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Assay Detail

CHEMBL641310

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

Binding
Ability to displace radioligand [3H]- CGS 21680 from adenosine A2A receptor on rat striatal membrane
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.
de Zwart M, Kourounakis A, Kooijman H, Spek AL, Link R, von Frijtag Drabbe Künzel JK, IJzerman AP.
J Med Chem (1999) 42 : 1384 -1392
PubMed 10212124 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.83 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261482 1 7.92
CHEMBL331372 CGS-21680 1 7.82
CHEMBL464859 NECA 1 7.80
CHEMBL2070507 1 7.31
CHEMBL119709 IB-MECA 1 7.25
CHEMBL2113421 1 6.89
CHEMBL2113431 1 6.89
CHEMBL606095 1 6.80
CHEMBL519809 1 6.48
CHEMBL2113435 1 6.39
CHEMBL2070399 1 6.39
CHEMBL1235128 1 6.26
CHEMBL2070508 1 6.21
CHEMBL2113434 1 6.21
CHEMBL2113436 1 5.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261482 Ki = 12.0 nM 7.92
CHEMBL331372 CGS-21680 Ki = 15.0 nM 7.82
CHEMBL464859 NECA Ki = 16.0 nM 7.80
CHEMBL2070507 Ki = 49.0 nM 7.31
CHEMBL119709 IB-MECA Ki = 56.0 nM 7.25
CHEMBL2113421 Ki = 130.0 nM 6.89
CHEMBL2113431 Ki = 130.0 nM 6.89
CHEMBL606095 Ki = 160.0 nM 6.80
CHEMBL519809 Ki = 330.0 nM 6.48
CHEMBL2113435 Ki = 405.0 nM 6.39
CHEMBL2070399 Ki = 410.0 nM 6.39
CHEMBL1235128 Ki = 550.0 nM 6.26
CHEMBL2070508 Ki = 610.0 nM 6.21
CHEMBL2113434 Ki = 623.0 nM 6.21
CHEMBL2113436 Ki = 1340.0 nM 5.87