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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]