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Assay Detail

CHEMBL4189485

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

Binding
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
6
Total Activities
6
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

Fluorescent-Labeled Selective Adenosine A2B Receptor Antagonist Enables Competition Binding Assay by Flow Cytometry.
Köse M, Gollos S, Karcz T, Fiene A, Heisig F, Behrenswerth A, Kieć-Kononowicz K, Namasivayam V, Müller CE.
J Med Chem (2018) 61 : 4301 -4316
PubMed 29681156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.07 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483688 1 9.13
CHEMBL4215606 1 8.97
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 8.42
CHEMBL4203745 1 7.63
CHEMBL16687 CGS-15943 1 7.22
CHEMBL113142 ZM-241385 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483688 IC50 = 0.739 nM 9.13
CHEMBL4215606 IC50 = 1.06 nM 8.97
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] IC50 = 3.8 nM 8.42
CHEMBL4203745 IC50 = 23.5 nM 7.63
CHEMBL16687 CGS-15943 IC50 = 60.7 nM 7.22
CHEMBL113142 ZM-241385 IC50 = 94.9 nM 7.02