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Assay Detail

CHEMBL4835860

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Binding
Inhibition of NAAA (unknown origin)
9
Total Activities
9
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

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

Publication

Design and Structure-Activity Relationships of Isothiocyanates as Potent and Selective <i>N</i>-Acylethanolamine-Hydrolyzing Acid Amidase Inhibitors.
Malamas MS, Pavlopoulos S, Alapafuja SO, Farah SI, Zvonok A, Mohammad KA, West J, Perry NT, Pelekoudas DN, Rajarshi G, Shields C, Chandrashekhar H, Wood J, Makriyannis A.
J Med Chem (2021) 64 : 5956 -5972
PubMed 33900772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.86 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4633213 1 9.05
CHEMBL4642907 1 8.55
CHEMBL4647961 1 8.22
CHEMBL2419814 1 8.15
CHEMBL2064166 1 8.15
CHEMBL4215669 1 8.05
CHEMBL3770558 1 7.48
CHEMBL4871398 1 6.64
CHEMBL3770509 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4633213 IC50 = 0.9 nM 9.05
CHEMBL4642907 IC50 = 2.8 nM 8.55
CHEMBL4647961 IC50 = 6.0 nM 8.22
CHEMBL2419814 IC50 = 7.0 nM 8.15
CHEMBL2064166 IC50 = 7.0 nM 8.15
CHEMBL4215669 IC50 = 9.0 nM 8.05
CHEMBL3770558 IC50 = 33.0 nM 7.48
CHEMBL4871398 IC50 = 230.0 nM 6.64
CHEMBL3770509 IC50 = 340.0 nM 6.47