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Assay Detail

CHEMBL949090

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

Binding
Inhibition of TGH
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Liver carboxylesterase 1 (CHEMBL2265)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.
Kimball FS, Romero FA, Ezzili C, Garfunkle J, Rayl TJ, Hochstatter DG, Hwang I, Boger DL.
J Med Chem (2008) 51 : 937 -947
PubMed 18247553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.27 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261172 1 8.35
CHEMBL272038 1 7.80
CHEMBL220125 1 7.70
CHEMBL220770 1 7.70
CHEMBL272111 1 7.58
CHEMBL441735 1 7.52
CHEMBL258820 1 7.00
CHEMBL226990 1 6.70
CHEMBL272830 1 6.57
CHEMBL227046 1 5.92
CHEMBL220729 1 5.70
CHEMBL226938 1 5.70
CHEMBL272228 1 5.62
CHEMBL406659 1 5.16
CHEMBL271380 1 4.77
CHEMBL260535 1 4.58
CHEMBL271389 1 4.43
CHEMBL271382 1 4.05
CHEMBL260747 1 -
CHEMBL219942 1 -
CHEMBL270284 1 -
CHEMBL271789 1 -
CHEMBL177577 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261172 IC50 = 4.5 nM 8.35
CHEMBL272038 IC50 = 16.0 nM 7.80
CHEMBL220125 IC50 = 20.0 nM 7.70
CHEMBL220770 IC50 = 20.0 nM 7.70
CHEMBL272111 IC50 = 26.0 nM 7.58
CHEMBL441735 IC50 = 30.0 nM 7.52
CHEMBL258820 IC50 = 100.0 nM 7.00
CHEMBL226990 IC50 = 200.0 nM 6.70
CHEMBL272830 IC50 = 270.0 nM 6.57
CHEMBL227046 IC50 = 1200.0 nM 5.92
CHEMBL220729 IC50 = 2000.0 nM 5.70
CHEMBL226938 IC50 = 2000.0 nM 5.70
CHEMBL272228 IC50 = 2400.0 nM 5.62
CHEMBL406659 IC50 = 7000.0 nM 5.16
CHEMBL271380 IC50 = 17000.0 nM 4.77
CHEMBL260535 IC50 = 26000.0 nM 4.58
CHEMBL271389 IC50 = 37000.0 nM 4.43
CHEMBL271382 IC50 = 90000.0 nM 4.05
CHEMBL260747 IC50 > 100000.0 nM -
CHEMBL219942 IC50 > 100000.0 nM -
CHEMBL270284 IC50 > 100000.0 nM -
CHEMBL271789 IC50 > 100000.0 nM -
CHEMBL177577 IC50 > 600.0 nM -