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Assay Detail

CHEMBL828979

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

Binding
Displacement of [3H]CGS-21680 binding to adenosine A2A receptors of bovine striatal membranes
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.
Cappellacci L, Franchetti P, Pasqualini M, Petrelli R, Vita P, Lavecchia A, Novellino E, Costa B, Martini C, Klotz KN, Grifantini M.
J Med Chem (2005) 48 : 1550 -1562
PubMed 15743197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.07 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 7.80
CHEMBL119709 IB-MECA 1 7.40
CHEMBL66393 1 6.92
CHEMBL2113418 1 6.66
CHEMBL431733 NAMODENOSON 3.0 1 6.40
CHEMBL444550 2 6.33
CHEMBL194031 1 5.90
CHEMBL2113608 1 5.56
CHEMBL2113642 1 5.50
CHEMBL2113640 1 5.40
CHEMBL251997 1 5.34
CHEMBL606495 1 5.31
CHEMBL73809 1 5.24
CHEMBL400189 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA Ki = 16.0 nM 7.80
CHEMBL119709 IB-MECA Ki = 40.0 nM 7.40
CHEMBL66393 Ki = 121.0 nM 6.92
CHEMBL2113418 Ki = 220.0 nM 6.66
CHEMBL431733 NAMODENOSON Ki = 401.0 nM 6.40
CHEMBL444550 Ki = 470.0 nM 6.33
CHEMBL444550 Ki = 680.0 nM 6.17
CHEMBL194031 Ki = 1260.0 nM 5.90
CHEMBL2113608 Ki = 2780.0 nM 5.56
CHEMBL2113642 Ki = 3200.0 nM 5.50
CHEMBL2113640 Ki = 4000.0 nM 5.40
CHEMBL251997 Ki = 4560.0 nM 5.34
CHEMBL606495 Ki = 4890.0 nM 5.31
CHEMBL73809 Ki = 5800.0 nM 5.24
CHEMBL400189 Ki = 7560.0 nM 5.12