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Assay Detail

CHEMBL2404651

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

Binding
Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyluronamide from mouse adenosine A3 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL1075269)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain.
Paoletta S, Tosh DK, Finley A, Gizewski ET, Moss SM, Gao ZG, Auchampach JA, Salvemini D, Jacobson KA.
J Med Chem (2013) 56 : 5949 -5963
PubMed 23789857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.01 8.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2064653 1 8.91
CHEMBL2402024 1 8.06
CHEMBL2401954 1 8.01
CHEMBL2401955 1 7.95
CHEMBL2402025 1 7.15
CHEMBL2089345 1 6.59
CHEMBL2089346 1 6.32
CHEMBL2089339 1 5.83
CHEMBL2089335 1 5.82
CHEMBL2402023 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2064653 Ki = 1.23 nM 8.91
CHEMBL2402024 Ki = 8.75 nM 8.06
CHEMBL2401954 Ki = 9.68 nM 8.01
CHEMBL2401955 Ki = 11.3 nM 7.95
CHEMBL2402025 Ki = 71.1 nM 7.15
CHEMBL2089345 Ki = 255.0 nM 6.59
CHEMBL2089346 Ki = 480.0 nM 6.32
CHEMBL2089339 Ki = 1480.0 nM 5.83
CHEMBL2089335 Ki = 1530.0 nM 5.82
CHEMBL2402023 Ki = 3920.0 nM 5.41