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Assay Detail

CHEMBL672170

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

Binding
Binding affinity towards human Dopamine receptor D2 using [3H]spiroperidol as radioligand
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.
Leopoldo M, Berardi F, Colabufo NA, De Giorgio P, Lacivita E, Perrone R, Tortorella V.
J Med Chem (2002) 45 : 5727 -5735
PubMed 12477356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 6.22 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.92
CHEMBL152262 1 7.20
CHEMBL433741 1 7.11
CHEMBL152010 1 6.97
CHEMBL346692 1 6.87
CHEMBL2112910 1 6.77
CHEMBL423040 1 6.68
CHEMBL152869 1 6.60
CHEMBL196476 1 6.43
CHEMBL152304 1 6.37
CHEMBL286725 1 6.33
CHEMBL152159 1 6.17
CHEMBL152587 1 6.11
CHEMBL345820 1 6.08
CHEMBL152756 1 6.03
CHEMBL152576 1 5.95
CHEMBL152391 1 5.85
CHEMBL347290 1 5.81
CHEMBL93403 1 5.72
CHEMBL315879 1 5.63
CHEMBL357448 1 5.52
CHEMBL156599 1 5.43
CHEMBL61789 1 5.42
CHEMBL92713 1 5.40
CHEMBL154508 1 5.28
CHEMBL2112911 1 5.24
CHEMBL156845 1 5.13
CHEMBL152679 1 -
CHEMBL157222 1 -
CHEMBL157322 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.12 nM 9.92
CHEMBL152262 Ki = 63.0 nM 7.20
CHEMBL433741 Ki = 77.0 nM 7.11
CHEMBL152010 Ki = 107.0 nM 6.97
CHEMBL346692 Ki = 135.0 nM 6.87
CHEMBL2112910 Ki = 170.0 nM 6.77
CHEMBL423040 Ki = 210.0 nM 6.68
CHEMBL152869 Ki = 253.0 nM 6.60
CHEMBL196476 Ki = 373.0 nM 6.43
CHEMBL152304 Ki = 430.0 nM 6.37
CHEMBL286725 Ki = 467.0 nM 6.33
CHEMBL152159 Ki = 680.0 nM 6.17
CHEMBL152587 Ki = 770.0 nM 6.11
CHEMBL345820 Ki = 830.0 nM 6.08
CHEMBL152756 Ki = 930.0 nM 6.03
CHEMBL152576 Ki = 1130.0 nM 5.95
CHEMBL152391 Ki = 1410.0 nM 5.85
CHEMBL347290 Ki = 1560.0 nM 5.81
CHEMBL93403 Ki = 1900.0 nM 5.72
CHEMBL315879 Ki = 2350.0 nM 5.63
CHEMBL357448 Ki = 2990.0 nM 5.52
CHEMBL156599 Ki = 3680.0 nM 5.43
CHEMBL61789 Ki = 3800.0 nM 5.42
CHEMBL92713 Ki = 3960.0 nM 5.40
CHEMBL154508 Ki = 5200.0 nM 5.28
CHEMBL2112911 Ki = 5740.0 nM 5.24
CHEMBL156845 Ki = 7460.0 nM 5.13
CHEMBL2112905 Ki > 1000.0 nM -
CHEMBL345111 Ki > 1000.0 nM -
CHEMBL345848 Ki > 1000.0 nM -
CHEMBL154050 Ki > 1000.0 nM -
CHEMBL305362 Ki > 1000.0 nM -
CHEMBL94265 Ki > 850.0 nM -
CHEMBL157388 Ki > 1000.0 nM -
CHEMBL157322 Ki > 1000.0 nM -
CHEMBL157222 Ki > 8300.0 nM -
CHEMBL152679 Ki > 1000.0 nM -