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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
