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Assay Detail

CHEMBL2330946

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

Binding
Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO cells after 120 mins by scintillation counting analysis
4
Total Activities
4
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 A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Arylpyrazolo[4,3-d]pyrimidin-7-amino derivatives as new potent and selective human A3 adenosine receptor antagonists. Molecular modeling studies and pharmacological evaluation.
Squarcialupi L, Colotta V, Catarzi D, Varano F, Filacchioni G, Varani K, Corciulo C, Vincenzi F, Borea PA, Ghelardini C, Di Cesare Mannelli L, Ciancetta A, Moro S.
J Med Chem (2013) 56 : 2256 -2269
PubMed 23427825 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.85 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2322916 1 7.16
CHEMBL2322917 1 7.12
CHEMBL2322918 1 6.82
CHEMBL2322925 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2322916 Ki = 70.0 nM 7.16
CHEMBL2322917 Ki = 75.0 nM 7.12
CHEMBL2322918 Ki = 150.0 nM 6.82
CHEMBL2322925 Ki = 510.0 nM 6.29