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Assay Detail

CHEMBL640780

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Binding
Affinity for adenosine A1 receptor at rat cortical receptors using 1 nM [3H]PIA
6
Total Activities
6
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 6 7.52 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL262083 N6-PHENYLADENOSINE 1 8.46
CHEMBL2113406 1 8.12
CHEMBL2113484 1 7.92
CHEMBL604406 1 7.31
CHEMBL2364548 1 7.13
CHEMBL2113577 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL262083 N6-PHENYLADENOSINE Ki = 3.5 nM 8.46
CHEMBL2113406 Ki = 7.5 nM 8.12
CHEMBL2113484 Ki = 12.0 nM 7.92
CHEMBL604406 Ki = 49.0 nM 7.31
CHEMBL2364548 Ki = 74.0 nM 7.13
CHEMBL2113577 Ki = 712.0 nM 6.15