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Assay Detail

CHEMBL3745246

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Functional
Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 300 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)
1
Total Activities
1
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(2) dopamine receptor (CHEMBL217)
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 1 5.41 5.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3740778 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3740778 EC50 = 3930.0 nM 5.41