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) |
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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 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]
