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Assay Detail

CHEMBL3861345

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

Binding
Inhibition of human C-terminal his6-tagged/N-terminal T7 gene leader sequence-tagged LTA4H using L-arginine-7-amino-4-Methylcoumarine as substrate preincubated for 30 mins followed by substrate addition measured for 30 mins by fluorescence assay
5
Total Activities
5
Compounds Tested
1
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

Thermodynamic properties of leukotriene A4 hydrolase inhibitors.
Wittmann SK, Kalinowsky L, Kramer JS, Bloecher R, Knapp S, Steinhilber D, Pogoryelov D, Proschak E, Heering J.
Bioorg Med Chem (2016) 24 : 5243 -5248
PubMed 27651294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.76 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112671 1 8.22
CHEMBL3921982 1 7.22
CHEMBL29292 UBENIMEX 2.0 1 6.52
CHEMBL3883608 1 6.40
CHEMBL1560 CAPTOPRIL 4.0 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112671 IC50 = 6.0 nM 8.22
CHEMBL3921982 IC50 = 60.0 nM 7.22
CHEMBL29292 UBENIMEX IC50 = 300.0 nM 6.52
CHEMBL3883608 IC50 = 400.0 nM 6.40
CHEMBL1560 CAPTOPRIL IC50 = 3600.0 nM 5.44