Target
Adenosine receptor A1
Ligand
BDBM21238
Substrate
BDBM21173
Meas. Tech.
Human A1 Adenosine Receptor Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Comments
43% inhibition @ 10 uM.
Citation
 Cosimelli, BGreco, GEhlardo, MNovellino, EDa Settimo, FTaliani, SLa Motta, CBellandi, MTuccinardi, TMartinelli, ACiampi, OTrincavelli, MLMartini, C Derivatives of 4-Amino-6-hydroxy-2-mercaptopyrimidine as Novel, Potent, and Selective A3 Adenosine Receptor Antagonists. J Med Chem 51:1764-70 (2008) [PubMed]  Article 
Target
Name:
Adenosine receptor A1
Synonyms:
A1 adenosine receptor (hA1) | A1AR | AA1R_HUMAN | ADENOSINE A1 | ADORA1 | Adenosine A1 receptor (A1AR) | Adenosine A1-receptor | Adenosine receptor A1 (A1) | Adenosine receptor A1 (hA1) | Adenosine transporter (AdT)
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
36520.92
Organism:
Homo sapiens (Human)
Description:
P30542
Residue:
326
Sequence:
MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGALVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKMVVTPRRAAVAIAGCWILSFVVGLTPMFGWNNLSAVERAWAANGSMGEPVIKCEFEKVISMEYMVYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALILFLFALSWLPLHILNCITLFCPSCHKPSILTYIAIFLTHGNSAMNPIVYAFRIQKFRVTFLKIWNDHFRCQPAPPIDEDLPEERPDD
  
Inhibitor
Name:
BDBM21238
Synonyms:
2-mercaptopyrimidine analogue, 5q | N-[6-(cyclohexylmethoxy)-2-(propylsulfanyl)pyrimidin-4-yl]acetamide
Type:
Small organic molecule
Emp. Form.:
C16H25N3O2S
Mol. Mass.:
323.454
SMILES:
CCCSc1nc(NC(C)=O)cc(OCC2CCCCC2)n1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM21173
Synonyms:
1,3-dipropyl-8-cyclopentylxanthine | 8-cyclopentyl-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione | CHEMBL183 | DPCPX | PD116948 | [3H]DPCPX
Type:
radiolabeled ligand
Emp. Form.:
C16H24N4O2
Mol. Mass.:
304.3874
SMILES:
CCCn1c2nc([nH]c2c(=O)n(CCC)c1=O)C1CCCC1
Structure:
Search PDB for entries with ligand similarity: