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Assay Detail

CHEMBL706182

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

Binding
In vitro inhibition of recombinant human leukotriene A4 hydrolase.
18
Total Activities
18
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

Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase.
Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Malecha JW, Miyashiro JM, Russell MA, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG.
Bioorg Med Chem Lett (2003) 13 : 1137 -1139
PubMed 12643929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.14 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273570 1 9.10
CHEMBL279577 1 8.10
CHEMBL14814 1 7.96
CHEMBL14608 1 7.58
CHEMBL14387 1 7.51
CHEMBL14857 1 7.44
CHEMBL14547 1 7.40
CHEMBL14789 1 7.33
CHEMBL276096 1 7.09
CHEMBL441950 1 6.92
CHEMBL279643 1 6.92
CHEMBL14739 1 6.85
CHEMBL14549 1 6.75
CHEMBL416349 1 6.30
CHEMBL14760 1 6.25
CHEMBL14502 1 6.14
CHEMBL15036 1 5.70
CHEMBL14790 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273570 IC50 = 0.8 nM 9.10
CHEMBL279577 IC50 = 8.0 nM 8.10
CHEMBL14814 IC50 = 11.0 nM 7.96
CHEMBL14608 IC50 = 26.0 nM 7.58
CHEMBL14387 IC50 = 31.0 nM 7.51
CHEMBL14857 IC50 = 36.0 nM 7.44
CHEMBL14547 IC50 = 40.0 nM 7.40
CHEMBL14789 IC50 = 47.0 nM 7.33
CHEMBL276096 IC50 = 82.0 nM 7.09
CHEMBL441950 IC50 = 120.0 nM 6.92
CHEMBL279643 IC50 = 120.0 nM 6.92
CHEMBL14739 IC50 = 140.0 nM 6.85
CHEMBL14549 IC50 = 180.0 nM 6.75
CHEMBL416349 IC50 = 500.0 nM 6.30
CHEMBL14760 IC50 = 560.0 nM 6.25
CHEMBL14502 IC50 = 730.0 nM 6.14
CHEMBL15036 IC50 = 2000.0 nM 5.70
CHEMBL14790 IC50 > 3000.0 nM -