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

CHEMBL4053573

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

Binding
Competitive antagonist activity at D2 long receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of dopamine induced beta-arrestin recruitment after 90 mins by DiscoveRx PathHunter assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R).
Kumar V, Moritz AE, Keck TM, Bonifazi A, Ellenberger MP, Sibley CD, Free RB, Shi L, Lane JR, Sibley DR, Newman AH.
J Med Chem (2017) 60 : 1478 -1494
PubMed 28186762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 8.55 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26 SULPIRIDE 3.0 1 8.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26 SULPIRIDE Kd = 2.818 nM 8.55