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Assay Detail

CHEMBL642299

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

Binding
Displacement of [3H]PIA from adenosine A1 receptor of rat brain membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.
Cristalli G, Franchetti P, Grifantini M, Vittori S, Klotz KN, Lohse MJ.
J Med Chem (1988) 31 : 1179 -1183
PubMed 3373486 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.02 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 9.10
CHEMBL139000 (R)-PIA 1 8.89
CHEMBL2113390 1 8.80
CHEMBL2113389 1 8.12
CHEMBL606016 1 8.11
CHEMBL464859 NECA 1 8.09
CHEMBL2113387 1 7.80
CHEMBL605008 1 7.75
CHEMBL2113391 1 7.33
CHEMBL2113396 1 7.29
CHEMBL115824 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 0.8 nM 9.10
CHEMBL139000 (R)-PIA Ki = 1.3 nM 8.89
CHEMBL2113390 Ki = 1.6 nM 8.80
CHEMBL2113389 Ki = 7.5 nM 8.12
CHEMBL606016 Ki = 7.7 nM 8.11
CHEMBL464859 NECA Ki = 8.2 nM 8.09
CHEMBL2113387 Ki = 16.0 nM 7.80
CHEMBL605008 Ki = 18.0 nM 7.75
CHEMBL2113391 Ki = 47.0 nM 7.33
CHEMBL2113396 Ki = 51.0 nM 7.29
CHEMBL115824 Ki = 115.0 nM 6.94