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Assay Detail

CHEMBL642893

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

Binding
Displacement of [3H]R-PIA from adenosine A1 receptor of Wistar rat forebrain
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL318)
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 7.62 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 8.92
CHEMBL139000 (R)-PIA 1 8.59
CHEMBL116903 1 8.51
CHEMBL117974 1 8.44
CHEMBL423315 1 8.33
CHEMBL2112564 1 8.00
CHEMBL327073 1 7.82
CHEMBL115471 1 7.37
CHEMBL117904 1 7.12
CHEMBL331382 METRIFUDIL 2.0 1 7.01
CHEMBL326838 1 7.00
CHEMBL411732 1 6.90
CHEMBL331372 CGS-21680 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 1.2 nM 8.92
CHEMBL139000 (R)-PIA Ki = 2.6 nM 8.59
CHEMBL116903 Ki = 3.1 nM 8.51
CHEMBL117974 Ki = 3.6 nM 8.44
CHEMBL423315 Ki = 4.7 nM 8.33
CHEMBL2112564 Ki = 10.0 nM 8.00
CHEMBL327073 Ki = 15.0 nM 7.82
CHEMBL115471 Ki = 43.0 nM 7.37
CHEMBL117904 Ki = 76.0 nM 7.12
CHEMBL331382 METRIFUDIL Ki = 98.0 nM 7.01
CHEMBL326838 Ki = 100.0 nM 7.00
CHEMBL411732 Ki = 126.0 nM 6.90
CHEMBL331372 CGS-21680 Ki = 9900.0 nM 5.00