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Assay Detail

CHEMBL640428

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Binding
Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A3 adenosine receptors.
Kim HO, Ji XD, Siddiqi SM, Olah ME, Stiles GL, Jacobson KA.
J Med Chem (1994) 37 : 3614 -3621
PubMed 7932588 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.83 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1950647 1 8.24
CHEMBL331372 CGS-21680 1 7.82
CHEMBL66393 1 7.76
CHEMBL307199 1 7.42
CHEMBL119709 IB-MECA 1 7.25
CHEMBL285819 1 7.20
CHEMBL2113561 1 6.93
CHEMBL1256714 1 6.76
CHEMBL133566 1 6.71
CHEMBL431733 NAMODENOSON 3.0 1 6.33
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.33
CHEMBL284969 1 6.02
CHEMBL2113557 1 5.49
CHEMBL2113562 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1950647 Ki = 5.7 nM 8.24
CHEMBL331372 CGS-21680 Ki = 15.0 nM 7.82
CHEMBL66393 Ki = 17.5 nM 7.76
CHEMBL307199 Ki = 38.5 nM 7.42
CHEMBL119709 IB-MECA Ki = 56.0 nM 7.25
CHEMBL285819 Ki = 63.0 nM 7.20
CHEMBL2113561 Ki = 117.0 nM 6.93
CHEMBL1256714 Ki = 172.0 nM 6.76
CHEMBL133566 Ki = 197.0 nM 6.71
CHEMBL431733 NAMODENOSON Ki = 470.0 nM 6.33
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 462.0 nM 6.33
CHEMBL284969 Ki = 950.0 nM 6.02
CHEMBL2113557 Ki = 3210.0 nM 5.49
CHEMBL2113562 Ki = 4120.0 nM 5.38