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Assay Detail

CHEMBL4682730

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

Binding
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Substituted 4-phenylthiazoles: Development of potent and selective A, A and dual A/A adenosine receptor antagonists.
Abdelrahman A,Yerande SG,Namasivayam V,Klapschinski TA,Alnouri MW,El-Tayeb A,Müller CE
Eur J Med Chem (2020) 186 : 111879 -111879
PubMed 31780082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 5.85 8.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2391834 1 8.56
CHEMBL1316674 1 6.73
CHEMBL52333 ROLOFYLLINE 3.0 1 6.53
CHEMBL589080 1 5.50
CHEMBL1625681 1 5.43
CHEMBL1355736 THEOPHYLLINE 4.0 1 5.04
CHEMBL1562432 1 4.52
CHEMBL113 CAFFEINE 4.0 1 4.47
CHEMBL4780555 1 -
CHEMBL111545 1 -
CHEMBL4757397 1 -
CHEMBL4763881 1 -
CHEMBL4746936 1 -
CHEMBL4796077 1 -
CHEMBL4797325 1 -
CHEMBL4745527 1 -
CHEMBL4758461 1 -
CHEMBL4752438 1 -
CHEMBL4747947 1 -
CHEMBL4797181 1 -
CHEMBL4790122 1 -
CHEMBL4795542 1 -
CHEMBL4755914 1 -
CHEMBL1242892 1 -
CHEMBL1242426 1 -
CHEMBL4787673 1 -
CHEMBL1242247 1 -
CHEMBL4764086 1 -
CHEMBL4784975 1 -
CHEMBL4779033 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2391834 Ki = 2.78 nM 8.56
CHEMBL1316674 Ki = 187.0 nM 6.73
CHEMBL52333 ROLOFYLLINE Ki = 296.0 nM 6.53
CHEMBL589080 Ki = 3200.0 nM 5.50
CHEMBL1625681 Ki = 3700.0 nM 5.43
CHEMBL1355736 THEOPHYLLINE Ki = 9070.0 nM 5.04
CHEMBL1562432 Ki = 30000.0 nM 4.52
CHEMBL113 CAFFEINE Ki = 33800.0 nM 4.47
CHEMBL4757397 Ki > 100.0 nM -
CHEMBL592679 Ki > 1000.0 nM -
CHEMBL4763881 Ki > 100.0 nM -
CHEMBL4746936 Ki > 100.0 nM -
CHEMBL4796077 Ki > 100.0 nM -
CHEMBL4797325 Ki > 100.0 nM -
CHEMBL4745527 Ki > 100.0 nM -
CHEMBL4758461 Ki > 100.0 nM -
CHEMBL4752438 Ki > 100.0 nM -
CHEMBL4747947 Ki > 100.0 nM -
CHEMBL111545 Ki > 10000.0 nM -
CHEMBL4780555 Ki > 100.0 nM -
CHEMBL4797181 Ki > 100.0 nM -
CHEMBL4790122 Ki > 100.0 nM -
CHEMBL4795542 Ki > 100.0 nM -
CHEMBL4755914 Ki > 100.0 nM -
CHEMBL1242892 Ki > 100.0 nM -
CHEMBL1242426 Ki > 100.0 nM -
CHEMBL4787673 Ki > 100.0 nM -
CHEMBL1242247 Ki > 100.0 nM -
CHEMBL4764086 Ki > 100.0 nM -
CHEMBL4784975 Ki > 100.0 nM -
CHEMBL4779033 Ki > 100.0 nM -