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

CHEMBL5151483

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

Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Abolishing Dopamine D<sub>2long</sub>/D<sub>3</sub> Receptor Affinity of Subtype-Selective Carbamoylguanidine-Type Histamine H<sub>2</sub> Receptor Agonists.
Tropmann K, Bresinsky M, Forster L, Mönnich D, Buschauer A, Wittmann HJ, Hübner H, Gmeiner P, Pockes S, Strasser A.
J Med Chem (2021) 64 : 8684 -8709
PubMed 34110814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.64 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301265 PRAMIPEXOLE 4.0 1 9.09
CHEMBL240773 QUINPIROLE 2.0 1 8.75
CHEMBL5183205 1 7.40
CHEMBL5178472 1 7.17
CHEMBL5176229 1 6.53
CHEMBL5198795 1 6.33
CHEMBL5200771 1 6.09
CHEMBL5202592 1 5.98
CHEMBL5208845 1 5.97
CHEMBL5206565 1 5.92
CHEMBL5204599 1 5.87
CHEMBL5184911 1 5.72
CHEMBL5207281 1 5.55
CHEMBL5201074 1 -
CHEMBL5180504 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301265 PRAMIPEXOLE EC50 = 0.8128 nM 9.09
CHEMBL240773 QUINPIROLE EC50 = 1.778 nM 8.75
CHEMBL5183205 EC50 = 39.81 nM 7.40
CHEMBL5178472 EC50 = 67.61 nM 7.17
CHEMBL5176229 EC50 = 295.12 nM 6.53
CHEMBL5198795 EC50 = 467.74 nM 6.33
CHEMBL5200771 EC50 = 812.83 nM 6.09
CHEMBL5202592 EC50 = 1047.13 nM 5.98
CHEMBL5208845 EC50 = 1071.52 nM 5.97
CHEMBL5206565 EC50 = 1202.26 nM 5.92
CHEMBL5204599 EC50 = 1348.96 nM 5.87
CHEMBL5184911 EC50 = 1905.46 nM 5.72
CHEMBL5207281 EC50 = 2818.38 nM 5.55
CHEMBL5201074 EC50 > 10000.0 nM -
CHEMBL5180504 EC50 > 10000.0 nM -