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Assay Detail

CHEMBL853019

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

Binding
Binding affinity to recombinant human adenosine A3 receptor
27
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor.
Carotti A, Cadavid MI, Centeno NB, Esteve C, Loza MI, Martinez A, Nieto R, Raviña E, Sanz F, Segarra V, Sotelo E, Stefanachi A, Vidal B.
J Med Chem (2006) 49 : 282 -299
PubMed 16392813 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
pKi 17 - -
Ki 10 5.85 6.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16677 1 6.86
CHEMBL275605 1 6.85
CHEMBL273807 1 6.24
CHEMBL199611 1 6.04
CHEMBL278039 1 5.90
CHEMBL275427 1 5.73
CHEMBL17003 1 5.63
CHEMBL27041 1 5.40
CHEMBL201750 1 4.97
CHEMBL372148 1 4.91
CHEMBL199910 1 -
CHEMBL199717 1 -
CHEMBL201003 1 -
CHEMBL197606 1 -
CHEMBL199808 1 -
CHEMBL203208 1 -
CHEMBL199856 1 -
CHEMBL201608 1 -
CHEMBL203467 1 -
CHEMBL201217 1 -
CHEMBL201228 1 -
CHEMBL201591 1 -
CHEMBL381747 1 -
CHEMBL201578 1 -
CHEMBL201536 1 -
CHEMBL202925 1 -
CHEMBL383031 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16677 Ki = 138.04 nM 6.86
CHEMBL275605 Ki = 141.25 nM 6.85
CHEMBL273807 Ki = 575.44 nM 6.24
CHEMBL199611 Ki = 912.01 nM 6.04
CHEMBL278039 Ki = 1258.93 nM 5.90
CHEMBL275427 Ki = 1862.09 nM 5.73
CHEMBL17003 Ki = 2344.23 nM 5.63
CHEMBL27041 Ki = 3981.07 nM 5.40
CHEMBL201750 Ki = 10715.19 nM 4.97
CHEMBL372148 Ki = 12302.69 nM 4.91
CHEMBL199910 pKi - -
CHEMBL199717 pKi - -
CHEMBL201003 pKi - -
CHEMBL197606 pKi - -
CHEMBL199808 pKi - -
CHEMBL203208 pKi - -
CHEMBL199856 pKi - -
CHEMBL201608 pKi - -
CHEMBL203467 pKi - -
CHEMBL201217 pKi - -
CHEMBL201228 pKi - -
CHEMBL201591 pKi - -
CHEMBL381747 pKi - -
CHEMBL201578 pKi - -
CHEMBL201536 pKi - -
CHEMBL202925 pKi - -
CHEMBL383031 pKi - -