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Assay Detail

CHEMBL640785

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

Binding
Inhibition of [3H]CHA (N6-cyclohexyl adenosine) to rat brain membrane Adenosine A1 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Ribose-modified nucleosides as ligands for adenosine receptors: synthesis, conformational analysis, and biological evaluation of 1'-C-methyl adenosine analogues.
Cappellacci L, Barboni G, Palmieri M, Pasqualini M, Grifantini M, Costa B, Martini C, Franchetti P.
J Med Chem (2002) 45 : 1196 -1202
PubMed 11881988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.26 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 9.52
CHEMBL139000 (R)-PIA 1 9.22
CHEMBL2113388 1 8.33
CHEMBL400189 1 8.02
CHEMBL420705 (S)-PIA 1 7.96
CHEMBL3143982 1 7.64
CHEMBL603977 1 7.30
CHEMBL3143985 1 7.00
CHEMBL3143983 1 6.57
CHEMBL73809 1 6.13
CHEMBL3143984 1 5.11
CHEMBL480143 1 4.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 0.3 nM 9.52
CHEMBL139000 (R)-PIA Ki = 0.6 nM 9.22
CHEMBL2113388 Ki = 4.7 nM 8.33
CHEMBL400189 Ki = 9.5 nM 8.02
CHEMBL420705 (S)-PIA Ki = 11.0 nM 7.96
CHEMBL3143982 Ki = 23.0 nM 7.64
CHEMBL603977 Ki = 50.0 nM 7.30
CHEMBL3143985 Ki = 100.0 nM 7.00
CHEMBL3143983 Ki = 270.0 nM 6.57
CHEMBL73809 Ki = 740.0 nM 6.13
CHEMBL3143984 Ki = 7700.0 nM 5.11
CHEMBL480143 Ki = 51000.0 nM 4.29