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Assay Detail

CHEMBL3384492

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

Binding
Inhibition of human recombinant FAAH expressed in COS7 cells using anandamide as substrate
34
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
Korhonen J, Kuusisto A, van Bruchem J, Patel JZ, Laitinen T, Navia-Paldanius D, Laitinen JT, Savinainen JR, Parkkari T, Nevalainen TJ.
Bioorg Med Chem (2014) 22 : 6694 -6705
PubMed 25282655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.83 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356971 2 8.57
CHEMBL3356980 2 8.47
CHEMBL3356960 2 8.22
CHEMBL3356959 2 7.96
CHEMBL3356977 2 7.82
CHEMBL3356975 2 7.64
CHEMBL3356974 2 7.05
CHEMBL3356962 2 6.85
CHEMBL3356961 2 6.64
CHEMBL1232635 2 6.55
CHEMBL3356956 2 6.35
CHEMBL3356979 2 6.15
CHEMBL3356957 2 6.01
CHEMBL3356985 2 5.79
CHEMBL3356958 2 5.64
CHEMBL2164594 2 5.52
CHEMBL3087181 2 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356971 IC50 = 2.692 nM 8.57
CHEMBL3356971 IC50 = 2.7 nM 8.57
CHEMBL3356980 IC50 = 3.4 nM 8.47
CHEMBL3356960 IC50 = 6.026 nM 8.22
CHEMBL3356960 IC50 = 6.0 nM 8.22
CHEMBL3356959 IC50 = 11.0 nM 7.96
CHEMBL3356959 IC50 = 11.22 nM 7.95
CHEMBL3356977 IC50 = 15.0 nM 7.82
CHEMBL3356977 IC50 = 15.49 nM 7.81
CHEMBL3356980 IC50 = 17.38 nM 7.76
CHEMBL3356975 IC50 = 23.0 nM 7.64
CHEMBL3356975 IC50 = 22.91 nM 7.64
CHEMBL3356974 IC50 = 89.13 nM 7.05
CHEMBL3356974 IC50 = 89.0 nM 7.05
CHEMBL3356962 IC50 = 141.25 nM 6.85
CHEMBL3356962 IC50 = 141.0 nM 6.85
CHEMBL3356961 IC50 = 229.09 nM 6.64
CHEMBL3356961 IC50 = 231.0 nM 6.64
CHEMBL1232635 IC50 = 282.0 nM 6.55
CHEMBL1232635 IC50 = 281.84 nM 6.55
CHEMBL3356956 IC50 = 446.68 nM 6.35
CHEMBL3356956 IC50 = 452.0 nM 6.34
CHEMBL3356979 IC50 = 707.95 nM 6.15
CHEMBL3356979 IC50 = 708.0 nM 6.15
CHEMBL3356957 IC50 = 977.24 nM 6.01
CHEMBL3356957 IC50 = 971.0 nM 6.01
CHEMBL3356985 IC50 = 1621.81 nM 5.79
CHEMBL3356985 IC50 = 1622.0 nM 5.79
CHEMBL3356958 IC50 = 2300.0 nM 5.64
CHEMBL3356958 IC50 = 2290.87 nM 5.64
CHEMBL2164594 IC50 = 3020.0 nM 5.52
CHEMBL2164594 IC50 = 3019.95 nM 5.52
CHEMBL3087181 IC50 = 4786.3 nM 5.32
CHEMBL3087181 IC50 = 4800.0 nM 5.32