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Assay Detail

CHEMBL864800

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

Binding
Displacement of [3H]MSX2 from human recombinant adenosine A2A receptor expressed in CHO cells
15
Total Activities
15
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 Expert

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
Yan L, Bertarelli DC, Hayallah AM, Meyer H, Klotz KN, Müller CE.
J Med Chem (2006) 49 : 4384 -4391
PubMed 16821798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.68 7.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210585 1 7.49
CHEMBL209230 1 6.79
CHEMBL212625 1 6.32
CHEMBL211521 1 6.11
CHEMBL8565 1 -
CHEMBL8488 1 -
CHEMBL213878 1 -
CHEMBL377106 1 -
CHEMBL212626 1 -
CHEMBL209366 1 -
CHEMBL377246 1 -
CHEMBL208550 1 -
CHEMBL212217 1 -
CHEMBL378102 1 -
CHEMBL418333 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210585 Ki = 32.6 nM 7.49
CHEMBL209230 Ki = 162.0 nM 6.79
CHEMBL212625 Ki = 484.0 nM 6.32
CHEMBL211521 Ki = 769.0 nM 6.11
CHEMBL8565 Ki - -
CHEMBL8488 Ki - -
CHEMBL213878 Ki - -
CHEMBL377106 Ki - -
CHEMBL212626 Ki - -
CHEMBL209366 Ki - -
CHEMBL377246 Ki - -
CHEMBL208550 Ki - -
CHEMBL212217 Ki - -
CHEMBL378102 Ki - -
CHEMBL418333 Ki - -