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Assay Detail

CHEMBL759774

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Binding
Inhibition of Phenylethylamine N-Methyltransferase (PNMT) using radiochemical assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Binding orientation of amphetamine and norfenfluramine analogues in the benzonorbornene and benzobicyclo[3.2.1]octane ring systems at the active site of phenylethanolamine N-methyltransferase (PNMT)
Grunewald GL, Markovich KM, Sall DJ.
J Med Chem (1987) 30 : 2191 -2208
PubMed 3681889 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 4.63 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70357 1 4.92
CHEMBL30294 1 4.82
CHEMBL303481 1 4.50
CHEMBL71964 1 4.29
CHEMBL308587 1 -
CHEMBL60005 1 -
CHEMBL49263 1 -
CHEMBL70384 1 -
CHEMBL302285 1 -
CHEMBL304541 1 -
CHEMBL71566 1 -
CHEMBL314304 1 -
CHEMBL71771 1 -
CHEMBL305281 1 -
CHEMBL299436 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70357 Ki = 12100.0 nM 4.92
CHEMBL30294 Ki = 15000.0 nM 4.82
CHEMBL303481 Ki = 31800.0 nM 4.50
CHEMBL71964 Ki = 51100.0 nM 4.29
CHEMBL308587 Ki = 1803000.0 nM -
CHEMBL60005 Ki = 1296000.0 nM -
CHEMBL49263 Ki = 479000.0 nM -
CHEMBL70384 Ki = 1429000.0 nM -
CHEMBL302285 Ki = 350000.0 nM -
CHEMBL304541 Ki = 8900000.0 nM -
CHEMBL71566 Ki = 801000.0 nM -
CHEMBL314304 Ki = 191000.0 nM -
CHEMBL71771 Ki = 106000.0 nM -
CHEMBL305281 Ki = 204000.0 nM -
CHEMBL299436 Ki = 258000.0 nM -