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Assay Detail

CHEMBL5335380

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

Functional
Antagonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK-T cell
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Selective Dopamine Receptor Ligands Derived from (-)-Stepholidine via C-3 Alkoxylation and C-3/C-9 Dialkoxylation.
Namballa HK, Dorogan M, Gudipally AR, Okafor S, Gadhiya S, Harding WW.
J Med Chem (2023) 66 : 10060 -10079
PubMed 37421373 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.56 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8514 BUTACLAMOL 2.0 1 7.89
CHEMBL5429932 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8514 BUTACLAMOL IC50 = 13.0 nM 7.89
CHEMBL5429932 IC50 = 59.0 nM 7.23