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Assay Detail

CHEMBL4610452

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

Binding
Inhibition of activated human NAAA using fluorogenic PAMCA and N-4-methylcoumarin as substrate incubated for 90 mins by fluorescence based assay
41
Total Activities
41
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 synthesis of cyanamides as potent and selective N-acylethanolamine acid amidase inhibitors.
Malamas MS, Farah SI, Lamani M, Pelekoudas DN, Perry NT, Rajarshi G, Miyabe CY, Chandrashekhar H, West J, Pavlopoulos S, Makriyannis A.
Bioorg Med Chem (2020) 28 : 115195 -115195
PubMed 31761726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 8.33 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4633233 1 9.46
CHEMBL4640552 1 9.34
CHEMBL4642793 1 9.33
CHEMBL4635208 1 9.17
CHEMBL4640519 1 9.07
CHEMBL4644090 1 9.06
CHEMBL4633213 1 9.05
CHEMBL4649536 1 9.03
CHEMBL4637701 1 8.99
CHEMBL4646880 1 8.96
CHEMBL4632623 1 8.85
CHEMBL4645560 1 8.80
CHEMBL4635238 1 8.80
CHEMBL4646586 1 8.80
CHEMBL4641417 1 8.74
CHEMBL4643427 1 8.60
CHEMBL4642907 1 8.55
CHEMBL4636322 1 8.55
CHEMBL4637755 1 8.55
CHEMBL4643588 1 8.49
CHEMBL4645262 1 8.47
CHEMBL4638402 1 8.34
CHEMBL4638779 1 8.24
CHEMBL4639554 1 8.24
CHEMBL4643074 1 8.21
CHEMBL4649749 1 8.19
CHEMBL4634952 1 8.18
CHEMBL4637132 1 8.07
CHEMBL4637050 1 8.04
CHEMBL4641400 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4633233 IC50 = 0.35 nM 9.46
CHEMBL4640552 IC50 = 0.46 nM 9.34
CHEMBL4642793 IC50 = 0.47 nM 9.33
CHEMBL4635208 IC50 = 0.68 nM 9.17
CHEMBL4640519 IC50 = 0.85 nM 9.07
CHEMBL4644090 IC50 = 0.88 nM 9.06
CHEMBL4633213 IC50 = 0.89 nM 9.05
CHEMBL4649536 IC50 = 0.94 nM 9.03
CHEMBL4637701 IC50 = 1.03 nM 8.99
CHEMBL4646880 IC50 = 1.1 nM 8.96
CHEMBL4632623 IC50 = 1.4 nM 8.85
CHEMBL4645560 IC50 = 1.6 nM 8.80
CHEMBL4646586 IC50 = 1.6 nM 8.80
CHEMBL4635238 IC50 = 1.58 nM 8.80
CHEMBL4641417 IC50 = 1.8 nM 8.74
CHEMBL4643427 IC50 = 2.5 nM 8.60
CHEMBL4642907 IC50 = 2.8 nM 8.55
CHEMBL4636322 IC50 = 2.8 nM 8.55
CHEMBL4637755 IC50 = 2.8 nM 8.55
CHEMBL4643588 IC50 = 3.2 nM 8.49
CHEMBL4645262 IC50 = 3.4 nM 8.47
CHEMBL4638402 IC50 = 4.6 nM 8.34
CHEMBL4638779 IC50 = 5.8 nM 8.24
CHEMBL4639554 IC50 = 5.7 nM 8.24
CHEMBL4643074 IC50 = 6.1 nM 8.21
CHEMBL4649749 IC50 = 6.5 nM 8.19
CHEMBL4634952 IC50 = 6.6 nM 8.18
CHEMBL4637132 IC50 = 8.5 nM 8.07
CHEMBL4637050 IC50 = 9.2 nM 8.04
CHEMBL4641400 IC50 = 9.1 nM 8.04
CHEMBL4632779 IC50 = 11.6 nM 7.94
CHEMBL4636756 IC50 = 12.0 nM 7.92
CHEMBL4648948 IC50 = 20.8 nM 7.68
CHEMBL4637179 IC50 = 23.7 nM 7.62
CHEMBL4645479 IC50 = 26.4 nM 7.58
CHEMBL4633126 IC50 = 29.0 nM 7.54
CHEMBL4641015 IC50 = 40.0 nM 7.40
CHEMBL4636537 IC50 = 67.5 nM 7.17
CHEMBL4643165 IC50 = 74.7 nM 7.13
CHEMBL4644779 IC50 = 91.2 nM 7.04
CHEMBL4643680 IC50 = 315.0 nM 6.50