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Assay Detail

CHEMBL995104

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

Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies.
Dörfler M, Tschammer N, Hamperl K, Hübner H, Gmeiner P.
J Med Chem (2008) 51 : 6829 -6838
PubMed 18834111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.46 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484358 1 8.68
CHEMBL240773 QUINPIROLE 2.0 1 8.54
CHEMBL484202 1 8.51
CHEMBL162762 1 8.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484358 EC50 = 2.1 nM 8.68
CHEMBL240773 QUINPIROLE EC50 = 2.9 nM 8.54
CHEMBL484202 EC50 = 3.1 nM 8.51
CHEMBL162762 EC50 = 7.7 nM 8.11