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Assay Detail

CHEMBL954162

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

Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 17 5.96 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL715 OLANZAPINE 4.0 1 7.60
CHEMBL85 RISPERIDONE 4.0 1 7.30
CHEMBL54 HALOPERIDOL 4.0 1 6.50
CHEMBL42 CLOZAPINE 4.0 1 6.45
CHEMBL1112 ARIPIPRAZOLE 4.0 1 5.71
CHEMBL496739 1 5.48
CHEMBL497574 1 5.37
CHEMBL496531 1 5.36
CHEMBL462508 1 5.34
CHEMBL461236 1 5.26
CHEMBL495572 1 5.15
CHEMBL522044 1 -
CHEMBL495573 1 -
CHEMBL497573 1 -
CHEMBL497604 1 -
CHEMBL461023 1 -
CHEMBL517730 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL715 OLANZAPINE Ki = 25.0 nM 7.60
CHEMBL85 RISPERIDONE Ki = 50.0 nM 7.30
CHEMBL54 HALOPERIDOL Ki = 318.0 nM 6.50
CHEMBL42 CLOZAPINE Ki = 353.0 nM 6.45
CHEMBL1112 ARIPIPRAZOLE Ki = 1960.0 nM 5.71
CHEMBL496739 Ki = 3290.0 nM 5.48
CHEMBL497574 Ki = 4315.0 nM 5.37
CHEMBL496531 Ki = 4370.0 nM 5.36
CHEMBL462508 Ki = 4600.0 nM 5.34
CHEMBL461236 Ki = 5500.0 nM 5.26
CHEMBL495572 Ki = 7124.0 nM 5.15
CHEMBL522044 Ki - -
CHEMBL495573 Ki > 10000.0 nM -
CHEMBL497573 Ki > 10000.0 nM -
CHEMBL497604 Ki > 10000.0 nM -
CHEMBL461023 Ki > 10000.0 nM -
CHEMBL517730 Ki > 10000.0 nM -