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BioAssay: AID 504400

Late-stage counterscreen panel assay for S1P4 agonists: Ricerca HitProfilingScreen + CYP450

Pandemic influenza represents a significant public health threat, due in part to immune cell-mediated lung tissue damage induced during viral infection. Sphingosine 1-phosphate (S1P) is a bioactive phospholipid released by activated blood platelets and serves to influence endothelial integrity, lung epithelial integrity (1), and lymphocyte recirculation (2-5) through five related high affinity more ..
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 Tested Compounds
 Tested Compounds
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Unspecified(1)
 
 
 Tested Substances
 Tested Substances
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Unspecified(1)
 
 
AID: 504400
Data Source: The Scripps Research Institute Molecular Screening Center (S1P4_AG_RICERCA HITPROFILING SCREEN_2X%INH)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
BioAssay Version:
Deposit Date: 2011-03-01
Hold-until Date: 2011-04-12
Modify Date: 2011-04-13

Data Table ( Complete ):           All
Tested Compound:
Depositor Specified Assays
Show more
AIDNameTypeProbeComment
1509Primary Cell-Based Assay to Identify Agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4)screening Primary screen (S1P4 agonists in singlicate)
1523Confirmation cell-based high throughput assay for agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4)screening Confirmation screen (S1P4 agonists in triplicate)
1563Counterscreen assay for S1P4 agonists: Cell-based high throughput screening assay to identify agonists of the Sphingosine 1-Phosphate Receptor 1 (S1P1)screening Counterscreen (S1P1 agonists in triplicate)
1686Fluorescence dose response cell-based high throughput screening assay for agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4)confirmatory Dose response (S1P4 agonists in triplicate)
1701Fluorescence-based counterscreen assay for S1P4 agonists: Cell-based dose response high throughput screening assay to identify agonists of the Sphingosine 1-Phosphate Receptor 1 (S1P1)confirmatory Dose response counterscreen (S1P1 agonists in triplicate)
1801Summary of probe development efforts to identify agonists of Sphingosine 1-Phosphate Receptor 4 (S1P4)summary2 Summary (S1P4 agonists)
463107Late-stage fluorescence dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Synthesized compoundsconfirmatory Late stage dose response (S1P4 agonists in triplicate)
463118Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 1 (S1P1) counterscreen assayconfirmatory Late stage dose response counterscreen (S1P1 agonists in triplicate)
463119Late-stage assay provider results from the probe development effort to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): luminescence-based cell-based dose response assay to determine cytotoxicity of agonist compoundsconfirmatory Late stage dose response counterscreen (Cytotoxicity in quadruplicate)
463122Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 2 (S1P2) counterscreen assayconfirmatory Late stage dose response counterscreen (S1P2 agonists in triplicate)
463123Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 3 (S1P3) counterscreen assayconfirmatory Late stage dose response counterscreen (S1P3 agonists in triplicate)
463129Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) counterscreen assayconfirmatory Late stage dose response counterscreen (S1P5 agonists in triplicate)
463225Late-stage fluorescence dose response cell-based counterscreening assay for agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonistconfirmatory Late stage dose response counterscreen (inhibition by S1P4-selective antagonist)
504871Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist controlconfirmatory
504877Late-stage fluorescence dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Synthesized compounds set 2other
504869Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) antagonist assay Set 2confirmatory
504872Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 3 (S1P3) antagonist assay Set 2confirmatory
504875Late-stage assay provider results from the probe development effort to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): luminescence-based cell-based dose response assay to determine cytotoxicity of agonist compounds Set 2confirmatory
540332Late-stage counterscreen panel assay for S1P4 agonists: Ricerca HitProfilingScreen + CYP450: Set 2other
504917Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 1.2 nMconfirmatory
504923Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 100 nMconfirmatory
504879Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 3 (S1P3) agonist assay Set 2confirmatory
504881Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 2 (S1P2) antagonist assay Set 2confirmatory
504919Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 11 nMconfirmatory
504918Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 0.4 nMconfirmatory
504921Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 33 nMconfirmatory
504924Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 3.7 nMconfirmatory
504867Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) agonist assay Set 2confirmatory
504870Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 1 (S1P1) agonist assay Set 2confirmatory
504873Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 2 (S1P2) agonist assay Set 2confirmatory
504880Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 1 (S1P1) antagonist assayconfirmatory
504876Late-stage fluorescence dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 4 (S1P4) antagonist assay Set 2confirmatory
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRISMC)
Center Affiliation: The Scripps Research Institute (TSRI)
Assay Provider: Michael Oldstone, TSRI
Network: Molecular Library Probe Production Centers Network (MLPCN)
Grant Proposal Number: U01 AI074564 Fast Track
Grant Proposal PI: Michael Oldstone, TSRI
External Assay ID: S1P4_AG_RICERCA HITPROFILING SCREEN_2X%INH

Name: Late-stage counterscreen panel assay for S1P4 agonists: Ricerca HitProfilingScreen + CYP450

Description:

Pandemic influenza represents a significant public health threat, due in part to immune cell-mediated lung tissue damage induced during viral infection. Sphingosine 1-phosphate (S1P) is a bioactive phospholipid released by activated blood platelets and serves to influence endothelial integrity, lung epithelial integrity (1), and lymphocyte recirculation (2-5) through five related high affinity G-protein coupled receptors. Recently, modulation of S1P receptors locally in the lungs was shown to alter dendritic cell activation and accumulation in the mediastinal lymph nodes, resulting in blunted T cell responses and control of immunopathological features of influenza virus infection (6). Reports showing that S1P5 expression is very low in dendritic cells but that S1P4 is highly expressed (7), suggest that chemical activation of the S1P4 receptor subtype in the airways could be efficient at controlling the immunopathological response to viral infection. S1P4 is coupled to Galphai and Galphao G-proteins and activates ERK MAPK and PLC downstream pathways (8), indicating that selective antagonists of S1P4 may also serve as useful tools for understanding S1P4 biological function.

References:

1. Sanna, M.G., J. Liao, E. Jo, C. Alfonso, M.Y. Ahn, M.S. Peterson, B. Webb, S. Lefebvre, J. Chun, N. Gray, and H. Rosen, Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J Biol Chem, 2004. 279(14): p. 13839-48.
2. Forrest, M., S.Y. Sun, R. Hajdu, J. Bergstrom, D. Card, G. Doherty, J. Hale, C. Keohane, C. Meyers, J. Milligan, S. Mills, N. Nomura, H. Rosen, M. Rosenbach, G.J. Shei, Singer, II, M. Tian, S. West, V. White, J. Xie, R.L. Proia, and S. Mandala, Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes. J Pharmacol Exp Ther, 2004. 309(2): p. 758-68.
3. Gon, Y., M.R. Wood, W.B. Kiosses, E. Jo, M.G. Sanna, J. Chun, and H. Rosen, S1P3 receptor-induced reorganization of epithelial tight junctions compromises lung barrier integrity and is potentiated by TNF. Proc Natl Acad Sci U S A, 2005. 102(26): p. 9270-5.
4. Wei, S.H., H. Rosen, M.P. Matheu, M.G. Sanna, S.K. Wang, E. Jo, C.H. Wong, I. Parker, and M.D. Cahalan, Sphingosine 1-phosphate type 1 receptor agonism inhibits transendothelial migration of medullary T cells to lymphatic sinuses. Nat Immunol, 2005. 6(12): p. 1228-35.
5. Alfonso, C., M.G. McHeyzer-Williams, and H. Rosen, CD69 down-modulation and inhibition of thymic egress by short- and long-term selective chemical agonism of sphingosine 1-phosphate receptors. Eur J Immunol, 2006. 36(1): p. 149-59.
6. Jo, E., M.G. Sanna, P.J. Gonzalez-Cabrera, S. Thangada, G. Tigyi, D.A. Osborne, T. Hla, A.L. Parrill, and H. Rosen, S1P1-selective in vivo-active agonists from high-throughput screening: off-the-shelf chemical probes of receptor interactions, signaling, and fate. Chem Biol, 2005. 12(6): p. 703-15.
7. Maeda, Y., Matsuyuki, H., Shimano, K., Kataoka, H., Sugahara, K., and Chiba, K., Migration of CD4 T cells and dendritic cells toward sphingosine 1-phosphate (S1P) is mediated by different receptor subtypes: S1P regulates the functions of murine mature dendritic cells via S1P receptor type 3. J Immunol, 2007. 178(6): p. 3437-46.
8. Toman, R.E. and S. Spiegel, Lysophospholipid receptors in the nervous system. Neurochem Res, 2002. 27(7-8): p. 619-27.

Keywords:

sphingosine receptor, sphingosine-1-phosphate receptor 4, S1P4, EDG6, LPC1, agonist, activator, GPCR, counterscreen, panel assay, Ricerca, HitProfilingScreen, Sf9 cells, radioligand binding, late stage, late stage AID, powders, Scripps, Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Library Probe Production Centers Network, MLPCN
Panel Information
Targets
    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 S1P4 agonist compound SID 87544119 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 D2S (Inhibition) (10μM**)Value of % inhibition at 10 uM compound concentration.16dopamine receptor D2 isoform short [Homo sapiens]Float%
32Dopamine D2S (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: U01 AI074564

Classification
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