GSK334429 [Ligand Id: 9103] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2151157 (GSK334429)
  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Binding affinity to human histamine H3 receptor B 9.5 pKi 0.32 nM Ki J Med Chem (2011) 54: 26-53 [PMID:21062081]
GtoPdb - - 9.89 pKi 0.13 nM Ki J Med Chem (2011) 54: 26-53 [PMID:21062081];
Eur J Med Chem (2014) 86: 578-88 [PMID:25218907]
ChEMBL Displacement of [3H]N-alpha-Methylhistamine from human recombinant H3 receptor expressed in HEK293 cells by competitive binding assay B 9.9 pKi 0.13 nM Ki Eur J Med Chem (2014) 86: 578-588 [PMID:25218907]
ChEMBL Inverse agonist activity at human histamine H3 receptor by GTPgammaS binding assay F 8.6 pIC50 2.51 nM IC50 J Med Chem (2011) 54: 26-53 [PMID:21062081]

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]