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BioAssay: AID 540345

Late-stage counterscreen panel assay for GPR7 antagonists: Ricerca HitProfilingScreen + CYP450: Set 2

Name: Late-stage counterscreen panel assay for GPR7 antagonists: Ricerca HitProfilingScreen + CYP450: Set 2. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
AID: 540345
Data Source: The Scripps Research Institute Molecular Screening Center (GPR7_ANT_RICERCA HITPROFILING SCREEN_2X%INH_Set 2)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
BioAssay Version:
Deposit Date: 2011-08-12
Hold-until Date: 2012-03-01
Modify Date: 2012-03-01

Data Table ( Complete ):           All
Tested Compound:
Depositor Specified Assays
Show more
AIDNameTypeProbeComment
1861Fluorescence-based primary cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7).screening Primary screen (GPR7 antagonists in singlicate)
1880Summary of probe development efforts to identify antagonists of the G-protein coupled receptor 7 (GPR7).summary2 Summary (GPR7 antagonists)
1952Fluorescence-based confirmation cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7).screening Confirmation screen (GPR& antagonists in triplicate)
2148Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput screening assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1).screening Counterscreen (MCHR1 antagonists in triplicate)
2251Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7).confirmatory Dose response (GPR7 antagonists in triplicate)
2257Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1).confirmatory Dose response counterscreen (MCHR1 antagonists in triplicate)
463250Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1)confirmatory Dose response counterscreen (MCHR1 antagonists in triplicate)
463251Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7)confirmatory Dose response (GPR7 antagonists in triplicate)
463253Late-stage luminescence-based cell-based dose response assay to identify antagonists of the G-protein coupled receptor 7 (GPR7): Cytotoxicity assayconfirmatory Dose response counterscreen (Cytotoxicity in triplicate)
485339Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7): Intracellular calcium releaseconfirmatory Dose response (GPR7 antagonists in triplicate)
504868Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7) Set 2confirmatory Dose response (GPR7 antagonists in triplicate)
504886Late-stage results from the probe development effort to identify antagonists of the G-protein coupled receptor 7 (GPR7): luminescence-based cell-based dose response counterscreen assay to determine cytotoxicity of antagonist compounds Set 2confirmatory Dose response counterscreen (Cytotoxicity in triplicate)
504889Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1) Set 2confirmatory Dose response counterscreen (MCHR1 antagonists in triplicate)
540365Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7) Set 3confirmatory
540371Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1) Set 3confirmatory
588562Late-stage fluorescence-based cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7): percent inhibitionother
588563Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1) Set 5confirmatory
588564Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7) Set 4confirmatory
588566Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7) Set 5confirmatory
588568Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1) Set 4confirmatory
588581Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1) Set 6confirmatory
588583Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7) Set 6confirmatory
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center
Affiliation: The Scripps Research Institute, TSRI
Assay Provider: Olivier Civelli, University of California, Irvine
Network: Molecular Library Probe Production Centers Network (MLPCN)
Grant Proposal Number 1-R03-DA026557-01
Grant Proposal PI: Olivier Civelli
External Assay ID: GPR7_ANT_RICERCA HITPROFILING SCREEN_2X%INH_Set 2

Name: Late-stage counterscreen panel assay for GPR7 antagonists: Ricerca HitProfilingScreen + CYP450: Set 2.

Description:

Heterotrimeric G-protein coupled receptors (GPCRs) are major targets for disease therapeutics, due in part to their broad tissue distribution, structural diversity, varied modes of action, and disease-associated mutations (1-4). For example, targeting of opiod receptors by opiates such as morphine is a widespread clinical application for GPCR modulation in pain management. The recently de-orphanized GPR7 (5) is localized predominantly in the cerebellum and prefrontal cortex (6), with additional expression in the pituitary, hippocampus, amygdala, and spinal cord (7-9). GPR7 is highly conserved in humans and rodents (6), and exhibits structural features of both GPCRs and somatostatin receptors (7). Studies identifying the energy-regulating neuropeptides Neuropeptide W (NPW) and Neuropeptide B (NPB) as endogenous ligands of GPR7 (5, 10), and the development of hyperphagia and obesity in male GPR7 knockout mice (11, 12), implicate GPR7 in feeding behavior. Additional studies identifying GPR7 expression in peripheral Schwann cells (13) and increased GPR7 expression in rat models and human patients with inflammation-associated neuropathic pain (11, 13), suggest a role for GPR7 in mediating the inflammatory pain response. The identification of modulators of GPR7 will provide useful tools to elucidate the diverse roles of this receptor in central neuropeptide signaling and nociception in general.

References:

1. Pan, H.L., Wu, Z.Z., Zhou, H.Y., Chen, S.R., Zhang, H.M., and Li, D.P., Modulation of pain transmission by G-protein-coupled receptors. Pharmacol Ther, 2008. 117(1): p. 141-61.
2. Lagerstrom, M.C. and Schioth, H.B., Structural diversity of G protein-coupled receptors and significance for drug discovery. Nat Rev Drug Discov, 2008. 7(4): p. 339-57.
3. Thompson, M.D., Cole, D.E., and Jose, P.A., Pharmacogenomics of G protein-coupled receptor signaling: insights from health and disease. Methods Mol Biol, 2008. 448: p. 77-107.
4. Bosier, B. and Hermans, E., Versatility of GPCR recognition by drugs: from biological implications to therapeutic relevance. Trends Pharmacol Sci, 2007. 28(8): p. 438-46.
5. Tanaka, H., Yoshida, T., Miyamoto, N., Motoike, T., Kurosu, H., Shibata, K., Yamanaka, A., Williams, S.C., Richardson, J.A., Tsujino, N., Garry, M.G., Lerner, M.R., King, D.S., O'Dowd, B.F., Sakurai, T., and Yanagisawa, M., Characterization of a family of endogenous neuropeptide ligands for the G protein-coupled receptors GPR7 and GPR8. Proc Natl Acad Sci U S A, 2003. 100(10): p. 6251-6.
6. O'Dowd, B.F., Scheideler, M.A., Nguyen, T., Cheng, R., Rasmussen, J.S., Marchese, A., Zastawny, R., Heng, H.H., Tsui, L.C., Shi, X., and et al., The cloning and chromosomal mapping of two novel human opioid-somatostatin-like receptor genes, GPR7 and GPR8, expressed in discrete areas of the brain. Genomics, 1995. 28(1): p. 84-91.
7. Brezillon, S., Lannoy, V., Franssen, J.D., Le Poul, E., Dupriez, V., Lucchetti, J., Detheux, M., and Parmentier, M., Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8. J Biol Chem, 2003. 278(2): p. 776-83.
8. Singh, G., Maguire, J.J., Kuc, R.E., Fidock, M., and Davenport, A.P., Identification and cellular localisation of NPW1 (GPR7) receptors for the novel neuropeptide W-23 by [125I]-NPW radioligand binding and immunocytochemistry. Brain Res, 2004. 1017(1-2): p. 222-6.
9. Lee, D.K., Nguyen, T., Porter, C.A., Cheng, R., George, S.R., and O'Dowd, B.F., Two related G protein-coupled receptors: the distribution of GPR7 in rat brain and the absence of GPR8 in rodents. Brain Res Mol Brain Res, 1999. 71(1): p. 96-103.
10. Fujii, R., Yoshida, H., Fukusumi, S., Habata, Y., Hosoya, M., Kawamata, Y., Yano, T., Hinuma, S., Kitada, C., Asami, T., Mori, M., Fujisawa, Y., and Fujino, M., Identification of a neuropeptide modified with bromine as an endogenous ligand for GPR7. J Biol Chem, 2002. 277(37): p. 34010-6.
11. Kelly, M.A., Beuckmann, C.T., Williams, S.C., Sinton, C.M., Motoike, T., Richardson, J.A., Hammer, R.E., Garry, M.G., and Yanagisawa, M., Neuropeptide B-deficient mice demonstrate hyperalgesia in response to inflammatory pain. Proc Natl Acad Sci U S A, 2005. 102(28): p. 9942-7.
12. Ishii, M., Fei, H., and Friedman, J.M., Targeted disruption of GPR7, the endogenous receptor for neuropeptides B and W, leads to metabolic defects and adult-onset obesity. Proc Natl Acad Sci U S A, 2003. 100(18): p. 10540-5.
13. Zaratin, P.F., Quattrini, A., Previtali, S.C., Comi, G., Hervieu, G., and Scheideler, M.A., Schwann cell overexpression of the GPR7 receptor in inflammatory and painful neuropathies. Mol Cell Neurosci, 2005. 28(1): p. 55-63.

Keywords:

Late stage, late stage AID, powders, GPR7, NPBWR1, G-protein coupled receptor 7, pain, feeding, antagonist, antagonism, inhibitor, inhibition, counterscreen, panel assay, Ricerca, HitProfilingScreen, Sf9 cells, radioligand binding, Scripps, The Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN.
Panel Information
Assays
    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1CYP450, 1A21cytochrome P450, family 1, subfamily A, polypeptide 2 [Homo sapiens] [gi:119619719]
Taxonomy id: 9606
Gene id: 1544
2CYP450, 2C191cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:55665398]
Taxonomy id: 9606
Gene id: 1557
3CYP450, 2C91Cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] [gi:115529027]
Taxonomy id: 9606
Gene id: 1559
4CYP450, 2D61Cytochrome P450, family 2, subfamily D, polypeptide 6 [Homo sapiens] [gi:117558701]
Taxonomy id: 9606
Gene id: 1565
5CYP450, 3A41cytochrome P450 family 3 subfamily A polypeptide 4 [Homo sapiens] [gi:115371803]
Taxonomy id: 9606
Gene id: 1576
6Adenosine A11adenosine A1 receptor [Homo sapiens] [gi:119611871]
Taxonomy id: 9606
Gene id: 134
7Adenosine A2A1adenosine A2a receptor [Homo sapiens] [gi:119580062]
Taxonomy id: 9606
Gene id: 135
8Adrenergic alpha1A1adrenergic receptor, alpha 1a [Rattus norvegicus] [gi:149030335]
Taxonomy id: 10116
Gene id: 29412
9Adrenergic alpha1B1Adrenergic, alpha-1B-, receptor [Homo sapiens] [gi:187953275]
Taxonomy id: 10116
Gene id: 147
10Adrenergic alpha2A1alpha-2A adrenergic receptor [Homo sapiens] [gi:194353970]
Taxonomy id: 9606
Gene id: 150
11Adrenergic beta11adrenergic, beta-1-, receptor [Homo sapiens] [gi:166706747]
Taxonomy id: 9606
Gene id: 153
12Adrenergic beta21Adrenergic, beta-2-, receptor, surface [Homo sapiens] [gi:127798637]
Taxonomy id: 9606
Gene id: 154
13Calcium Channel L-Type, Dihydropyridine1voltage-dependent calcium channel subunit alpha-2/delta-1 isoform 2 [Rattus norvegicus] [gi:161086906]
Taxonomy id: 10116
Gene id: 25399
14Cannabinoid CB11cannabinoid receptor [Homo sapiens] [gi:67550212]
Taxonomy id: 9606
Gene id: 1268
15Dopamine D11Dopamine receptor D1 [Homo sapiens] [gi:67677841]
Taxonomy id: 9606
Gene id: 1812
16Dopamine D2S1dopamine receptor D2 isoform short [Homo sapiens] [gi:197692661]
Taxonomy id: 9606
Gene id: 1813
17GABAA, Flunitrazepam, Central1gamma-aminobutyric acid A receptor, gamma 2 [Rattus norvegicus] [gi:149052302]
Taxonomy id: 10116
Gene id: 29709
18GABAA, Muscimol, Central1testis gamma-aminobutyric acid receptor subunit beta 3 [Rattus norvegicus] [gi:53765741]
Taxonomy id: 10116
Gene id: 24922
19Glutamate, NMDA, Phencyclidine1glutamate receptor, ionotropic, N-methyl D-aspartate 1, isoform CRA_h [Rattus norvegicus] [gi:149039393]
Taxonomy id: 10116
Gene id: 24408
20Histamine H11histamine H1 receptor [Homo sapiens] [gi:149158709]
Taxonomy id: 9606
Gene id: 3269
21Imidazoline I2, Central1Taxonomy id: 10116
22Muscarinic M21cholinergic receptor, muscarinic 2 [Homo sapiens] [gi:119604271]
Taxonomy id: 9606
Gene id: 1129
23Muscarinic M31Cholinergic receptor, muscarinic 3 [Homo sapiens] [gi:111306506]
Taxonomy id: 9606
Gene id: 1131
24Nicotinic Acetylcholine1cholinergic receptor, nicotinic, alpha 3, isoform CRA_a [Homo sapiens] [gi:119619563]
Taxonomy id: 9606
Gene id: 1136
25Nicotinic Acetylcholine alpha 1, Bungarotoxin1cholinergic receptor, nicotinic, alpha 1 (muscle), isoform CRA_a [Homo sapiens] [gi:119631533]
Taxonomy id: 9606
Gene id: 1134
26Opiate mu (OP3, MOP)1mu-type opioid receptor isoform MOR-1B2 [Homo sapiens] [gi:223718719]
Taxonomy id: 9606
Gene id: 4988
27Phorbol Ester1Taxonomy id: 10090
28Potassium Channel [KATP]1Taxonomy id: 10036
29Potassium Channel hERG1voltage-gated potassium channel subfamily H isoform 3.1 [Homo sapiens] [gi:237862038]
Taxonomy id: 9606
Gene id: 3757
30Prostanoid EP41Prostaglandin E receptor 4 (subtype EP4) [Homo sapiens] [gi:109731195]
Taxonomy id: 9606
Gene id: 5734
31Rolipram1Taxonomy id: 10116
32Serotonin (5-Hydroxytryptamine) 5-HT2B15-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] [gi:119591355]
Taxonomy id: 9606
Gene id: 3357
33Sigma 11opioid receptor, sigma 1 [Homo sapiens] [gi:123231939]
Taxonomy id: 9606
Gene id: 10280
34Sodium Channel, Site 21sodium channel, nonvoltage-gated 1 alpha [Rattus norvegicus] [gi:149049394]
Taxonomy id: 10116
Gene id: 25122
35Transporter, Norepinephrine (NET)1Net [Homo sapiens] [gi:531523]
Taxonomy id: 9606
Gene id: 2004

§ 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 GPR7 antagonist compound SID 110923218 displays affinity.

Protocol Summary:

Assays for CYP450, 1A2; CYP450, 2C19; CYP450, 2C9; CYP450, 2D6; and CYP450, 3A4 were enzyme assays using human recombinant insect Sf9 cells with 5 uM 3-cyano-7-ethoxycoumarin as substrate (except for CYP450, 3A4, which used 50 uM 7-benzyloxy-4-(trifluoromethyl)-coumarin as substrate). Detection was based on spectrofluorimetric quantitation of the enzymatic product produced. Assays for the other targets were radioligand binding assays.

A response of greater than or equal to 50% inhibition or stimulation is considered active. Negative inhibition represents a stimulation of binding.

List of Reagents:

Reagents were provided by Ricerca Biosciences, LLC.
Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1CYP450, 1A2 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.1cytochrome P450, family 1, subfamily A, polypeptide 2 [Homo sapiens]Float%
2CYP450, 1A2 (Outcome)The assay outcome, one of Inactive or Active.1Outcome
3CYP450, 2C19 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.2cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens]Float%
4CYP450, 2C19 (Outcome)The assay outcome, one of Inactive or Active.2Outcome
5CYP450, 2C9 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.3Cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens]Float%
6CYP450, 2C9 (Outcome)The assay outcome, one of Inactive or Active.3Outcome
7CYP450, 2D6 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.4Cytochrome P450, family 2, subfamily D, polypeptide 6 [Homo sapiens]Float%
8CYP450, 2D6 (Outcome)The assay outcome, one of Inactive or Active.4Outcome
9CYP450, 3A4 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.5cytochrome P450 family 3 subfamily A polypeptide 4 [Homo sapiens]Float%
10CYP450, 3A4 (Outcome)The assay outcome, one of Inactive or Active.5Outcome
11Adenosine A1 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.6adenosine A1 receptor [Homo sapiens]Float%
12Adenosine A1 (Outcome)The assay outcome, one of Inactive or Active.6Outcome
13Adenosine A2A (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.7adenosine A2a receptor [Homo sapiens]Float%
14Adenosine A2A (Outcome)The assay outcome, one of Inactive or Active.7Outcome
15Adrenergic alpha1A (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.8adrenergic receptor, alpha 1a [Rattus norvegicus]Float%
16Adrenergic alpha1A (Outcome)The assay outcome, one of Inactive or Active.8Outcome
17Adrenergic alpha1B (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.9Adrenergic, alpha-1B-, receptor [Homo sapiens]Float%
18Adrenergic alpha1B (Outcome)The assay outcome, one of Inactive or Active.9Outcome
19Adrenergic alpha2A (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.10alpha-2A adrenergic receptor [Homo sapiens]Float%
20Adrenergic alpha2A (Outcome)The assay outcome, one of Inactive or Active.10Outcome
21Adrenergic beta1 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.11adrenergic, beta-1-, receptor [Homo sapiens]Float%
22Adrenergic beta1 (Outcome)The assay outcome, one of Inactive or Active.11Outcome
23Adrenergic beta2 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.12Adrenergic, beta-2-, receptor, surface [Homo sapiens]Float%
24Adrenergic beta2 (Outcome)The assay outcome, one of Inactive or Active.12Outcome
25Calcium Channel L-Type, Dihydropyridine (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.13voltage-dependent calcium channel subunit alpha-2/delta-1 isoform 2 [Rattus norvegicus]Float%
26Calcium Channel L-Type, Dihydropyridine (Outcome)The assay outcome, one of Inactive or Active.13Outcome
27Cannabinoid CB1 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.14cannabinoid receptor [Homo sapiens]Float%
28Cannabinoid CB1 (Outcome)The assay outcome, one of Inactive or Active.14Outcome
29Dopamine D1 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.15Dopamine receptor D1 [Homo sapiens]Float%
30Dopamine D1 (Outcome)The assay outcome, one of Inactive or Active.15Outcome
31Dopamine D25 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.16dopamine receptor D2 isoform short [Homo sapiens]Float%
32Dopamine D25 (Outcome)The assay outcome, one of Inactive or Active.16Outcome
33GABAA, Flunitrazepam, Central (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.17gamma-aminobutyric acid A receptor, gamma 2 [Rattus norvegicus]Float%
34GABAA, Flunitrazepam, Central (Outcome)The assay outcome, one of Inactive or Active.17Outcome
35GABAA, Muscimol, Central (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.18testis gamma-aminobutyric acid receptor subunit beta 3 [Rattus norvegicus]Float%
36GABAA, Muscimol, Central (Outcome)The assay outcome, one of Inactive or Active.18Outcome
37Glutamate, NMDA, Phencyclidine (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.19glutamate receptor, ionotropic, N-methyl D-aspartate 1, isoform CRA_h [Rattus norvegicus]Float%
38Glutamate, NMDA, Phencyclidine (Outcome)The assay outcome, one of Inactive or Active.19Outcome
39Histamine H1 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.20histamine H1 receptor [Homo sapiens]Float%
40Histamine H1 (Outcome)The assay outcome, one of Inactive or Active.20Outcome
41Imidazoline I2, Central (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.21Float%
42Imidazoline I2, Central (Outcome)The assay outcome, one of Inactive or Active.21Outcome
43Muscarinic M2 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.22cholinergic receptor, muscarinic 2 [Homo sapiens]Float%
44Muscarinic M2 (Outcome)The assay outcome, one of Inactive or Active.22Outcome
45Muscarinic M3 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.23Cholinergic receptor, muscarinic 3 [Homo sapiens]Float%
46Muscarinic M3 (Outcome)The assay outcome, one of Inactive or Active.23Outcome
47Nicotinic Acetylcholine (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.24cholinergic receptor, nicotinic, alpha 3, isoform CRA_a [Homo sapiens]Float%
48Nicotinic Acetylcholine (Outcome)The assay outcome, one of Inactive or Active.24Outcome
49Nicotinic Acetylcholine alpha 1, Bungarotoxin (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.25cholinergic receptor, nicotinic, alpha 1 (muscle), isoform CRA_a [Homo sapiens]Float%
50Nicotinic Acetylcholine alpha 1, Bungarotoxin (Outcome)The assay outcome, one of Inactive or Active.25Outcome
51Opiate mu (OP3, MOP) (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.26mu-type opioid receptor isoform MOR-1B2 [Homo sapiens]Float%
52Opiate mu (OP3, MOP) (Outcome)The assay outcome, one of Inactive or Active.26Outcome
53Phorbol Ester (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.27Float%
54Phorbol Ester (Outcome)The assay outcome, one of Inactive or Active.27Outcome
55Potassium Channel [KATP] (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.28Float%
56Potassium Channel [KATP] (Outcome)The assay outcome, one of Inactive or Active.28Outcome
57Potassium Channel hERG (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.29voltage-gated potassium channel subfamily H isoform 3.1 [Homo sapiens]Float%
58Potassium Channel hERG (Outcome)The assay outcome, one of Inactive or Active.29Outcome
59Prostanoid EP4 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.30Prostaglandin E receptor 4 (subtype EP4) [Homo sapiens]Float%
60Prostanoid EP4 (Outcome)The assay outcome, one of Inactive or Active.30Outcome
61Rolipram (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.31Float%
62Rolipram (Outcome)The assay outcome, one of Inactive or Active.31Outcome
63Serotonin (5-Hydroxytryptamine) 5-HT2B (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.325-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens]Float%
64Serotonin (5-Hydroxytryptamine) 5-HT2B (Outcome)The assay outcome, one of Inactive or Active.32Outcome
65Sigma 1 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.33opioid receptor, sigma 1 [Homo sapiens]Float%
66Sigma 1 (Outcome)The assay outcome, one of Inactive or Active.33Outcome
67Sodium Channel, Site 2 (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.34sodium channel, nonvoltage-gated 1 alpha [Rattus norvegicus]Float%
68Sodium Channel, Site 2 (Outcome)The assay outcome, one of Inactive or Active.34Outcome
69Transporter, Norepinephrine (NET) (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.35Net [Homo sapiens]Float%
70Transporter, Norepinephrine (NET) (Outcome)The assay outcome, one of Inactive or Active.35Outcome

** Test Concentration. § Panel component ID.
Additional Information
Grant Number: 1-R03-DA026557-01

Classification
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