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Assay Detail

CHEMBL5129746

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Functional
Antagonist activity at human adenosine A2A receptor expressed in HEK293T cells assessed as inhibition of NECA-induced Gs short protein activation by TRUPATH assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.
Shepherd C, Robinson S, Berizzi A, Thompson LEJ, Bird L, Culurgioni S, Varzandeh S, Rawlins PB, Olsen RHJ, Navratilova IH.
ACS Med Chem Lett (2022) 13 : 1172 -1181
PubMed 35859869 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.80 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113142 ZM-241385 1 8.82
CHEMBL4550896 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113142 ZM-241385 IC50 = 1.514 nM 8.82
CHEMBL4550896 IC50 = 165.96 nM 6.78