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Assay Detail

CHEMBL641348

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

Binding
Displacement of [3H]-CGS- 51680 from Adenosine A2A receptor of rat striatum.
14
Total Activities
14
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 A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2-alkenyl and 2-alkyl derivatives of adenosine and adenosine-5'-N-ethyluronamide: different affinity and selectivity of E- and Z-diastereomers at A2A adenosine receptors.
Vittori S, Camaioni E, Di Francesco E, Volpini R, Monopoli A, Dionisotti S, Ongini E, Cristalli G.
J Med Chem (1996) 39 : 4211 -4217
PubMed 8863798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.73 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113450 1 8.92
CHEMBL2113528 1 8.80
CHEMBL319387 1 8.66
CHEMBL410873 1 8.66
CHEMBL2304158 1 8.46
CHEMBL464859 NECA 1 8.11
CHEMBL98603 1 7.85
CHEMBL2113525 1 7.29
CHEMBL611256 1 7.16
CHEMBL223270 1 6.92
CHEMBL2113529 1 6.87
CHEMBL2113526 1 6.63
CHEMBL2113527 1 6.12
CHEMBL608918 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113450 Ki = 1.2 nM 8.92
CHEMBL2113528 Ki = 1.6 nM 8.80
CHEMBL319387 Ki = 2.2 nM 8.66
CHEMBL410873 Ki = 2.2 nM 8.66
CHEMBL2304158 Ki = 3.5 nM 8.46
CHEMBL464859 NECA Ki = 7.8 nM 8.11
CHEMBL98603 Ki = 14.0 nM 7.85
CHEMBL2113525 Ki = 51.0 nM 7.29
CHEMBL611256 Ki = 70.0 nM 7.16
CHEMBL223270 Ki = 120.0 nM 6.92
CHEMBL2113529 Ki = 136.0 nM 6.87
CHEMBL2113526 Ki = 234.0 nM 6.63
CHEMBL2113527 Ki = 757.0 nM 6.12
CHEMBL608918 Ki > 1.0 nM -