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Assay Detail

CHEMBL954164

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

Binding
Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
Butini S, Gemma S, Campiani G, Franceschini S, Trotta F, Borriello M, Ceres N, Ros S, Coccone SS, Bernetti M, De Angelis M, Brindisi M, Nacci V, Fiorini I, Novellino E, Cagnotto A, Mennini T, Sandager-Nielsen K, Andreasen JT, Scheel-Kruger J, Mikkelsen JD, Fattorusso C.
J Med Chem (2009) 52 : 151 -169
PubMed 19072656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.60 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL462508 1 10.00
CHEMBL496531 1 9.98
CHEMBL495572 1 9.85
CHEMBL339960 1 9.74
CHEMBL461236 1 9.57
CHEMBL126889 1 9.42
CHEMBL497604 1 9.27
CHEMBL54 HALOPERIDOL 4.0 1 9.05
CHEMBL497574 1 8.49
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.48
CHEMBL497573 1 8.43
CHEMBL496739 1 8.35
CHEMBL517730 1 8.22
CHEMBL85 RISPERIDONE 4.0 1 8.17
CHEMBL497988 1 8.09
CHEMBL495573 1 8.07
CHEMBL522044 1 7.48
CHEMBL461023 1 7.47
CHEMBL715 OLANZAPINE 4.0 1 7.41
CHEMBL42 CLOZAPINE 4.0 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL462508 Ki = 0.099 nM 10.00
CHEMBL496531 Ki = 0.105 nM 9.98
CHEMBL495572 Ki = 0.14 nM 9.85
CHEMBL339960 Ki = 0.18 nM 9.74
CHEMBL461236 Ki = 0.27 nM 9.57
CHEMBL126889 Ki = 0.38 nM 9.42
CHEMBL497604 Ki = 0.54 nM 9.27
CHEMBL54 HALOPERIDOL Ki = 0.9 nM 9.05
CHEMBL497574 Ki = 3.2 nM 8.49
CHEMBL1112 ARIPIPRAZOLE Ki = 3.3 nM 8.48
CHEMBL497573 Ki = 3.7 nM 8.43
CHEMBL496739 Ki = 4.5 nM 8.35
CHEMBL517730 Ki = 6.0 nM 8.22
CHEMBL85 RISPERIDONE Ki = 6.7 nM 8.17
CHEMBL497988 Ki = 8.2 nM 8.09
CHEMBL495573 Ki = 8.6 nM 8.07
CHEMBL522044 Ki = 32.92 nM 7.48
CHEMBL461023 Ki = 33.5 nM 7.47
CHEMBL715 OLANZAPINE Ki = 39.0 nM 7.41
CHEMBL42 CLOZAPINE Ki = 319.0 nM 6.50