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Assay Detail

CHEMBL990976

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

Binding
Inhibition of human recombinant leukotriene A4 hydrolase by enzyme immunoassay
42
Total Activities
42
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

Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
Grice CA, Tays KL, Savall BM, Wei J, Butler CR, Axe FU, Bembenek SD, Fourie AM, Dunford PJ, Lundeen K, Coles F, Xue X, Riley JP, Williams KN, Karlsson L, Edwards JP.
J Med Chem (2008) 51 : 4150 -4169
PubMed 18588282 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 7.53 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL482254 1 8.40
CHEMBL518156 1 8.22
CHEMBL479958 1 8.15
CHEMBL479383 1 8.10
CHEMBL446514 1 8.10
CHEMBL481343 1 8.05
CHEMBL518155 1 8.00
CHEMBL481280 1 7.96
CHEMBL481863 1 7.96
CHEMBL472138 1 7.96
CHEMBL480131 1 7.92
CHEMBL480130 1 7.92
CHEMBL480137 1 7.89
CHEMBL521259 1 7.89
CHEMBL482058 1 7.89
CHEMBL481351 1 7.85
CHEMBL519127 1 7.85
CHEMBL480336 1 7.80
CHEMBL517533 1 7.77
CHEMBL470753 1 7.77
CHEMBL479382 1 7.68
CHEMBL517998 1 7.57
CHEMBL511292 1 7.55
CHEMBL482056 1 7.54
CHEMBL481173 1 7.51
CHEMBL479752 1 7.47
CHEMBL520942 1 7.46
CHEMBL482057 1 7.30
CHEMBL519128 1 7.27
CHEMBL482256 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL482254 IC50 = 4.0 nM 8.40
CHEMBL518156 IC50 = 6.0 nM 8.22
CHEMBL479958 IC50 = 7.0 nM 8.15
CHEMBL479383 IC50 = 8.0 nM 8.10
CHEMBL446514 IC50 = 8.0 nM 8.10
CHEMBL481343 IC50 = 9.0 nM 8.05
CHEMBL518155 IC50 = 10.0 nM 8.00
CHEMBL481280 IC50 = 11.0 nM 7.96
CHEMBL481863 IC50 = 11.0 nM 7.96
CHEMBL472138 IC50 = 11.0 nM 7.96
CHEMBL480131 IC50 = 12.0 nM 7.92
CHEMBL480130 IC50 = 12.0 nM 7.92
CHEMBL480137 IC50 = 13.0 nM 7.89
CHEMBL482058 IC50 = 13.0 nM 7.89
CHEMBL521259 IC50 = 13.0 nM 7.89
CHEMBL481351 IC50 = 14.0 nM 7.85
CHEMBL519127 IC50 = 14.0 nM 7.85
CHEMBL480336 IC50 = 16.0 nM 7.80
CHEMBL517533 IC50 = 17.0 nM 7.77
CHEMBL470753 IC50 = 17.0 nM 7.77
CHEMBL479382 IC50 = 21.0 nM 7.68
CHEMBL517998 IC50 = 27.0 nM 7.57
CHEMBL511292 IC50 = 28.0 nM 7.55
CHEMBL482056 IC50 = 29.0 nM 7.54
CHEMBL481173 IC50 = 31.0 nM 7.51
CHEMBL479752 IC50 = 34.0 nM 7.47
CHEMBL520942 IC50 = 35.0 nM 7.46
CHEMBL482057 IC50 = 50.0 nM 7.30
CHEMBL519128 IC50 = 54.0 nM 7.27
CHEMBL482256 IC50 = 58.0 nM 7.24
CHEMBL454760 IC50 = 59.0 nM 7.23
CHEMBL520120 IC50 = 66.0 nM 7.18
CHEMBL480327 IC50 = 66.0 nM 7.18
CHEMBL480136 IC50 = 66.0 nM 7.18
CHEMBL470929 IC50 = 70.0 nM 7.16
CHEMBL481862 IC50 = 84.0 nM 7.08
CHEMBL479788 IC50 = 87.0 nM 7.06
CHEMBL454177 IC50 = 110.0 nM 6.96
CHEMBL482255 IC50 = 140.0 nM 6.85
CHEMBL520287 IC50 = 350.0 nM 6.46
CHEMBL481690 IC50 = 710.0 nM 6.15
CHEMBL521257 IC50 = 3000.0 nM 5.52