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Assay Detail

CHEMBL1074282

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

Binding
Displacement of [3H]MSX2 from adenosine A2A receptor in rat brain striatum membrane
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
Scheiff AB, Yerande SG, El-Tayeb A, Li W, Inamdar GS, Vasu KK, Sudarsanam V, Müller CE.
Bioorg Med Chem (2010) 18 : 2195 -2203
PubMed 20188574 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.73 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.80
CHEMBL591710 1 6.18
CHEMBL603129 1 5.79
CHEMBL590301 1 5.74
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 5.61
CHEMBL600232 1 5.52
CHEMBL113 CAFFEINE 4.0 1 4.49
CHEMBL602950 1 -
CHEMBL592681 1 -
CHEMBL602519 1 -
CHEMBL590024 1 -
CHEMBL591730 1 -
CHEMBL608671 1 -
CHEMBL592680 1 -
CHEMBL602722 1 -
CHEMBL590302 1 -
CHEMBL602539 1 -
CHEMBL590034 1 -
CHEMBL602717 1 -
CHEMBL590033 1 -
CHEMBL592679 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 157.0 nM 6.80
CHEMBL591710 Ki = 662.0 nM 6.18
CHEMBL603129 Ki = 1640.0 nM 5.79
CHEMBL590301 Ki = 1840.0 nM 5.74
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 2470.0 nM 5.61
CHEMBL600232 Ki = 3030.0 nM 5.52
CHEMBL113 CAFFEINE Ki = 32500.0 nM 4.49
CHEMBL602950 Ki > 1000.0 nM -
CHEMBL592681 Ki > 1000.0 nM -
CHEMBL602519 Ki > 1000.0 nM -
CHEMBL590024 Ki > 1000.0 nM -
CHEMBL591730 Ki > 1000.0 nM -
CHEMBL608671 Ki > 1000.0 nM -
CHEMBL592680 Ki > 1000.0 nM -
CHEMBL602722 Ki > 1000.0 nM -
CHEMBL590302 Ki > 1000.0 nM -
CHEMBL602539 Ki > 1000.0 nM -
CHEMBL590034 Ki > 1000.0 nM -
CHEMBL602717 Ki > 1000.0 nM -
CHEMBL590033 Ki > 1000.0 nM -
CHEMBL592679 Ki > 1000.0 nM -