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Assay Detail

CHEMBL671225

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Binding
Inhibitory activity was determined against bovine dopamine beta-hydroxylase (DBH)
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dopamine beta-hydroxylase (CHEMBL4702)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Some benzyl-substituted imidazoles, triazoles, tetrazoles, pyridinethiones, and structural relatives as multisubstrate inhibitors of dopamine beta-hydroxylase. 4. Structure-activity relationships at the copper binding site.
Kruse LI, Kaiser C, DeWolf WE, Finkelstein JA, Frazee JS, Hilbert EL, Ross ST, Flaim KE, Sawyer JL.
J Med Chem (1990) 33 : 781 -789
PubMed 2299645 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.34 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL351873 1 7.46
CHEMBL433493 1 7.13
CHEMBL165242 1 6.18
CHEMBL165150 1 6.00
CHEMBL278068 1 5.92
CHEMBL352449 1 5.85
CHEMBL165032 1 5.81
CHEMBL165206 1 5.72
CHEMBL350128 1 5.66
CHEMBL164747 1 5.58
CHEMBL351468 1 5.55
CHEMBL351936 1 5.43
CHEMBL63907 1 5.25
CHEMBL165154 1 5.21
CHEMBL350557 1 5.21
CHEMBL348820 1 4.87
CHEMBL352685 1 4.82
CHEMBL349152 1 4.80
CHEMBL349889 1 4.62
CHEMBL164791 1 4.50
CHEMBL352155 1 4.24
CHEMBL355612 1 4.21
CHEMBL351892 1 4.12
CHEMBL423819 1 4.10
CHEMBL165087 1 -
CHEMBL164646 1 -
CHEMBL351275 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL351873 IC50 = 35.0 nM 7.46
CHEMBL433493 IC50 = 74.0 nM 7.13
CHEMBL165242 IC50 = 660.0 nM 6.18
CHEMBL165150 IC50 = 1000.0 nM 6.00
CHEMBL278068 IC50 = 1200.0 nM 5.92
CHEMBL352449 IC50 = 1400.0 nM 5.85
CHEMBL165032 IC50 = 1540.0 nM 5.81
CHEMBL165206 IC50 = 1900.0 nM 5.72
CHEMBL350128 IC50 = 2200.0 nM 5.66
CHEMBL164747 IC50 = 2600.0 nM 5.58
CHEMBL351468 IC50 = 2800.0 nM 5.55
CHEMBL351936 IC50 = 3700.0 nM 5.43
CHEMBL63907 IC50 = 5600.0 nM 5.25
CHEMBL165154 IC50 = 6200.0 nM 5.21
CHEMBL350557 IC50 = 6200.0 nM 5.21
CHEMBL348820 IC50 = 13400.0 nM 4.87
CHEMBL352685 IC50 = 15000.0 nM 4.82
CHEMBL349152 IC50 = 16000.0 nM 4.80
CHEMBL349889 IC50 = 24000.0 nM 4.62
CHEMBL164791 IC50 = 32000.0 nM 4.50
CHEMBL352155 IC50 = 57000.0 nM 4.24
CHEMBL355612 IC50 = 61000.0 nM 4.21
CHEMBL351892 IC50 = 75000.0 nM 4.12
CHEMBL423819 IC50 = 79000.0 nM 4.10
CHEMBL165087 IC50 = 112000.0 nM -
CHEMBL164646 IC50 = 240000.0 nM -
CHEMBL351275 IC50 = 165000.0 nM -