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Assay Detail

CHEMBL633041

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

Binding
Displacement of [3H]-CGS- 21680 from adenosine A2A receptor of rat striatal tissue
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
Knutsen LJ, Lau J, Petersen H, Thomsen C, Weis JU, Shalmi M, Judge ME, Hansen AJ, Sheardown MJ.
J Med Chem (1999) 42 : 3463 -3477
PubMed 10479279 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.24 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL331372 CGS-21680 1 7.96
CHEMBL331382 METRIFUDIL 2.0 1 7.60
CHEMBL139000 (R)-PIA 1 6.93
CHEMBL327073 1 6.61
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.49
CHEMBL2112564 1 6.20
CHEMBL115471 1 5.96
CHEMBL117974 1 5.94
CHEMBL116903 1 5.89
CHEMBL423315 1 5.83
CHEMBL411732 1 5.38
CHEMBL117904 1 5.24
CHEMBL326838 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL331372 CGS-21680 Ki = 11.0 nM 7.96
CHEMBL331382 METRIFUDIL Ki = 25.0 nM 7.60
CHEMBL139000 (R)-PIA Ki = 117.0 nM 6.93
CHEMBL327073 Ki = 245.0 nM 6.61
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 321.0 nM 6.49
CHEMBL2112564 Ki = 630.0 nM 6.20
CHEMBL115471 Ki = 1086.0 nM 5.96
CHEMBL117974 Ki = 1150.0 nM 5.94
CHEMBL116903 Ki = 1300.0 nM 5.89
CHEMBL423315 Ki = 1485.0 nM 5.83
CHEMBL411732 Ki = 4200.0 nM 5.38
CHEMBL117904 Ki = 5700.0 nM 5.24
CHEMBL326838 Ki = 7420.0 nM 5.13