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Assay Detail

CHEMBL895618

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

Binding
Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
Lange JH, Reinders JH, Tolboom JT, Glennon JC, Coolen HK, Kruse CG.
J Med Chem (2007) 50 : 5103 -5108
PubMed 17880057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.11 9.10
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196514 1 9.10
CHEMBL131495 1 8.50
CHEMBL221692 ADOPRAZINE 2.0 1 8.40
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.30
CHEMBL54 HALOPERIDOL 4.0 1 8.30
CHEMBL85 RISPERIDONE 4.0 1 8.20
CHEMBL71 CHLORPROMAZINE 4.0 1 8.00
CHEMBL243712 AMISULPRIDE 4.0 1 7.90
CHEMBL708 ZIPRASIDONE 4.0 1 7.90
CHEMBL715 OLANZAPINE 4.0 1 7.70
CHEMBL42 CLOZAPINE 4.0 1 6.90
CHEMBL716 QUETIAPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196514 Ki = 0.7943 nM 9.10
CHEMBL131495 Ki = 3.162 nM 8.50
CHEMBL221692 ADOPRAZINE Ki = 3.981 nM 8.40
CHEMBL1112 ARIPIPRAZOLE Ki = 5.012 nM 8.30
CHEMBL54 HALOPERIDOL Ki = 5.012 nM 8.30
CHEMBL85 RISPERIDONE Ki = 6.31 nM 8.20
CHEMBL71 CHLORPROMAZINE Ki = 10.0 nM 8.00
CHEMBL243712 AMISULPRIDE Ki = 12.59 nM 7.90
CHEMBL708 ZIPRASIDONE Ki = 12.59 nM 7.90
CHEMBL715 OLANZAPINE Ki = 19.95 nM 7.70
CHEMBL42 CLOZAPINE Ki = 125.89 nM 6.90
CHEMBL716 QUETIAPINE Activity - -