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Assay Detail

CHEMBL944310

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

Binding
Inhibition of Wistar rat brain FAAH assessed as [3H]arachidonoylethanolamide hydrolysis
22
Total Activities
22
Compounds Tested
1
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

Discovery of boronic acids as novel and potent inhibitors of fatty acid amide hydrolase.
Minkkilä A, Saario SM, Käsnänen H, Leppänen J, Poso A, Nevalainen T.
J Med Chem (2008) 51 : 7057 -7060
PubMed 18983140 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.34 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485946 1 8.04
CHEMBL453758 1 7.85
CHEMBL485742 BIPHENYLBORONIC ACID 1 7.68
CHEMBL143654 1 7.44
CHEMBL336239 1 7.10
CHEMBL488800 1 6.92
CHEMBL20421 1 6.89
CHEMBL34964 1 6.82
CHEMBL91108 1 6.68
CHEMBL500339 1 6.54
CHEMBL143399 1 6.48
CHEMBL505047 1 6.15
CHEMBL20461 PHENETHYLBORONIC ACID 1 5.89
CHEMBL344890 1 5.82
CHEMBL485740 1 5.80
CHEMBL485741 1 5.72
CHEMBL21427 1 5.70
CHEMBL21485 PHENYLBORONIC ACID 1 5.58
CHEMBL487369 1 5.00
CHEMBL348732 1 4.89
CHEMBL349181 1 4.17
CHEMBL467355 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485946 IC50 = 9.1 nM 8.04
CHEMBL453758 IC50 = 14.0 nM 7.85
CHEMBL485742 BIPHENYLBORONIC ACID IC50 = 21.0 nM 7.68
CHEMBL143654 IC50 = 36.0 nM 7.44
CHEMBL336239 IC50 = 80.0 nM 7.10
CHEMBL488800 IC50 = 120.0 nM 6.92
CHEMBL20421 IC50 = 130.0 nM 6.89
CHEMBL34964 IC50 = 150.0 nM 6.82
CHEMBL91108 IC50 = 210.0 nM 6.68
CHEMBL500339 IC50 = 290.0 nM 6.54
CHEMBL143399 IC50 = 330.0 nM 6.48
CHEMBL505047 IC50 = 710.0 nM 6.15
CHEMBL20461 PHENETHYLBORONIC ACID IC50 = 1300.0 nM 5.89
CHEMBL344890 IC50 = 1500.0 nM 5.82
CHEMBL485740 IC50 = 1600.0 nM 5.80
CHEMBL485741 IC50 = 1900.0 nM 5.72
CHEMBL21427 IC50 = 2000.0 nM 5.70
CHEMBL21485 PHENYLBORONIC ACID IC50 = 2600.0 nM 5.58
CHEMBL487369 IC50 = 10000.0 nM 5.00
CHEMBL348732 IC50 = 13000.0 nM 4.89
CHEMBL349181 IC50 = 68000.0 nM 4.17
CHEMBL467355 IC50 = 110000.0 nM -