Target
Adenosine receptor A3
Ligand
BDBM50257074
Substrate
n/a
Meas. Tech.
ChEMBL_562709 (CHEMBL1012744)
EC50
36.3±n/a nM
Citation
 Colotta, VLenzi, OCatarzi, DVarano, FFilacchioni, GMartini, CTrincavelli, LCiampi, OPugliese, AMTraini, CPedata, FMorizzo, EMoro, S Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies. J Med Chem 52:2407-19 (2009) [PubMed]  Article 
Target
Name:
Adenosine receptor A3
Synonyms:
A3 adenosine receptor (hA3) | AA3R_HUMAN | ADORA3 | Adenosine A3 receptor (A3AR)
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
36197.32
Organism:
Homo sapiens (Human)
Description:
P0DMS8
Residue:
318
Sequence:
MPNNSTALSLANVTYITMEIFIGLCAIVGNVLVICVVKLNPSLQTTTFYFIVSLALADIAVGVLVMPLAIVVSLGITIHFYSCLFMTCLLLIFTHASIMSLLAIAVDRYLRVKLTVRYKRVTTHRRIWLALGLCWLVSFLVGLTPMFGWNMKLTSEYHRNVTFLSCQFVSVMRMDYMVYFSFLTWIFIPLVVMCAIYLDIFYIIRNKLSLNLSNSKETGAFYGREFKTAKSLFLVLFLFALSWLPLSIINCIIYFNGEVPQLVLYMGILLSHANSMMNPIVYAYKIKKFKETYLLILKACVVCHPSDSLDTSIEKNSE
  
Inhibitor
Name:
BDBM50257074
Synonyms:
CHEMBL474016 | N-(2-(4-methoxyphenyl)-1-oxo-1,2-dihydropyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazin-4-yl)benzamide
Type:
Small organic molecule
Emp. Form.:
C22H16N6O3
Mol. Mass.:
412.4008
SMILES:
COc1ccc(cc1)-n1nc2c(NC(=O)c3ccccc3)nc3ncccc3n2c1=O
Structure:
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