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Assay Detail

CHEMBL5126844

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Functional
Antagonist activity at human adenosine A2A receptor
8
Total Activities
8
Compounds Tested
2
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

Adenosine receptor antagonists: Recent advances and therapeutic perspective.
Saini A, Patel R, Gaba S, Singh G, Gupta GD, Monga V.
Eur J Med Chem (2022) 227 : 113907 -113907
PubMed 34695776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.26 7.22
Ki 1 8.11 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3951351 1 8.11
CHEMBL5182020 1 7.22
CHEMBL5172541 1 6.26
CHEMBL1939337 1 6.26
CHEMBL5173144 1 6.26
CHEMBL5206639 1 6.26
CHEMBL5207175 1 5.78
CHEMBL5193510 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3951351 Ki = 7.7 nM 8.11
CHEMBL5182020 IC50 = 60.0 nM 7.22
CHEMBL5172541 IC50 = 545.7 nM 6.26
CHEMBL1939337 IC50 = 545.7 nM 6.26
CHEMBL5173144 IC50 = 545.7 nM 6.26
CHEMBL5206639 IC50 = 545.7 nM 6.26
CHEMBL5207175 IC50 = 1670.0 nM 5.78
CHEMBL5193510 IC50 = 1800.0 nM 5.75