Float%
119Outcome [Serotonin (5-Hydroxytryptamine) 5-HT3 ]The assay outcome, one of Inactive or Active.605-hydroxytryptamine receptor 3A isoform b precursor [Homo sapiens]Outcome
120Inhibition at 10 uM [Serotonin (5-Hydroxytryptamine) 5-HT3 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.60Float%
121Outcome [Sigma 1]The assay outcome, one of Inactive or Active.61opioid receptor, sigma 1 [Homo sapiens]Outcome
122Inhibition at 10 uM [Sigma 1] (10μM**)Value of average % inhibition at 10 uM compound concentration.61Float%
123Outcome [Tachykinin NK1 ]The assay outcome, one of Inactive or Active.62tachykinin receptor 1, isoform CRA_a [Homo sapiens]Outcome
124Inhibition at 10 uM [Tachykinin NK1 ] (10μM**)Value of average % inhibition at 10 uM compound concentration.62Float%
125Outcome [Thyroid Hormone ]The assay outcome, one of Inactive or Active.63thyroid hormone receptor alpha isoform TRalpha1 [Rattus norvegicus]Outcome
126Inhibition at 10 uM [Thyroid Hormone ] (10μM**)Value of average % inhibition at 10 uM compound concentration.63Float%
127Outcome [Transporter, Dopamine (DAT) ]The assay outcome, one of Inactive or Active.64sodium-dependent dopamine transporter [Homo sapiens]Outcome
128Inhibition at 10 uM [Transporter, Dopamine (DAT) ] (10μM**)Value of average % inhibition at 10 uM compound concentration.64Float%
129Outcome [Transporter, GABA ]The assay outcome, one of Inactive or Active.65sodium- and chloride-dependent GABA transporter 1 [Rattus norvegicus]Outcome
130Inhibition at 10 uM [Transporter, GABA ] (10μM**)Value of average % inhibition at 10 uM compound concentration.65Float%
131Outcome [Transporter, Norepinephrine (NET)]The assay outcome, one of Inactive or Active.66Net [Homo sapiens]Outcome
132Inhibition at 10 uM [Transporter, Norepinephrine (NET)] (10μM**)Value of average % inhibition at 10 uM compound concentration.66Float%
133Outcome [Transporter, Serotonin (5-Hydroxytryptamine) ]The assay outcome, one of Inactive or Active.67sodium-dependent serotonin transporter [Homo sapiens]Outcome
134Inhibition at 10 uM [Transporter, Serotonin (5-Hydroxytryptamine) ] (10μM**)Value of average % inhibition at 10 uM compound concentration.67Float%

** Test Concentration. § Panel component ID.
Additional Information
Grant Number: 1-X01-MH085709-01

Classification
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