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Assay Detail

CHEMBL4259829

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Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
4
Total Activities
4
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

Design, synthesis, and evaluation of bitopic arylpiperazine-phthalimides as selective dopamine D<sub>3</sub> receptor agonists.
Cao Y, Sun N, Zhang J, Liu Z, Tang YZ, Wu Z, Kim KM, Cheon SH.
Medchemcomm (2018) 9 : 1457 -1465
PubMed 30288220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 9.85 10.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4285942 1 10.59
CHEMBL240773 QUINPIROLE 2.0 1 10.01
CHEMBL4287055 1 8.96
CHEMBL4294744 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4285942 EC50 = 0.026 nM 10.59
CHEMBL240773 QUINPIROLE EC50 = 0.097 nM 10.01
CHEMBL4287055 EC50 = 1.1 nM 8.96
CHEMBL4294744 EC50 = 0.00048 nM -