verlukast [Ligand Id: 6193] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL280481 (L-668,019, L-668019, MK-0679, MK-679, Verlukast)
  • 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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  • ABCC1/Multidrug resistance-associated protein 1 in Human [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
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  • OATP2B1 in Human [GtoPdb: 1224] [UniProtKB: O94956]
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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 Antagonism of [3H]leukotriene D4 binding in dimethyl sulfoxide differentiated U937 cell membrane preparations. - 7.97 pIC50 10.7 nM IC50 Can J Physiol Pharmacol (1991) 69: 1847-54 [PMID:1666333]
ChEMBL In vitro inhibitory activity against Cysteinyl leukotriene D4 receptor from human lung membrane B 8.1 pIC50 8 nM IC50 J Med Chem (1990) 33: 2841-2845 [PMID:2170650]
GtoPdb against [3H]LTD4 in human lung homogenate - 8.1 pIC50 8 nM IC50 Can J Physiol Pharmacol (1991) 69: 1847-54 [PMID:1666333]
Cysteinyl leukotriene receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
ChEMBL Inhibition of [3H]LTD4 binding on guinea-pig lung membranes B 8.41 pIC50 3.9 nM IC50 Bioorg Med Chem Lett (1995) 5: 1615-1620
ChEMBL Binding affinity against Cysteinyl leukotriene D4 receptor from guinea pig lung membrane B 8.49 pIC50 3.2 nM IC50 J Med Chem (1990) 33: 2841-2845 [PMID:2170650]
ChEMBL Displacement of [3H]LTD4 from LTD4 receptor in guinea pig lung membrane B 8.51 pIC50 3.1 nM IC50 J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
ChEMBL Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay B 5.55 pIC50 2800 nM IC50 J Med Chem (2012) 55: 424-436 [PMID:22112208]
OATP2B1 in Human [GtoPdb: 1224] [UniProtKB: O94956]
GtoPdb - - 5.55 pKi 2800 nM Ki J Med Chem (2012) 55: 4740-63 [PMID:22541068]

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]