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ChEMBL ligand: CHEMBL565789 |
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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 | Binding affinity to human recombinant LTA4H by isothermal calorimetry | B | 7.6 | pKd | 25 | nM | Kd | J Med Chem (2010) 53: 573-585 [PMID:19950900] |
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 | 6.29 | pIC50 | 510 | nM | IC50 | J Med Chem (2021) 64: 1889-1903 [PMID:33592148] |
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 | 7.13 | pIC50 | 74 | 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 | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (2021) 64: 1889-1903 [PMID:33592148] |
GtoPdb | - | - | 7.3 | pIC50 | 47 | nM | IC50 | J Med Chem (2010) 53: 573-85 [PMID:19950900] |
ChEMBL | Inhibition of human recombinant LTA4H hydrolysis assessed as inhibition of LTB4 formation by LC-MS/MS | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2010) 53: 573-585 [PMID:19950900] |
ChEMBL | Inhibition of human LTA4H hydrolysis assessed as inhibition of Ca2+ ionophore-stimulated LTB4 formation in human whole blood by ELISA | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2010) 53: 573-585 [PMID:19950900] |
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]