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Assay Detail

CHEMBL895617

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

Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
11
Total Activities
11
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(4) dopamine receptor (CHEMBL219)
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 10 7.71 8.80
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196514 1 8.80
CHEMBL54 HALOPERIDOL 4.0 1 8.20
CHEMBL85 RISPERIDONE 4.0 1 8.00
CHEMBL221692 ADOPRAZINE 2.0 1 8.00
CHEMBL715 OLANZAPINE 4.0 1 7.70
CHEMBL71 CHLORPROMAZINE 4.0 1 7.60
CHEMBL42 CLOZAPINE 4.0 1 7.40
CHEMBL708 ZIPRASIDONE 4.0 1 7.30
CHEMBL131495 1 7.10
CHEMBL1112 ARIPIPRAZOLE 4.0 1 7.00
CHEMBL716 QUETIAPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196514 Ki = 1.585 nM 8.80
CHEMBL54 HALOPERIDOL Ki = 6.31 nM 8.20
CHEMBL85 RISPERIDONE Ki = 10.0 nM 8.00
CHEMBL221692 ADOPRAZINE Ki = 10.0 nM 8.00
CHEMBL715 OLANZAPINE Ki = 19.95 nM 7.70
CHEMBL71 CHLORPROMAZINE Ki = 25.12 nM 7.60
CHEMBL42 CLOZAPINE Ki = 39.81 nM 7.40
CHEMBL708 ZIPRASIDONE Ki = 50.12 nM 7.30
CHEMBL131495 Ki = 79.43 nM 7.10
CHEMBL1112 ARIPIPRAZOLE Ki = 100.0 nM 7.00
CHEMBL716 QUETIAPINE Activity - -