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Assay Detail

CHEMBL3586822

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

Binding
Inhibition of Sprague-Dawley rat brain microsomal FAAH using N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide as substrate assessed as 4-pyren-1-ylbutanoic acid release preincubated for 10 mins with substrate followed by protein addition measured after 60 mins by reverse phase HPLC with fluorescence detection method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

-Heteroarylalkylcarbamates as inhibitors of fatty acid amide hydrolase (FAAH)
Terwege T, Dahlhaus H, Hanekamp W, Lehr M
Medchemcomm (2014) 5 : 932 -936
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.50 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175854 1 8.54
CHEMBL3585527 1 8.44
CHEMBL3585528 1 8.28
CHEMBL184238 URB-597 1.0 1 7.22
CHEMBL3585525 1 7.05
CHEMBL3585524 1 7.03
CHEMBL3585526 1 6.62
CHEMBL3585519 1 6.60
CHEMBL3585522 1 6.54
CHEMBL3585515 1 6.51
CHEMBL233593 1 6.46
CHEMBL3585514 1 6.34
CHEMBL3585518 1 6.28
CHEMBL3585521 1 6.09
CHEMBL3585520 1 6.04
CHEMBL3585523 1 6.02
CHEMBL3585508 1 5.58
CHEMBL3585516 1 5.33
CHEMBL3585517 1 5.31
CHEMBL3585509 1 5.21
CHEMBL3585513 1 5.06
CHEMBL3585511 1 -
CHEMBL3585512 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175854 IC50 = 2.9 nM 8.54
CHEMBL3585527 IC50 = 3.6 nM 8.44
CHEMBL3585528 IC50 = 5.2 nM 8.28
CHEMBL184238 URB-597 IC50 = 60.0 nM 7.22
CHEMBL3585525 IC50 = 90.0 nM 7.05
CHEMBL3585524 IC50 = 94.0 nM 7.03
CHEMBL3585526 IC50 = 240.0 nM 6.62
CHEMBL3585519 IC50 = 250.0 nM 6.60
CHEMBL3585522 IC50 = 290.0 nM 6.54
CHEMBL3585515 IC50 = 310.0 nM 6.51
CHEMBL233593 IC50 = 350.0 nM 6.46
CHEMBL3585514 IC50 = 460.0 nM 6.34
CHEMBL3585518 IC50 = 520.0 nM 6.28
CHEMBL3585521 IC50 = 810.0 nM 6.09
CHEMBL3585520 IC50 = 920.0 nM 6.04
CHEMBL3585523 IC50 = 960.0 nM 6.02
CHEMBL3585508 IC50 = 2600.0 nM 5.58
CHEMBL3585516 IC50 = 4700.0 nM 5.33
CHEMBL3585517 IC50 = 4900.0 nM 5.31
CHEMBL3585509 IC50 = 6200.0 nM 5.21
CHEMBL3585513 IC50 = 8700.0 nM 5.06
CHEMBL3585511 IC50 > 10000.0 nM -
CHEMBL3585512 IC50 > 10000.0 nM -