acebilustat [Ligand Id: 11984] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4297604 (Acebilustat, Ctx-4430, CTX-4430, EP-501) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960] | ||||||||
| ChEMBL | Inhibition of LTA4H in human whole blood assessed as reduction of calcium ionophore A23187-stimulated LTB4 generation preincubated for 4 hrs followed by ionophore stimulation and measured after 15 hrs by EIA assay | B | 6.85 | pIC50 | 142 | nM | IC50 | J Med Chem (2021) 64: 1889-1903 [PMID:33592148] |
| GtoPdb | Inhibition of LTA4H activity by the inhibitor is measured as reduction in LTB4 production in human whole blood, by ELISA | - | 7.22 | pIC50 | 60 | nM | IC50 | WO2014164658A1. Methods of inhibiting leukotriene a4 hydrolase (2014) |
| ChEMBL | Inhibition of LTA4H in human PBMC assessed as reduction of calcium ionophore A23187-stimulated LTB4 generation preincubated for 4 hrs followed by ionophore stimulation and measured after 2 hrs by EIA assay | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2021) 64: 1889-1903 [PMID:33592148] |
| ChEMBL | Inhibition of recombinant full length N-terminal His6-tagged LTA4H (unknown origin) expressed in Escherichia coli BL21 DE3 cells at enzyme concentration <1 nM using Arg-AMC as substrate preincubated for 15 mins followed by substrate addition and measured every 10 mins for 300 mins by fluorescence based assay | B | 8.31 | pIC50 | 4.9 | nM | IC50 | J Med Chem (2021) 64: 1889-1903 [PMID:33592148] |
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]
