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Assay Detail

CHEMBL641042

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
13
Total Activities
13
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 13 6.56 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77699 1 7.43
CHEMBL77698 1 7.11
CHEMBL77691 1 6.96
CHEMBL76931 1 6.82
CHEMBL283937 1 6.80
CHEMBL312079 1 6.66
CHEMBL306633 1 6.47
CHEMBL27508 1 6.41
CHEMBL78317 1 6.25
CHEMBL431770 ISTRADEFYLLINE 4.0 1 6.24
CHEMBL306313 1 5.96
CHEMBL73827 1 5.60
CHEMBL306945 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77699 Ki = 37.0 nM 7.43
CHEMBL77698 Ki = 78.0 nM 7.11
CHEMBL77691 Ki = 110.0 nM 6.96
CHEMBL76931 Ki = 150.0 nM 6.82
CHEMBL283937 Ki = 160.0 nM 6.80
CHEMBL312079 Ki = 220.0 nM 6.66
CHEMBL306633 Ki = 340.0 nM 6.47
CHEMBL27508 Ki = 390.0 nM 6.41
CHEMBL78317 Ki = 560.0 nM 6.25
CHEMBL431770 ISTRADEFYLLINE Ki = 580.0 nM 6.24
CHEMBL306313 Ki = 1100.0 nM 5.96
CHEMBL73827 Ki = 2500.0 nM 5.60
CHEMBL306945 Ki > 100000.0 nM -