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Assay Detail

CHEMBL3861350

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

Binding
Binding affinity to human C-terminal his6-tagged/N-terminal T7 gene leader sequence-tagged LTA4H at 25 degC by ITC method
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
Kd 5 6.10 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3921982 1 6.57
CHEMBL112671 1 6.54
CHEMBL3883608 1 6.51
CHEMBL29292 UBENIMEX 2.0 1 5.69
CHEMBL1560 CAPTOPRIL 4.0 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3921982 Kd = 270.0 nM 6.57
CHEMBL112671 Kd = 290.0 nM 6.54
CHEMBL3883608 Kd = 310.0 nM 6.51
CHEMBL29292 UBENIMEX Kd = 2050.0 nM 5.69
CHEMBL1560 CAPTOPRIL Kd = 6250.0 nM 5.20