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Assay Detail

CHEMBL895325

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

Binding
Inhibition of human PNMT K57A mutant
7
Total Activities
7
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

Phenylethanolamine N-methyltransferase (CHEMBL4617)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Enzyme adaptation to inhibitor binding: a cryptic binding site in phenylethanolamine N-methyltransferase.
Gee CL, Drinkwater N, Tyndall JD, Grunewald GL, Wu Q, McLeish MJ, Martin JL.
J Med Chem (2007) 50 : 4845 -4853
PubMed 17845018 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.99 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290890 1 9.00
CHEMBL286497 1 8.89
CHEMBL176112 1 8.85
CHEMBL355581 1 8.74
CHEMBL177621 1 7.77
CHEMBL59441 1 6.84
CHEMBL281289 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290890 Ki = 1.0 nM 9.00
CHEMBL286497 Ki = 1.3 nM 8.89
CHEMBL176112 Ki = 1.4 nM 8.85
CHEMBL355581 Ki = 1.8 nM 8.74
CHEMBL177621 Ki = 17.0 nM 7.77
CHEMBL59441 Ki = 145.0 nM 6.84
CHEMBL281289 Ki = 1370.0 nM 5.86