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Assay Detail

CHEMBL4433969

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Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
Wang P, Felsing DE, Chen H, Raval SR, Allen JA, Zhou J.
ACS Med Chem Lett (2019) 10 : 792 -799
PubMed 31098001 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 9.00 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59 DOPAMINE 4.0 1 9.10
CHEMBL240773 QUINPIROLE 2.0 1 8.89
CHEMBL353335 1 -
CHEMBL4453318 1 -
CHEMBL3697578 RAZPIPADON 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59 DOPAMINE EC50 = 0.8 nM 9.10
CHEMBL240773 QUINPIROLE EC50 = 1.3 nM 8.89
CHEMBL353335 EC50 - -
CHEMBL4453318 EC50 - -
CHEMBL3697578 RAZPIPADON EC50 - -