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

CHEMBL2168902

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

Functional
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-functional selectivity relationship studies of β-arrestin-biased dopamine D₂ receptor agonists.
Chen X, Sassano MF, Zheng L, Setola V, Chen M, Bai X, Frye SV, Wetsel WC, Roth BL, Jin J.
J Med Chem (2012) 55 : 7141 -7153
PubMed 22845053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.36 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160296 1 9.22
CHEMBL2165126 1 8.70
CHEMBL2165133 1 8.40
CHEMBL2165135 1 7.80
CHEMBL2165136 1 7.20
CHEMBL2165134 1 7.00
CHEMBL2165129 1 6.70
CHEMBL2165131 1 6.50
CHEMBL2165132 1 6.30
CHEMBL2165128 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160296 EC50 = 0.6 nM 9.22
CHEMBL2165126 EC50 = 2.0 nM 8.70
CHEMBL2165133 EC50 = 4.0 nM 8.40
CHEMBL2165135 EC50 = 16.0 nM 7.80
CHEMBL2165136 EC50 = 63.0 nM 7.20
CHEMBL2165134 EC50 = 100.0 nM 7.00
CHEMBL2165129 EC50 = 199.0 nM 6.70
CHEMBL2165131 EC50 = 316.0 nM 6.50
CHEMBL2165132 EC50 = 501.0 nM 6.30
CHEMBL2165128 EC50 = 1580.0 nM 5.80