toreforant [Ligand Id: 9276] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3301609 (Jnj-38518168, JNJ-38518168, Toreforant)
  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
GtoPdb Displacament of histamine from human H4 recepotor expressed in mammalian cells. - 7.08 pKi 83 nM Ki WO2007117399. Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor (2007)
ChEMBL Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method B 7.96 pKi 11 nM Ki US-20070244126-A1. Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor (2007)
ChEMBL Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant B 8.08 pKi 8.4 nM Ki Eur J Med Chem (2023) 249: 115151-115151 [PMID:36731273]

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]