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Assay Detail

CHEMBL680041

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

Binding
Inhibition of fatty acid amide hydrolase (FAAH) was determined using rat brain homogenates as the enzyme source and [3H]anandamide as substrate
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase.
López-Rodríguez ML, Viso A, Ortega-Gutiérrez S, Fowler CJ, Tiger G, de Lago E, Fernández-Ruiz J, Ramos JA.
J Med Chem (2003) 46 : 1512 -1522
PubMed 12672252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 4.61 5.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39878 1 5.43
CHEMBL36774 1 4.92
CHEMBL37297 1 4.92
CHEMBL37089 1 4.82
CHEMBL36708 1 4.62
CHEMBL288003 1 4.55
CHEMBL39409 1 4.54
CHEMBL434778 1 4.52
CHEMBL39460 1 4.47
CHEMBL286465 1 4.44
CHEMBL287130 1 4.36
CHEMBL38293 1 4.28
CHEMBL284300 1 4.08
CHEMBL1907956 1 -
CHEMBL39399 1 -
CHEMBL2093099 1 -
CHEMBL40065 1 -
CHEMBL287364 1 -
CHEMBL291021 1 -
CHEMBL285061 1 -
CHEMBL431128 1 -
CHEMBL38282 1 -
CHEMBL41226 1 -
CHEMBL290716 1 -
CHEMBL287788 1 -
CHEMBL39351 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39878 IC50 = 3700.0 nM 5.43
CHEMBL36774 IC50 = 12000.0 nM 4.92
CHEMBL37297 IC50 = 12000.0 nM 4.92
CHEMBL37089 IC50 = 15000.0 nM 4.82
CHEMBL36708 IC50 = 24000.0 nM 4.62
CHEMBL288003 IC50 = 28000.0 nM 4.55
CHEMBL39409 IC50 = 29000.0 nM 4.54
CHEMBL434778 IC50 = 30000.0 nM 4.52
CHEMBL39460 IC50 = 34000.0 nM 4.47
CHEMBL286465 IC50 = 36000.0 nM 4.44
CHEMBL287130 IC50 = 44000.0 nM 4.36
CHEMBL38293 IC50 = 53000.0 nM 4.28
CHEMBL284300 IC50 = 84000.0 nM 4.08
CHEMBL1907956 IC50 > 120000.0 nM -
CHEMBL39399 IC50 > 120000.0 nM -
CHEMBL2093099 IC50 > 120000.0 nM -
CHEMBL40065 IC50 > 120000.0 nM -
CHEMBL287364 IC50 > 120000.0 nM -
CHEMBL291021 IC50 - -
CHEMBL285061 IC50 = 102000.0 nM -
CHEMBL431128 IC50 = 112000.0 nM -
CHEMBL38282 IC50 > 120000.0 nM -
CHEMBL41226 IC50 > 120000.0 nM -
CHEMBL290716 IC50 = 103000.0 nM -
CHEMBL287788 IC50 = 113000.0 nM -
CHEMBL39351 IC50 > 120000.0 nM -