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Assay Detail

CHEMBL947865

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

Binding
Displacement of [3H]CCPA from human adenosine A1 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 A1 (CHEMBL226)
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 5.71 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL486893 1 6.35
CHEMBL483469 1 5.96
CHEMBL486282 1 5.93
CHEMBL519813 1 5.74
CHEMBL520297 1 5.74
CHEMBL212625 1 5.68
CHEMBL484899 1 5.68
CHEMBL482436 1 5.65
CHEMBL484900 1 5.64
CHEMBL519390 1 5.64
CHEMBL486688 1 5.58
CHEMBL482648 1 5.42
CHEMBL486479 1 5.25
CHEMBL486478 1 -
CHEMBL520617 1 -
CHEMBL518972 1 -
CHEMBL482855 1 -
CHEMBL483065 1 -
CHEMBL483261 1 -
CHEMBL483487 1 -
CHEMBL483688 1 -
CHEMBL519253 1 -
CHEMBL520899 1 -
CHEMBL486481 1 -
CHEMBL519556 1 -
CHEMBL488541 1 -
CHEMBL488542 1 -
CHEMBL486281 1 -
CHEMBL520830 1 -
CHEMBL482638 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL486893 Ki = 443.0 nM 6.35
CHEMBL483469 Ki = 1090.0 nM 5.96
CHEMBL486282 Ki = 1170.0 nM 5.93
CHEMBL519813 Ki = 1840.0 nM 5.74
CHEMBL520297 Ki = 1820.0 nM 5.74
CHEMBL212625 Ki = 2067.0 nM 5.68
CHEMBL484899 Ki = 2070.0 nM 5.68
CHEMBL482436 Ki = 2240.0 nM 5.65
CHEMBL484900 Ki = 2300.0 nM 5.64
CHEMBL519390 Ki = 2300.0 nM 5.64
CHEMBL486688 Ki = 2610.0 nM 5.58
CHEMBL482648 Ki = 3800.0 nM 5.42
CHEMBL486479 Ki = 5630.0 nM 5.25
CHEMBL486478 Ki > 10000.0 nM -
CHEMBL520617 Ki - -
CHEMBL518972 Ki - -
CHEMBL482855 Ki > 10000.0 nM -
CHEMBL483065 Ki > 10000.0 nM -
CHEMBL483261 Ki > 10000.0 nM -
CHEMBL483487 Ki > 1000.0 nM -
CHEMBL483688 Ki > 10000.0 nM -
CHEMBL519253 Ki - -
CHEMBL520899 Ki - -
CHEMBL486481 Ki > 10000.0 nM -
CHEMBL519556 Ki - -
CHEMBL488541 Ki > 10000.0 nM -
CHEMBL488542 Ki - -
CHEMBL486281 Ki - -
CHEMBL520830 Ki - -
CHEMBL482638 Ki - -