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Assay Detail

CHEMBL3801490

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

Binding
Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.
Weichert D, Stanek M, Hübner H, Gmeiner P.
Bioorg Med Chem (2016) 24 : 2641 -2653
PubMed 27132867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 5.86 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240773 QUINPIROLE 2.0 1 7.07
CHEMBL3799455 1 6.62
CHEMBL3800341 1 5.96
CHEMBL3800636 1 5.58
CHEMBL3797205 1 5.06
CHEMBL3798748 1 4.89
CHEMBL3800400 1 -
CHEMBL3800468 1 -
CHEMBL3799427 1 -
CHEMBL3799593 1 -
CHEMBL434 ISOPROTERENOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240773 QUINPIROLE EC50 = 86.0 nM 7.07
CHEMBL3799455 EC50 = 240.0 nM 6.62
CHEMBL3800341 EC50 = 1100.0 nM 5.96
CHEMBL3800636 EC50 = 2600.0 nM 5.58
CHEMBL3797205 EC50 = 8800.0 nM 5.06
CHEMBL3798748 EC50 = 13000.0 nM 4.89
CHEMBL3800400 EC50 - -
CHEMBL3800468 EC50 - -
CHEMBL3799427 EC50 - -
CHEMBL3799593 EC50 - -
CHEMBL434 ISOPROTERENOL EC50 - -