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Assay Detail

CHEMBL3057563

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

Binding
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL3138)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Heterodimerization of G-Protein-Coupled Receptors Reveals an Unexpected Level of Pharmacological Diversity
Maggio R, Scarselli M, Novi F, Corsini GU
Med Chem Res (2004) 13 : 25 -33
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.01 9.39
Ki 5 7.81 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL540612 1 9.39
CHEMBL285755 1 8.90
CHEMBL65280 1 8.62
CHEMBL484599 1 8.38
CHEMBL54 HALOPERIDOL 4.0 1 8.30
CHEMBL531 PERGOLIDE 4.0 1 8.29
CHEMBL301265 PRAMIPEXOLE 4.0 1 8.11
CHEMBL219916 DOMPERIDONE 3.0 1 7.93
CHEMBL240773 QUINPIROLE 2.0 1 7.60
CHEMBL53 APOMORPHINE 4.0 1 7.53
CHEMBL715 OLANZAPINE 4.0 1 7.39
CHEMBL589 ROPINIROLE 4.0 1 6.97
CHEMBL59 DOPAMINE 4.0 1 6.96
CHEMBL42 CLOZAPINE 4.0 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL540612 IC50 = 0.41 nM 9.39
CHEMBL285755 IC50 = 1.25 nM 8.90
CHEMBL65280 Ki = 2.42 nM 8.62
CHEMBL484599 IC50 = 4.13 nM 8.38
CHEMBL54 HALOPERIDOL Ki = 5.04 nM 8.30
CHEMBL531 PERGOLIDE IC50 = 5.12 nM 8.29
CHEMBL301265 PRAMIPEXOLE IC50 = 7.8 nM 8.11
CHEMBL219916 DOMPERIDONE Ki = 11.7 nM 7.93
CHEMBL240773 QUINPIROLE IC50 = 25.0 nM 7.60
CHEMBL53 APOMORPHINE IC50 = 29.4 nM 7.53
CHEMBL715 OLANZAPINE Ki = 40.6 nM 7.39
CHEMBL589 ROPINIROLE IC50 = 107.0 nM 6.97
CHEMBL59 DOPAMINE IC50 = 111.0 nM 6.96
CHEMBL42 CLOZAPINE Ki = 161.0 nM 6.79