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Assay Detail

CHEMBL5129724

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Binding
Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as inhibition constant by surface plasmon resonance assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Expi293F
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
Ki 6 7.78 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113142 ZM-241385 1 9.40
CHEMBL1256672 1 7.12
CHEMBL477 ADENOSINE 4.0 1 6.82
CHEMBL1355736 THEOPHYLLINE 4.0 1 -
CHEMBL1467 ALLOPURINOL 4.0 1 -
CHEMBL113 CAFFEINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113142 ZM-241385 Ki = 0.395 nM 9.40
CHEMBL1256672 Ki = 76.0 nM 7.12
CHEMBL477 ADENOSINE Ki = 150.0 nM 6.82
CHEMBL1355736 THEOPHYLLINE Ki - -
CHEMBL1467 ALLOPURINOL Ki - -
CHEMBL113 CAFFEINE Ki - -