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Assay Detail

CHEMBL5164005

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

Binding
Displacement of [3H]DPCPX from human A1AR incubated for 60 mins by scintillation counter analysis
3
Total Activities
3
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 A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual-acting antitumor agents targeting the A<sub>2A</sub> adenosine receptor and histone deacetylases: Design and synthesis of 4-(furan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine derivatives.
Zhang J, Luo Z, Duan W, Yang K, Ling L, Yan W, Liu R, Wüthrich K, Jiang H, Xie C, Cheng J.
Eur J Med Chem (2022) 236 : 114326 -114326
PubMed 35390714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.49 6.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5201523 1 6.98
CHEMBL5199428 1 6.30
CHEMBL5188801 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5201523 Ki = 105.6 nM 6.98
CHEMBL5199428 Ki = 503.3 nM 6.30
CHEMBL5188801 Ki = 641.0 nM 6.19