acebilustat [Ligand Id: 11984] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4297604 (Acebilustat, Ctx-4430, CTX-4430, EP-501)
  • Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]