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Assay Detail

CHEMBL637901

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

Binding
Displacement of [3H]DPCPX (without GTP) from Adenosine A1 receptor of rat cortical membrane
14
Total Activities
14
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 A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N6,C8-distributed adenosine derivatives as partial agonists for adenosine A1 receptors.
Roelen H, Veldman N, Spek AL, von Frijtag Drabbe Künzel J, Mathôt RA, IJzerman AP.
J Med Chem (1996) 39 : 1463 -1471
PubMed 8691477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.99 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 8.23
CHEMBL2113442 1 6.51
CHEMBL2113438 1 6.46
CHEMBL2113439 1 6.33
CHEMBL605687 1 6.30
CHEMBL2113448 1 6.12
CHEMBL2113440 1 5.96
CHEMBL604232 1 5.80
CHEMBL451058 1 5.62
CHEMBL2113462 1 5.25
CHEMBL603605 1 5.22
CHEMBL604447 1 5.18
CHEMBL2113473 1 4.94
CHEMBL604854 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 5.9 nM 8.23
CHEMBL2113442 Ki = 310.0 nM 6.51
CHEMBL2113438 Ki = 350.0 nM 6.46
CHEMBL2113439 Ki = 470.0 nM 6.33
CHEMBL605687 Ki = 500.0 nM 6.30
CHEMBL2113448 Ki = 760.0 nM 6.12
CHEMBL2113440 Ki = 1090.0 nM 5.96
CHEMBL604232 Ki = 1590.0 nM 5.80
CHEMBL451058 Ki = 2420.0 nM 5.62
CHEMBL2113462 Ki = 5610.0 nM 5.25
CHEMBL603605 Ki = 5960.0 nM 5.22
CHEMBL604447 Ki = 6560.0 nM 5.18
CHEMBL2113473 Ki = 11400.0 nM 4.94
CHEMBL604854 Ki - nM -