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Assay Detail

CHEMBL950423

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Binding
Binding affinity to human adenosine A2A receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease.
Zhang X, Tellew JE, Luo Z, Moorjani M, Lin E, Lanier MC, Chen Y, Williams JP, Saunders J, Lechner SM, Markison S, Joswig T, Petroski R, Piercey J, Kargo W, Malany S, Santos M, Gross RS, Wen J, Jalali K, O'Brien Z, Stotz CE, Crespo MI, Díaz JL, Slee DH.
J Med Chem (2008) 51 : 7099 -7110
PubMed 18947224 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.57 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401321 1 9.22
CHEMBL270467 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401321 Ki = 0.6 nM 9.22
CHEMBL270467 Ki = 12.0 nM 7.92