Assay Detail

CHEMBL672805

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Binding

In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay

ChEMBL ↗

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Target

D(2) dopamine receptor (CHEMBL339) ↗

Open DB target context

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D(2) dopamine receptor (CHEMBL339) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target D(2) dopamine receptor

CHEMBL339

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	Binding
Cell Type	HEK293
Confidence	8 — Homologous single protein target
Curated By	Autocuration

Target

D(2) dopamine receptor (CHEMBL339) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.

Cowart M, Latshaw SP, Bhatia P, Daanen JF, Rohde J, Nelson SL, Patel M, Kolasa T, Nakane M, Uchic ME, Miller LN, Terranova MA, Chang R, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Martino BR, Lynch JJ, Sullivan JP, Hsieh GC, Moreland RB, Brioni JD, Stewart AO.
J Med Chem (2004) 47 : 3853 -3864
PubMed 15239663 · 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