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Assay Detail

CHEMBL853546

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

Functional
Antagonist potency at cloned recombinant human adenosine A2A receptor transfected in CHO cells by cAMP assay
23
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A2a (CHEMBL251)
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
pA2 17 - -
Kd 6 6.36 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL382135 1 7.30
CHEMBL199446 1 7.24
CHEMBL201721 1 6.20
CHEMBL370378 1 5.99
CHEMBL201750 1 5.90
CHEMBL372148 1 5.50
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
CHEMBL382135 Kd = 50.12 nM 7.30
CHEMBL199446 Kd = 57.54 nM 7.24
CHEMBL201721 Kd = 630.96 nM 6.20
CHEMBL370378 Kd = 1023.29 nM 5.99
CHEMBL201750 Kd = 1258.93 nM 5.90
CHEMBL372148 Kd = 3162.28 nM 5.50
CHEMBL199910 pA2 - -
CHEMBL199717 pA2 - -
CHEMBL201003 pA2 - -
CHEMBL197606 pA2 - -
CHEMBL199808 pA2 - -
CHEMBL203208 pA2 - -
CHEMBL199856 pA2 - -
CHEMBL201608 pA2 - -
CHEMBL203467 pA2 - -
CHEMBL201217 pA2 - -
CHEMBL201228 pA2 - -
CHEMBL201591 pA2 - -
CHEMBL381747 pA2 - -
CHEMBL201578 pA2 - -
CHEMBL201536 pA2 - -
CHEMBL202925 pA2 - -
CHEMBL383031 pA2 - -