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Assay Detail

CHEMBL1014568

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

Binding
Displacement of [3H]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells
34
Total Activities
34
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

Structure-activity relationship studies of a new series of imidazo[2,1-f]purinones as potent and selective A(3) adenosine receptor antagonists.
Baraldi PG, Preti D, Tabrizi MA, Romagnoli R, Saponaro G, Baraldi S, Botta M, Bernardini C, Tafi A, Tuccinardi T, Martinelli A, Varani K, Borea PA.
Bioorg Med Chem (2008) 16 : 10281 -10294
PubMed 19006671 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 6.39 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL364036 1 6.46
CHEMBL526122 1 6.43
CHEMBL188269 1 6.34
CHEMBL520767 1 6.32
CHEMBL465090 1 -
CHEMBL464075 1 -
CHEMBL373090 1 -
CHEMBL434534 1 -
CHEMBL191414 1 -
CHEMBL191421 1 -
CHEMBL372026 1 -
CHEMBL481383 1 -
CHEMBL464438 1 -
CHEMBL518703 1 -
CHEMBL464437 1 -
CHEMBL465290 1 -
CHEMBL506908 1 -
CHEMBL465089 1 -
CHEMBL454444 1 -
CHEMBL480529 1 -
CHEMBL480599 1 -
CHEMBL193130 1 -
CHEMBL188506 1 -
CHEMBL189904 1 -
CHEMBL193100 1 -
CHEMBL426271 1 -
CHEMBL190472 1 -
CHEMBL189922 1 -
CHEMBL435887 1 -
CHEMBL371404 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL364036 Ki = 350.0 nM 6.46
CHEMBL526122 Ki = 373.0 nM 6.43
CHEMBL188269 Ki = 460.0 nM 6.34
CHEMBL520767 Ki = 476.0 nM 6.32
CHEMBL434534 Ki > 1000.0 nM -
CHEMBL465949 Ki > 1000.0 nM -
CHEMBL191414 Ki > 1000.0 nM -
CHEMBL191421 Ki > 1000.0 nM -
CHEMBL372026 Ki > 1000.0 nM -
CHEMBL481383 Ki > 1000.0 nM -
CHEMBL464438 Ki > 1000.0 nM -
CHEMBL518703 Ki > 1000.0 nM -
CHEMBL464437 Ki > 1000.0 nM -
CHEMBL465290 Ki > 1000.0 nM -
CHEMBL506908 Ki > 1000.0 nM -
CHEMBL464075 Ki > 1000.0 nM -
CHEMBL465281 Ki > 1000.0 nM -
CHEMBL464076 Ki > 1000.0 nM -
CHEMBL518729 Ki > 1000.0 nM -
CHEMBL373090 Ki > 1000.0 nM -
CHEMBL465090 Ki > 1000.0 nM -
CHEMBL465089 Ki > 1000.0 nM -
CHEMBL454444 Ki > 1000.0 nM -
CHEMBL480529 Ki > 1000.0 nM -
CHEMBL480599 Ki > 1000.0 nM -
CHEMBL193130 Ki > 1000.0 nM -
CHEMBL188506 Ki > 1000.0 nM -
CHEMBL189904 Ki > 1000.0 nM -
CHEMBL193100 Ki > 1000.0 nM -
CHEMBL426271 Ki > 1000.0 nM -
CHEMBL190472 Ki > 1000.0 nM -
CHEMBL189922 Ki > 1000.0 nM -
CHEMBL435887 Ki > 1000.0 nM -
CHEMBL371404 Ki > 1000.0 nM -