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Assay Detail

CHEMBL670426

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Binding
Inhibition of human dopamine receptor D3
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

From hit to lead. Analyzing structure-profile relationships.
Poulain R, Horvath D, Bonnet B, Eckhoff C, Chapelain B, Bodinier MC, Déprez B.
J Med Chem (2001) 44 : 3391 -3401
PubMed 11585444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.32 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325750 1 7.54
CHEMBL115280 1 6.83
CHEMBL114484 1 6.81
CHEMBL326962 1 6.80
CHEMBL326263 1 6.71
CHEMBL113956 1 6.47
CHEMBL325516 1 6.34
CHEMBL116463 1 6.27
CHEMBL117537 1 6.12
CHEMBL116735 1 6.01
CHEMBL114379 1 5.72
CHEMBL115222 1 5.71
CHEMBL115652 1 5.67
CHEMBL325674 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325750 IC50 = 29.0 nM 7.54
CHEMBL115280 IC50 = 149.0 nM 6.83
CHEMBL114484 IC50 = 154.0 nM 6.81
CHEMBL326962 IC50 = 160.0 nM 6.80
CHEMBL326263 IC50 = 195.0 nM 6.71
CHEMBL113956 IC50 = 341.0 nM 6.47
CHEMBL325516 IC50 = 456.0 nM 6.34
CHEMBL116463 IC50 = 538.0 nM 6.27
CHEMBL117537 IC50 = 758.0 nM 6.12
CHEMBL116735 IC50 = 977.0 nM 6.01
CHEMBL114379 IC50 = 1910.0 nM 5.72
CHEMBL115222 IC50 = 1930.0 nM 5.71
CHEMBL115652 IC50 = 2120.0 nM 5.67
CHEMBL325674 IC50 = 3180.0 nM 5.50