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Assay Detail

CHEMBL5332633

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

Binding
Inhibition of human recombinant FAAH using AMC-AA as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by multimode plate reader analysis
23
Total Activities
23
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

Fatty-acid amide hydrolase 1 (CHEMBL2243)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of potent and selective FAAH inhibitors with improved drug-like properties as potential tools to treat neuroinflammatory conditions.
Papa A, Pasquini S, Galvani F, Cammarota M, Contri C, Carullo G, Gemma S, Ramunno A, Lamponi S, Gorelli B, Saponara S, Varani K, Mor M, Campiani G, Boscia F, Vincenzi F, Lodola A, Butini S.
Eur J Med Chem (2023) 246 : 114952 -114952
PubMed 36462439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.11 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2165084 1 8.43
CHEMBL5401122 1 8.12
CHEMBL5430250 1 8.08
CHEMBL5417524 1 8.00
CHEMBL5410254 1 7.98
CHEMBL5432036 1 7.93
CHEMBL5405509 1 7.81
CHEMBL5420923 1 7.80
CHEMBL5436635 1 7.58
CHEMBL184238 URB-597 1.0 1 7.51
CHEMBL5429985 1 7.32
CHEMBL2165094 1 6.99
CHEMBL5440014 1 6.89
CHEMBL5419246 1 6.78
CHEMBL5403566 1 6.73
CHEMBL5403865 1 6.71
CHEMBL5419615 1 6.60
CHEMBL5427155 1 6.50
CHEMBL5396366 1 6.39
CHEMBL5416058 1 5.98
CHEMBL5419776 1 5.18
CHEMBL5430706 1 5.07
CHEMBL5412058 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2165084 IC50 = 3.72 nM 8.43
CHEMBL5401122 IC50 = 7.54 nM 8.12
CHEMBL5430250 IC50 = 8.29 nM 8.08
CHEMBL5417524 IC50 = 10.1 nM 8.00
CHEMBL5410254 IC50 = 10.5 nM 7.98
CHEMBL5432036 IC50 = 11.7 nM 7.93
CHEMBL5405509 IC50 = 15.6 nM 7.81
CHEMBL5420923 IC50 = 15.8 nM 7.80
CHEMBL5436635 IC50 = 26.3 nM 7.58
CHEMBL184238 URB-597 IC50 = 31.1 nM 7.51
CHEMBL5429985 IC50 = 47.4 nM 7.32
CHEMBL2165094 IC50 = 102.0 nM 6.99
CHEMBL5440014 IC50 = 128.0 nM 6.89
CHEMBL5419246 IC50 = 165.0 nM 6.78
CHEMBL5403566 IC50 = 188.0 nM 6.73
CHEMBL5403865 IC50 = 194.0 nM 6.71
CHEMBL5419615 IC50 = 253.0 nM 6.60
CHEMBL5427155 IC50 = 315.0 nM 6.50
CHEMBL5396366 IC50 = 407.0 nM 6.39
CHEMBL5416058 IC50 = 1044.0 nM 5.98
CHEMBL5419776 IC50 = 6556.0 nM 5.18
CHEMBL5430706 IC50 = 8450.0 nM 5.07
CHEMBL5412058 IC50 > 10000.0 nM -