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Assay Detail

CHEMBL987749

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Functional
Antagonist activity at human adenosine A2A receptor assessed as inhibition of CGS-21680-stimulated cAMP production
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy.
Lanier MC, Moorjani M, Luo Z, Chen Y, Lin E, Tellew JE, Zhang X, Williams JP, Gross RS, Lechner SM, Markison S, Joswig T, Kargo W, Piercey J, Santos M, Malany S, Zhao M, Petroski R, Crespo MI, Díaz JL, Saunders J, Wen J, O'Brien Z, Jalali K, Madan A, Slee DH.
J Med Chem (2009) 52 : 709 -717
PubMed 19140664 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.71 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL458242 1 7.07
CHEMBL458224 1 7.07
CHEMBL515992 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL458242 IC50 = 85.0 nM 7.07
CHEMBL458224 IC50 = 85.0 nM 7.07
CHEMBL515992 IC50 = 1000.0 nM 6.00