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Assay Detail

CHEMBL1052237

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

Binding
Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.
Tosh DK, Chinn M, Ivanov AA, Klutz AM, Gao ZG, Jacobson KA.
J Med Chem (2009) 52 : 7580 -7592
PubMed 19499950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.08 7.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573937 1 7.74
CHEMBL567226 1 6.58
CHEMBL583132 1 6.34
CHEMBL565678 1 6.32
CHEMBL583637 1 6.16
CHEMBL490606 1 5.75
CHEMBL490605 1 5.52
CHEMBL523797 1 5.51
CHEMBL257833 1 4.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573937 Ki = 18.3 nM 7.74
CHEMBL567226 Ki = 260.0 nM 6.58
CHEMBL583132 Ki = 454.0 nM 6.34
CHEMBL565678 Ki = 482.0 nM 6.32
CHEMBL583637 Ki = 700.0 nM 6.16
CHEMBL490606 Ki = 1760.0 nM 5.75
CHEMBL490605 Ki = 3040.0 nM 5.52
CHEMBL523797 Ki = 3070.0 nM 5.51
CHEMBL257833 Ki = 14900.0 nM 4.83