Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL951835

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

Functional
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Jurkat
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
IC50 30 8.34 8.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483688 1 8.95
CHEMBL486479 1 8.79
CHEMBL483469 1 8.72
CHEMBL519390 1 8.64
CHEMBL484900 1 8.49
CHEMBL486688 1 8.45
CHEMBL482436 1 8.44
CHEMBL519813 1 8.35
CHEMBL482648 1 8.28
CHEMBL483065 1 8.27
CHEMBL212625 1 8.00
CHEMBL488541 1 7.96
CHEMBL482855 1 7.79
CHEMBL486893 1 7.63
CHEMBL483261 1 -
CHEMBL482638 1 -
CHEMBL520297 1 -
CHEMBL520830 1 -
CHEMBL484899 1 -
CHEMBL486478 1 -
CHEMBL520617 1 -
CHEMBL518972 1 -
CHEMBL483487 1 -
CHEMBL486282 1 -
CHEMBL519253 1 -
CHEMBL520899 1 -
CHEMBL486281 1 -
CHEMBL488542 1 -
CHEMBL486481 1 -
CHEMBL519556 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483688 IC50 = 1.13 nM 8.95
CHEMBL486479 IC50 = 1.62 nM 8.79
CHEMBL483469 IC50 = 1.91 nM 8.72
CHEMBL519390 IC50 = 2.29 nM 8.64
CHEMBL484900 IC50 = 3.23 nM 8.49
CHEMBL486688 IC50 = 3.56 nM 8.45
CHEMBL482436 IC50 = 3.64 nM 8.44
CHEMBL519813 IC50 = 4.49 nM 8.35
CHEMBL482648 IC50 = 5.26 nM 8.28
CHEMBL483065 IC50 = 5.34 nM 8.27
CHEMBL212625 IC50 = 10.1 nM 8.00
CHEMBL488541 IC50 = 10.9 nM 7.96
CHEMBL482855 IC50 = 16.2 nM 7.79
CHEMBL486893 IC50 = 23.4 nM 7.63
CHEMBL483261 IC50 - -
CHEMBL482638 IC50 - -
CHEMBL520297 IC50 - -
CHEMBL520830 IC50 - -
CHEMBL484899 IC50 - -
CHEMBL486478 IC50 - -
CHEMBL520617 IC50 - -
CHEMBL518972 IC50 - -
CHEMBL483487 IC50 - -
CHEMBL486282 IC50 - -
CHEMBL519253 IC50 - -
CHEMBL520899 IC50 - -
CHEMBL486281 IC50 - -
CHEMBL488542 IC50 - -
CHEMBL486481 IC50 - -
CHEMBL519556 IC50 - -