Assay Detail

CHEMBL5363881

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

Functional

Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay

ChEMBL ↗

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Target

D(3) dopamine receptor (CHEMBL234) ↗

Open DB target context

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D(3) dopamine receptor (CHEMBL234) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target D(3) dopamine receptor

CHEMBL234

Anchored from Assay target.

Protein identity D(3) dopamine receptor

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Organism	Homo sapiens
Cell Type	HEK293T
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

D(3) dopamine receptor (CHEMBL234) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Pharmacological and Physicochemical Properties Optimization for Dual-Target Dopamine D<sub>3</sub> (D<sub>3</sub>R) and μ-Opioid (MOR) Receptor Ligands as Potentially Safer Analgesics.

Bonifazi A, Saab E, Sanchez J, Nazarova AL, Zaidi SA, Jahan K, Katritch V, Canals M, Lane JR, Newman AH.
J Med Chem (2023) 66 : 10304 -10341
PubMed 37467430 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	4	8.91	9.17

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL59	DOPAMINE	4.0	2	9.17
CHEMBL240773	QUINPIROLE	2.0	2	8.64

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL59	DOPAMINE	EC50	=	0.6761	nM	9.17
CHEMBL59	DOPAMINE	EC50	=	0.68	nM	9.17
CHEMBL240773	QUINPIROLE	EC50	=	2.291	nM	8.64
CHEMBL240773	QUINPIROLE	EC50	=	2.27	nM	8.64