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Assay Detail

CHEMBL641716

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

Binding
Affinity for the Adenosine A1 receptor in the presence of GTP (A1+GTP) by using [3H]-DPCPX as radioligand
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Ribose-modified adenosine analogues as potential partial agonists for the adenosine receptor.
van der Wenden EM, von Frijtag Drabbe Künzel JK, Mathôt RA, Danhof M, IJzerman AP, Soudijn W.
J Med Chem (1995) 38 : 4000 -4006
PubMed 7562934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 5.58 7.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 7.45
CHEMBL139000 (R)-PIA 1 7.21
CHEMBL150197 1 6.35
CHEMBL2112619 1 6.33
CHEMBL2112569 1 6.00
CHEMBL607763 1 5.97
CHEMBL2112665 1 5.90
CHEMBL1790733 1 5.12
CHEMBL443485 5'-Deoxyadenosine 1 4.92
CHEMBL128173 1 4.84
CHEMBL65976 1 4.83
CHEMBL305686 CORDYCEPIN 1.0 1 4.82
CHEMBL2112664 1 4.76
CHEMBL1790730 1 4.64
CHEMBL449329 DEOXYADENOSINE 1 4.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 35.2 nM 7.45
CHEMBL139000 (R)-PIA Ki = 62.0 nM 7.21
CHEMBL150197 Ki = 450.0 nM 6.35
CHEMBL2112619 Ki = 470.0 nM 6.33
CHEMBL2112569 Ki = 1010.0 nM 6.00
CHEMBL607763 Ki = 1070.0 nM 5.97
CHEMBL2112665 Ki = 1260.0 nM 5.90
CHEMBL1790733 Ki = 7600.0 nM 5.12
CHEMBL443485 5'-Deoxyadenosine Ki = 12100.0 nM 4.92
CHEMBL128173 Ki = 14400.0 nM 4.84
CHEMBL65976 Ki = 14700.0 nM 4.83
CHEMBL305686 CORDYCEPIN Ki = 15200.0 nM 4.82
CHEMBL2112664 Ki = 17500.0 nM 4.76
CHEMBL1790730 Ki = 22800.0 nM 4.64
CHEMBL449329 DEOXYADENOSINE Ki = 23300.0 nM 4.63