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Assay Detail

CHEMBL1959513

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Binding
Binding affinity to human adenosine A1 receptor
5
Total Activities
5
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

Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A₂B adenosine receptor antagonists.
Baraldi PG, Baraldi S, Saponaro G, Preti D, Romagnoli R, Piccagli L, Cavalli A, Recanatini M, Moorman AR, Zaid AN, Varani K, Borea PA, Tabrizi MA.
J Med Chem (2012) 55 : 797 -811
PubMed 22148859 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.84 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485862 1 7.43
CHEMBL260331 1 6.70
CHEMBL273807 1 6.39
CHEMBL260933 GS 6201 1.0 1 -
CHEMBL180693 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485862 Ki = 37.0 nM 7.43
CHEMBL260331 Ki = 200.0 nM 6.70
CHEMBL273807 Ki = 403.0 nM 6.39
CHEMBL260933 GS 6201 Ki > 10000.0 nM -
CHEMBL180693 Ki > 10000.0 nM -