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Assay Detail

CHEMBL763768

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Binding
In vitro inhibitory activity measured against bovine adrenal phenylethanolamine N-methyltransferase(PNMT)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Phenylethanolamine N-methyltransferase (CHEMBL2331)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Synthesis and evaluation of 3-substituted analogues of 1,2,3,4-tetrahydroisoquinoline as inhibitors of phenylethanolamine N-methyltransferase.
Grunewald GL, Sall DJ, Monn JA.
J Med Chem (1988) 31 : 824 -830
PubMed 3351861 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.45 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287837 1 6.62
CHEMBL342957 1 6.42
CHEMBL60068 1 5.62
CHEMBL60434 1 5.52
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE 1 4.99
CHEMBL59994 1 4.62
CHEMBL60724 1 4.39
CHEMBL11912 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287837 Ki = 240.0 nM 6.62
CHEMBL342957 Ki = 380.0 nM 6.42
CHEMBL60068 Ki = 2400.0 nM 5.62
CHEMBL60434 Ki = 3000.0 nM 5.52
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE Ki = 10300.0 nM 4.99
CHEMBL59994 Ki = 23900.0 nM 4.62
CHEMBL60724 Ki = 40500.0 nM 4.39
CHEMBL11912 Ki > 2000000.0 nM -