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Assay Detail

CHEMBL646485

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

Binding
Displacement of [3H]-NECA from adenosine A2 receptor of rat striatal membrane
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

N6-cycloalkyladenosines. Potent, A1-selective adenosine agonists.
Moos WH, Szotek DS, Bruns RF.
J Med Chem (1985) 28 : 1383 -1384
PubMed 2995663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.12 7.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 7.97
CHEMBL285819 1 7.20
CHEMBL139000 (R)-PIA 1 6.91
CHEMBL569275 1 6.58
CHEMBL45891 1 6.44
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.33
CHEMBL2113423 1 5.91
CHEMBL2113430 1 5.77
CHEMBL420705 (S)-PIA 1 5.74
CHEMBL2113424 1 5.61
CHEMBL606090 1 5.49
CHEMBL603382 1 5.29
CHEMBL604646 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA Ki = 10.6 nM 7.97
CHEMBL285819 Ki = 63.1 nM 7.20
CHEMBL139000 (R)-PIA Ki = 124.0 nM 6.91
CHEMBL569275 Ki = 263.0 nM 6.58
CHEMBL45891 Ki = 363.0 nM 6.44
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 462.0 nM 6.33
CHEMBL2113423 Ki = 1240.0 nM 5.91
CHEMBL2113430 Ki = 1690.0 nM 5.77
CHEMBL420705 (S)-PIA Ki = 1810.0 nM 5.74
CHEMBL2113424 Ki = 2450.0 nM 5.61
CHEMBL606090 Ki = 3250.0 nM 5.49
CHEMBL603382 Ki = 5190.0 nM 5.29
CHEMBL604646 Ki = 47700.0 nM 4.32