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Assay Detail

CHEMBL2014405

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

Binding
Displacement of [3H]R-PIA from rat forebrain adenosine receptor-1
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.
Tosh DK, Phan K, Deflorian F, Wei Q, Gao ZG, Jacobson KA.
ACS Med Chem Lett (2011) 2 : 626 -631
PubMed 21858244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 9.00 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2012678 1 9.47
CHEMBL2012674 1 9.15
CHEMBL2012679 1 9.15
CHEMBL2012684 1 9.10
CHEMBL2012686 1 9.10
CHEMBL2012675 1 9.05
CHEMBL2012682 1 8.72
CHEMBL2012687 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2012678 Ki = 0.34 nM 9.47
CHEMBL2012674 Ki = 0.7 nM 9.15
CHEMBL2012679 Ki = 0.7 nM 9.15
CHEMBL2012684 Ki = 0.8 nM 9.10
CHEMBL2012686 Ki = 0.8 nM 9.10
CHEMBL2012675 Ki = 0.9 nM 9.05
CHEMBL2012682 Ki = 1.9 nM 8.72
CHEMBL2012687 Ki = 6.0 nM 8.22