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Assay Detail

CHEMBL759409

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

Binding
In vitro inhibition of bovine phenylethylamine N-methyl-transferase (PNMT) using radiochemical assay.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Inhibition of phenylethanolamine N-methyltransferase (PNMT) by aromatic hydroxy-substituted 1,2,3,4,-tetrahydroisoquinolines: further studies on the hydrophilic pocket of the aromatic ring binding region of the active site.
Sall DJ, Grunewald GL.
J Med Chem (1987) 30 : 2208 -2216
PubMed 3681890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 5.17 6.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26717 1 6.26
CHEMBL27730 1 5.58
CHEMBL71354 1 5.42
CHEMBL11862 1 5.24
CHEMBL310736 1 5.11
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE 1 4.99
CHEMBL26640 1 4.70
CHEMBL308021 1 4.05
CHEMBL70415 1 -
CHEMBL306199 1 -
CHEMBL309111 1 -
CHEMBL69312 1 -
CHEMBL61749 1 -
CHEMBL61595 1 -
CHEMBL71308 1 -
CHEMBL302963 1 -
CHEMBL68977 1 -
CHEMBL299436 1 -
CHEMBL71563 1 -
CHEMBL49263 1 -
CHEMBL61712 1 -
CHEMBL292281 1 -
CHEMBL291584 1 -
CHEMBL70546 1 -
CHEMBL303839 1 -
CHEMBL70397 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26717 Ki = 550.0 nM 6.26
CHEMBL27730 Ki = 2600.0 nM 5.58
CHEMBL71354 Ki = 3800.0 nM 5.42
CHEMBL11862 Ki = 5700.0 nM 5.24
CHEMBL310736 Ki = 7800.0 nM 5.11
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE Ki = 10300.0 nM 4.99
CHEMBL26640 Ki = 20000.0 nM 4.70
CHEMBL308021 Ki = 90000.0 nM 4.05
CHEMBL70415 Ki = 1100000.0 nM -
CHEMBL306199 Ki = 735000.0 nM -
CHEMBL309111 Ki > 4000000.0 nM -
CHEMBL69312 Ki = 1082000.0 nM -
CHEMBL61749 Ki = 304000.0 nM -
CHEMBL61595 Ki = 487000.0 nM -
CHEMBL71308 Ki = 1259000.0 nM -
CHEMBL302963 Ki > 2000000.0 nM -
CHEMBL68977 Ki = 169000.0 nM -
CHEMBL299436 Ki = 258000.0 nM -
CHEMBL71563 Ki = 108000.0 nM -
CHEMBL49263 Ki = 479000.0 nM -
CHEMBL61712 Ki > 10000000.0 nM -
CHEMBL292281 Ki > 3000000.0 nM -
CHEMBL291584 Ki = 1114000.0 nM -
CHEMBL70546 Ki = 550000.0 nM -
CHEMBL303839 Ki > 2000000.0 nM -
CHEMBL70397 Ki > 2000000.0 nM -