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Assay Detail

CHEMBL643123

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

Binding
Affinity to Adenosine A3 receptor of rat testis membrane using [3H](R)-PIA with 150 nM DPCPX
9
Total Activities
9
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 A3 (CHEMBL3360)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Ribose-modified nucleosides as ligands for adenosine receptors: synthesis, conformational analysis, and biological evaluation of 1'-C-methyl adenosine analogues.
Cappellacci L, Barboni G, Palmieri M, Pasqualini M, Grifantini M, Costa B, Martini C, Franchetti P.
J Med Chem (2002) 45 : 1196 -1202
PubMed 11881988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.09 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139000 (R)-PIA 1 7.28
CHEMBL400189 1 6.68
CHEMBL420705 (S)-PIA 1 6.62
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.58
CHEMBL3143982 1 6.17
CHEMBL2113388 1 5.97
CHEMBL3143985 1 5.29
CHEMBL3143983 1 5.21
CHEMBL603977 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139000 (R)-PIA Ki = 53.0 nM 7.28
CHEMBL400189 Ki = 210.0 nM 6.68
CHEMBL420705 (S)-PIA Ki = 240.0 nM 6.62
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 260.0 nM 6.58
CHEMBL3143982 Ki = 670.0 nM 6.17
CHEMBL2113388 Ki = 1080.0 nM 5.97
CHEMBL3143985 Ki = 5170.0 nM 5.29
CHEMBL3143983 Ki = 6160.0 nM 5.21
CHEMBL603977 Ki = 10000.0 nM 5.00