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Assay Detail

CHEMBL706181

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

Binding
Inhibitory activity against recombinant human Leukotriene A4 hydrolase
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Kelatorphan and related analogs: potent and selective inhibitors of leukotriene A4 hydrolase
Penning TD, Askonas LJ, Djuric SW, Haack RA, Yu SS, Michener ML, Krivi GG, Pyla E
Bioorg Med Chem Lett (1995) 5 : 2517 -2522
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.22 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86211 1 8.52
CHEMBL315255 1 8.30
CHEMBL85320 KELATORPHAN 1 8.30
CHEMBL419305 1 8.10
CHEMBL431019 1 8.00
CHEMBL83291 1 8.00
CHEMBL85430 1 7.92
CHEMBL85512 1 7.52
CHEMBL82898 1 6.52
CHEMBL85542 1 5.75
CHEMBL1560 CAPTOPRIL 4.0 1 5.00
CHEMBL311933 1 4.70
CHEMBL82343 1 -
CHEMBL313284 1 -
CHEMBL86201 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86211 IC50 = 3.0 nM 8.52
CHEMBL315255 IC50 = 5.0 nM 8.30
CHEMBL85320 KELATORPHAN IC50 = 5.0 nM 8.30
CHEMBL419305 IC50 = 8.0 nM 8.10
CHEMBL431019 IC50 = 10.0 nM 8.00
CHEMBL83291 IC50 = 10.0 nM 8.00
CHEMBL85430 IC50 = 12.0 nM 7.92
CHEMBL85512 IC50 = 30.0 nM 7.52
CHEMBL82898 IC50 = 300.0 nM 6.52
CHEMBL85542 IC50 = 1800.0 nM 5.75
CHEMBL1560 CAPTOPRIL IC50 = 10000.0 nM 5.00
CHEMBL311933 IC50 = 20000.0 nM 4.70
CHEMBL82343 IC50 > 10000.0 nM -
CHEMBL313284 IC50 > 3000.0 nM -
CHEMBL86201 IC50 > 3000.0 nM -