[3H]WAY100635 [Ligand Id: 3251] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL31354 (WAY-100635) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Inhibition of adrenergic alpha1A receptor | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2011) 54: 3480-3491 [PMID:21520940] |
| ChEMBL | Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique | B | 7.73 | pKi | 18.62 | nM | Ki | Eur J Med Chem (2010) 45: 3740-3751 [PMID:20605276] |
| ChEMBL | Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting | B | 7.73 | pKi | 18.62 | nM | Ki | Eur J Med Chem (2019) 176: 310-325 [PMID:31112892] |
| ChEMBL | Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | B | 7.73 | pKi | 18.62 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Inhibition of adrenergic Alpha-1B receptor | B | 6.49 | pKi | 322 | nM | Ki | J Med Chem (2011) 54: 3480-3491 [PMID:21520940] |
| ChEMBL | Displacement [3H]prazosin of human recombinant Alpha-1B adrenergic receptor expressed in CHO cells by rapid filtration technique | B | 7.18 | pKi | 66.07 | nM | Ki | Eur J Med Chem (2010) 45: 3740-3751 [PMID:20605276] |
| ChEMBL | Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1B expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counter | B | 7.18 | pKi | 66.07 | nM | Ki | Eur J Med Chem (2019) 176: 310-325 [PMID:31112892] |
| ChEMBL | Displacement of [3H]Prazosin from human recombinant alpha 1B adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | B | 7.18 | pKi | 66.07 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | Displacement [3H]prazosin of human recombinant Alpha-1D adrenergic receptor expressed in CHO cells by rapid filtration technique | B | 8.34 | pKi | 4.57 | nM | Ki | Eur J Med Chem (2010) 45: 3740-3751 [PMID:20605276] |
| ChEMBL | Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1D expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counter | B | 8.34 | pKi | 4.57 | nM | Ki | Eur J Med Chem (2019) 176: 310-325 [PMID:31112892] |
| ChEMBL | Displacement of [3H]Prazosin from human recombinant alpha 1D adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | B | 8.34 | pKi | 4.57 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Inhibition of dopamine D4 receptor | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2011) 54: 3480-3491 [PMID:21520940] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 9.5 | pKd | 0.3 | nM | Kd | Life Sci (1997) 60: 653-65 [PMID:9048968] |
| ChEMBL | Inhibition of 5HT1A receptor | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2011) 54: 3480-3491 [PMID:21520940] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells after 120 mins | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2009) 52: 7892-7896 [PMID:19705871] |
| ChEMBL | Binding affinity against human 5-hydroxytryptamine 1A receptor in CHO cells labeled with [3H]8-OH-DPAT radioligand | B | 9.02 | pKi | 0.96 | nM | Ki | J Med Chem (2004) 47: 3823-3842 [PMID:15239661] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2010) 53: 4066-4084 [PMID:20443629] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem (2008) 16: 6707-6723 [PMID:18571421] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2009) 52: 4955-4959 [PMID:19719241] |
| ChEMBL | Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor | B | 9.1 | pKi | 0.79 | nM | Ki | J Med Chem (2008) 51: 2887-2890 [PMID:18433113] |
| ChEMBL | In vitro inhibition of [3H]- 8-OH-DPAT binding to cloned cell line containing human 5-hydroxytryptamine 1A receptor | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1999) 42: 1576-1586 [PMID:10229627] |
| ChEMBL | Binding affinity at human 5-hydroxytryptamine 1A receptor by inhibition of [3H]8-OH-DPAT binding in Chinese hamster ovary cell line | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2002) 45: 165-176 [PMID:11754589] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting | B | 9.41 | pKi | 0.39 | nM | Ki | J Med Chem (2011) 54: 3480-3491 [PMID:21520940] |
| ChEMBL | Displacement [3H]8-OH-DPAT of human cloned 5HT1A receptor expressed in human HeLa cells by rapid filtration technique | B | 9.48 | pKi | 0.33 | nM | Ki | Eur J Med Chem (2010) 45: 3740-3751 [PMID:20605276] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5HT-1AR transfected in HeLa cells incubated for 30 mins by liquid scintillation counter | B | 9.48 | pKi | 0.33 | nM | Ki | Eur J Med Chem (2019) 176: 310-325 [PMID:31112892] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in human HeLa cells incubated for 30 mins by radioligand competition binding assay | B | 9.48 | pKi | 0.33 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2008) 51: 2887-2890 [PMID:18433113] |
| ChEMBL | Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay | F | 7.95 | pIC50 | 11.3 | nM | IC50 | J Med Chem (2018) 61: 10017-10039 [PMID:30383372] |
| ChEMBL | Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level | F | 8.15 | pIC50 | 7.1 | nM | IC50 | J Med Chem (2010) 53: 4066-4084 [PMID:20443629] |
| ChEMBL | Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay | F | 8.55 | pIC50 | 2.8 | nM | IC50 | Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting | B | 9.04 | pIC50 | 0.91 | nM | IC50 | J Med Chem (2011) 54: 3480-3491 [PMID:21520940] |
| ChEMBL | Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor | F | 8.15 | pEC50 | 7.1 | nM | EC50 | J Med Chem (2004) 47: 3823-3842 [PMID:15239661] |
| ChEMBL | Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells | B | 8.15 | pEC50 | 7.1 | nM | EC50 | J Med Chem (2004) 47: 3823-3842 [PMID:15239661] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes. | F | 9.69 | pKd | 0.2 | nM | Kd | Bioorg Med Chem Lett (1998) 8: 2457-2462 [PMID:9873561] |
| ChEMBL | In vitro binding affinity for 5-hydroxytryptamine 1A receptor was determined by measuring specific inhibition of [125I]-binding to rat hippocampal membrane preparations | B | 10 | pKd | 0.1 | nM | Kd | J Med Chem (1998) 41: 157-166 [PMID:9457239] |
| ChEMBL | Inhibition of binding of [125I]8-OH-PIPAT ligand to 5-hydroxytryptamine 1A receptor of rat hippocampal homogenates | B | 9.08 | pKi | 0.84 | nM | Ki | J Med Chem (1994) 37: 1406-1407 [PMID:8182697] |
| ChEMBL | Compound was tested for inhibition constant against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes. | B | 9.3 | pKi | 0.5 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2457-2462 [PMID:9873561] |
| ChEMBL | In vitro binding affinity to 5-hydroxytryptamine 1A receptor using [125I](R)-(+)-trans-8-OH-PIPAT as radioligand in rat hippocampal homogenate | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (1994) 37: 4572-4575 [PMID:7799409] |
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 1A receptor of rat hippocampal homogenates | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (1994) 37: 1406-1407 [PMID:8182697] |
| ChEMBL | In vitro affinity against 5-hydroxytryptamine 1A receptor using [3H]-8-OH-DPAT in rat hippocampus | B | 9.43 | pIC50 | 0.37 | nM | IC50 | J Med Chem (2000) 43: 432-439 [PMID:10669570] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Inhibition of 5HT1B receptor | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (2011) 54: 3480-3491 [PMID:21520940] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4297] [GtoPdb: 3] [UniProtKB: Q61224] | ||||||||
| ChEMBL | Receptor-linked G protein activation at 5-hydroxytryptamine receptor was determined by measuring the stimulation of [35S]GTP-gamma-S, binding (Experiment 1) | F | 8.96 | pKi | 1.09 | nM | Ki | J Med Chem (1999) 42: 1576-1586 [PMID:10229627] |
| ChEMBL | Receptor-linked G protein activation at 5-hydroxytryptamine receptor was determined by measuring the stimulation of [35S]GTP-gamma-S, binding (Experiment 2) | F | 9.47 | pKi | 0.34 | nM | Ki | J Med Chem (1999) 42: 1576-1586 [PMID:10229627] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Inhibition of 5HT7 receptor | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (2011) 54: 3480-3491 [PMID:21520940] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells | B | 5.35 | pIC50 | >4500 | nM | IC50 | J Med Chem (2004) 47: 3823-3842 [PMID:15239661] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Binding affinity against serotonin transporter in rat cortical tissues using radioligand [3H]paroxetine | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2004) 47: 3823-3842 [PMID:15239661] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
