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Assay Detail

CHEMBL3768874

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

Binding
Inhibition of DAGLbeta (unknown origin)
6
Total Activities
6
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

Diacylglycerol lipase-beta (CHEMBL5521)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.
Chupak LS, Zheng X, Hu S, Huang Y, Ding M, Lewis MA, Westphal RS, Blat Y, McClure A, Gentles RG.
Bioorg Med Chem (2016) 24 : 1455 -1468
PubMed 26917221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.01 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3764876 1 7.40
CHEMBL3764017 1 7.40
CHEMBL3764093 1 7.10
CHEMBL3765022 1 6.95
CHEMBL3765421 1 6.84
CHEMBL175247 ORLISTAT 4.0 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3764876 IC50 = 40.0 nM 7.40
CHEMBL3764017 IC50 = 40.0 nM 7.40
CHEMBL3764093 IC50 = 80.0 nM 7.10
CHEMBL3765022 IC50 = 112.0 nM 6.95
CHEMBL3765421 IC50 = 146.0 nM 6.84
CHEMBL175247 ORLISTAT IC50 = 420.0 nM 6.38