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Assay Detail

CHEMBL642018

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

Binding
Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Testis
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL3360)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.
Franchetti P, Cappellacci L, Marchetti S, Trincavelli L, Martini C, Mazzoni MR, Lucacchini A, Grifantini M.
J Med Chem (1998) 41 : 1708 -1715
PubMed 9572897 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.57 7.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66393 1 7.99
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 7.58
CHEMBL284969 1 7.52
CHEMBL119709 IB-MECA 1 7.52
CHEMBL464859 NECA 1 7.31
CHEMBL139000 (R)-PIA 1 7.28
CHEMBL400189 1 6.68
CHEMBL420705 (S)-PIA 1 6.62
CHEMBL605034 1 6.50
CHEMBL2113418 1 6.26
CHEMBL2113388 1 5.97
CHEMBL285819 1 5.50
CHEMBL444550 1 5.49
CHEMBL251997 1 5.30
CHEMBL603977 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66393 Ki = 10.2 nM 7.99
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 26.0 nM 7.58
CHEMBL284969 Ki = 30.0 nM 7.52
CHEMBL119709 IB-MECA Ki = 30.0 nM 7.52
CHEMBL464859 NECA Ki = 49.0 nM 7.31
CHEMBL139000 (R)-PIA Ki = 53.0 nM 7.28
CHEMBL400189 Ki = 208.0 nM 6.68
CHEMBL420705 (S)-PIA Ki = 241.0 nM 6.62
CHEMBL605034 Ki = 320.0 nM 6.50
CHEMBL2113418 Ki = 550.0 nM 6.26
CHEMBL2113388 Ki = 1082.0 nM 5.97
CHEMBL285819 Ki = 3200.0 nM 5.50
CHEMBL444550 Ki = 3250.0 nM 5.49
CHEMBL251997 Ki = 5000.0 nM 5.30
CHEMBL603977 Ki = 10000.0 nM 5.00