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Assay Detail

CHEMBL2212808

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

Binding
Inhibition of human recombinant LTA4 hydrolase expressed in SF9 cells using LTA4 as substrate assessed as LTB4 production incubated for 10 mins prior to substrate addition measured after 10 to 30 mins by enzyme immunoassay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Azabenzthiazole inhibitors of leukotriene A₄ hydrolase.
Tanis VM, Bacani GM, Blevitt JM, Chrovian CC, Crawford S, De Leon A, Fourie AM, Gomez L, Grice CA, Herman K, Kearney AM, Landry-Bayle AM, Lee-Dutra A, Nelson J, Riley JP, Santillán A, Wiener JJ, Xue X, Young AL.
Bioorg Med Chem Lett (2012) 22 : 7504 -7511
PubMed 23127888 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.92 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2207747 1 9.52
CHEMBL2207751 1 9.00
CHEMBL2207749 1 8.52
CHEMBL2207730 1 8.52
CHEMBL2207742 1 8.52
CHEMBL2207741 1 8.40
CHEMBL2207750 1 8.30
CHEMBL2207752 1 8.22
CHEMBL2207738 1 8.22
CHEMBL2207745 1 8.22
CHEMBL2207748 1 8.22
CHEMBL2207739 1 8.15
CHEMBL2207740 1 8.15
CHEMBL2207736 1 8.10
CHEMBL2207743 1 7.96
CHEMBL2207744 1 7.85
CHEMBL2207746 1 7.85
CHEMBL2207737 1 7.80
CHEMBL2207735 1 7.54
CHEMBL2207733 1 7.48
CHEMBL2207734 1 7.40
CHEMBL2207731 1 6.21
CHEMBL2207729 1 6.13
CHEMBL2207732 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2207747 IC50 = 0.3 nM 9.52
CHEMBL2207751 IC50 = 1.0 nM 9.00
CHEMBL2207749 IC50 = 3.0 nM 8.52
CHEMBL2207730 IC50 = 3.0 nM 8.52
CHEMBL2207742 IC50 = 3.0 nM 8.52
CHEMBL2207741 IC50 = 4.0 nM 8.40
CHEMBL2207750 IC50 = 5.0 nM 8.30
CHEMBL2207752 IC50 = 6.0 nM 8.22
CHEMBL2207738 IC50 = 6.0 nM 8.22
CHEMBL2207745 IC50 = 6.0 nM 8.22
CHEMBL2207748 IC50 = 6.0 nM 8.22
CHEMBL2207739 IC50 = 7.0 nM 8.15
CHEMBL2207740 IC50 = 7.0 nM 8.15
CHEMBL2207736 IC50 = 8.0 nM 8.10
CHEMBL2207743 IC50 = 11.0 nM 7.96
CHEMBL2207744 IC50 = 14.0 nM 7.85
CHEMBL2207746 IC50 = 14.0 nM 7.85
CHEMBL2207737 IC50 = 16.0 nM 7.80
CHEMBL2207735 IC50 = 29.0 nM 7.54
CHEMBL2207733 IC50 = 33.0 nM 7.48
CHEMBL2207734 IC50 = 40.0 nM 7.40
CHEMBL2207731 IC50 = 614.0 nM 6.21
CHEMBL2207729 IC50 = 733.0 nM 6.13
CHEMBL2207732 IC50 = 1800.0 nM 5.75