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Assay Detail

CHEMBL927300

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

Binding
Displacement of [3H]CCPA from adenosine A1 receptor in pig cortical membrane
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

A1 adenosine receptor (CHEMBL1075029)
Type SINGLE PROTEIN
Organism Sus scrofa

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 32 6.59 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284969 1 9.52
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 9.28
CHEMBL251997 1 8.44
CHEMBL252198 1 8.18
CHEMBL392149 TECADENOSON 2.0 1 8.12
CHEMBL400189 1 8.00
CHEMBL399514 1 7.89
CHEMBL400782 1 7.17
CHEMBL254064 1 7.14
CHEMBL400190 1 6.82
CHEMBL254483 1 6.76
CHEMBL254896 1 6.56
CHEMBL254270 1 6.47
CHEMBL427718 1 6.43
CHEMBL254481 1 6.42
CHEMBL254271 1 6.42
CHEMBL400330 1 6.39
CHEMBL254065 1 6.29
CHEMBL254693 1 6.27
CHEMBL254482 1 6.12
CHEMBL399306 1 5.99
CHEMBL254897 1 5.84
CHEMBL398544 1 5.73
CHEMBL429667 1 5.73
CHEMBL254063 1 5.69
CHEMBL251799 1 5.69
CHEMBL251798 1 5.54
CHEMBL254691 1 5.50
CHEMBL400331 1 5.41
CHEMBL254898 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284969 Ki = 0.3 nM 9.52
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 0.53 nM 9.28
CHEMBL251997 Ki = 3.6 nM 8.44
CHEMBL252198 Ki = 6.6 nM 8.18
CHEMBL392149 TECADENOSON Ki = 7.6 nM 8.12
CHEMBL400189 Ki = 10.0 nM 8.00
CHEMBL399514 Ki = 13.0 nM 7.89
CHEMBL400782 Ki = 67.0 nM 7.17
CHEMBL254064 Ki = 72.0 nM 7.14
CHEMBL400190 Ki = 150.0 nM 6.82
CHEMBL254483 Ki = 173.0 nM 6.76
CHEMBL254896 Ki = 276.0 nM 6.56
CHEMBL254270 Ki = 337.0 nM 6.47
CHEMBL427718 Ki = 370.0 nM 6.43
CHEMBL254271 Ki = 380.0 nM 6.42
CHEMBL254481 Ki = 380.0 nM 6.42
CHEMBL400330 Ki = 410.0 nM 6.39
CHEMBL254065 Ki = 513.0 nM 6.29
CHEMBL254693 Ki = 534.0 nM 6.27
CHEMBL254482 Ki = 760.0 nM 6.12
CHEMBL399306 Ki = 1026.0 nM 5.99
CHEMBL254897 Ki = 1450.0 nM 5.84
CHEMBL398544 Ki = 1848.0 nM 5.73
CHEMBL429667 Ki = 1850.0 nM 5.73
CHEMBL254063 Ki = 2052.0 nM 5.69
CHEMBL251799 Ki = 2053.0 nM 5.69
CHEMBL251798 Ki = 2870.0 nM 5.54
CHEMBL254691 Ki = 3200.0 nM 5.50
CHEMBL400331 Ki = 3879.0 nM 5.41
CHEMBL254898 Ki = 4100.0 nM 5.39
CHEMBL398543 Ki = 9800.0 nM 5.01
CHEMBL254692 Ki = 16200.0 nM 4.79