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Assay Detail

CHEMBL948833

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

Binding
Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells
30
Total Activities
30
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 A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Borrmann T, Hinz S, Bertarelli DC, Li W, Florin NC, Scheiff AB, Müller CE.
J Med Chem (2009) 52 : 3994 -4006
PubMed 19569717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 5.81 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL486281 1 6.85
CHEMBL518972 1 6.81
CHEMBL488542 1 6.68
CHEMBL483487 1 6.36
CHEMBL482638 1 6.25
CHEMBL520830 1 6.12
CHEMBL486282 1 5.68
CHEMBL484899 1 5.24
CHEMBL486893 1 4.75
CHEMBL483469 1 4.62
CHEMBL486688 1 4.52
CHEMBL484900 1 -
CHEMBL486478 1 -
CHEMBL486479 1 -
CHEMBL519390 1 -
CHEMBL520617 1 -
CHEMBL482648 1 -
CHEMBL482855 1 -
CHEMBL483065 1 -
CHEMBL482436 1 -
CHEMBL483688 1 -
CHEMBL519253 1 -
CHEMBL520899 1 -
CHEMBL486481 1 -
CHEMBL519556 1 -
CHEMBL488541 1 -
CHEMBL483261 1 -
CHEMBL519813 1 -
CHEMBL520297 1 -
CHEMBL212625 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL486281 Ki = 140.0 nM 6.85
CHEMBL518972 Ki = 156.0 nM 6.81
CHEMBL488542 Ki = 209.0 nM 6.68
CHEMBL483487 Ki = 434.0 nM 6.36
CHEMBL482638 Ki = 557.0 nM 6.25
CHEMBL520830 Ki = 758.0 nM 6.12
CHEMBL486282 Ki = 2080.0 nM 5.68
CHEMBL484899 Ki = 5780.0 nM 5.24
CHEMBL486893 Ki = 17600.0 nM 4.75
CHEMBL483469 Ki = 24200.0 nM 4.62
CHEMBL486688 Ki = 30000.0 nM 4.52
CHEMBL484900 Ki > 1000.0 nM -
CHEMBL486478 Ki > 10000.0 nM -
CHEMBL486479 Ki > 10000.0 nM -
CHEMBL519390 Ki > 10000.0 nM -
CHEMBL520617 Ki > 1000.0 nM -
CHEMBL482648 Ki > 1000.0 nM -
CHEMBL482855 Ki > 10000.0 nM -
CHEMBL483065 Ki > 10000.0 nM -
CHEMBL482436 Ki > 1000.0 nM -
CHEMBL483688 Ki > 10000.0 nM -
CHEMBL519253 Ki > 1000.0 nM -
CHEMBL520899 Ki > 1000.0 nM -
CHEMBL486481 Ki > 1000.0 nM -
CHEMBL519556 Ki > 1000.0 nM -
CHEMBL488541 Ki > 1000.0 nM -
CHEMBL483261 Ki > 10000.0 nM -
CHEMBL519813 Ki > 10000.0 nM -
CHEMBL520297 Ki > 1000.0 nM -
CHEMBL212625 Ki > 1000.0 nM -