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Assay Detail

CHEMBL970754

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Binding
Inhibition of rat FAAH expressed in Escherichia coli
89
Total Activities
79
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase.
Garfunkle J, Ezzili C, Rayl TJ, Hochstatter DG, Hwang I, Boger DL.
J Med Chem (2008) 51 : 4392 -4403
PubMed 18630870 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 53 7.61 10.30
IC50 36 6.84 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477372 2 10.30
CHEMBL178398 1 9.54
CHEMBL468226 1 9.52
CHEMBL469198 2 9.47
CHEMBL469241 1 9.42
CHEMBL513534 1 9.20
CHEMBL468357 1 9.10
CHEMBL426967 1 9.00
CHEMBL450158 2 9.00
CHEMBL467796 1 9.00
CHEMBL513358 1 9.00
CHEMBL502051 1 9.00
CHEMBL469051 2 8.96
CHEMBL512104 1 8.80
CHEMBL178563 1 8.52
CHEMBL467368 2 8.52
CHEMBL512965 1 8.52
CHEMBL511436 1 8.44
CHEMBL448922 1 8.40
CHEMBL177577 1 8.33
CHEMBL467161 1 8.30
CHEMBL468189 2 8.15
CHEMBL219880 1 8.10
CHEMBL467353 1 8.10
CHEMBL467817 1 8.10
CHEMBL467141 1 8.00
CHEMBL177356 1 7.92
CHEMBL461163 2 7.85
CHEMBL362705 1 7.80
CHEMBL452886 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477372 Ki = 0.05 nM 10.30
CHEMBL178398 Ki = 0.29 nM 9.54
CHEMBL468226 Ki = 0.3 nM 9.52
CHEMBL469198 Ki = 0.34 nM 9.47
CHEMBL469241 Ki = 0.38 nM 9.42
CHEMBL513534 Ki = 0.63 nM 9.20
CHEMBL468357 Ki = 0.8 nM 9.10
CHEMBL502051 Ki = 1.0 nM 9.00
CHEMBL426967 IC50 = 1.0 nM 9.00
CHEMBL467796 IC50 = 1.0 nM 9.00
CHEMBL513358 Ki = 1.0 nM 9.00
CHEMBL450158 Ki = 1.0 nM 9.00
CHEMBL469051 Ki = 1.1 nM 8.96
CHEMBL512104 Ki = 1.6 nM 8.80
CHEMBL178563 Ki = 3.0 nM 8.52
CHEMBL467368 IC50 = 3.0 nM 8.52
CHEMBL512965 IC50 = 3.0 nM 8.52
CHEMBL469198 Ki = 3.0 nM 8.52
CHEMBL511436 Ki = 3.6 nM 8.44
CHEMBL448922 IC50 = 4.0 nM 8.40
CHEMBL177577 Ki = 4.7 nM 8.33
CHEMBL467161 Ki = 5.0 nM 8.30
CHEMBL468189 Ki = 7.0 nM 8.15
CHEMBL469051 IC50 = 7.0 nM 8.15
CHEMBL467353 Ki = 8.0 nM 8.10
CHEMBL467817 IC50 = 8.0 nM 8.10
CHEMBL219880 IC50 = 8.0 nM 8.10
CHEMBL468189 IC50 = 10.0 nM 8.00
CHEMBL467141 Ki = 10.0 nM 8.00
CHEMBL467368 Ki = 11.0 nM 7.96
CHEMBL177356 IC50 = 12.0 nM 7.92
CHEMBL461163 Ki = 14.0 nM 7.85
CHEMBL362705 Ki = 16.0 nM 7.80
CHEMBL452886 Ki = 18.0 nM 7.75
CHEMBL426230 Ki = 18.0 nM 7.75
CHEMBL219942 Ki = 20.0 nM 7.70
CHEMBL467364 Ki = 20.0 nM 7.70
CHEMBL178115 IC50 = 25.0 nM 7.60
CHEMBL220784 IC50 = 30.0 nM 7.52
CHEMBL477372 Ki = 30.0 nM 7.52
CHEMBL467173 Ki = 37.0 nM 7.43
CHEMBL466961 IC50 = 40.0 nM 7.40
CHEMBL469268 Ki = 48.0 nM 7.32
CHEMBL468220 Ki = 53.0 nM 7.28
CHEMBL174048 Ki = 54.0 nM 7.27
CHEMBL178071 IC50 = 55.0 nM 7.26
CHEMBL450158 IC50 = 60.0 nM 7.22
CHEMBL468220 IC50 = 70.0 nM 7.16
CHEMBL173992 IC50 = 80.0 nM 7.10
CHEMBL178640 Ki = 89.0 nM 7.05