Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL927301

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

Binding
Displacement of [3H]CGS21680 from adenosine A1 receptor in bovine striatum membrane
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Striatum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A1 (CHEMBL4975)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.
Cappellacci L, Franchetti P, Vita P, Petrelli R, Lavecchia A, Costa B, Spinetti F, Martini C, Klotz KN, Grifantini M.
Bioorg Med Chem (2008) 16 : 336 -353
PubMed 17933541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.20 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284969 1 6.14
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 5.91
CHEMBL251997 1 5.34
CHEMBL252198 1 5.33
CHEMBL392149 TECADENOSON 2.0 1 5.14
CHEMBL400189 1 5.14
CHEMBL254271 1 5.10
CHEMBL254481 1 5.09
CHEMBL254897 1 5.00
CHEMBL399306 1 4.96
CHEMBL427718 1 4.89
CHEMBL399514 1 4.82
CHEMBL400330 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284969 Ki = 730.0 nM 6.14
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 1220.0 nM 5.91
CHEMBL251997 Ki = 4560.0 nM 5.34
CHEMBL252198 Ki = 4689.0 nM 5.33
CHEMBL392149 TECADENOSON Ki = 7300.0 nM 5.14
CHEMBL400189 Ki = 7230.0 nM 5.14
CHEMBL254271 Ki = 7900.0 nM 5.10
CHEMBL254481 Ki = 8092.0 nM 5.09
CHEMBL254897 Ki = 10000.0 nM 5.00
CHEMBL399306 Ki = 11000.0 nM 4.96
CHEMBL427718 Ki = 12750.0 nM 4.89
CHEMBL399514 Ki = 15000.0 nM 4.82
CHEMBL400330 Ki = 19300.0 nM 4.71