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Assay Detail

CHEMBL873042

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

Binding
Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes.
16
Total Activities
16
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

2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.
Franchetti P, Cappellacci L, Marchetti S, Trincavelli L, Martini C, Mazzoni MR, Lucacchini A, Grifantini M.
J Med Chem (1998) 41 : 1708 -1715
PubMed 9572897 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.40 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL251997 1 8.41
CHEMBL464859 NECA 1 7.80
CHEMBL66393 1 7.69
CHEMBL119709 IB-MECA 1 6.94
CHEMBL285819 1 6.92
CHEMBL2113418 1 6.66
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.42
CHEMBL284969 1 6.24
CHEMBL139000 (R)-PIA 1 6.12
CHEMBL444550 1 6.03
CHEMBL606495 1 5.88
CHEMBL605034 1 5.81
CHEMBL420705 (S)-PIA 1 5.75
CHEMBL73809 1 5.47
CHEMBL400189 1 5.14
CHEMBL2113388 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL251997 Ki = 3.9 nM 8.41
CHEMBL464859 NECA Ki = 16.0 nM 7.80
CHEMBL66393 Ki = 20.4 nM 7.69
CHEMBL119709 IB-MECA Ki = 116.0 nM 6.94
CHEMBL285819 Ki = 120.0 nM 6.92
CHEMBL2113418 Ki = 218.0 nM 6.66
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 385.0 nM 6.42
CHEMBL284969 Ki = 580.0 nM 6.24
CHEMBL139000 (R)-PIA Ki = 750.0 nM 6.12
CHEMBL444550 Ki = 935.0 nM 6.03
CHEMBL606495 Ki = 1330.0 nM 5.88
CHEMBL605034 Ki = 1533.0 nM 5.81
CHEMBL420705 (S)-PIA Ki = 1800.0 nM 5.75
CHEMBL73809 Ki = 3420.0 nM 5.47
CHEMBL400189 Ki = 7220.0 nM 5.14
CHEMBL2113388 Ki = 7440.0 nM 5.13