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Assay Detail

CHEMBL953297

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

Binding
Inhibition of FAAH-mediated [3H]anandamide hydrolysis in mouse brain
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fatty-acid amide hydrolase 1 (CHEMBL3455)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels.
Nomura DK, Hudak CS, Ward AM, Burston JJ, Issa RS, Fisher KJ, Abood ME, Wiley JL, Lichtman AH, Casida JE.
Bioorg Med Chem Lett (2008) 18 : 5875 -5878
PubMed 18752948 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.33 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL462609 METHYL ICOSYLPHOSPHONOFLUORIDATE 1 10.00
CHEMBL450965 1 9.82
CHEMBL499569 1 8.72
CHEMBL97038 DODECANESULFONYL FLUORIDE 1 8.70
CHEMBL333149 ISOPROPYL DODECYLFLUOROPHOSPHONATE 1 8.52
CHEMBL512224 1 8.52
CHEMBL462582 1 7.92
CHEMBL444970 CHLORPHRIFOS OXON 1 7.40
CHEMBL462610 1 7.38
CHEMBL23838 PARAOXON -1.0 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL462609 METHYL ICOSYLPHOSPHONOFLUORIDATE IC50 = 0.1 nM 10.00
CHEMBL450965 IC50 = 0.15 nM 9.82
CHEMBL499569 IC50 = 1.9 nM 8.72
CHEMBL97038 DODECANESULFONYL FLUORIDE IC50 = 2.0 nM 8.70
CHEMBL333149 ISOPROPYL DODECYLFLUOROPHOSPHONATE IC50 = 3.0 nM 8.52
CHEMBL512224 IC50 = 3.0 nM 8.52
CHEMBL462582 IC50 = 12.0 nM 7.92
CHEMBL444970 CHLORPHRIFOS OXON IC50 = 40.0 nM 7.40
CHEMBL462610 IC50 = 42.0 nM 7.38
CHEMBL23838 PARAOXON IC50 = 540.0 nM 6.27