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Assay Detail

CHEMBL5032902

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

Binding
Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells by liquid scintillation counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Adenosine A<sub>2A</sub>R/A<sub>1</sub>R Antagonists Enabling Additional H<sub>3</sub>R Antagonism for the Treatment of Parkinson's Disease.
Hagenow S, Affini A, Pioli EY, Hinz S, Zhao Y, Porras G, Namasivayam V, Müller CE, Lin JS, Bezard E, Stark H.
J Med Chem (2021) 64 : 8246 -8262
PubMed 34107215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.57 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5088622 1 6.82
CHEMBL5082650 1 6.82
CHEMBL5082920 1 6.70
CHEMBL5084903 1 6.64
CHEMBL1095488 1 6.37
CHEMBL5081556 1 6.07
CHEMBL5072724 1 -
CHEMBL5094263 1 -
CHEMBL5093935 1 -
CHEMBL5094415 1 -
CHEMBL5089580 1 -
CHEMBL5093850 1 -
CHEMBL5087059 1 -
CHEMBL240624 PRELADENANT 3.0 1 -
CHEMBL2297871 1 -
CHEMBL14638 CIPROXIFAN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5088622 Ki = 150.0 nM 6.82
CHEMBL5082650 Ki = 150.0 nM 6.82
CHEMBL5082920 Ki = 199.0 nM 6.70
CHEMBL5084903 Ki = 231.0 nM 6.64
CHEMBL1095488 Ki = 430.0 nM 6.37
CHEMBL5081556 Ki = 846.0 nM 6.07
CHEMBL5072724 Ki > 1000.0 nM -
CHEMBL5094263 Ki > 1000.0 nM -
CHEMBL5093935 Ki > 1000.0 nM -
CHEMBL5094415 Ki > 1000.0 nM -
CHEMBL5089580 Ki > 1000.0 nM -
CHEMBL5093850 Ki > 1000.0 nM -
CHEMBL5087059 Ki > 1000.0 nM -
CHEMBL240624 PRELADENANT Ki > 1000.0 nM -
CHEMBL2297871 Ki > 1000.0 nM -
CHEMBL14638 CIPROXIFAN Ki > 1000.0 nM -