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Assay Detail

CHEMBL4259139

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Binding
Binding affinity to human adenosine A3 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 A3 (CHEMBL256)
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 5.18 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL320872 1 5.64
CHEMBL52333 ROLOFYLLINE 3.0 1 5.36
CHEMBL431770 ISTRADEFYLLINE 4.0 1 5.35
CHEMBL113 CAFFEINE 4.0 1 4.88
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL320872 Ki = 2300.0 nM 5.64
CHEMBL52333 ROLOFYLLINE Ki = 4390.0 nM 5.36
CHEMBL431770 ISTRADEFYLLINE Ki = 4470.0 nM 5.35
CHEMBL113 CAFFEINE Ki = 13300.0 nM 4.88
CHEMBL1355736 THEOPHYLLINE Ki = 22300.0 nM 4.65