SB 221284 [Ligand Id: 191] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL276140
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511]
ChEMBL Inhibition of heterologously expressed human Cytochrome P450 19A1 at 100 uM B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 3494-3496 [PMID:9357513]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 6.3 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL Displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor expressed in HEK 293 cells B 6.4 pKi 398.11 nM Ki J Med Chem (1997) 40: 3494-3496 [PMID:9357513]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 2A receptor expressed in HEK 293 cells using [3H]ketanserin as radioligand B 6.4 pKi 398.11 nM Ki J Med Chem (1998) 41: 1598-1612 [PMID:9572885]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells B 7.9 pKi 12.59 nM Ki J Med Chem (1997) 40: 3494-3496 [PMID:9357513]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand B 7.9 pKi 12.59 nM Ki J Med Chem (1998) 41: 1598-1612 [PMID:9572885]
GtoPdb - - 8.6 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Displacement of [3H]mesulergine from 5-hydroxytryptamine 2C receptor expressed in HEK 293 cells B 8.6 pKi 2.51 nM Ki J Med Chem (1997) 40: 3494-3496 [PMID:9357513]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 2C receptor expressed in HEK 293 cells using [3H]mesulergine as radioligand B 8.6 pKi 2.51 nM Ki J Med Chem (1998) 41: 1598-1612 [PMID:9572885]
GtoPdb - - 8.7 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]

ChEMBL data shown on this page come from version 32:

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]