SB 272183 [Ligand Id: 75] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL191971 (SB-272183)
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 8 pKi - - - Br J Pharmacol (2001) 133: 797-806 [PMID:11454652]
ChEMBL Mean binding affinity towards 5-hydroxytryptamine 1A receptor using [3H]-5-HT or [3H]8-OH-DPAT as the radioligand B 8 pKi 10 nM Ki Bioorg Med Chem Lett (2005) 15: 4370-4374 [PMID:16039851]
ChEMBL Binding affinity against cloned human 5-hydroxytryptamine 1A receptor B 8.4 pKi 3.98 nM Ki Bioorg Med Chem Lett (2005) 15: 4708-4712 [PMID:16153839]
ChEMBL Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S F 7.72 pEC50 19.05 nM EC50 J Med Chem (2003) 46: 5117-5120 [PMID:14613313]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 8.1 pKi - - - Br J Pharmacol (2001) 133: 797-806 [PMID:11454652]
ChEMBL Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand B 8.1 pKi 7.94 nM Ki Bioorg Med Chem Lett (2005) 15: 4370-4374 [PMID:16039851]
ChEMBL Binding affinity against cloned human 5-hydroxytryptamine 1B receptor B 8.4 pKi 3.98 nM Ki Bioorg Med Chem Lett (2005) 15: 4708-4712 [PMID:16153839]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 8.7 pKi - - - Br J Pharmacol (2001) 133: 797-806 [PMID:11454652]
ChEMBL Mean binding affinity towards 5-hydroxytryptamine 1D receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand B 8.7 pKi 2 nM Ki Bioorg Med Chem Lett (2005) 15: 4370-4374 [PMID:16039851]
ChEMBL Binding affinity against cloned human 5-hydroxytryptamine 1D receptor B 9 pKi 1 nM Ki Bioorg Med Chem Lett (2005) 15: 4708-4712 [PMID:16153839]

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]