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Assay Detail

CHEMBL4700997

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Antagonist activity at human adenosine 2A receptor
4
Total Activities
4
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

Adenosine A Receptor Antagonists for Cancer Immunotherapy.
Yu F,Zhu C,Xie Q,Wang Y
J Med Chem (2020) 63 : 12196 -12212
PubMed 32667814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.53 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113142 ZM-241385 1 9.10
CHEMBL17127 SCH-58261 1 8.96
CHEMBL431770 ISTRADEFYLLINE 4.0 1 7.44
CHEMBL113 CAFFEINE 4.0 1 4.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113142 ZM-241385 Ki = 0.8 nM 9.10
CHEMBL17127 SCH-58261 Ki = 1.1 nM 8.96
CHEMBL431770 ISTRADEFYLLINE Ki = 36.0 nM 7.44
CHEMBL113 CAFFEINE Ki = 23400.0 nM 4.63