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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]