[3H]ICI-198615 [Ligand Id: 3414] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL22033 (ICI-198615)
  • Cysteinyl leukotriene receptor 1 in Guinea pig [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
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  • CysLT1 receptor in Human [GtoPdb: 269] [UniProtKB: Q9Y271]
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  • CysLT2 receptor in Human [GtoPdb: 270] [UniProtKB: Q9NS75]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Cysteinyl leukotriene receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
ChEMBL Dissociation constant for CysLT1 receptor was determined by the displacement of [3H]LTD4 from guinea pig lung membranes B 4.52 pKd 30100 nM Kd Bioorg Med Chem Lett (1997) 7: 1331-1336
ChEMBL Binding affinity against LTD4 receptor in guinea pig lung membranes. B 9.52 pKi 0.3 nM Ki J Med Chem (1991) 34: 1704-1707 [PMID:1851845]
ChEMBL Compound was evaluated for its ability to displace [3H]LTD4 from LTD4 receptor in guinea pig lung membranes B 9.52 pKi 0.3 nM Ki J Med Chem (1991) 34: 1235-1242 [PMID:1849993]
CysLT1 receptor in Human [GtoPdb: 269] [UniProtKB: Q9Y271]
GtoPdb in human lung parenchyma - 10.6 pKd 0.03 nM Kd Biochem Pharmacol (1992) 44: 1411-5 [PMID:1329767]
CysLT2 receptor in Human [GtoPdb: 270] [UniProtKB: Q9NS75]
GtoPdb - - 5.2 pKd - - - Biochem Pharmacol (1992) 44: 1411-5 [PMID:1329767]

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]