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Assay Detail

CHEMBL642211

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

Binding
Ability to displace the specific binding of [3H](R)-PIA to adenosine A3 receptor from rat testis membranes
34
Total Activities
34
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

A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives.
Ferrarini PL, Mori C, Manera C, Martinelli A, Mori F, Saccomanni G, Barili PL, Betti L, Giannaccini G, Trincavelli L, Lucacchini A.
J Med Chem (2000) 43 : 2814 -2823
PubMed 10956189 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 6.27 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45891 1 7.60
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 7.58
CHEMBL464859 NECA 1 7.31
CHEMBL139000 (R)-PIA 1 7.28
CHEMBL420705 (S)-PIA 1 6.62
CHEMBL273094 XANTHINE AMINE CONGENER 1 6.38
CHEMBL97760 1 5.68
CHEMBL97687 1 5.68
CHEMBL97037 1 5.52
CHEMBL95384 1 5.34
CHEMBL313864 1 5.21
CHEMBL97549 1 5.06
CHEMBL316630 1 -
CHEMBL319580 1 -
CHEMBL97344 1 -
CHEMBL96617 1 -
CHEMBL97757 1 -
CHEMBL329294 1 -
CHEMBL415697 1 -
CHEMBL102430 1 -
CHEMBL328214 1 -
CHEMBL97896 1 -
CHEMBL97904 1 -
CHEMBL96576 1 -
CHEMBL94538 1 -
CHEMBL97663 1 -
CHEMBL97778 1 -
CHEMBL97624 1 -
CHEMBL98227 1 -
CHEMBL329293 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45891 Ki = 25.0 nM 7.60
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 26.0 nM 7.58
CHEMBL464859 NECA Ki = 49.0 nM 7.31
CHEMBL139000 (R)-PIA Ki = 53.0 nM 7.28
CHEMBL420705 (S)-PIA Ki = 241.0 nM 6.62
CHEMBL273094 XANTHINE AMINE CONGENER Ki = 418.0 nM 6.38
CHEMBL97760 Ki = 2100.0 nM 5.68
CHEMBL97687 Ki = 2100.0 nM 5.68
CHEMBL97037 Ki = 3000.0 nM 5.52
CHEMBL95384 Ki = 4600.0 nM 5.34
CHEMBL313864 Ki = 6100.0 nM 5.21
CHEMBL97549 Ki = 8800.0 nM 5.06
CHEMBL328334 Ki > 10000.0 nM -
CHEMBL97337 Ki > 10000.0 nM -
CHEMBL97665 Ki > 10000.0 nM -
CHEMBL97895 Ki > 10000.0 nM -
CHEMBL316630 Ki > 10000.0 nM -
CHEMBL319580 Ki > 10000.0 nM -
CHEMBL97344 Ki > 10000.0 nM -
CHEMBL96617 Ki > 10000.0 nM -
CHEMBL97757 Ki > 10000.0 nM -
CHEMBL329294 Ki > 10000.0 nM -
CHEMBL415697 Ki > 10000.0 nM -
CHEMBL102430 Ki > 10000.0 nM -
CHEMBL328214 Ki > 10000.0 nM -
CHEMBL97896 Ki > 10000.0 nM -
CHEMBL97904 Ki > 10000.0 nM -
CHEMBL96576 Ki > 10000.0 nM -
CHEMBL94538 Ki > 10000.0 nM -
CHEMBL97663 Ki > 10000.0 nM -
CHEMBL97778 Ki > 10000.0 nM -
CHEMBL97624 Ki > 10000.0 nM -
CHEMBL98227 Ki > 10000.0 nM -
CHEMBL329293 Ki > 10000.0 nM -