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Assay Detail

CHEMBL3616301

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

Binding
Binding affinity to canine adenosine A3 receptor expressed in HEK293 cell membranes
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL3611963)
Type SINGLE PROTEIN
Organism Canis lupus familiaris

Publication

Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.
Tosh DK, Crane S, Chen Z, Paoletta S, Gao ZG, Gizewski E, Auchampach JA, Salvemini D, Jacobson KA.
ACS Med Chem Lett (2015) 6 : 804 -808
PubMed 26191370 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.87 8.82
IC50 1 5.07 5.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3612931 1 8.82
CHEMBL3612932 1 8.24
CHEMBL3612940 1 7.31
CHEMBL3612939 1 7.12
CHEMBL3407784 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3612931 Ki = 1.5 nM 8.82
CHEMBL3612932 Ki = 5.8 nM 8.24
CHEMBL3612940 Ki = 49.0 nM 7.31
CHEMBL3612939 Ki = 75.0 nM 7.12
CHEMBL3407784 IC50 = 8500.0 nM 5.07