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Assay Detail

CHEMBL647730

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

Binding
Displacement of [3H]-CGS- 21680 from Adenosine A2a receptor of rat forebrain membranes (shielded from light)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Adenosine A2A antagonists with potent anti-cataleptic activity
Shimada J, Koike N, Nonaka H, Shiozaki S, Yanagawa K, Kanda T, Kobayashi H, Ichimura M, Nakamura J, Kase H, Suzuki F
Bioorg Med Chem Lett (1997) 7 : 2349 -2352
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.62 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77691 1 9.17
CHEMBL77698 1 9.17
CHEMBL27508 1 9.00
CHEMBL306313 1 8.77
CHEMBL77699 1 8.66
CHEMBL431770 ISTRADEFYLLINE 4.0 1 8.66
CHEMBL422399 1 8.62
CHEMBL306633 1 8.35
CHEMBL312079 1 8.31
CHEMBL75093 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77691 Ki = 0.67 nM 9.17
CHEMBL77698 Ki = 0.67 nM 9.17
CHEMBL27508 Ki = 1.0 nM 9.00
CHEMBL306313 Ki = 1.7 nM 8.77
CHEMBL77699 Ki = 2.2 nM 8.66
CHEMBL431770 ISTRADEFYLLINE Ki = 2.2 nM 8.66
CHEMBL422399 Ki = 2.4 nM 8.62
CHEMBL306633 Ki = 4.5 nM 8.35
CHEMBL312079 Ki = 4.9 nM 8.31
CHEMBL75093 Ki = 35.0 nM 7.46