Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4158339

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

Binding
Inhibition of c-terminal hexa-His tagged rat S-COMT expressed in HEK293-6E cell membrane homogenate using 7,8-dihydroxy-4-methylcoumarin as substrate after 1 hr in presence of SAM by MTase glo methyltransferase assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Catechol O-methyltransferase (CHEMBL2372)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Optimization of 8-Hydroxyquinolines as Inhibitors of Catechol O-Methyltransferase.
Buchler I, Akuma D, Au V, Carr G, de León P, DePasquale M, Ernst G, Huang Y, Kimos M, Kolobova A, Poslusney M, Wei H, Swinnen D, Montel F, Moureau F, Jigorel E, Schulze MED, Wood M, Barrow JC.
J Med Chem (2018) 61 : 9647 -9665
PubMed 30272964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.25 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4172614 1 5.40
CHEMBL4167128 1 5.10
CHEMBL4171117 1 -
CHEMBL4176008 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4172614 IC50 = 3981.07 nM 5.40
CHEMBL4167128 IC50 = 7943.28 nM 5.10
CHEMBL4171117 IC50 > 10000.0 nM -
CHEMBL4176008 IC50 > 10000.0 nM -