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Assay Detail

CHEMBL1052236

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

Binding
Displacement of [3H]NECA from human recombinant adenosine A1 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
5
Total Activities
5
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 5 6.15 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL576395 1 6.96
CHEMBL568307 1 6.29
CHEMBL567412 1 6.08
CHEMBL583862 1 5.80
CHEMBL582921 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL576395 Ki = 109.0 nM 6.96
CHEMBL568307 Ki = 513.0 nM 6.29
CHEMBL567412 Ki = 839.0 nM 6.08
CHEMBL583862 Ki = 1600.0 nM 5.80
CHEMBL582921 Ki = 2320.0 nM 5.63