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Assay Detail

CHEMBL4828923

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

Binding
Displacement [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane incubated for 60 mins by microplate beta scintillation counting based radioligand inhibition assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of adenosine derivatives as A<sub>1</sub>, A<sub>2A</sub>, A<sub>2B</sub> and A<sub>3</sub> adenosine receptor ligands containing boron clusters as phenyl isosteres and selective A<sub>3</sub> agonists.
Bednarska-Szczepaniak K, Mieczkowski A, Kierozalska A, Pavlović Saftić D, Głąbała K, Przygodzki T, Stańczyk L, Karolczak K, Watała C, Rao H, Gao ZG, Jacobson KA, Leśnikowski ZJ.
Eur J Med Chem (2021) 223 : 113607 -113607
PubMed 34171656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.93 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113484 1 7.10
CHEMBL375190 1 6.19
CHEMBL4861092 1 6.09
CHEMBL2113406 1 6.06
CHEMBL4852007 1 5.71
CHEMBL4864883 1 5.48
CHEMBL4873585 1 4.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113484 Ki = 78.8 nM 7.10
CHEMBL375190 Ki = 646.0 nM 6.19
CHEMBL4861092 Ki = 803.0 nM 6.09
CHEMBL2113406 Ki = 864.0 nM 6.06
CHEMBL4852007 Ki = 1940.0 nM 5.71
CHEMBL4864883 Ki = 3340.0 nM 5.48
CHEMBL4873585 Ki = 13300.0 nM 4.88