Assay Detail

CHEMBL5145883

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Binding

Modulation of human D2L receptor

ChEMBL ↗

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Target

D(2) dopamine receptor (CHEMBL217) ↗

Open DB target context

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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	Binding
Organism	Homo sapiens
Cell Type	HEK293
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

D(2) dopamine receptor (CHEMBL217) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Novel D<sub>2</sub>/5-HT receptor modulators related to cariprazine with potential implication to schizophrenia treatment.

Juza R, Vojtechova I, Stefkova-Mazochova K, Dehaen W, Petrasek T, Prchal L, Kobrlova T, Janousek J, Vlcek P, Mezeiova E, Svozil D, Karasova JZ, Pejchal J, Stark H, Satala G, Bojarski AJ, Kubacka M, Mogilski S, Randakova A, Musilek K, Soukup O, Korabecny J.
Eur J Med Chem (2022) 232 : 114193 -114193
PubMed 35176563 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	2	9.41	9.52

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1112	ARIPIPRAZOLE	4.0	1	9.52
CHEMBL2028019	CARIPRAZINE	4.0	1	9.30

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1112	ARIPIPRAZOLE	Ki	=	0.3	nM	9.52
CHEMBL2028019	CARIPRAZINE	Ki	=	0.5012	nM	9.30