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Assay Detail

CHEMBL831110

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

Binding
Inhibitory concentration against Triacylglycerol hydrolase
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.
Boger DL, Miyauchi H, Du W, Hardouin C, Fecik RA, Cheng H, Hwang I, Hedrick MP, Leung D, Acevedo O, Guimarães CR, Jorgensen WL, Cravatt BF.
J Med Chem (2005) 48 : 1849 -1856
PubMed 15771430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.15 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413727 1 9.30
CHEMBL175854 1 9.00
CHEMBL91416 1 9.00
CHEMBL93675 1 8.70
CHEMBL367966 1 8.52
CHEMBL293277 1 8.40
CHEMBL91417 1 8.30
CHEMBL90258 1 8.00
CHEMBL292454 1 8.00
CHEMBL366907 1 7.70
CHEMBL90308 1 7.22
CHEMBL175580 1 6.30
CHEMBL177577 1 6.22
CHEMBL35925 1 6.00
CHEMBL89946 1 5.34
CHEMBL422064 1 5.32
CHEMBL39412 1 5.05
CHEMBL285678 1 5.00
CHEMBL174397 1 4.52
CHEMBL426230 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413727 IC50 = 0.5 nM 9.30
CHEMBL175854 IC50 = 1.0 nM 9.00
CHEMBL91416 IC50 = 1.0 nM 9.00
CHEMBL93675 IC50 = 2.0 nM 8.70
CHEMBL367966 IC50 = 3.0 nM 8.52
CHEMBL293277 IC50 = 4.0 nM 8.40
CHEMBL91417 IC50 = 5.0 nM 8.30
CHEMBL90258 IC50 = 10.0 nM 8.00
CHEMBL292454 IC50 = 10.0 nM 8.00
CHEMBL366907 IC50 = 20.0 nM 7.70
CHEMBL90308 IC50 = 60.0 nM 7.22
CHEMBL175580 IC50 = 500.0 nM 6.30
CHEMBL177577 IC50 = 600.0 nM 6.22
CHEMBL35925 IC50 = 1000.0 nM 6.00
CHEMBL89946 IC50 = 4600.0 nM 5.34
CHEMBL422064 IC50 = 4800.0 nM 5.32
CHEMBL39412 IC50 = 9000.0 nM 5.05
CHEMBL285678 IC50 = 10000.0 nM 5.00
CHEMBL174397 IC50 = 30000.0 nM 4.52
CHEMBL426230 IC50 > 100000.0 nM -