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Assay Detail

CHEMBL640781

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Binding
Inhibition of [3H]PIA binding to rat cortical 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

Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective adenosine agonists.
Jacobson KA, Nikodijevic O, Ji XD, Berkich DA, Eveleth D, Dean RL, Hiramatsu K, Kassell NF, van Galen PJ, Lee KS.
J Med Chem (1992) 35 : 4143 -4149
PubMed 1433217 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.68 9.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 9.23
CHEMBL1512545 1 9.07
CHEMBL2092973 1 8.92
CHEMBL45891 1 8.89
CHEMBL285819 1 8.03
CHEMBL610099 1 8.03
CHEMBL464859 NECA 1 7.99
CHEMBL610435 1 7.39
CHEMBL2364548 1 7.13
CHEMBL2113576 1 6.21
CHEMBL1788287 1 5.74
CHEMBL331372 CGS-21680 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 0.59 nM 9.23
CHEMBL1512545 Ki = 0.85 nM 9.07
CHEMBL2092973 Ki = 1.2 nM 8.92
CHEMBL45891 Ki = 1.3 nM 8.89
CHEMBL285819 Ki = 9.3 nM 8.03
CHEMBL610099 Ki = 9.3 nM 8.03
CHEMBL464859 NECA Ki = 10.3 nM 7.99
CHEMBL610435 Ki = 41.0 nM 7.39
CHEMBL2364548 Ki = 74.0 nM 7.13
CHEMBL2113576 Ki = 610.0 nM 6.21
CHEMBL1788287 Ki = 1820.0 nM 5.74
CHEMBL331372 CGS-21680 Ki = 2600.0 nM 5.58