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Assay Detail

CHEMBL1074285

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

Binding
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2b (CHEMBL255)
Type SINGLE PROTEIN
Organism Homo sapiens

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 5.78 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL590302 1 6.47
CHEMBL603129 1 6.41
CHEMBL113 CAFFEINE 4.0 1 4.47
CHEMBL591710 1 -
CHEMBL592681 1 -
CHEMBL608671 1 -
CHEMBL592680 1 -
CHEMBL592679 1 -
CHEMBL590033 1 -
CHEMBL600232 1 -
CHEMBL602717 1 -
CHEMBL590034 1 -
CHEMBL602950 1 -
CHEMBL602722 1 -
CHEMBL590301 1 -
CHEMBL591730 1 -
CHEMBL590024 1 -
CHEMBL602519 1 -
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 -
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 -
CHEMBL602539 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL590302 Ki = 337.0 nM 6.47
CHEMBL603129 Ki = 391.0 nM 6.41
CHEMBL113 CAFFEINE Ki = 33800.0 nM 4.47
CHEMBL591710 Ki > 1000.0 nM -
CHEMBL592681 Ki > 1000.0 nM -
CHEMBL608671 Ki > 1000.0 nM -
CHEMBL592680 Ki > 1000.0 nM -
CHEMBL592679 Ki > 1000.0 nM -
CHEMBL590033 Ki > 1000.0 nM -
CHEMBL600232 Ki > 1000.0 nM -
CHEMBL602717 Ki > 1000.0 nM -
CHEMBL590034 Ki > 1000.0 nM -
CHEMBL602950 Ki > 1000.0 nM -
CHEMBL602722 Ki > 1000.0 nM -
CHEMBL590301 Ki > 1000.0 nM -
CHEMBL591730 Ki > 1000.0 nM -
CHEMBL590024 Ki > 1000.0 nM -
CHEMBL602519 Ki > 1000.0 nM -
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki - -
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki - -
CHEMBL602539 Ki > 1000.0 nM -