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Assay Detail

CHEMBL3772809

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

Binding
Inhibition of recombinant human NAAA expressed in HEK293 cells after 30 mins by UPLC/MS analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

N-acylethanolamine-hydrolyzing acid amidase (CHEMBL4349)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent α-amino-β-lactam carbamic acid ester as NAAA inhibitors. Synthesis and structure-activity relationship (SAR) studies.
Nuzzi A, Fiasella A, Ortega JA, Pagliuca C, Ponzano S, Pizzirani D, Bertozzi SM, Ottonello G, Tarozzo G, Reggiani A, Bandiera T, Bertozzi F, Piomelli D.
Eur J Med Chem (2016) 111 : 138 -159
PubMed 26866968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.62 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770896 1 8.15
CHEMBL3770525 1 7.92
CHEMBL3771111 1 7.66
CHEMBL3770726 1 7.57
CHEMBL3769689 1 7.32
CHEMBL3769678 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770896 IC50 = 7.0 nM 8.15
CHEMBL3770525 IC50 = 12.0 nM 7.92
CHEMBL3771111 IC50 = 22.0 nM 7.66
CHEMBL3770726 IC50 = 27.0 nM 7.57
CHEMBL3769689 IC50 = 48.0 nM 7.32
CHEMBL3769678 IC50 = 76.0 nM 7.12