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Assay Detail

CHEMBL5111996

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

Binding
Binding affinity to wild type A3R (unknown origin) expressed in Flp-In-CHO cells assessed as dissociation constant by by Schild analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Flp-In-CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure-Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations.
Stampelou M, Suchankova A, Tzortzini E, Dhingra L, Barkan K, Lougiakis N, Marakos P, Pouli N, Ladds G, Kolocouris A.
J Med Chem (2022) 65 : 13305 -13327
PubMed 36173355 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 16 6.94 10.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88147 1 10.01
CHEMBL5181728 1 7.87
CHEMBL5180268 1 7.77
CHEMBL3929812 1 7.05
CHEMBL5180010 1 7.05
CHEMBL5189470 1 6.89
CHEMBL5185003 1 6.80
CHEMBL5186062 1 6.77
CHEMBL3929143 1 6.60
CHEMBL5196781 1 6.59
CHEMBL5174600 1 6.52
CHEMBL5173159 1 6.45
CHEMBL5201810 1 6.31
CHEMBL3927012 1 6.26
CHEMBL5189274 1 6.24
CHEMBL5187501 1 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88147 Kd = 0.09772 nM 10.01
CHEMBL5181728 Kd = 13.49 nM 7.87
CHEMBL5180268 Kd = 16.98 nM 7.77
CHEMBL3929812 Kd = 89.13 nM 7.05
CHEMBL5180010 Kd = 89.13 nM 7.05
CHEMBL5189470 Kd = 128.82 nM 6.89
CHEMBL5185003 Kd = 158.49 nM 6.80
CHEMBL5186062 Kd = 169.82 nM 6.77
CHEMBL3929143 Kd = 251.19 nM 6.60
CHEMBL5196781 Kd = 257.04 nM 6.59
CHEMBL5174600 Kd = 302.0 nM 6.52
CHEMBL5173159 Kd = 354.81 nM 6.45
CHEMBL5201810 Kd = 489.78 nM 6.31
CHEMBL3927012 Kd = 549.54 nM 6.26
CHEMBL5189274 Kd = 575.44 nM 6.24
CHEMBL5187501 Kd = 1230.27 nM 5.91