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Assay Detail

CHEMBL763763

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

Binding
Inhibitory activity against phenylethanolamine N-methyl-transferase
69
Total Activities
69
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

Importance of the aromatic ring in adrenergic amines. 5. Nonaromatic analogues of phenylethanolamine as inhibitors of phenylethanolamine N-methyltransferase: role of hydrophobic and steric interactions.
Vincek WC, Aldrich CS, Borchardt RT, Grunewald GL.
J Med Chem (1981) 24 : 7 -12
PubMed 7205880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 69 4.78 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18718 1 5.22
CHEMBL278978 1 5.22
CHEMBL18486 CYCLONONANECARBALDEHYDE 1 5.22
CHEMBL18686 1 5.16
CHEMBL280477 1 5.10
CHEMBL277996 CYCLOHEPTANE CARBALDEHYDE 1 5.10
CHEMBL275870 1 5.10
CHEMBL18921 1 5.10
CHEMBL18707 1 5.10
CHEMBL18302 1 5.05
CHEMBL279363 CYCLOUNDECANE CARBALDEHYDE 1 5.05
CHEMBL19170 1 5.05
CHEMBL18970 1 4.85
CHEMBL276087 CYCLONONANONE 1 4.77
CHEMBL278410 1 4.77
CHEMBL278693 1 4.77
CHEMBL18481 1 4.42
CHEMBL18594 1 4.28
CHEMBL278921 1 4.24
CHEMBL18878 1 4.14
CHEMBL19000 1 4.14
CHEMBL18737 CYCLOOCTANONE 1 4.14
CHEMBL275390 1 4.05
CHEMBL18945 1 -
CHEMBL280259 1 -
CHEMBL275140 1 -
CHEMBL18634 1 -
CHEMBL275388 1 -
CHEMBL19249 1 -
CHEMBL278058 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18718 IC50 = 6000.0 nM 5.22
CHEMBL18486 CYCLONONANECARBALDEHYDE IC50 = 6000.0 nM 5.22
CHEMBL278978 IC50 = 6000.0 nM 5.22
CHEMBL18686 IC50 = 7000.0 nM 5.16
CHEMBL280477 IC50 = 8000.0 nM 5.10
CHEMBL277996 CYCLOHEPTANE CARBALDEHYDE IC50 = 8000.0 nM 5.10
CHEMBL275870 IC50 = 8000.0 nM 5.10
CHEMBL18921 IC50 = 8000.0 nM 5.10
CHEMBL18707 IC50 = 8000.0 nM 5.10
CHEMBL279363 CYCLOUNDECANE CARBALDEHYDE IC50 = 9000.0 nM 5.05
CHEMBL19170 IC50 = 9000.0 nM 5.05
CHEMBL18302 IC50 = 9000.0 nM 5.05
CHEMBL18970 IC50 = 14000.0 nM 4.85
CHEMBL278693 IC50 = 17000.0 nM 4.77
CHEMBL278410 IC50 = 17000.0 nM 4.77
CHEMBL276087 CYCLONONANONE IC50 = 17000.0 nM 4.77
CHEMBL18481 IC50 = 38000.0 nM 4.42
CHEMBL18594 IC50 = 52000.0 nM 4.28
CHEMBL278921 IC50 = 57000.0 nM 4.24
CHEMBL19000 IC50 = 72000.0 nM 4.14
CHEMBL18737 CYCLOOCTANONE IC50 = 72000.0 nM 4.14
CHEMBL18878 IC50 = 72000.0 nM 4.14
CHEMBL275390 IC50 = 89000.0 nM 4.05
CHEMBL18654 IC50 > 1000000.0 nM -
CHEMBL18585 IC50 > 1000000.0 nM -
CHEMBL280235 IC50 = 510000.0 nM -
CHEMBL18294 IC50 = 109000.0 nM -
CHEMBL18104 HEPTANAL IC50 = 109000.0 nM -
CHEMBL18666 IC50 > 1000000.0 nM -
CHEMBL274711 CYCLOPENTANECARBALDEHYDE IC50 = 446000.0 nM -
CHEMBL18278 IC50 = 403000.0 nM -
CHEMBL18384 IC50 = 216000.0 nM -
CHEMBL18549 IC50 = 664000.0 nM -
CHEMBL18828 IC50 = 403000.0 nM -
CHEMBL18407 OCTANAL IC50 = 216000.0 nM -
CHEMBL18893 IC50 = 669000.0 nM -
CHEMBL429382 IC50 = 195000.0 nM -
CHEMBL18542 IC50 = 109000.0 nM -
CHEMBL280453 IC50 = 1000000.0 nM -
CHEMBL18843 IC50 = 345000.0 nM -
CHEMBL280331 HEXANAL IC50 = 314000.0 nM -
CHEMBL18444 IC50 = 664000.0 nM -
CHEMBL18982 IC50 = 446000.0 nM -
CHEMBL278058 IC50 = 195000.0 nM -
CHEMBL19249 IC50 = 510000.0 nM -
CHEMBL275388 IC50 > 1000000.0 nM -
CHEMBL18634 IC50 = 664000.0 nM -
CHEMBL275140 IC50 = 760000.0 nM -
CHEMBL280259 IC50 = 403000.0 nM -
CHEMBL18945 IC50 = 545000.0 nM -