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BioAssay: AID 489017

Counterscreen panel assay for S1P4 antagonists: 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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Unspecified(1)
 
 
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Unspecified(1)
 
 
 Related BioAssays
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AID: 489017
Data Source: The Scripps Research Institute Molecular Screening Center (S1P4_ANT_RICERCA HITPROFILING SCREEN_%INH)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2010-11-17

Data Table ( Complete ):           All
Tested Compound:
Depositor Specified Assays
Show more
AIDNameTypeProbeComment
1510Primary Cell-Based Assay to Identify Antagonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4)screening Primary screen (S1P4 antagonists in singlicate)
1524Confirmation cell-based high throughput assay for antagonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4)screening Confirmation screen (S1P4 antagonists in triplicate)
1564Counterscreen assay for S1P4 antagonists: Cell-based high throughput screening assay to identify antagonists of the Sphingosine 1-Phosphate Receptor 1 (S1P1)screening Counterscreen (S1P1 antagonists in triplicate)
1692Fluorescence dose response cell-based high throughput screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4)confirmatory Dose response (S1P4 antagonists in triplicate)
1821Fluorescence-based counterscreen assay for S1P4 antagonists: Cell-based dose response high throughput screening assay to identify antagonists of the Sphingosine 1-Phosphate Receptor 1 (S1P1)confirmatory Dose response counterscreen (S1P1 antagonists in triplicate)
1853Summary of probe development efforts to identify antagonists of Sphingosine 1-Phosphate Receptor 4 (S1P4)summary1 Summary AID (S1P4 antagonists)
2332Late stage fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4)confirmatory Dose response (S1P4 antagonists in triplicate)
2346Late stage fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Synthesized analoguesconfirmatory Late stage dose response (S1P4 antagonists in triplicate)
2349Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 3 (S1P3)confirmatory Late stage dose response counterscreen (S1P3 antagonists in triplicate)
2350Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5)confirmatory Late stage dose response counterscreen (S1P5 antagonists in triplicate)
2351Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 1 (S1P1)confirmatory Late stage dose response counterscreen (S1P1 antagonists in triplicate)
2354Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 2 (S1P2)confirmatory Late stage dose response counterscreen (S1P2 antagonists in triplicate)
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_ANT_RICERCA HITPROFILING SCREEN_%INH

Name: Counterscreen panel assay for S1P4 antagonists: 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 Gai and Gao 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, Endothelial differentiation gene 6, EDG6, counterscreen, antagonist, inhibitor, Ricerca, HitProfilingScreen, Sf9 cells, radioligand binding, 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
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 antagonist compound SID 87357351 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.

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 Ricerca Biosciences, LLC.
Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Outcome [CYP450, 1A2]The assay outcome, one of Inactive or Active1cytochrome P450, family 1, subfamily A, polypeptide 2 [Homo sapiens]Outcome
2Inhibition at 10 uM [CYP450, 1A2] (10μM**)Value of % inhibition at 10 uM compound concentration.1Float%
3Outcome [CYP450, 2C19]The assay outcome, one of Inactive or Active2cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens]Outcome
4Inhibition at 10 uM [CYP450, 2C19] (10μM**)Value of % inhibition at 10 uM compound concentration.2Float%
5Outcome [CYP450, 2C9]The assay outcome, one of Inactive or Active3Cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens]Outcome
6Inhibition at 10 uM [CYP450, 2C9] (10μM**)Value of % inhibition at 10 uM compound concentration.3Float%
7Outcome [CYP450, 2D6]The assay outcome, one of Inactive or Active4Cytochrome P450, family 2, subfamily D, polypeptide 6 [Homo sapiens]Outcome
8Inhibition at 10 uM [CYP450, 2D6] (10μM**)Value of % inhibition at 10 uM compound concentration.4Float%
9Outcome [CYP450, 3A4]The assay outcome, one of Inactive or Active5cytochrome P450 family 3 subfamily A polypeptide 4 [Homo sapiens]Outcome
10Inhibition at 10 uM [CYP450, 3A4] (10μM**)Value of % inhibition at 10 uM compound concentration.5Float%
11Outcome [Adenosine A1]The assay outcome, one of Inactive or Active6adenosine A1 receptor [Homo sapiens]Outcome
12Inhibition at 10 uM [Adenosine A1] (10μM**)Value of % inhibition at 10 uM compound concentration.6Float%
13Outcome [Adenosine A2A]The assay outcome, one of Inactive or Active7adenosine A2a receptor [Homo sapiens]Outcome
14Inhibition at 10 uM [Adenosine A2A] (10μM**)Value of % inhibition at 10 uM compound concentration.7Float%
15Outcome [Adrenergic alpha1A]The assay outcome, one of Inactive or Active8adrenergic receptor, alpha 1a [Rattus norvegicus]Outcome
16Inhibition at 10 uM [Adrenergic alpha1A] (10μM**)Value of % inhibition at 10 uM compound concentration.8Float%
17Outcome [Adrenergic alpha1B]The assay outcome, one of Inactive or Active9Adrenergic, alpha-1B-, receptor [Homo sapiens]Outcome
18Inhibition at 10 uM [Adrenergic alpha1B] (10μM**)Value of % inhibition at 10 uM compound concentration.9Float%
19Outcome [Adrenergic alpha2A]The assay outcome, one of Inactive or Active10alpha-2A adrenergic receptor [Homo sapiens]Outcome
20Inhibition at 10 uM [Adrenergic alpha2A] (10μM**)Value of % inhibition at 10 uM compound concentration.10Float%
21Outcome [Adrenergic beta1]The assay outcome, one of Inactive or Active11adrenergic, beta-1-, receptor [Homo sapiens]Outcome
22Inhibition at 10 uM [Adrenergic beta1] (10μM**)Value of % inhibition at 10 uM compound concentration.11Float%
23Outcome [Adrenergic beta2]The assay outcome, one of Inactive or Active12Adrenergic, beta-2-, receptor, surface [Homo sapiens]Outcome
24Inhibition at 10 uM [Adrenergic beta2] (10μM**)Value of % inhibition at 10 uM compound concentration.12Float%
25Outcome [Calcium Channel L-Type, Dihydropyridine]The assay outcome, one of Inactive or Active13voltage-dependent calcium channel subunit alpha-2/delta-1 isoform 2 [Rattus norvegicus]Outcome
26Inhibition at 10 uM [Calcium Channel L-Type, Dihydropyridine] (10μM**)Value of % inhibition at 10 uM compound concentration.13Float%
27Outcome [Cannabinoid CB1]The assay outcome, one of Inactive or Active14cannabinoid receptor [Homo sapiens]Outcome
28Inhibition at 10 uM [Cannabinoid CB1] (10μM**)Value of % inhibition at 10 uM compound concentration.14Float%
29Outcome [Dopamine D1]The assay outcome, one of Inactive or Active15Dopamine receptor D1 [Homo sapiens]Outcome
30Inhibition at 10 uM [Dopamine D1] (10μM**)Value of % inhibition at 10 uM compound concentration.15Float%
31Outcome [Dopamine D2S]The assay outcome, one of Inactive or Active16dopamine receptor D2 isoform short [Homo sapiens]Outcome
32Inhibition at 10 uM [Dopamine D2S] (10μM**)Value of % inhibition at 10 uM compound concentration.16Float%
33Outcome [GABAA, Flunitrazepam, Central]The assay outcome, one of Inactive or Active17gamma-aminobutyric acid A receptor, gamma 2 [Rattus norvegicus]Outcome
34Inhibition at 10 uM [GABAA, Flunitrazepam, Central] (10μM**)Value of % inhibition at 10 uM compound concentration.17Float%
35Outcome [GABAA, Muscimol, Central]The assay outcome, one of Inactive or Active18testis gamma-aminobutyric acid receptor subunit beta 3 [Rattus norvegicus]Outcome
36Inhibition at 10 uM [GABAA, Muscimol, Central] (10μM**)Value of % inhibition at 10 uM compound concentration.18Float%
37Outcome [Glutamate, NMDA, Phencyclidine]The assay outcome, one of Inactive or Active19glutamate receptor, ionotropic, N-methyl D-aspartate 1, isoform CRA_h [Rattus norvegicus]Outcome
38Inhibition at 10 uM [Glutamate, NMDA, Phencyclidine] (10μM**)Value of % inhibition at 10 uM compound concentration.19Float%
39Outcome [Histamine H1]The assay outcome, one of Inactive or Active20histamine H1 receptor [Homo sapiens]Outcome
40Inhibition at 10 uM [Histamine H1] (10μM**)Value of % inhibition at 10 uM compound concentration.20Float%
41Outcome [Imidazoline I2, Central]The assay outcome, one of Inactive or Active21Outcome
42Inhibition at 10 uM [Imidazoline I2, Central] (10μM**)Value of % inhibition at 10 uM compound concentration.21Float%
43Outcome [Muscarinic M2]The assay outcome, one of Inactive or Active22cholinergic receptor, muscarinic 2 [Homo sapiens]Outcome
44Inhibition at 10 uM [Muscarinic M2] (10μM**)Value of % inhibition at 10 uM compound concentration.22Float%
45Outcome [Muscarinic M3]The assay outcome, one of Inactive or Active23Cholinergic receptor, muscarinic 3 [Homo sapiens]Outcome
46Inhibition at 10 uM [Muscarinic M3] (10μM**)Value of % inhibition at 10 uM compound concentration.23Float%
47Outcome [Nicotinic Acetylcholine]The assay outcome, one of Inactive or Active24cholinergic receptor, nicotinic, alpha 3, isoform CRA_a [Homo sapiens]Outcome
48Inhibition at 10 uM [Nicotinic Acetylcholine] (10μM**)Value of % inhibition at 10 uM compound concentration.24Float%
49Outcome [Nicotinic Acetylcholine alpha 1, Bungarotoxin]The assay outcome, one of Inactive or Active25cholinergic receptor, nicotinic, alpha 1 (muscle), isoform CRA_a [Homo sapiens]Outcome
50Inhibition at 10 uM [Nicotinic Acetylcholine alpha 1, Bungarotoxin] (10μM**)Value of % inhibition at 10 uM compound concentration.25Float%
51Outcome [Opiate mu (OP3, MOP)]The assay outcome, one of Inactive or Active26mu-type opioid receptor isoform MOR-1B2 [Homo sapiens]Outcome
52Inhibition at 10 uM [Opiate mu (OP3, MOP)] (10μM**)Value of % inhibition at 10 uM compound concentration.26Float%
53Outcome [Phorbol Ester]The assay outcome, one of Inactive or Active27Outcome
54Inhibition at 10 uM [Phorbol Ester] (10μM**)Value of % inhibition at 10 uM compound concentration.27Float%
55Outcome [Potassium Channel [KATP]]The assay outcome, one of Inactive or Active28Outcome
56Inhibition at 10 uM [Potassium Channel [KATP]] (10μM**)Value of % inhibition at 10 uM compound concentration.28Float%
57Outcome [Potassium Channel hERG]The assay outcome, one of Inactive or Active29voltage-gated potassium channel subfamily H isoform 3.1 [Homo sapiens]Outcome
58Inhibition at 10 uM [Potassium Channel hERG] (10μM**)Value of % inhibition at 10 uM compound concentration.29Float%
59Outcome [Prostanoid EP4]The assay outcome, one of Inactive or Active30Prostaglandin E receptor 4 (subtype EP4) [Homo sapiens]Outcome
60Inhibition at 10 uM [Prostanoid EP4] (10μM**)Value of % inhibition at 10 uM compound concentration.30Float%
61Outcome [Rolipram]The assay outcome, one of Inactive or Active31Outcome
62Inhibition at 10 uM [Rolipram] (10μM**)Value of % inhibition at 10 uM compound concentration.31Float%
63Outcome [Serotonin (5-Hydroxytryptamine) 5-HT2B]The assay outcome, one of Inactive or Active325-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens]Outcome
64Inhibition at 10 uM [Serotonin (5-Hydroxytryptamine) 5-HT2B] (10μM**)Value of % inhibition at 10 uM compound concentration.32Float%
65Outcome [Sigma 1]The assay outcome, one of Inactive or Active33opioid receptor, sigma 1 [Homo sapiens]Outcome
66Inhibition at 10 uM [Sigma 1] (10μM**)Value of % inhibition at 10 uM compound concentration.33Float%
67Outcome [Sodium Channel, Site 2]The assay outcome, one of Inactive or Active34sodium channel, nonvoltage-gated 1 alpha [Rattus norvegicus]Outcome
68Inhibition at 10 uM [Sodium Channel, Site 2] (10μM**)Value of % inhibition at 10 uM compound concentration.34Float%
69Outcome [Transporter, Norepinephrine (NET)]The assay outcome, one of Inactive or Active35Net [Homo sapiens]Outcome
70Inhibition at 10 uM [Transporter, Norepinephrine (NET)] (10μM**)Value of % inhibition at 10 uM compound concentration.35Float%

** Test Concentration. § Panel component ID.
Additional Information
Grant Number: U01 AI074564

Classification
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