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Assay Detail

CHEMBL5236915

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

Binding
Partial agonist activity at human D2 receptor assessed as increase in cAMP accumulation
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent and Subtype-Selective Dopamine D<sub>2</sub> Receptor Biased Partial Agonists Discovered via an Ugi-Based Approach.
Mallo-Abreu A, Reyes-Resina I, Azuaje J, Franco R, García-Rey A, Majellaro M, Miranda-Pastoriza D, García-Mera X, Jespers W, Gutiérrez-de-Terán H, Navarro G, Sotelo E.
J Med Chem (2021) 64 : 8710 -8726
PubMed 34110150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.86 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028019 CARIPRAZINE 4.0 1 9.74
CHEMBL1112 ARIPIPRAZOLE 4.0 1 7.42
CHEMBL5272965 1 7.21
CHEMBL5289063 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028019 CARIPRAZINE EC50 = 0.18 nM 9.74
CHEMBL1112 ARIPIPRAZOLE EC50 = 38.0 nM 7.42
CHEMBL5272965 EC50 = 61.7 nM 7.21
CHEMBL5289063 EC50 = 90.0 nM 7.05