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BioAssay: AID 652083

Late-stage results from the probe development effort to identify antagonists of OPRK1: CEREP radiometric-based biochemical counterscreen panel assay

Name: Late-stage results from the probe development effort to identify antagonists of OPRK1: CEREP radiometric-based biochemical counterscreen panel assay. ..more
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 Tested Compounds
 Tested Compounds
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Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
AID: 652083
Data Source: The Scripps Research Institute Molecular Screening Center (OPRK1_ANT_CEREP SCREEN_RAD_2X%INH)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
BioAssay Version:
Deposit Date: 2013-03-05
Hold-until Date: 2013-10-21
Modify Date: 2013-10-21

Data Table ( Complete ):           View All Data
Tested Compound:
Related Experiments
Show more
AIDNameTypeComment
652031Maybridge screen to identify antagonists of kappa opioid receptor 1 (OPRK1): fluorescence-based cell-based assayScreeningdepositor-specified cross reference: Maybridge screen (OPRK1 inhibitors in singlicate)
652032Late-stage results from the probe development effort to identify antagonists of OPRK1: fluorescence-based cell-based dose response assayConfirmatorydepositor-specified cross reference: Late-stage dose response (OPRK1 antagonists in quadruplicate)
652033Late-stage results from the probe development effort to identify antagonists of OPRK1: fluorescence-based cell-based dose response OPRD1 counterscreenConfirmatorydepositor-specified cross reference: Late-stage dose response counterscreen (OPRD1 antagonists in quadruplicate)
652034Late-stage results from the probe development effort to identify antagonists of OPRK1: luminescence-based cell-based dose response OPRM1 counterscreenConfirmatorydepositor-specified cross reference: Late-stage dose response counterscreen (OPRM1 antagonists in quadruplicate)
652045Summary of the probe development efforts to identify antagonists of the kappa 1 (OPRK1) opioid receptorSummarydepositor-specified cross reference: Summary (OPRK1 antagonists)
652108Late-stage results from the probe development effort to identify antagonists of OPRK1: In vivo tail flick assayOtherdepositor-specified cross reference
652075Late-stage results from the probe development effort to identify antagonists of OPRK1: radiometric-based biochemical hERG counterscreen assayOthersame project related to Summary assay
652076Late-stage results from the probe development effort to identify antagonists of OPRK1: LCMS-based biochemical cytochrome P450 inhibition assayOthersame project related to Summary assay
652077Late-stage fluorescence-based cell-based dose response assay for antagonists of kappa opioid receptor 1 (OPRK1)Confirmatorysame project related to Summary assay
652078Late-stage results from the probe development effort to identify antagonists of OPRK1: LCMS-based pharmacokinetic plasma protein binding assayOthersame project related to Summary assay
652079Late-stage counterscreen for antagonists of kappa opioid receptor 1 (OPRK1): fluorescence-based cell-based dose response assay to identify antagonists of Sphingosine 1-Phosphate Receptor 1 (S1P1)Confirmatorysame project related to Summary assay
652080Late-stage results from the probe development effort to identify antagonists of OPRK1: fluorescence-based cell-based dose response OPRD1 counterscreen, Set 2Confirmatorysame project related to Summary assay
652081Late-stage results from the probe development effort to identify antagonists of OPRK1: luminescence-based cell-based dose response OPRM1 counterscreen, Set 2Confirmatorysame project related to Summary assay
652082Fluorescence-based cell-based confirmation assay for antagonists of kappa opioid receptor 1 (OPRK1)Othersame project related to Summary assay
652084Late-stage results from the probe development effort to identify antagonists of OPRK1: fluorescence-based cell-based dose response assay, Set 2.Confirmatorysame project related to Summary assay
652085Late-stage results from the probe development effort to identify antagonists of OPRK1: LCMS-based in vivo plasma and brain levelsOthersame project related to Summary assay
652086Late-stage results from the probe development effort to identify antagonists of OPRK1: luminescence-based cell-based dose response counterscreen assay to determine cytotoxicity of test compoundsConfirmatorysame project related to Summary assay
652087Counterscreen for antagonists of kappa opioid receptor 1 (OPRK1): fluorescence-based cell-based assay to identify antagonists of Sphingosine 1-Phosphate Receptor 1 (S1P1)Othersame project related to Summary assay
652088Late-stage results from the probe development effort to identify antagonists of OPRK1: LCMS-based biochemical hepatic microsome stability assayOthersame project related to Summary assay
652113Late-stage results from the probe development effort to identify antagonists of OPRK1: LCMS-based parallel artificial membrane permeability (PAMPA) assayOthersame project related to Summary assay
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC)
Affiliation: The Scripps Research Institute, TSRI
Assay Provider: Lakshmi A. Devi, Mount Sinai School of Medicine
Network: Molecular Library Probe Production Centers Network (MLPCN)
Grant Proposal Number: R03NS053751
Grant Proposal PI: Lakshmi A. Devi, Mount Sinai School of Medicine
External Assay ID: OPRK1_ANT_CEREP SCREEN_RAD_2X%INH

Name: Late-stage results from the probe development effort to identify antagonists of OPRK1: CEREP radiometric-based biochemical counterscreen panel assay.

Description:

Potent and selective OPRK antagonists will be useful for studying the mechanisms involved in OPRK-mediated analgesia and may have therapeutic value as novel analgesics with an improved side effect profile to currently available drugs. Studies have identified a role for dynorphin and OPRK stimulation in neuropathic pain (1). The dynorphins act as endogenous agonists at the opioid receptors, including OPRK (2), and the increased dynorphin expression in neuropathic pain also leads to a sustained activation of OPRK (1, 3). The mechanisms and neural circuits in OPRK-mediated analgesia are active areas of study; it is hoped those studies will assist in the development of novel analgesics that bypass OPRK-mediated depression (4-5). A role for dynorphin/OPRK in modulating drug addiction has been proposed (for review, see (6-7)). The function of dynorphin/OPRK systems in addiction appears to be diverse, and may modulate drug-seeking behavior depending on factors such as drug history, pattern of intake, and stress (for review, see (6)). The availability of potent and selective OPRK ligands may help unravel these mechanisms, as well as prove to be of therapeutic utility. Evidence from preclinical studies indicates that the dynorphin/OPRK system may be dysregulated in affective psychiatric disorders (for review, see (6, 8)). However, solid evidence from clinical studies is lacking. There is increasing evidence for a potential involvement of dynorphin/OPRK in schizophrenia; OPRK agonists appear to induce symptoms in humans and animals that are present in schizophrenia (8-10). Thus, the availability of new research tools such as potent and selective OPRK antagonists will facilitate understanding the physiological and pathophysiological mechanisms of dynorphin/OPRK systems and their roles in psychiatric disease in humans.

References:

1. Xu, M., et al., Neuropathic pain activates the endogenous kappa opioid system in mouse spinal cord and induces opioid receptor tolerance. J Neurosci, 2004. 24(19): p. 4576-84.
2. Chavkin, C., I.F. James, and A. Goldstein, Dynorphin is a specific endogenous ligand of the kappa opioid receptor. Science, 1982. 215(4531): p. 413-5.
3. Xu, M., et al., Sciatic nerve ligation-induced proliferation of spinal cord astrocytes is mediated by kappa opioid activation of p38 mitogen-activated protein kinase. J Neurosci, 2007. 27(10): p. 2570-81.
4. Al-Hasani, R. and M.R. Bruchas, Molecular mechanisms of opioid receptor-dependent signaling and behavior. Anesthesiology, 2011. 115(6): p. 1363-81.
5. Muschamp, J.W., A. Van't Veer, and W.A. Carlezon, Jr., Tracking down the molecular substrates of stress: new roles for p38alpha MAPK and kappa-opioid receptors. Neuron, 2011. 71(3): p. 383-5.
6. Tejeda, H.A., T.S. Shippenberg, and R. Henriksson, The dynorphin/kappa-opioid receptor system and its role in psychiatric disorders. Cell Mol Life Sci, 2012. 69(6): p. 857-96.
7. Yoo, J.H., I. Kitchen, and A. Bailey, The endogenous opioid system in cocaine addiction: what lessons have opioid peptide and receptor knockout mice taught us? Br J Pharmacol, 2012. 166(7): p. 1993-2014.
8. Schwarzer, C., 30 years of dynorphins--new insights on their functions in neuropsychiatric diseases. Pharmacol Ther, 2009. 123(3): p. 353-70.
9. Bortolato, M. and M.V. Solbrig, The price of seizure control: dynorphins in interictal and postictal psychosis. Psychiatry Res, 2007. 151(1-2): p. 139-43.
10. Sheffler, D.J. and B.L. Roth, Salvinorin A: the "magic mint" hallucinogen finds a molecular target in the kappa opioid receptor. Trends Pharmacol Sci, 2003. 24(3): p. 107-9.

Keywords:

Late stage, late stage AID, OPRK1, kappa, opioid, receptor, GPCR, CEREP, panel, panel screen, radiometric, counterscreen, receptors, transporters, ion channels, antagonist, inhibitor, inhibit, pain, analgesic, dynorphin, neuropathic pain, drug addiction, addiction, 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
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 A31RecName: Full=Adenosine receptor A3 [gi:1351831]
Taxonomy id: 9606
Gene id: 140
4Adrenergic alpha 1 (non-selective)1Taxonomy id: 10116
5Adrenergic alpha 2 (non-selective)1Taxonomy id: 10116
6Adrenergic beta 11adrenergic, beta-1-, receptor [Homo sapiens] [gi:166706747]
Taxonomy id: 9606
Gene id: 153
7Adrenergic beta 21Adrenergic, beta-2-, receptor, surface [Homo sapiens] [gi:127798637]
Taxonomy id: 9606
Gene id: 154
8Angiotensin receptor 11Angiotensin II receptor, type 1 [Homo sapiens] [gi:46250427]
Taxonomy id: 9606
Gene id: 185
9BZD (central)1Taxonomy id: 10116
Gene id: 25045
10Bradykinin receptor 21B2 bradykinin receptor [Homo sapiens] [gi:4557359]
Taxonomy id: 9606
Gene id: 624
11Cannabinoid CB11cannabinoid receptor [Homo sapiens] [gi:67550212]
Taxonomy id: 9606
Gene id: 1268
12Cholecystokinin A receptor1cholecystokinin receptor type A [Homo sapiens] [gi:4502607]
Taxonomy id: 9606
Gene id: 886
13Dopamine D11Dopamine receptor D1 [Homo sapiens] [gi:67677841]
Taxonomy id: 9606
Gene id: 1812
14Dopamine D2S1dopamine receptor D2 isoform short [Homo sapiens] [gi:197692661]
Taxonomy id: 9606
Gene id: 1813
15Endothelin receptor A1Endothelin receptor type A [Homo sapiens] [gi:18490298]
Taxonomy id: 9606
Gene id: 1909
16GABA (non-selective)1Taxonomy id: 10116
17Galanin receptor 21galanin receptor type 2 [Homo sapiens] [gi:4503905]
Taxonomy id: 9606
Gene id: 8811
18CXCR2 (IL-8B)1C-X-C chemokine receptor type 2 [Homo sapiens] [gi:4504683]
Taxonomy id: 9606
Gene id: 3579
19CCR11chemokine (C-C motif) receptor 1 [Homo sapiens] [gi:54696680]
Taxonomy id: 9606
Gene id: 1230
20Histamine H11histamine H1 receptor [Homo sapiens] [gi:149158709]
Taxonomy id: 9606
Gene id: 3269
21Histamine H21histamine receptor H2 [Homo sapiens] [gi:119581773]
Taxonomy id: 9606
Gene id: 3274
22Melanocortin receptor MC41melanocortin receptor 4 [Homo sapiens] [gi:119508433]
Taxonomy id: 9606
Gene id: 4160
23Melatonin receptor MT11melatonin receptor type 1A [Homo sapiens] [gi:5174593]
Taxonomy id: 9606
Gene id: 4543
24Muscarinic receptor M11muscarinic acetylcholine receptor M1 [Homo sapiens] [gi:37622910]
Taxonomy id: 9606
Gene id: 1128
25Muscarinic receptor M21cholinergic receptor, muscarinic 2 [Homo sapiens] [gi:119604271]
Taxonomy id: 9606
Gene id: 1129
26Muscarinic receptor M31Cholinergic receptor, muscarinic 3 [Homo sapiens] [gi:111306506]
Taxonomy id: 9606
Gene id: 1131
27Tachykinin receptor NK21Tachykinin receptor 2 [Homo sapiens] [gi:67678462]
Taxonomy id: 9606
Gene id: 6865
28Tachykinin receptor NK31tachykinin receptor 3 [Homo sapiens] [gi:119626578]
Taxonomy id: 9606
Gene id: 6870
29Neuropeptide receptor Y11neuropeptide Y receptor type 1 [Homo sapiens] [gi:4505445]
Taxonomy id: 9606
Gene id: 4886
30Neuropeptide receptor Y21neuropeptide Y receptor type 2 [Homo sapiens] [gi:4505447]
Taxonomy id: 9606
Gene id: 4887
31Neurotensin receptor 11neurotensin receptor type 1 [Homo sapiens] [gi:110611243]
Taxonomy id: 9606
Gene id: 4923
32delta 2 (DOP)1delta-type opioid receptor [Homo sapiens] [gi:63477962]
Taxonomy id: 9606
Gene id: 4985
33kappa (KOP)1kappa-type opioid receptor [Rattus norvegicus] [gi:8393879]
Taxonomy id: 10116
Gene id: 29335
34mu (MOP)1Opioid receptor, mu 1 [Homo sapiens] [gi:50959650]
Taxonomy id: 9606
Gene id: 4988
35NOP (ORL1)1OPRL1 protein [Homo sapiens] [gi:23468341]
Taxonomy id: 9606
Gene id: 4987
36Serotonin 5-HT1a15-hydroxytryptamine receptor 1A [Homo sapiens] [gi:55956923]
Taxonomy id: 9606
Gene id: 3350
37Serotonin 5-HT1b15-hydroxytryptamine receptor 1B [Rattus norvegicus] [gi:11560016]
Taxonomy id: 10116
Gene id: 25075
38Serotonin 5-HT2A15-hydroxytryptamine receptor 2A isoform 2 [Homo sapiens] [gi:260099679]
Taxonomy id: 9606
Gene id: 3356
39Serotonin 5-HT2B15-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] [gi:119591355]
Taxonomy id: 9606
Gene id: 3357
40Serotonin 5-HT315-hydroxytryptamine (serotonin) receptor 3A [Homo sapiens] [gi:37514834]
Taxonomy id: 9606
Gene id: 3359
41Serotonin 5-HT5A15-hydroxytryptamine receptor 5A [Homo sapiens] [gi:13236497]
Taxonomy id: 9606
Gene id: 3361
42Serotonin 5-HT615-hydroxytryptamine (serotonin) receptor 6 [Homo sapiens] [gi:119615302]
Taxonomy id: 9606
Gene id: 3362
43Serotonin 5-HT71serotonin 5-HT7 receptor protein [Homo sapiens] [gi:413866]
Taxonomy id: 9606
Gene id: 3362
44Somatostatin sst (non-selective)1somatostatin [Mus musculus] [gi:148665257]
Taxonomy id: 10090
Gene id: 20604
45Vasoactive intestinal peptide receptor 11Vasoactive intestinal peptide receptor 1 [Homo sapiens] [gi:39963603]
Taxonomy id: 9606
Gene id: 7433
46Arginine vasopressin receptor 1A1vasopressin V1a receptor [Homo sapiens] [gi:4502331]
Taxonomy id: 9606
Gene id: 522
47Ca2+ channel (L, verapamil site) (phenylalkylamine)1voltage-dependent L-type calcium channel subunit alpha-1C [Rattus norvegicus] [gi:158186633]
Taxonomy id: 10116
Gene id: 24239
48KV channel1Taxonomy id: 10116
49SKCa channelTaxonomy id: 10116
50Na+ channel (site 2)1Taxonomy id: 10116
51Cl# channel (GABA-gated)1Taxonomy id: 10116
52Norepinephrine transporter1Net [Homo sapiens] [gi:531523]
Taxonomy id: 9606
Gene id: 2004
53Dopamine transporter1Taxonomy id: 9606
545-HT transporter1Taxonomy id: 9606

§ Panel component ID.
Protocol
Assay Overview:

The purpose of this panel of binding assays performed by CEREP, is to identify a subset of potential receptors, transporters, ion channels, etc. for which the OPRK antagonist compound SID 144087319 displays affinity. Assays were run in duplicate.

Protocol Summary:

The panel assays were radioligand binding assays performed by CEREP. The specific ligand binding to the targets is defined as the difference between the total binding in the presence of 10 uM test compound and the nonspecific binding determined in the presence of 10 uM compound and an excess of unlabelled ligand. The results are expressed as a percent inhibition of control specific binding:

%_Inhibition = 100 - ( ( [measured_specific_binding] / [control_specific_binding] ) x 100 )

PubChem Activity Outcome and Score:

The following applies to each panel in this assay:

A response of >= 50% inhibition or stimulation is considered active. Negative inhibition represents a stimulation of binding.

List of Reagents:

Reagents were provided by CEREP.
Comment
This assay was performed by CEREP.
Categorized Comment - additional comments and annotations
From PubChem:
Assay Format: Biochemical
Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Outcome [Adenosine A1]One of Active, Inactive, or Not Tested1adenosine A1 receptor [Homo sapiens]Outcome
2Radioligand Type [Adenosine A1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist1String
3Inhibition at 10 uM [Adenosine A1] (10μM**)Value of % Inhibition at 10 uM compound concentration.1Float%
4Outcome [Adenosine A2A]One of Active, Inactive, or Not Tested2adenosine A2a receptor [Homo sapiens]Outcome
5Radioligand Type [Adenosine A2A]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist2String
6Inhibition at 10 uM [Adenosine A2A] (10μM**)Value of % Inhibition at 10 uM compound concentration.2Float%
7Outcome [Adenosine A3]One of Active, Inactive, or Not Tested3RecName: Full=Adenosine receptor A3Outcome
8Radioligand Type [Adenosine A3]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist3String
9Inhibition at 10 uM [Adenosine A3] (10μM**)Value of % Inhibition at 10 uM compound concentration.3Float%
10Outcome [Adrenergic alpha 1 (non-selective)]One of Active, Inactive, or Not Tested4Outcome
11Radioligand Type [Adrenergic alpha 1 (non-selective)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist4String
12Inhibition at 10 uM [Adrenergic alpha 1 (non-selective)] (10μM**)Value of % Inhibition at 10 uM compound concentration.4Float%
13Outcome [Adrenergic alpha 2 (non-selective)]One of Active, Inactive, or Not Tested5Outcome
14Radioligand Type [Adrenergic alpha 2 (non-selective)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist5String
15Inhibition at 10 uM [Adrenergic alpha 2 (non-selective)] (10μM**)Value of % Inhibition at 10 uM compound concentration.5Float%
16Outcome [Adrenergic beta 1]One of Active, Inactive, or Not Tested6adrenergic, beta-1-, receptor [Homo sapiens]Outcome
17Radioligand Type [Adrenergic beta 1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist6String
18Inhibition at 10 uM [Adrenergic beta 1] (10μM**)Value of % Inhibition at 10 uM compound concentration.6Float%
19Outcome [Adrenergic beta 2]One of Active, Inactive, or Not Tested7Adrenergic, beta-2-, receptor, surface [Homo sapiens]Outcome
20Radioligand Type [Adrenergic beta 2]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist7String
21Inhibition at 10 uM [Adrenergic beta 2] (10μM**)Value of % Inhibition at 10 uM compound concentration.7Float%
22Outcome [Angiotensin receptor 1]One of Active, Inactive, or Not Tested8Angiotensin II receptor, type 1 [Homo sapiens]Outcome
23Radioligand Type [Angiotensin receptor 1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist8String
24Inhibition at 10 uM [Angiotensin receptor 1] (10μM**)Value of % Inhibition at 10 uM compound concentration.8Float%
25Outcome [BZD (central)]One of Active, Inactive, or Not Tested9Outcome
26Radioligand Type [BZD (central)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist9String
27Inhibition at 10 uM [BZD (central)] (10μM**)Value of % Inhibition at 10 uM compound concentration.9Float%
28Outcome [Bradykinin receptor 2]One of Active, Inactive, or Not Tested10B2 bradykinin receptor [Homo sapiens]Outcome
29Radioligand Type [Bradykinin receptor 2]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist10String
30Inhibition at 10 uM [Bradykinin receptor 2] (10μM**)Value of % Inhibition at 10 uM compound concentration.10Float%
31Outcome [Cannabinoid CB1]One of Active, Inactive, or Not Tested11cannabinoid receptor [Homo sapiens]Outcome
32Radioligand Type [Cannabinoid CB1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist11String
33Inhibition at 10 uM [Cannabinoid CB1] (10μM**)Value of % Inhibition at 10 uM compound concentration.11Float%
34Outcome [Cholecystokinin A receptor]One of Active, Inactive, or Not Tested12cholecystokinin receptor type A [Homo sapiens]Outcome
35Radioligand Type [Cholecystokinin A receptor]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist12String
36Inhibition at 10 uM [Cholecystokinin A receptor] (10μM**)Value of % Inhibition at 10 uM compound concentration.12Float%
37Outcome [Dopamine D1]One of Active, Inactive, or Not Tested13Dopamine receptor D1 [Homo sapiens]Outcome
38Radioligand Type [Dopamine D1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist13String
39Inhibition at 10 uM [Dopamine D1] (10μM**)Value of % Inhibition at 10 uM compound concentration.13Float%
40Outcome [Dopamine D2S]One of Active, Inactive, or Not Tested14dopamine receptor D2 isoform short [Homo sapiens]Outcome
41Radioligand Type [Dopamine D2S]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist14String
42Inhibition at 10 uM [Dopamine D2S] (10μM**)Value of % Inhibition at 10 uM compound concentration.14Float%
43Outcome [Endothelin receptor A]One of Active, Inactive, or Not Tested15Endothelin receptor type A [Homo sapiens]Outcome
44Radioligand Type [Endothelin receptor A]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist15String
45Inhibition at 10 uM [Endothelin receptor A] (10μM**)Value of % Inhibition at 10 uM compound concentration.15Float%
46Outcome [GABA (non-selective)]One of Active, Inactive, or Not Tested16Outcome
47Radioligand Type [GABA (non-selective)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist16String
48Inhibition at 10 uM [GABA (non-selective)] (10μM**)Value of % Inhibition at 10 uM compound concentration.16Float%
49Outcome [Galanin receptor 2]One of Active, Inactive, or Not Tested17galanin receptor type 2 [Homo sapiens]Outcome
50Radioligand Type [Galanin receptor 2]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist17String
51Inhibition at 10 uM [Galanin receptor 2] (10μM**)Value of % Inhibition at 10 uM compound concentration.17Float%
52Outcome [CXCR2 (IL-8B)]One of Active, Inactive, or Not Tested18C-X-C chemokine receptor type 2 [Homo sapiens]Outcome
53Radioligand Type [CXCR2 (IL-8B)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist18String
54Inhibition at 10 uM [CXCR2 (IL-8B)] (10μM**)Value of % Inhibition at 10 uM compound concentration.18Float%
55Outcome [CCR1]One of Active, Inactive, or Not Tested19chemokine (C-C motif) receptor 1 [Homo sapiens]Outcome
56Radioligand Type [CCR1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist19String
57Inhibition at 10 uM [CCR1] (10μM**)Value of % Inhibition at 10 uM compound concentration.19Float%
58Outcome [Histamine H1]One of Active, Inactive, or Not Tested20histamine H1 receptor [Homo sapiens]Outcome
59Radioligand Type [Histamine H1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist20String
60Inhibition at 10 uM [Histamine H1] (10μM**)Value of % Inhibition at 10 uM compound concentration.20Float%
61Outcome [Histamine H2]One of Active, Inactive, or Not Tested21histamine receptor H2 [Homo sapiens]Outcome
62Radioligand Type [Histamine H2]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist21String
63Inhibition at 10 uM [Histamine H2] (10μM**)Value of % Inhibition at 10 uM compound concentration.21Float%
64Outcome [Melanocortin receptor MC4]One of Active, Inactive, or Not Tested22melanocortin receptor 4 [Homo sapiens]Outcome
65Radioligand Type [Melanocortin receptor MC4]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist22String
66Inhibition at 10 uM [Melanocortin receptor MC4] (10μM**)Value of % Inhibition at 10 uM compound concentration.22Float%
67Outcome [Melatonin receptor MT1]One of Active, Inactive, or Not Tested23melatonin receptor type 1A [Homo sapiens]Outcome
68Radioligand Type [Melatonin receptor MT1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist23String
69Inhibition at 10 uM [Melatonin receptor MT1] (10μM**)Value of % Inhibition at 10 uM compound concentration.23Float%
70Outcome [Muscarinic receptor M1]One of Active, Inactive, or Not Tested24muscarinic acetylcholine receptor M1 [Homo sapiens]Outcome
71Radioligand Type [Muscarinic receptor M1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist24String
72Inhibition at 10 uM [Muscarinic receptor M1] (10μM**)Value of % Inhibition at 10 uM compound concentration.24Float%
73Outcome [Muscarinic receptor M2]One of Active, Inactive, or Not Tested25cholinergic receptor, muscarinic 2 [Homo sapiens]Outcome
74Radioligand Type [Muscarinic receptor M2]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist25String
75Inhibition at 10 uM [Muscarinic receptor M2] (10μM**)Value of % Inhibition at 10 uM compound concentration.25Float%
76Outcome [Muscarinic receptor M3]One of Active, Inactive, or Not Tested26Cholinergic receptor, muscarinic 3 [Homo sapiens]Outcome
77Radioligand Type [Muscarinic receptor M3]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist26String
78Inhibition at 10 uM [Muscarinic receptor M3] (10μM**)Value of % Inhibition at 10 uM compound concentration.26Float%
79Outcome [Tachykinin receptor NK2]One of Active, Inactive, or Not Tested27Tachykinin receptor 2 [Homo sapiens]Outcome
80Radioligand Type [Tachykinin receptor NK2]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist27String
81Inhibition at 10 uM [Tachykinin receptor NK2] (10μM**)Value of % Inhibition at 10 uM compound concentration.27Float%
82Outcome [Tachykinin receptor NK3]One of Active, Inactive, or Not Tested28tachykinin receptor 3 [Homo sapiens]Outcome
83Radioligand Type [Tachykinin receptor NK3]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist28String
84Inhibition at 10 uM [Tachykinin receptor NK3] (10μM**)Value of % Inhibition at 10 uM compound concentration.28Float%
85Outcome [Neuropeptide receptor Y1]One of Active, Inactive, or Not Tested29neuropeptide Y receptor type 1 [Homo sapiens]Outcome
86Radioligand Type [Neuropeptide receptor Y1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist29String
87Inhibition at 10 uM [Neuropeptide receptor Y1] (10μM**)Value of % Inhibition at 10 uM compound concentration.29Float%
88Outcome [Neuropeptide receptor Y2]One of Active, Inactive, or Not Tested30neuropeptide Y receptor type 2 [Homo sapiens]Outcome
89Radioligand Type [Neuropeptide receptor Y2]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist30String
90Inhibition at 10 uM [Neuropeptide receptor Y2] (10μM**)Value of % Inhibition at 10 uM compound concentration.30Float%
91Outcome [Neurotensin receptor 1]One of Active, Inactive, or Not Tested31neurotensin receptor type 1 [Homo sapiens]Outcome
92Radioligand Type [Neurotensin receptor 1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist31String
93Inhibition at 10 uM [Neurotensin receptor 1] (10μM**)Value of % Inhibition at 10 uM compound concentration.31Float%
94Outcome [delta 2 (DOP)]One of Active, Inactive, or Not Tested32delta-type opioid receptor [Homo sapiens]Outcome
95Radioligand Type [delta 2 (DOP)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist32String
96Inhibition at 10 uM [delta 2 (DOP)] (10μM**)Value of % Inhibition at 10 uM compound concentration.32Float%
97Outcome [kappa (KOP)]One of Active, Inactive, or Not Tested33kappa-type opioid receptor [Rattus norvegicus]Outcome
98Radioligand Type [kappa (KOP)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist33String
99Inhibition at 10 uM [kappa (KOP)] (10μM**)Value of % Inhibition at 10 uM compound concentration.33Float%
100Outcome [mu (MOP)]One of Active, Inactive, or Not Tested34Opioid receptor, mu 1 [Homo sapiens]Outcome
101Radioligand Type [mu (MOP)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist34String
102Inhibition at 10 uM [mu (MOP)] (10μM**)Value of % Inhibition at 10 uM compound concentration.34Float%
103Outcome [NOP (ORL1)]One of Active, Inactive, or Not Tested35OPRL1 protein [Homo sapiens]Outcome
104Radioligand Type [NOP (ORL1)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist35String
105Inhibition at 10 uM [NOP (ORL1)] (10μM**)Value of % Inhibition at 10 uM compound concentration.35Float%
106Outcome [Serotonin 5-HT1a]One of Active, Inactive, or Not Tested365-hydroxytryptamine receptor 1A [Homo sapiens]Outcome
107Radioligand Type [Serotonin 5-HT1a]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist36String
108Inhibition at 10 uM [Serotonin 5-HT1a] (10μM**)Value of % Inhibition at 10 uM compound concentration.36Float%
109Outcome [Serotonin 5-HT1b]One of Active, Inactive, or Not Tested375-hydroxytryptamine receptor 1B [Rattus norvegicus]Outcome
110Radioligand Type [Serotonin 5-HT1b]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist37String
111Inhibition at 10 uM [Serotonin 5-HT1b] (10μM**)Value of % Inhibition at 10 uM compound concentration.37Float%
112Outcome [Serotonin 5-HT2A]One of Active, Inactive, or Not Tested385-hydroxytryptamine receptor 2A isoform 2 [Homo sapiens]Outcome
113Radioligand Type [Serotonin 5-HT2A]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist38String
114Inhibition at 10 uM [Serotonin 5-HT2A] (10μM**)Value of % Inhibition at 10 uM compound concentration.38Float%
115Outcome [Serotonin 5-HT2B]One of Active, Inactive, or Not Tested395-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens]Outcome
116Radioligand Type [Serotonin 5-HT2B]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist39String
117Inhibition at 10 uM [Serotonin 5-HT2B] (10μM**)Value of % Inhibition at 10 uM compound concentration.39Float%
118Outcome [Serotonin 5-HT3]One of Active, Inactive, or Not Tested405-hydroxytryptamine (serotonin) receptor 3A [Homo sapiens]Outcome
119Radioligand Type [Serotonin 5-HT3]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist40String
120Inhibition at 10 uM [Serotonin 5-HT3] (10μM**)Value of % Inhibition at 10 uM compound concentration.40Float%
121Outcome [Serotonin 5-HT5A]One of Active, Inactive, or Not Tested415-hydroxytryptamine receptor 5A [Homo sapiens]Outcome
122Radioligand Type [Serotonin 5-HT5A]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist41String
123Inhibition at 10 uM [Serotonin 5-HT5A] (10μM**)Value of % Inhibition at 10 uM compound concentration.41Float%
124Outcome [Serotonin 5-HT6]One of Active, Inactive, or Not Tested425-hydroxytryptamine (serotonin) receptor 6 [Homo sapiens]Outcome
125Radioligand Type [Serotonin 5-HT6]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist42String
126Inhibition at 10 uM [Serotonin 5-HT6] (10μM**)Value of % Inhibition at 10 uM compound concentration.42Float%
127Outcome [Serotonin 5-HT7]One of Active, Inactive, or Not Tested43serotonin 5-HT7 receptor protein [Homo sapiens]Outcome
128Radioligand Type [Serotonin 5-HT7]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist43String
129Inhibition at 10 uM [Serotonin 5-HT7] (10μM**)Value of % Inhibition at 10 uM compound concentration.43Float%
130Outcome [Somatostatin sst (non-selective)]One of Active, Inactive, or Not Tested44somatostatin [Mus musculus]Outcome
131Radioligand Type [Somatostatin sst (non-selective)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist44String
132Inhibition at 10 uM [Somatostatin sst (non-selective)] (10μM**)Value of % Inhibition at 10 uM compound concentration.44Float%
133Outcome [Vasoactive intestinal peptide receptor 1]One of Active, Inactive, or Not Tested45Vasoactive intestinal peptide receptor 1 [Homo sapiens]Outcome
134Radioligand Type [Vasoactive intestinal peptide receptor 1]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist45String
135Inhibition at 10 uM [Vasoactive intestinal peptide receptor 1] (10μM**)Value of % Inhibition at 10 uM compound concentration.45Float%
136Outcome [Arginine vasopressin receptor 1A]One of Active, Inactive, or Not Tested46vasopressin V1a receptor [Homo sapiens]Outcome
137Radioligand Type [Arginine vasopressin receptor 1A]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist46String
138Inhibition at 10 uM [Arginine vasopressin receptor 1A] (10μM**)Value of % Inhibition at 10 uM compound concentration.46Float%
139Outcome [Ca2+ channel (L, verapamil site) (phenylalkylamine)]One of Active, Inactive, or Not Tested47voltage-dependent L-type calcium channel subunit alpha-1C [Rattus norvegicus]Outcome
140Radioligand Type [Ca2+ channel (L, verapamil site) (phenylalkylamine)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist47String
141Inhibition at 10 uM [Ca2+ channel (L, verapamil site) (phenylalkylamine)] (10μM**)Value of % Inhibition at 10 uM compound concentration.47Float%
142Outcome [KV channel]One of Active, Inactive, or Not Tested48Outcome
143Radioligand Type [KV channel]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist48String
144Inhibition at 10 uM [KV channel] (10μM**)Value of % Inhibition at 10 uM compound concentration.48Float%
145Outcome [SKCa channel]One of Active, Inactive, or Not Tested49Outcome
146Radioligand Type [SKCa channel]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist49String
147Inhibition at 10 uM [SKCa channel] (10μM**)Value of % Inhibition at 10 uM compound concentration.49Float%
148Outcome [Na+ channel (site 2)]One of Active, Inactive, or Not Tested50Outcome
149Radioligand Type [Na+ channel (site 2)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist50String
150Inhibition at 10 uM [Na+ channel (site 2)] (10μM**)Value of % Inhibition at 10 uM compound concentration.50Float%
151Outcome [Cl- channel (GABA-gated)]One of Active, Inactive, or Not Tested51Outcome
152Radioligand Type [Cl- channel (GABA-gated)]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist51String
153Inhibition at 10 uM [Cl- channel (GABA-gated)] (10μM**)Value of % Inhibition at 10 uM compound concentration.51Float%
154Outcome [Norepinephrine transporter]One of Active, Inactive, or Not Tested52Net [Homo sapiens]Outcome
155Radioligand Type [Norepinephrine transporter]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist52String
156Inhibition at 10 uM [Norepinephrine transporter] (10μM**)Value of % Inhibition at 10 uM compound concentration.52Float%
157Outcome [Dopamine transporter]One of Active, Inactive, or Not Tested53Outcome
158Radioligand Type [Dopamine transporter]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist53String
159Inhibition at 10 uM [Dopamine transporter] (10μM**)Value of % Inhibition at 10 uM compound concentration.53Float%
160Outcome [5-HT transporter]One of Active, Inactive, or Not Tested54Outcome
161Radioligand Type [5-HT transporter]The type of radioactively-labeled ligand used in the assay, one of antagonist or agonist54String
162Inhibition at 10 uM [5-HT transporter] (10μM**)Value of % Inhibition at 10 uM compound concentration.54Float%

** Test Concentration. § Panel component ID.
Additional Information
Grant Number: R03NS053751

Classification
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