Assay Detail

CHEMBL910423

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Functional

Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR

ChEMBL ↗

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Target

D(2) dopamine receptor (CHEMBL217) ↗

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D(2) dopamine receptor (CHEMBL217) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target D(2) dopamine receptor

CHEMBL217

Anchored from Assay target.

Protein identity D(2) 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	Mustela putorius furo
Cell Type	HEK293
Confidence	8 — Homologous single protein target
Curated By	Expert

Target

D(2) dopamine receptor (CHEMBL217) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.

Patel MV, Kolasa T, Mortell K, Matulenko MA, Hakeem AA, Rohde JJ, Nelson SL, Cowart MD, Nakane M, Miller LN, Uchic ME, Terranova MA, El-Kouhen OF, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Chang R, Martino BR, Wetter JM, Marsh KC, Martin R, Darbyshire JF, Gintant G, Hsieh GC, Moreland RB, Sullivan JP, Brioni JD, Stewart AO.
J Med Chem (2006) 49 : 7450 -7465
PubMed 17149874 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	2	8.42	8.74

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL53	APOMORPHINE	4.0	1	8.74
CHEMBL59	DOPAMINE	4.0	1	8.10

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL53	APOMORPHINE	EC50	=	1.8	nM	8.74
CHEMBL59	DOPAMINE	EC50	=	8.0	nM	8.10