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Assay Detail

CHEMBL4406543

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

Functional
Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay
2
Total Activities
2
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(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D3 Dopamine Receptor Agonist.
Moritz AE, Free RB, Weiner WS, Akano EO, Gandhi D, Abramyan A, Keck TM, Ferrer M, Hu X, Southall N, Steiner J, Aubé J, Shi L, Frankowski KJ, Sibley DR.
J Med Chem (2020) 63 : 5526 -5567
PubMed 32342685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.77 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59 DOPAMINE 4.0 1 8.46
CHEMBL4476784 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59 DOPAMINE EC50 = 3.5 nM 8.46
CHEMBL4476784 EC50 = 86.0 nM 7.07