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 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]