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Assay Detail

CHEMBL961602

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Binding
Inhibition of TGH
10
Total Activities
10
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

Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase.
DeMartino JK, Garfunkle J, Hochstatter DG, Cravatt BF, Boger DL.
Bioorg Med Chem Lett (2008) 18 : 5842 -5846
PubMed 18639454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.65 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220125 1 7.70
CHEMBL220770 1 7.70
CHEMBL462423 1 7.52
CHEMBL461544 1 7.22
CHEMBL373606 1 6.70
CHEMBL177577 1 6.22
CHEMBL513787 1 6.16
CHEMBL460317 1 5.60
CHEMBL461541 1 5.00
CHEMBL220729 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220125 IC50 = 20.0 nM 7.70
CHEMBL220770 IC50 = 20.0 nM 7.70
CHEMBL462423 IC50 = 30.0 nM 7.52
CHEMBL461544 IC50 = 60.0 nM 7.22
CHEMBL373606 IC50 = 200.0 nM 6.70
CHEMBL177577 IC50 = 600.0 nM 6.22
CHEMBL513787 IC50 = 700.0 nM 6.16
CHEMBL460317 IC50 = 2500.0 nM 5.60
CHEMBL461541 IC50 = 10000.0 nM 5.00
CHEMBL220729 IC50 > 100000.0 nM -