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Assay Detail

CHEMBL1022293

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

Binding
Inhibition of rat cortex FAAH by [3H]anandamide carbon filtration assay
34
Total Activities
34
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

Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors.
Wang X, Sarris K, Kage K, Zhang D, Brown SP, Kolasa T, Surowy C, El Kouhen OF, Muchmore SW, Brioni JD, Stewart AO.
J Med Chem (2009) 52 : 170 -180
PubMed 19072118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.26 8.77
Ki 6 8.56 10.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL367966 1 10.55
CHEMBL459920 1 8.77
CHEMBL232782 1 8.70
CHEMBL184238 URB-597 1.0 1 8.40
CHEMBL177577 1 8.33
CHEMBL509860 1 7.92
CHEMBL467426 1 7.89
CHEMBL516782 1 7.85
CHEMBL460798 1 7.85
CHEMBL461411 1 7.82
CHEMBL460127 1 7.80
CHEMBL460340 1 7.75
CHEMBL460129 1 7.72
CHEMBL460128 1 7.68
CHEMBL517903 1 7.60
CHEMBL512590 1 7.54
CHEMBL513789 1 7.48
CHEMBL462464 1 7.36
CHEMBL511915 1 7.32
CHEMBL513142 1 7.20
CHEMBL460588 1 7.19
CHEMBL459919 1 7.15
CHEMBL446296 1 7.04
CHEMBL462465 1 6.96
CHEMBL518028 1 6.68
CHEMBL462466 1 6.63
CHEMBL468258 1 6.58
CHEMBL518329 1 6.57
CHEMBL511421 1 5.75
CHEMBL467428 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL367966 Ki = 0.028 nM 10.55
CHEMBL459920 IC50 = 1.7 nM 8.77
CHEMBL232782 Ki = 2.0 nM 8.70
CHEMBL184238 URB-597 Ki = 4.0 nM 8.40
CHEMBL177577 Ki = 4.7 nM 8.33
CHEMBL509860 Ki = 12.0 nM 7.92
CHEMBL467426 IC50 = 13.0 nM 7.89
CHEMBL516782 IC50 = 14.0 nM 7.85
CHEMBL460798 IC50 = 14.0 nM 7.85
CHEMBL461411 IC50 = 15.0 nM 7.82
CHEMBL460127 IC50 = 16.0 nM 7.80
CHEMBL460340 IC50 = 18.0 nM 7.75
CHEMBL460129 IC50 = 19.0 nM 7.72
CHEMBL460128 IC50 = 21.0 nM 7.68
CHEMBL517903 IC50 = 25.0 nM 7.60
CHEMBL512590 IC50 = 29.0 nM 7.54
CHEMBL513789 Ki = 33.0 nM 7.48
CHEMBL462464 IC50 = 44.0 nM 7.36
CHEMBL511915 IC50 = 48.0 nM 7.32
CHEMBL513142 IC50 = 63.0 nM 7.20
CHEMBL460588 IC50 = 65.0 nM 7.19
CHEMBL459919 IC50 = 71.0 nM 7.15
CHEMBL446296 IC50 = 91.0 nM 7.04
CHEMBL462465 IC50 = 109.0 nM 6.96
CHEMBL518028 IC50 = 210.0 nM 6.68
CHEMBL462466 IC50 = 235.0 nM 6.63
CHEMBL468258 IC50 = 263.0 nM 6.58
CHEMBL518329 IC50 = 270.0 nM 6.57
CHEMBL511421 IC50 = 1780.0 nM 5.75
CHEMBL467428 IC50 = 2370.0 nM 5.62
CHEMBL461435 IC50 > 10000.0 nM -
CHEMBL467427 IC50 > 10000.0 nM -
CHEMBL460589 IC50 > 10000.0 nM -
CHEMBL462682 IC50 > 10000.0 nM -