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Assay Detail

CHEMBL645016

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

Binding
Displacement of [3H]CHA from Adenosine A1 receptor of rat forebrain membranes (shielded from light)
9
Total Activities
9
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 A1 (CHEMBL318)
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 9 6.97 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27508 1 7.21
CHEMBL77699 1 7.21
CHEMBL306633 1 7.20
CHEMBL77691 1 7.08
CHEMBL312079 1 7.00
CHEMBL77698 1 6.92
CHEMBL306313 1 6.92
CHEMBL431770 ISTRADEFYLLINE 4.0 1 6.82
CHEMBL75093 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27508 Ki = 62.0 nM 7.21
CHEMBL77699 Ki = 61.0 nM 7.21
CHEMBL306633 Ki = 63.0 nM 7.20
CHEMBL77691 Ki = 83.0 nM 7.08
CHEMBL312079 Ki = 100.0 nM 7.00
CHEMBL77698 Ki = 120.0 nM 6.92
CHEMBL306313 Ki = 120.0 nM 6.92
CHEMBL431770 ISTRADEFYLLINE Ki = 150.0 nM 6.82
CHEMBL75093 Ki = 470.0 nM 6.33