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Assay Detail

CHEMBL1777073

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of LTA4 hydrolase in human whole blood assessed as inhibition of calcium ionophore A23187-induced LTB4 production after 0.5 hrs by ELISA
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Leukotriene A-4 hydrolase (CHEMBL4618)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of dual target inhibitors against cyclooxygenases and leukotriene A4 hydrolyase.
Chen Z, Wu Y, Liu Y, Yang S, Chen Y, Lai L.
J Med Chem (2011) 54 : 3650 -3660
PubMed 21542630 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.09 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1775107 1 7.54
CHEMBL1775105 1 6.96
CHEMBL1775091 1 6.75
CHEMBL1775104 1 6.54
CHEMBL1775092 1 6.17
CHEMBL1775089 1 6.16
CHEMBL1775103 1 6.14
CHEMBL1775099 1 6.14
CHEMBL162424 1 6.11
CHEMBL1775106 1 6.01
CHEMBL1775102 1 6.00
CHEMBL1775088 1 5.85
CHEMBL1775101 1 5.70
CHEMBL1775110 1 5.68
CHEMBL1775087 1 5.16
CHEMBL1775098 1 4.47
CHEMBL1775100 1 -
CHEMBL56367 NIMESULIDE 4.0 1 -
CHEMBL1775097 1 -
CHEMBL1775096 1 -
CHEMBL1775095 1 -
CHEMBL1775094 1 -
CHEMBL1775093 1 -
CHEMBL1775108 1 -
CHEMBL1775109 1 -
CHEMBL1775090 1 -
CHEMBL1775111 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1775107 IC50 = 29.0 nM 7.54
CHEMBL1775105 IC50 = 110.0 nM 6.96
CHEMBL1775091 IC50 = 180.0 nM 6.75
CHEMBL1775104 IC50 = 290.0 nM 6.54
CHEMBL1775092 IC50 = 670.0 nM 6.17
CHEMBL1775089 IC50 = 690.0 nM 6.16
CHEMBL1775103 IC50 = 730.0 nM 6.14
CHEMBL1775099 IC50 = 730.0 nM 6.14
CHEMBL162424 IC50 = 780.0 nM 6.11
CHEMBL1775106 IC50 = 970.0 nM 6.01
CHEMBL1775102 IC50 = 990.0 nM 6.00
CHEMBL1775088 IC50 = 1400.0 nM 5.85
CHEMBL1775101 IC50 = 2000.0 nM 5.70
CHEMBL1775110 IC50 = 2100.0 nM 5.68
CHEMBL1775087 IC50 = 6900.0 nM 5.16
CHEMBL1775098 IC50 = 34000.0 nM 4.47
CHEMBL1775100 IC50 > 100000.0 nM -
CHEMBL56367 NIMESULIDE IC50 > 100000.0 nM -
CHEMBL1775097 IC50 > 100000.0 nM -
CHEMBL1775096 IC50 > 100000.0 nM -
CHEMBL1775095 IC50 > 100000.0 nM -
CHEMBL1775094 IC50 > 100000.0 nM -
CHEMBL1775093 IC50 > 100000.0 nM -
CHEMBL1775108 IC50 > 100000.0 nM -
CHEMBL1775109 IC50 > 100000.0 nM -
CHEMBL1775090 IC50 > 100000.0 nM -
CHEMBL1775111 IC50 > 100000.0 nM -