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Assay Detail

CHEMBL3117733

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

Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
8
Total Activities
8
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 characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
van Wieringen JP, Shalgunov V, Janssen HM, Fransen PM, Janssen AG, Michel MC, Booij J, Elsinga PH.
J Med Chem (2014) 57 : 391 -410
PubMed 24325578 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 9.74 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134807 1 10.70
CHEMBL3115575 1 10.50
CHEMBL3115585 1 10.30
CHEMBL3115582 1 9.80
CHEMBL3115579 1 9.40
CHEMBL3115574 1 9.20
CHEMBL1557 DOPAMINE HYDROCHLORIDE 4.0 1 9.20
CHEMBL3115578 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134807 EC50 = 0.01995 nM 10.70
CHEMBL3115575 EC50 = 0.03162 nM 10.50
CHEMBL3115585 EC50 = 0.05012 nM 10.30
CHEMBL3115582 EC50 = 0.1585 nM 9.80
CHEMBL3115579 EC50 = 0.3981 nM 9.40
CHEMBL3115574 EC50 = 0.631 nM 9.20
CHEMBL1557 DOPAMINE HYDROCHLORIDE EC50 = 0.631 nM 9.20
CHEMBL3115578 EC50 = 1.585 nM 8.80