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Assay Detail

CHEMBL641721

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

Binding
Displacement of [3H]R-PIA from 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

Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.
Jacobson KA, Ji X, Li AH, Melman N, Siddiqui MA, Shin KJ, Marquez VE, Ravi RG.
J Med Chem (2000) 43 : 2196 -2203
PubMed 10841798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.26 8.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284969 1 8.88
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 8.82
CHEMBL27952 1 8.30
CHEMBL284216 1 8.06
CHEMBL477 ADENOSINE 4.0 1 8.00
CHEMBL307199 1 7.73
CHEMBL66393 1 7.70
CHEMBL417292 1 7.16
CHEMBL27809 1 6.85
CHEMBL287321 1 5.78
CHEMBL49935 ARISTEROMYCIN 1 5.20
CHEMBL71385 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284969 Ki = 1.33 nM 8.88
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 1.5 nM 8.82
CHEMBL27952 Ki = 5.06 nM 8.30
CHEMBL284216 Ki = 8.76 nM 8.06
CHEMBL477 ADENOSINE Ki = 10.0 nM 8.00
CHEMBL307199 Ki = 18.5 nM 7.73
CHEMBL66393 Ki = 20.0 nM 7.70
CHEMBL417292 Ki = 69.2 nM 7.16
CHEMBL27809 Ki = 141.0 nM 6.85
CHEMBL287321 Ki = 1680.0 nM 5.78
CHEMBL49935 ARISTEROMYCIN Ki = 6260.0 nM 5.20
CHEMBL71385 Ki = 25900.0 nM 4.59