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Assay Detail

CHEMBL3291944

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

Binding
Inhibition of catalytic activity of human cloned COMT expressed in Escherichia coli using [3H]-S-adenosylmethionine as substrate after 20 mins by liquid scintillation counting
10
Total Activities
5
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

Catechol O-methyltransferase (CHEMBL2023)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A fragment-based approach to identifying S-adenosyl-l-methionine -competitive inhibitors of catechol O-methyl transferase (COMT).
Lanier M, Ambrus G, Cole DC, Davenport R, Ellery J, Fosbeary R, Jennings AJ, Kadotani A, Kamada Y, Kamran R, Matsumoto S, Mizukami A, Okubo S, Okada K, Saikatendu K, Walsh L, Wu H, Hixon MS.
J Med Chem (2014) 57 : 5459 -5463
PubMed 24847974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.36 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1089318 OPICAPONE 4.0 2 9.00
CHEMBL3289430 2 5.20
CHEMBL3289432 2 5.10
CHEMBL3289431 2 4.60
CHEMBL3289429 2 3.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1089318 OPICAPONE Ki = 1.0 nM 9.00
CHEMBL1089318 OPICAPONE Ki = 10.0 nM 8.00
CHEMBL3289430 Ki = 6300.0 nM 5.20
CHEMBL3289432 Ki = 7900.0 nM 5.10
CHEMBL3289432 Ki = 7943.28 nM 5.10
CHEMBL3289430 Ki = 15848.93 nM 4.80
CHEMBL3289431 Ki = 25000.0 nM 4.60
CHEMBL3289431 Ki = 25118.86 nM 4.60
CHEMBL3289429 Ki = 251000.0 nM 3.60
CHEMBL3289429 Ki = 251188.64 nM 3.60