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Assay Detail

CHEMBL706180

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

Binding
Inhibition of human leukotriene A4 hydrolase (LTA-4).
37
Total Activities
37
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 potent leukotriene A(4) hydrolase inhibitors. Identification of 3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid.
Penning TD, Russell MA, Chen BB, Chen HY, Liang CD, Mahoney MW, Malecha JW, Miyashiro JM, Yu SS, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG.
J Med Chem (2002) 45 : 3482 -3490
PubMed 12139459 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.11 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL323686 1 9.00
CHEMBL119683 1 8.89
CHEMBL117549 1 8.89
CHEMBL326601 1 8.70
CHEMBL543405 1 8.60
CHEMBL421048 1 8.40
CHEMBL119545 1 8.33
CHEMBL117654 1 8.15
CHEMBL119814 1 8.15
CHEMBL420502 1 7.85
CHEMBL116571 1 7.80
CHEMBL326507 1 7.75
CHEMBL117148 1 7.72
CHEMBL420866 1 7.57
CHEMBL117833 1 7.51
CHEMBL117132 1 7.37
CHEMBL117256 1 7.08
CHEMBL117455 1 6.96
CHEMBL119179 1 6.85
CHEMBL119529 1 6.80
CHEMBL115857 1 6.72
CHEMBL119054 1 6.70
CHEMBL119240 1 6.66
CHEMBL325224 1 6.66
CHEMBL117314 1 6.60
CHEMBL331917 1 6.35
CHEMBL119124 1 6.09
CHEMBL332556 1 6.06
CHEMBL419220 1 6.02
CHEMBL118014 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL323686 IC50 = 1.0 nM 9.00
CHEMBL119683 IC50 = 1.3 nM 8.89
CHEMBL117549 IC50 = 1.3 nM 8.89
CHEMBL326601 IC50 = 2.0 nM 8.70
CHEMBL543405 IC50 = 2.5 nM 8.60
CHEMBL421048 IC50 = 4.0 nM 8.40
CHEMBL119545 IC50 = 4.7 nM 8.33
CHEMBL117654 IC50 = 7.0 nM 8.15
CHEMBL119814 IC50 = 7.0 nM 8.15
CHEMBL420502 IC50 = 14.0 nM 7.85
CHEMBL116571 IC50 = 16.0 nM 7.80
CHEMBL326507 IC50 = 18.0 nM 7.75
CHEMBL117148 IC50 = 19.0 nM 7.72
CHEMBL420866 IC50 = 27.0 nM 7.57
CHEMBL117833 IC50 = 31.0 nM 7.51
CHEMBL117132 IC50 = 43.0 nM 7.37
CHEMBL117256 IC50 = 84.0 nM 7.08
CHEMBL117455 IC50 = 110.0 nM 6.96
CHEMBL119179 IC50 = 140.0 nM 6.85
CHEMBL119529 IC50 = 160.0 nM 6.80
CHEMBL115857 IC50 = 190.0 nM 6.72
CHEMBL119054 IC50 = 200.0 nM 6.70
CHEMBL119240 IC50 = 220.0 nM 6.66
CHEMBL325224 IC50 = 220.0 nM 6.66
CHEMBL117314 IC50 = 250.0 nM 6.60
CHEMBL331917 IC50 = 450.0 nM 6.35
CHEMBL119124 IC50 = 820.0 nM 6.09
CHEMBL332556 IC50 = 870.0 nM 6.06
CHEMBL419220 IC50 = 950.0 nM 6.02
CHEMBL118014 IC50 = 1650.0 nM 5.78
CHEMBL116908 IC50 = 2500.0 nM 5.60
CHEMBL323873 IC50 = 3000.0 nM 5.52
CHEMBL119024 IC50 = 3700.0 nM 5.43
CHEMBL119422 IC50 = 6600.0 nM 5.18
CHEMBL117472 IC50 = 10700.0 nM 4.97
CHEMBL117231 IC50 > 10000.0 nM -
CHEMBL119612 IC50 < 0.5 nM -