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Assay Detail

CHEMBL948832

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

Binding
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
35
Total Activities
35
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

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 35 8.52 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL486478 1 9.80
CHEMBL483261 1 9.67
CHEMBL519390 1 9.55
CHEMBL486479 1 9.52
CHEMBL482436 1 9.41
CHEMBL483487 1 9.39
CHEMBL484900 1 9.35
CHEMBL519253 1 9.32
CHEMBL483688 1 9.26
CHEMBL520830 1 9.22
CHEMBL482638 1 9.21
CHEMBL484899 1 9.16
CHEMBL483469 1 9.11
CHEMBL486688 1 9.11
CHEMBL518972 1 9.07
CHEMBL483065 1 9.06
CHEMBL482855 1 9.03
CHEMBL486893 1 8.97
CHEMBL519813 1 8.94
CHEMBL482648 1 8.92
CHEMBL520297 1 8.90
CHEMBL212625 1 8.88
CHEMBL520617 1 8.80
CHEMBL486481 1 8.70
CHEMBL486282 1 8.52
CHEMBL488542 1 8.27
CHEMBL519556 1 8.13
CHEMBL488541 1 8.12
CHEMBL520899 1 7.93
CHEMBL486281 1 7.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL486478 Ki = 0.157 nM 9.80
CHEMBL483261 Ki = 0.215 nM 9.67
CHEMBL519390 Ki = 0.281 nM 9.55
CHEMBL486479 Ki = 0.303 nM 9.52
CHEMBL482436 Ki = 0.393 nM 9.41
CHEMBL483487 Ki = 0.406 nM 9.39
CHEMBL484900 Ki = 0.446 nM 9.35
CHEMBL519253 Ki = 0.473 nM 9.32
CHEMBL483688 Ki = 0.553 nM 9.26
CHEMBL520830 Ki = 0.595 nM 9.22
CHEMBL482638 Ki = 0.61 nM 9.21
CHEMBL484899 Ki = 0.695 nM 9.16
CHEMBL483469 Ki = 0.782 nM 9.11
CHEMBL486688 Ki = 0.775 nM 9.11
CHEMBL518972 Ki = 0.858 nM 9.07
CHEMBL483065 Ki = 0.875 nM 9.06
CHEMBL482855 Ki = 0.944 nM 9.03
CHEMBL486893 Ki = 1.06 nM 8.97
CHEMBL519813 Ki = 1.15 nM 8.94
CHEMBL482648 Ki = 1.19 nM 8.92
CHEMBL520297 Ki = 1.27 nM 8.90
CHEMBL212625 Ki = 1.33 nM 8.88
CHEMBL520617 Ki = 1.58 nM 8.80
CHEMBL486481 Ki = 1.99 nM 8.70
CHEMBL486282 Ki = 3.03 nM 8.52
CHEMBL488542 Ki = 5.43 nM 8.27
CHEMBL519556 Ki = 7.49 nM 8.13
CHEMBL488541 Ki = 7.51 nM 8.12
CHEMBL520899 Ki = 11.7 nM 7.93
CHEMBL486281 Ki = 19.7 nM 7.71
CHEMBL16687 CGS-15943 Ki = 30.0 nM 7.52
CHEMBL452924 Ki = 237.0 nM 6.62
CHEMBL464859 NECA Ki = 1890.0 nM 5.72
CHEMBL285819 Ki = 21400.0 nM 4.67
CHEMBL113 CAFFEINE Ki = 33800.0 nM 4.47