pobilukast [Ligand Id: 3334] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL22776 (Pobilukast, SKF-104353)
  • CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
  • Cysteinyl leukotriene receptor 1 in Guinea pig [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
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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
CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
GtoPdb against [3H]LTD4 in human lung parenchyma - 7.1 pKi - - - Mol Pharmacol (1998) 53: 750-8 [PMID:9547367]
ChEMBL Binding affinity against Cysteinyl leukotriene D4 receptor in human lung membranes using [3H]LTD4 as the radioligand. B 8 pKi 10 nM Ki J Med Chem (1987) 30: 959-961 [PMID:3035179]
GtoPdb - - 7.52 pIC50 30 nM IC50 Mol Pharmacol (1999) 56: 657-63 [PMID:10462554]
GtoPdb - - 8.26 pIC50 5.5 nM IC50 Mol Pharmacol (1999) 56: 657-63 [PMID:10462554]
Cysteinyl leukotriene receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
ChEMBL Inhibition constant for displacement of [3H]-LTD4 on guinea pig lung parenchymal membranes. B 8.3 pKi 5 nM Ki J Med Chem (1990) 33: 1781-1790 [PMID:2342072]
ChEMBL Compound was evaluated for its ability to displace [3H]LTD4 from LTD4 receptor in guinea pig lung membranes B 8.3 pKi 5 nM Ki J Med Chem (1991) 34: 1235-1242 [PMID:1849993]
ChEMBL Binding affinity against Cysteinyl leukotriene D4 receptor in guinea pig lung membranes using [3H]LTD4 as the radioligand. B 8.3 pKi 5 nM Ki J Med Chem (1987) 30: 959-961 [PMID:3035179]
CysLT2 receptor in Human [GtoPdb: 270] [UniProtKB: Q9NS75]
GtoPdb against LTC4 Ca2+ mobilisation assay in HUVEC - 6.2 pA2 - - - Prostaglandins Other Lipid Mediat (2015) 120: 115-25 [PMID:25839425]

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]