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 ..
Tested Compound:
Depositor Specified Assays
Show more |
| AID | Name | Type | Probe | Comment |
|---|---|---|---|---|
| 1510 | Primary Cell-Based Assay to Identify Antagonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4) | screening | Primary screen (S1P4 antagonists in singlicate) | |
| 1524 | Confirmation cell-based high throughput assay for antagonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4) | screening | Confirmation screen (S1P4 antagonists in triplicate) | |
| 1564 | Counterscreen 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) | |
| 1692 | Fluorescence 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) | |
| 1821 | Fluorescence-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) | |
| 1853 | Summary of probe development efforts to identify antagonists of Sphingosine 1-Phosphate Receptor 4 (S1P4) | summary | 1 | Summary AID (S1P4 antagonists) |
| 2332 | Late 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) | |
| 2346 | Late stage fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Synthesized analogues | confirmatory | Late stage dose response (S1P4 antagonists in triplicate) | |
| 2349 | Late 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) | |
| 2350 | Late 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) | |
| 2351 | Late 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) | |
| 2354 | Late 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
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
§ Panel component ID.
| Data Table(All) | Show more |
| PID§ | Name | Substance | Panel Targets | Description | Additional Information | ||
|---|---|---|---|---|---|---|---|
| Active | Inactive | ||||||
| 1 | CYP450, 1A2 | 1 | cytochrome P450, family 1, subfamily A, polypeptide 2 [Homo sapiens] [gi:119619719] | Taxonomy id: 9606 Gene id: 1544 | |||
| 2 | CYP450, 2C19 | 1 | cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:55665398] | Taxonomy id: 9606 Gene id: 1557 | |||
| 3 | CYP450, 2C9 | 1 | Cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] [gi:115529027] | Taxonomy id: 9606 Gene id: 1559 | |||
| 4 | CYP450, 2D6 | 1 | Cytochrome P450, family 2, subfamily D, polypeptide 6 [Homo sapiens] [gi:117558701] | Taxonomy id: 9606 Gene id: 1565 | |||
| 5 | CYP450, 3A4 | 1 | cytochrome P450 family 3 subfamily A polypeptide 4 [Homo sapiens] [gi:115371803] | Taxonomy id: 9606 Gene id: 1576 | |||
| 6 | Adenosine A1 | 1 | adenosine A1 receptor [Homo sapiens] [gi:119611871] | Taxonomy id: 9606 Gene id: 134 | |||
| 7 | Adenosine A2A | 1 | adenosine A2a receptor [Homo sapiens] [gi:119580062] | Taxonomy id: 9606 Gene id: 135 | |||
| 8 | Adrenergic alpha1A | 1 | adrenergic receptor, alpha 1a [Rattus norvegicus] [gi:149030335] | Taxonomy id: 10116 Gene id: 29412 | |||
| 9 | Adrenergic alpha1B | 1 | Adrenergic, alpha-1B-, receptor [Homo sapiens] [gi:187953275] | Taxonomy id: 10116 Gene id: 147 | |||
| 10 | Adrenergic alpha2A | 1 | alpha-2A adrenergic receptor [Homo sapiens] [gi:194353970] | Taxonomy id: 9606 Gene id: 150 | |||
| 11 | Adrenergic beta1 | 1 | adrenergic, beta-1-, receptor [Homo sapiens] [gi:166706747] | Taxonomy id: 9606 Gene id: 153 | |||
| 12 | Adrenergic beta2 | 1 | Adrenergic, beta-2-, receptor, surface [Homo sapiens] [gi:127798637] | Taxonomy id: 9606 Gene id: 154 | |||
| 13 | Calcium Channel L-Type, Dihydropyridine | 1 | voltage-dependent calcium channel subunit alpha-2/delta-1 isoform 2 [Rattus norvegicus] [gi:161086906] | Taxonomy id: 10116 Gene id: 25399 | |||
| 14 | Cannabinoid CB1 | 1 | cannabinoid receptor [Homo sapiens] [gi:67550212] | Taxonomy id: 9606 Gene id: 1268 | |||
| 15 | Dopamine D1 | 1 | Dopamine receptor D1 [Homo sapiens] [gi:67677841] | Taxonomy id: 9606 Gene id: 1812 | |||
| 16 | Dopamine D2S | 1 | dopamine receptor D2 isoform short [Homo sapiens] [gi:197692661] | Taxonomy id: 9606 Gene id: 1813 | |||
| 17 | GABAA, Flunitrazepam, Central | 1 | gamma-aminobutyric acid A receptor, gamma 2 [Rattus norvegicus] [gi:149052302] | Taxonomy id: 10116 Gene id: 29709 | |||
| 18 | GABAA, Muscimol, Central | 1 | testis gamma-aminobutyric acid receptor subunit beta 3 [Rattus norvegicus] [gi:53765741] | Taxonomy id: 10116 Gene id: 24922 | |||
| 19 | Glutamate, NMDA, Phencyclidine | 1 | glutamate receptor, ionotropic, N-methyl D-aspartate 1, isoform CRA_h [Rattus norvegicus] [gi:149039393] | Taxonomy id: 10116 Gene id: 24408 | |||
| 20 | Histamine H1 | 1 | histamine H1 receptor [Homo sapiens] [gi:149158709] | Taxonomy id: 9606 Gene id: 3269 | |||
| 21 | Imidazoline I2, Central | 1 | Taxonomy id: 10116 | ||||
| 22 | Muscarinic M2 | 1 | cholinergic receptor, muscarinic 2 [Homo sapiens] [gi:119604271] | Taxonomy id: 9606 Gene id: 1129 | |||
| 23 | Muscarinic M3 | 1 | Cholinergic receptor, muscarinic 3 [Homo sapiens] [gi:111306506] | Taxonomy id: 9606 Gene id: 1131 | |||
| 24 | Nicotinic Acetylcholine | 1 | cholinergic receptor, nicotinic, alpha 3, isoform CRA_a [Homo sapiens] [gi:119619563] | Taxonomy id: 9606 Gene id: 1136 | |||
| 25 | Nicotinic Acetylcholine alpha 1, Bungarotoxin | 1 | cholinergic receptor, nicotinic, alpha 1 (muscle), isoform CRA_a [Homo sapiens] [gi:119631533] | Taxonomy id: 9606 Gene id: 1134 | |||
| 26 | Opiate mu (OP3, MOP) | 1 | mu-type opioid receptor isoform MOR-1B2 [Homo sapiens] [gi:223718719] | Taxonomy id: 9606 Gene id: 4988 | |||
| 27 | Phorbol Ester | 1 | Taxonomy id: 10090 | ||||
| 28 | Potassium Channel [KATP] | 1 | Taxonomy id: 10036 | ||||
| 29 | Potassium Channel hERG | 1 | voltage-gated potassium channel subfamily H isoform 3.1 [Homo sapiens] [gi:237862038] | Taxonomy id: 9606 Gene id: 3757 | |||
| 30 | Prostanoid EP4 | 1 | Prostaglandin E receptor 4 (subtype EP4) [Homo sapiens] [gi:109731195] | Taxonomy id: 9606 Gene id: 5734 | |||
| 31 | Rolipram | 1 | Taxonomy id: 10116 | ||||
| 32 | Serotonin (5-Hydroxytryptamine) 5-HT2B | 1 | 5-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] [gi:119591355] | Taxonomy id: 9606 Gene id: 3357 | |||
| 33 | Sigma 1 | 1 | opioid receptor, sigma 1 [Homo sapiens] [gi:123231939] | Taxonomy id: 9606 Gene id: 10280 | |||
| 34 | Sodium Channel, Site 2 | 1 | sodium channel, nonvoltage-gated 1 alpha [Rattus norvegicus] [gi:149049394] | Taxonomy id: 10116 Gene id: 25122 | |||
| 35 | Transporter, Norepinephrine (NET) | 1 | Net [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.
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 |
| TID | Name | Description | PID§ | Panel Targets | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||||
| 1 | Outcome [CYP450, 1A2] | The assay outcome, one of Inactive or Active | 1 | cytochrome P450, family 1, subfamily A, polypeptide 2 [Homo sapiens] |  | Outcome | ||
| 2 | Inhibition at 10 uM [CYP450, 1A2] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 1 | | Float | % | ||
| 3 | Outcome [CYP450, 2C19] | The assay outcome, one of Inactive or Active | 2 | cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] | | Outcome | ||
| 4 | Inhibition at 10 uM [CYP450, 2C19] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 2 | | Float | % | ||
| 5 | Outcome [CYP450, 2C9] | The assay outcome, one of Inactive or Active | 3 | Cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] | | Outcome | ||
| 6 | Inhibition at 10 uM [CYP450, 2C9] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 3 | | Float | % | ||
| 7 | Outcome [CYP450, 2D6] | The assay outcome, one of Inactive or Active | 4 | Cytochrome P450, family 2, subfamily D, polypeptide 6 [Homo sapiens] | | Outcome | ||
| 8 | Inhibition at 10 uM [CYP450, 2D6] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 4 | | Float | % | ||
| 9 | Outcome [CYP450, 3A4] | The assay outcome, one of Inactive or Active | 5 | cytochrome P450 family 3 subfamily A polypeptide 4 [Homo sapiens] | | Outcome | ||
| 10 | Inhibition at 10 uM [CYP450, 3A4] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 5 | | Float | % | ||
| 11 | Outcome [Adenosine A1] | The assay outcome, one of Inactive or Active | 6 | adenosine A1 receptor [Homo sapiens] | | Outcome | ||
| 12 | Inhibition at 10 uM [Adenosine A1] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 6 | | Float | % | ||
| 13 | Outcome [Adenosine A2A] | The assay outcome, one of Inactive or Active | 7 | adenosine A2a receptor [Homo sapiens] | | Outcome | ||
| 14 | Inhibition at 10 uM [Adenosine A2A] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 7 | | Float | % | ||
| 15 | Outcome [Adrenergic alpha1A] | The assay outcome, one of Inactive or Active | 8 | adrenergic receptor, alpha 1a [Rattus norvegicus] | | Outcome | ||
| 16 | Inhibition at 10 uM [Adrenergic alpha1A] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 8 | | Float | % | ||
| 17 | Outcome [Adrenergic alpha1B] | The assay outcome, one of Inactive or Active | 9 | Adrenergic, alpha-1B-, receptor [Homo sapiens] | | Outcome | ||
| 18 | Inhibition at 10 uM [Adrenergic alpha1B] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 9 | | Float | % | ||
| 19 | Outcome [Adrenergic alpha2A] | The assay outcome, one of Inactive or Active | 10 | alpha-2A adrenergic receptor [Homo sapiens] | | Outcome | ||
| 20 | Inhibition at 10 uM [Adrenergic alpha2A] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 10 | | Float | % | ||
| 21 | Outcome [Adrenergic beta1] | The assay outcome, one of Inactive or Active | 11 | adrenergic, beta-1-, receptor [Homo sapiens] | | Outcome | ||
| 22 | Inhibition at 10 uM [Adrenergic beta1] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 11 | | Float | % | ||
| 23 | Outcome [Adrenergic beta2] | The assay outcome, one of Inactive or Active | 12 | Adrenergic, beta-2-, receptor, surface [Homo sapiens] | | Outcome | ||
| 24 | Inhibition at 10 uM [Adrenergic beta2] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 12 | | Float | % | ||
| 25 | Outcome [Calcium Channel L-Type, Dihydropyridine] | The assay outcome, one of Inactive or Active | 13 | voltage-dependent calcium channel subunit alpha-2/delta-1 isoform 2 [Rattus norvegicus] | | Outcome | ||
| 26 | Inhibition at 10 uM [Calcium Channel L-Type, Dihydropyridine] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 13 | | Float | % | ||
| 27 | Outcome [Cannabinoid CB1] | The assay outcome, one of Inactive or Active | 14 | cannabinoid receptor [Homo sapiens] | | Outcome | ||
| 28 | Inhibition at 10 uM [Cannabinoid CB1] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 14 | | Float | % | ||
| 29 | Outcome [Dopamine D1] | The assay outcome, one of Inactive or Active | 15 | Dopamine receptor D1 [Homo sapiens] | | Outcome | ||
| 30 | Inhibition at 10 uM [Dopamine D1] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 15 | | Float | % | ||
| 31 | Outcome [Dopamine D2S] | The assay outcome, one of Inactive or Active | 16 | dopamine receptor D2 isoform short [Homo sapiens] | | Outcome | ||
| 32 | Inhibition at 10 uM [Dopamine D2S] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 16 | | Float | % | ||
| 33 | Outcome [GABAA, Flunitrazepam, Central] | The assay outcome, one of Inactive or Active | 17 | gamma-aminobutyric acid A receptor, gamma 2 [Rattus norvegicus] | | Outcome | ||
| 34 | Inhibition at 10 uM [GABAA, Flunitrazepam, Central] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 17 | | Float | % | ||
| 35 | Outcome [GABAA, Muscimol, Central] | The assay outcome, one of Inactive or Active | 18 | testis gamma-aminobutyric acid receptor subunit beta 3 [Rattus norvegicus] | | Outcome | ||
| 36 | Inhibition at 10 uM [GABAA, Muscimol, Central] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 18 | | Float | % | ||
| 37 | Outcome [Glutamate, NMDA, Phencyclidine] | The assay outcome, one of Inactive or Active | 19 | glutamate receptor, ionotropic, N-methyl D-aspartate 1, isoform CRA_h [Rattus norvegicus] | | Outcome | ||
| 38 | Inhibition at 10 uM [Glutamate, NMDA, Phencyclidine] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 19 | | Float | % | ||
| 39 | Outcome [Histamine H1] | The assay outcome, one of Inactive or Active | 20 | histamine H1 receptor [Homo sapiens] | | Outcome | ||
| 40 | Inhibition at 10 uM [Histamine H1] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 20 | | Float | % | ||
| 41 | Outcome [Imidazoline I2, Central] | The assay outcome, one of Inactive or Active | 21 | | Outcome | |||
| 42 | Inhibition at 10 uM [Imidazoline I2, Central] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 21 | | Float | % | ||
| 43 | Outcome [Muscarinic M2] | The assay outcome, one of Inactive or Active | 22 | cholinergic receptor, muscarinic 2 [Homo sapiens] | | Outcome | ||
| 44 | Inhibition at 10 uM [Muscarinic M2] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 22 | | Float | % | ||
| 45 | Outcome [Muscarinic M3] | The assay outcome, one of Inactive or Active | 23 | Cholinergic receptor, muscarinic 3 [Homo sapiens] | | Outcome | ||
| 46 | Inhibition at 10 uM [Muscarinic M3] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 23 | | Float | % | ||
| 47 | Outcome [Nicotinic Acetylcholine] | The assay outcome, one of Inactive or Active | 24 | cholinergic receptor, nicotinic, alpha 3, isoform CRA_a [Homo sapiens] | | Outcome | ||
| 48 | Inhibition at 10 uM [Nicotinic Acetylcholine] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 24 | | Float | % | ||
| 49 | Outcome [Nicotinic Acetylcholine alpha 1, Bungarotoxin] | The assay outcome, one of Inactive or Active | 25 | cholinergic receptor, nicotinic, alpha 1 (muscle), isoform CRA_a [Homo sapiens] | | Outcome | ||
| 50 | Inhibition at 10 uM [Nicotinic Acetylcholine alpha 1, Bungarotoxin] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 25 | | Float | % | ||
| 51 | Outcome [Opiate mu (OP3, MOP)] | The assay outcome, one of Inactive or Active | 26 | mu-type opioid receptor isoform MOR-1B2 [Homo sapiens] | | Outcome | ||
| 52 | Inhibition at 10 uM [Opiate mu (OP3, MOP)] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 26 | | Float | % | ||
| 53 | Outcome [Phorbol Ester] | The assay outcome, one of Inactive or Active | 27 | | Outcome | |||
| 54 | Inhibition at 10 uM [Phorbol Ester] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 27 | | Float | % | ||
| 55 | Outcome [Potassium Channel [KATP]] | The assay outcome, one of Inactive or Active | 28 | | Outcome | |||
| 56 | Inhibition at 10 uM [Potassium Channel [KATP]] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 28 | | Float | % | ||
| 57 | Outcome [Potassium Channel hERG] | The assay outcome, one of Inactive or Active | 29 | voltage-gated potassium channel subfamily H isoform 3.1 [Homo sapiens] | | Outcome | ||
| 58 | Inhibition at 10 uM [Potassium Channel hERG] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 29 | | Float | % | ||
| 59 | Outcome [Prostanoid EP4] | The assay outcome, one of Inactive or Active | 30 | Prostaglandin E receptor 4 (subtype EP4) [Homo sapiens] | | Outcome | ||
| 60 | Inhibition at 10 uM [Prostanoid EP4] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 30 | | Float | % | ||
| 61 | Outcome [Rolipram] | The assay outcome, one of Inactive or Active | 31 | | Outcome | |||
| 62 | Inhibition at 10 uM [Rolipram] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 31 | | Float | % | ||
| 63 | Outcome [Serotonin (5-Hydroxytryptamine) 5-HT2B] | The assay outcome, one of Inactive or Active | 32 | 5-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] | | Outcome | ||
| 64 | Inhibition at 10 uM [Serotonin (5-Hydroxytryptamine) 5-HT2B] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 32 | | Float | % | ||
| 65 | Outcome [Sigma 1] | The assay outcome, one of Inactive or Active | 33 | opioid receptor, sigma 1 [Homo sapiens] | | Outcome | ||
| 66 | Inhibition at 10 uM [Sigma 1] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 33 | | Float | % | ||
| 67 | Outcome [Sodium Channel, Site 2] | The assay outcome, one of Inactive or Active | 34 | sodium channel, nonvoltage-gated 1 alpha [Rattus norvegicus] | | Outcome | ||
| 68 | Inhibition at 10 uM [Sodium Channel, Site 2] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 34 | | Float | % | ||
| 69 | Outcome [Transporter, Norepinephrine (NET)] | The assay outcome, one of Inactive or Active | 35 | Net [Homo sapiens] | | Outcome | ||
| 70 | Inhibition at 10 uM [Transporter, Norepinephrine (NET)] (10μM**) | Value of % inhibition at 10 uM compound concentration. | 35 | | Float | % |
** Test Concentration. § Panel component ID.
Additional Information
Grant Number: U01 AI074564
Classification
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