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Assay Detail

CHEMBL978251

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

Binding
Inhibition of human FAAH preincubated for 10 mins
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fatty-acid amide hydrolase 1 (CHEMBL2243)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
Keith JM, Apodaca R, Xiao W, Seierstad M, Pattabiraman K, Wu J, Webb M, Karbarz MJ, Brown S, Wilson S, Scott B, Tham CS, Luo L, Palmer J, Wennerholm M, Chaplan S, Breitenbucher JG.
Bioorg Med Chem Lett (2008) 18 : 4838 -4843
PubMed 18693015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.07 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL527204 1 8.70
CHEMBL513553 1 8.01
CHEMBL508120 1 7.99
CHEMBL488708 1 7.89
CHEMBL528768 1 7.64
CHEMBL513073 1 7.57
CHEMBL488709 1 7.30
CHEMBL488867 1 7.16
CHEMBL460273 1 7.16
CHEMBL528107 1 6.60
CHEMBL486673 1 6.58
CHEMBL487847 1 6.50
CHEMBL488868 1 6.50
CHEMBL528547 1 5.98
CHEMBL488686 1 5.93
CHEMBL488523 1 5.57
CHEMBL487848 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL527204 IC50 = 2.02 nM 8.70
CHEMBL513553 IC50 = 9.8 nM 8.01
CHEMBL508120 IC50 = 10.3 nM 7.99
CHEMBL488708 IC50 = 13.0 nM 7.89
CHEMBL528768 IC50 = 23.0 nM 7.64
CHEMBL513073 IC50 = 26.7 nM 7.57
CHEMBL488709 IC50 = 50.0 nM 7.30
CHEMBL488867 IC50 = 70.0 nM 7.16
CHEMBL460273 IC50 = 70.0 nM 7.16
CHEMBL528107 IC50 = 253.0 nM 6.60
CHEMBL486673 IC50 = 266.0 nM 6.58
CHEMBL487847 IC50 = 320.0 nM 6.50
CHEMBL488868 IC50 = 320.0 nM 6.50
CHEMBL528547 IC50 = 1037.0 nM 5.98
CHEMBL488686 IC50 = 1167.0 nM 5.93
CHEMBL488523 IC50 = 2667.0 nM 5.57
CHEMBL487848 IC50 > 10000.0 nM -