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Assay Detail

CHEMBL673446

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

Binding
Binding affinity at dopamine receptor D3
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of [(2,3-dichlorophenyl)piperazin-1-yl]alkylfluorenylcarboxamides as novel ligands selective for the dopamine D3 receptor subtype.
Robarge MJ, Husbands SM, Kieltyka A, Brodbeck R, Thurkauf A, Newman AH.
J Med Chem (2001) 44 : 3175 -3186
PubMed 11543687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 40 6.97 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419505 1 9.05
CHEMBL301242 1 8.85
CHEMBL110411 1 8.85
CHEMBL69717 1 8.39
CHEMBL306672 1 8.11
CHEMBL2308105 1 7.86
CHEMBL307800 1 7.72
CHEMBL68860 1 7.62
CHEMBL68720 1 7.55
CHEMBL309118 1 7.44
CHEMBL109299 1 7.27
CHEMBL12375 1 7.20
CHEMBL106660 1 7.14
CHEMBL67750 1 6.96
CHEMBL12004 1 6.95
CHEMBL417249 1 6.89
CHEMBL317757 DIFLUOROBENZTROPINE 1 6.84
CHEMBL108527 1 6.77
CHEMBL320114 1 6.71
CHEMBL323997 1 6.67
CHEMBL3084884 1 6.66
CHEMBL267562 1 6.56
CHEMBL302796 1 6.47
CHEMBL322179 1 6.37
CHEMBL110349 1 6.37
CHEMBL108637 1 5.84
CHEMBL324896 1 5.62
CHEMBL110435 1 5.60
CHEMBL110120 1 5.40
CHEMBL310310 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL419505 Ki = 0.9 nM 9.05
CHEMBL301242 Ki = 1.4 nM 8.85
CHEMBL110411 Ki = 1.4 nM 8.85
CHEMBL69717 Ki = 4.1 nM 8.39
CHEMBL306672 Ki = 7.8 nM 8.11
CHEMBL2308105 Ki = 13.8 nM 7.86
CHEMBL307800 Ki = 19.0 nM 7.72
CHEMBL68860 Ki = 24.0 nM 7.62
CHEMBL68720 Ki = 28.0 nM 7.55
CHEMBL309118 Ki = 36.0 nM 7.44
CHEMBL109299 Ki = 53.2 nM 7.27
CHEMBL12375 Ki = 63.3 nM 7.20
CHEMBL106660 Ki = 72.7 nM 7.14
CHEMBL67750 Ki = 110.0 nM 6.96
CHEMBL12004 Ki = 112.0 nM 6.95
CHEMBL417249 Ki = 130.0 nM 6.89
CHEMBL317757 DIFLUOROBENZTROPINE Ki = 145.0 nM 6.84
CHEMBL108527 Ki = 170.0 nM 6.77
CHEMBL320114 Ki = 193.0 nM 6.71
CHEMBL323997 Ki = 214.0 nM 6.67
CHEMBL3084884 Ki = 220.0 nM 6.66
CHEMBL267562 Ki = 277.0 nM 6.56
CHEMBL302796 Ki = 340.0 nM 6.47
CHEMBL322179 Ki = 430.0 nM 6.37
CHEMBL110349 Ki = 430.0 nM 6.37
CHEMBL108637 Ki = 1460.0 nM 5.84
CHEMBL324896 Ki = 2420.0 nM 5.62
CHEMBL110435 Ki = 2520.0 nM 5.60
CHEMBL110120 Ki = 4010.0 nM 5.40
CHEMBL310310 Ki = 5380.0 nM 5.27
CHEMBL108495 Ki = 6100.0 nM 5.21
CHEMBL110247 Ki > 8000.0 nM -
CHEMBL109110 Ki > 5000.0 nM -
CHEMBL275707 RIMCAZOLE Ki > 8000.0 nM -
CHEMBL318770 Ki > 8000.0 nM -
CHEMBL110754 Ki > 4000.0 nM -
CHEMBL110726 Ki > 4000.0 nM -
CHEMBL314726 Ki > 8000.0 nM -
CHEMBL323220 Ki > 8000.0 nM -
CHEMBL323184 Ki > 8000.0 nM -