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Assay Detail

CHEMBL4259138

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Binding
Binding affinity to human adenosine A2B receptor by radioligand displacement assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2b (CHEMBL255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.
Załuski M, Stanuch K, Karcz T, Hinz S, Latacz G, Szymańska E, Schabikowski J, Doroż-Płonka A, Handzlik J, Drabczyńska A, Müller CE, Kieć-Kononowicz K.
Medchemcomm (2018) 9 : 951 -962
PubMed 30108984 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.70 6.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL320872 1 6.73
CHEMBL52333 ROLOFYLLINE 3.0 1 6.57
CHEMBL1355736 THEOPHYLLINE 4.0 1 5.04
CHEMBL113 CAFFEINE 4.0 1 4.47
CHEMBL431770 ISTRADEFYLLINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL320872 Ki = 187.0 nM 6.73
CHEMBL52333 ROLOFYLLINE Ki = 269.0 nM 6.57
CHEMBL1355736 THEOPHYLLINE Ki = 9070.0 nM 5.04
CHEMBL113 CAFFEINE Ki = 33800.0 nM 4.47
CHEMBL431770 ISTRADEFYLLINE Ki > 10000.0 nM -