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Assay Detail

CHEMBL970755

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

Binding
Inhibition of rat FAAH expressed in Escherichia coli at pH 9.0
56
Total Activities
56
Compounds Tested
1
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 56 7.95 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL178398 1 9.54
CHEMBL469198 1 9.47
CHEMBL426967 1 9.25
CHEMBL477372 1 9.10
CHEMBL467816 1 9.10
CHEMBL220784 1 9.05
CHEMBL469199 1 9.00
CHEMBL448922 1 9.00
CHEMBL450158 1 9.00
CHEMBL468188 1 9.00
CHEMBL467796 1 9.00
CHEMBL469051 1 8.96
CHEMBL467368 1 8.96
CHEMBL477371 1 8.85
CHEMBL466954 1 8.80
CHEMBL178115 1 8.66
CHEMBL504330 1 8.60
CHEMBL467817 1 8.52
CHEMBL512965 1 8.52
CHEMBL177577 1 8.33
CHEMBL468585 1 8.30
CHEMBL469050 1 8.15
CHEMBL468189 1 8.15
CHEMBL512107 1 8.15
CHEMBL517352 1 8.13
CHEMBL476511 1 8.11
CHEMBL219880 1 8.10
CHEMBL504091 1 8.07
CHEMBL511422 1 8.07
CHEMBL177356 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL178398 Ki = 0.29 nM 9.54
CHEMBL469198 Ki = 0.34 nM 9.47
CHEMBL426967 Ki = 0.56 nM 9.25
CHEMBL477372 Ki = 0.8 nM 9.10
CHEMBL467816 Ki = 0.8 nM 9.10
CHEMBL220784 Ki = 0.9 nM 9.05
CHEMBL469199 Ki = 1.0 nM 9.00
CHEMBL448922 Ki = 1.0 nM 9.00
CHEMBL450158 Ki = 1.0 nM 9.00
CHEMBL468188 Ki = 1.0 nM 9.00
CHEMBL467796 Ki = 1.0 nM 9.00
CHEMBL469051 Ki = 1.1 nM 8.96
CHEMBL467368 Ki = 1.1 nM 8.96
CHEMBL477371 Ki = 1.4 nM 8.85
CHEMBL466954 Ki = 1.6 nM 8.80
CHEMBL178115 Ki = 2.2 nM 8.66
CHEMBL504330 Ki = 2.5 nM 8.60
CHEMBL467817 Ki = 3.0 nM 8.52
CHEMBL512965 Ki = 3.0 nM 8.52
CHEMBL177577 Ki = 4.7 nM 8.33
CHEMBL468585 Ki = 5.0 nM 8.30
CHEMBL469050 Ki = 7.0 nM 8.15
CHEMBL468189 Ki = 7.0 nM 8.15
CHEMBL512107 Ki = 7.0 nM 8.15
CHEMBL517352 Ki = 7.4 nM 8.13
CHEMBL476511 Ki = 7.7 nM 8.11
CHEMBL219880 Ki = 8.0 nM 8.10
CHEMBL504091 Ki = 8.5 nM 8.07
CHEMBL511422 Ki = 8.5 nM 8.07
CHEMBL177356 Ki = 12.0 nM 7.92
CHEMBL466961 Ki = 13.0 nM 7.89
CHEMBL461163 Ki = 14.0 nM 7.85
CHEMBL467140 Ki = 16.0 nM 7.80
CHEMBL468222 Ki = 24.0 nM 7.62
CHEMBL476512 Ki = 25.0 nM 7.60
CHEMBL445514 Ki = 27.0 nM 7.57
CHEMBL503109 Ki = 40.0 nM 7.40
CHEMBL469056 Ki = 44.0 nM 7.36
CHEMBL478186 Ki = 46.0 nM 7.34
CHEMBL468220 Ki = 53.0 nM 7.28
CHEMBL178071 Ki = 55.0 nM 7.26
CHEMBL173992 Ki = 80.0 nM 7.10
CHEMBL478187 Ki = 110.0 nM 6.96
CHEMBL455556 Ki = 140.0 nM 6.85
CHEMBL515490 Ki = 360.0 nM 6.44
CHEMBL467182 Ki = 390.0 nM 6.41
CHEMBL478424 Ki = 500.0 nM 6.30
CHEMBL468221 Ki = 800.0 nM 6.10
CHEMBL469252 Ki = 1500.0 nM 5.82
CHEMBL512816 Ki = 2000.0 nM 5.70