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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 |
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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]