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Assay Detail

CHEMBL895174

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

Binding
Inhibition of FAAH in rat cerebellum membranes assessed as [3H]anandamide hydrolysis
62
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebellum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Fatty-acid amide hydrolase 1 (CHEMBL3229)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationship of a series of inhibitors of monoacylglycerol hydrolysis--comparison with effects upon fatty acid amide hydrolase.
Cisneros JA, Vandevoorde S, Ortega-Gutiérrez S, Paris C, Fowler CJ, López-Rodríguez ML.
J Med Chem (2007) 50 : 5012 -5023
PubMed 17764163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Log I50 32 - -
IC50 30 4.65 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL396951 2 5.80
CHEMBL230760 2 5.28
CHEMBL243922 2 5.22
CHEMBL397182 2 5.12
CHEMBL230968 2 5.09
CHEMBL230867 2 5.00
CHEMBL231074 2 5.00
CHEMBL230967 2 4.96
CHEMBL287788 2 4.96
CHEMBL244156 2 4.92
CHEMBL395492 2 4.92
CHEMBL243722 2 4.77
CHEMBL231177 2 4.75
CHEMBL230969 2 4.72
CHEMBL425843 2 4.68
CHEMBL244134 2 4.55
CHEMBL230970 2 4.54
CHEMBL231178 2 4.50
CHEMBL287364 2 4.48
CHEMBL231076 2 4.46
CHEMBL231077 2 4.37
CHEMBL230759 2 4.29
CHEMBL231179 2 4.28
CHEMBL287130 2 4.25
CHEMBL395015 2 4.21
CHEMBL244354 2 4.16
CHEMBL243923 2 4.05
CHEMBL230866 2 4.04
CHEMBL230225 2 4.01
CHEMBL388436 2 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL396951 IC50 = 1600.0 nM 5.80
CHEMBL230760 IC50 = 5300.0 nM 5.28
CHEMBL243922 IC50 = 6000.0 nM 5.22
CHEMBL397182 IC50 = 7500.0 nM 5.12
CHEMBL230968 IC50 = 8200.0 nM 5.09
CHEMBL230867 IC50 = 10000.0 nM 5.00
CHEMBL231074 IC50 = 10000.0 nM 5.00
CHEMBL287788 IC50 = 11000.0 nM 4.96
CHEMBL230967 IC50 = 11000.0 nM 4.96
CHEMBL244156 IC50 = 12000.0 nM 4.92
CHEMBL395492 IC50 = 12000.0 nM 4.92
CHEMBL243722 IC50 = 17000.0 nM 4.77
CHEMBL231177 IC50 = 18000.0 nM 4.75
CHEMBL230969 IC50 = 19000.0 nM 4.72
CHEMBL425843 IC50 = 21000.0 nM 4.68
CHEMBL244134 IC50 = 28000.0 nM 4.55
CHEMBL230970 IC50 = 29000.0 nM 4.54
CHEMBL231178 IC50 = 32000.0 nM 4.50
CHEMBL287364 IC50 = 33000.0 nM 4.48
CHEMBL231076 IC50 = 35000.0 nM 4.46
CHEMBL231077 IC50 = 43000.0 nM 4.37
CHEMBL230759 IC50 = 51000.0 nM 4.29
CHEMBL231179 IC50 = 53000.0 nM 4.28
CHEMBL287130 IC50 = 56000.0 nM 4.25
CHEMBL395015 IC50 = 61000.0 nM 4.21
CHEMBL244354 IC50 = 69000.0 nM 4.16
CHEMBL243923 IC50 = 90000.0 nM 4.05
CHEMBL230866 IC50 = 91000.0 nM 4.04
CHEMBL230225 IC50 = 98000.0 nM 4.01
CHEMBL388436 IC50 = 99000.0 nM 4.00
CHEMBL231077 Log I50 = 4.37 -
CHEMBL231177 Log I50 = 4.75 -
CHEMBL231179 Log I50 = 4.28 -
CHEMBL231178 Log I50 = 4.49 -
CHEMBL244157 BENZOIC ACID 2,3-EPOXYPROPYL ESTER Log I50 < 4.0 -
CHEMBL231074 Log I50 = 5.0 -
CHEMBL244156 Log I50 = 4.91 -
CHEMBL287364 Log I50 = 4.48 -
CHEMBL388436 Log I50 = 4.01 -
CHEMBL287788 Log I50 = 4.98 -
CHEMBL230225 Log I50 = 4.0 -
CHEMBL230968 Log I50 = 5.09 -
CHEMBL230760 Log I50 = 5.3 -
CHEMBL244354 Log I50 = 4.16 -
CHEMBL230759 Log I50 = 4.3 -
CHEMBL425843 Log I50 = 4.68 -
CHEMBL230866 Log I50 = 4.0 -
CHEMBL230867 Log I50 = 5.0 -
CHEMBL243722 Log I50 = 4.76 -
CHEMBL396951 Log I50 = 5.8 -