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Assay Detail

CHEMBL5155960

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Functional
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

A<sub>3</sub> adenosine receptor agonists containing dopamine moieties for enhanced interspecies affinity.
Tosh DK, Salmaso V, Campbell RG, Rao H, Bitant A, Pottie E, Stove CP, Liu N, Gavrilova O, Gao ZG, Auchampach JA, Jacobson KA.
Eur J Med Chem (2022) 228 : 113983 -113983
PubMed 34844790 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.18 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5170037 1 7.62
CHEMBL5178814 1 7.50
CHEMBL5196916 1 7.46
CHEMBL5181821 1 7.42
CHEMBL5190575 1 7.36
CHEMBL5202349 1 7.34
CHEMBL5175945 1 7.31
CHEMBL5203255 1 7.19
CHEMBL5195772 1 7.18
CHEMBL464859 NECA 1 6.81
CHEMBL5174613 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5170037 EC50 = 23.7 nM 7.62
CHEMBL5178814 EC50 = 31.3 nM 7.50
CHEMBL5196916 EC50 = 35.0 nM 7.46
CHEMBL5181821 EC50 = 38.5 nM 7.42
CHEMBL5190575 EC50 = 43.9 nM 7.36
CHEMBL5202349 EC50 = 45.9 nM 7.34
CHEMBL5175945 EC50 = 49.4 nM 7.31
CHEMBL5203255 EC50 = 64.9 nM 7.19
CHEMBL5195772 EC50 = 66.4 nM 7.18
CHEMBL464859 NECA EC50 = 154.0 nM 6.81
CHEMBL5174613 EC50 = 1430.0 nM 5.84