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Assay Detail

CHEMBL5732334

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

Binding
Enzyme Assay: The compounds of the invention are assessed for the ability to interact with human LTA4 hydrolase in an enzymatic assay that measures the ability of the enzyme to cleave the peptide bond of arginyl-aminomethylcoumarin (Arg-AMC). LTA4H Enzyme (1 nM final), Arg-AMC substrate (50 μM final), and compound are combined in a reaction buffer (50 mM Tris-HCl (pH 7.5), 100 mM KCl, 0.5% bovine serum albumin) at room temperature for 1 h. The formation of product is assessed by measuring the fluorescence of aminomethylcoumarin product (excitation wavelength 380 nm/emission wavelength 460 nm).
ChEMBL ↗
888
Total Activities
295
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Benzodioxane inhibitors of leukotriene production for combination therapy
(2017)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 296 9.17 10.38
kon 296 - -
k_off 296 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5924242 — — 3 10.38
CHEMBL6060058 — — 3 10.15
CHEMBL5797467 — — 3 10.10
CHEMBL6015103 — — 3 10.05
CHEMBL5990393 — — 3 10.05
CHEMBL5780202 — — 3 10.05
CHEMBL5904849 — — 3 10.05
CHEMBL5836580 — — 3 10.00
CHEMBL5809166 — — 3 10.00
CHEMBL5970714 — — 3 10.00
CHEMBL5862086 — — 3 10.00
CHEMBL5908013 — — 3 9.96
CHEMBL6046439 — — 3 9.96
CHEMBL6064488 — — 3 9.92
CHEMBL5822057 — — 3 9.92
CHEMBL5840601 — — 3 9.92
CHEMBL5956548 — — 3 9.89
CHEMBL5880832 — — 3 9.89
CHEMBL5839428 — — 3 9.89
CHEMBL5785797 — — 3 9.89
CHEMBL6036521 — — 3 9.89
CHEMBL6015459 — — 3 9.85
CHEMBL6009509 — — 3 9.85
CHEMBL5754908 — — 3 9.85
CHEMBL5971194 — — 3 9.85
CHEMBL5854837 — — 3 9.85
CHEMBL5785372 — — 3 9.82
CHEMBL5895730 — — 3 9.82
CHEMBL5791547 — — 3 9.82
CHEMBL5882143 — — 3 9.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5924242 — IC50 = 0.042 nM 10.38
CHEMBL6060058 — IC50 = 0.07 nM 10.15
CHEMBL5797467 — IC50 = 0.08 nM 10.10
CHEMBL5904849 — IC50 = 0.09 nM 10.05
CHEMBL6015103 — IC50 = 0.09 nM 10.05
CHEMBL5990393 — IC50 = 0.09 nM 10.05
CHEMBL5780202 — IC50 = 0.09 nM 10.05
CHEMBL5862086 — IC50 = 0.1 nM 10.00
CHEMBL5809166 — IC50 = 0.1 nM 10.00
CHEMBL5836580 — IC50 = 0.1 nM 10.00
CHEMBL5970714 — IC50 = 0.1 nM 10.00
CHEMBL6046439 — IC50 = 0.11 nM 9.96
CHEMBL5908013 — IC50 = 0.11 nM 9.96
CHEMBL5822057 — IC50 = 0.12 nM 9.92
CHEMBL5840601 — IC50 = 0.12 nM 9.92
CHEMBL6064488 — IC50 = 0.12 nM 9.92
CHEMBL5880832 — IC50 = 0.13 nM 9.89
CHEMBL5785797 — IC50 = 0.13 nM 9.89
CHEMBL5956548 — IC50 = 0.13 nM 9.89
CHEMBL6036521 — IC50 = 0.13 nM 9.89
CHEMBL5839428 — IC50 = 0.13 nM 9.89
CHEMBL6015459 — IC50 = 0.14 nM 9.85
CHEMBL5971194 — IC50 = 0.14 nM 9.85
CHEMBL6009509 — IC50 = 0.14 nM 9.85
CHEMBL5854837 — IC50 = 0.14 nM 9.85
CHEMBL5754908 — IC50 = 0.14 nM 9.85
CHEMBL5785372 — IC50 = 0.15 nM 9.82
CHEMBL6006360 — IC50 = 0.15 nM 9.82
CHEMBL5791547 — IC50 = 0.15 nM 9.82
CHEMBL5882143 — IC50 = 0.15 nM 9.82
CHEMBL5895730 — IC50 = 0.15 nM 9.82
CHEMBL5880083 — IC50 = 0.16 nM 9.80
CHEMBL5888738 — IC50 = 0.16 nM 9.80
CHEMBL5978426 — IC50 = 0.16 nM 9.80
CHEMBL5832817 — IC50 = 0.16 nM 9.80
CHEMBL5878596 — IC50 = 0.16 nM 9.80
CHEMBL5774953 — IC50 = 0.16 nM 9.80
CHEMBL5917850 — IC50 = 0.16 nM 9.80
CHEMBL5918365 — IC50 = 0.16 nM 9.80
CHEMBL5945629 — IC50 = 0.16 nM 9.80
CHEMBL5958377 — IC50 = 0.16 nM 9.80
CHEMBL6045833 — IC50 = 0.16 nM 9.80
CHEMBL5973813 — IC50 = 0.17 nM 9.77
CHEMBL6019068 — IC50 = 0.17 nM 9.77
CHEMBL5923789 — IC50 = 0.17 nM 9.77
CHEMBL5806002 — IC50 = 0.17 nM 9.77
CHEMBL5943998 — IC50 = 0.17 nM 9.77
CHEMBL5868663 — IC50 = 0.17 nM 9.77
CHEMBL5765160 — IC50 = 0.17 nM 9.77
CHEMBL5968539 — IC50 = 0.17 nM 9.77