Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3745238

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

Functional
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
6
Total Activities
6
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

Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treatment of Parkinson's Disease.
Das B, Vedachalam S, Luo D, Antonio T, Reith ME, Dutta AK.
J Med Chem (2015) 58 : 9179 -9195
PubMed 26555041 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 8.31 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3742140 1 9.08
CHEMBL3740041 1 8.85
CHEMBL3740286 1 8.41
CHEMBL59 DOPAMINE 4.0 1 8.27
CHEMBL3740778 1 7.96
CHEMBL7549 PRECLAMOL 2.0 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3742140 EC50 = 0.84 nM 9.08
CHEMBL3740041 EC50 = 1.41 nM 8.85
CHEMBL3740286 EC50 = 3.93 nM 8.41
CHEMBL59 DOPAMINE EC50 = 5.34 nM 8.27
CHEMBL3740778 EC50 = 10.9 nM 7.96
CHEMBL7549 PRECLAMOL EC50 = 51.9 nM 7.29