Target
Platelet-derived growth factor receptor beta
Ligand
BDBM6416
Substrate
PDGFR Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
IC50
360±n/a nM
Citation
 Kuo, GHWang, AEmanuel, SDeangelis, AZhang, RConnolly, PJMurray, WVGruninger, RHSechler, JFuentes-Pesquera, AJohnson, DMiddleton, SAJolliffe, LChen, X Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors. J Med Chem 48:1886-900 (2005) [PubMed]  Article 
Target
Name:
Platelet-derived growth factor receptor beta
Synonyms:
Beta-type platelet-derived growth factor receptor | CD140 antigen-like family member B | CD140b antigen | CD_antigen=CD140b | PDGF Receptor Substrate | PDGF-R-beta | PDGFR | PDGFR substrate | PDGFR-1 | PDGFR1 | PDGFRB | PDGFRbeta | PGFRB_HUMAN | Platelet-Derived Growth Factor Receptor, beta | Platelet-derived growth factor receptor 1 | Platelet-derived growth factor receptor beta | Platelet-derived growth factor receptor beta (PDGFR-beta) | Platelet-derived growth factor receptor beta (PDGFRB) | Platelet-derived growth factor receptor beta (PDGFRbeta) | VHL/PDGFRB
Type:
Enzyme
Mol. Mass.:
123922.25
Organism:
Homo sapiens (Human)
Description:
P09619
Residue:
1106
Sequence:
MRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTFVLTCSGSAPVVWERMSQEPPQEMAKAQDGTFSSVLTLTNLTGLDTGEYFCTHNDSRGLETDERKRLYIFVPDPTVGFLPNDAEELFIFLTEITEITIPCRVTDPQLVVTLHEKKGDVALPVPYDHQRGFSGIFEDRSYICKTTIGDREVDSDAYYVYRLQVSSINVSVNAVQTVVRQGENITLMCIVIGNEVVNFEWTYPRKESGRLVEPVTDFLLDMPYHIRSILHIPSAELEDSGTYTCNVTESVNDHQDEKAINITVVESGYVRLLGEVGTLQFAELHRSRTLQVVFEAYPPPTVLWFKDNRTLGDSSAGEIALSTRNVSETRYVSELTLVRVKVAEAGHYTMRAFHEDAEVQLSFQLQINVPVRVLELSESHPDSGEQTVRCRGRGMPQPNIIWSACRDLKRCPRELPPTLLGNSSEEESQLETNVTYWEEEQEFEVVSTLRLQHVDRPLSVRCTLRNAVGQDTQEVIVVPHSLPFKVVVISAILALVVLTIISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPMQLPYDSTWELPRDQLVLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGPHLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQHHSDKRRPPSAELYSNALPVGLPLPSHVSLTGESDGGYMDMSKDESVDYVPMLDMKGDVKYADIESSNYMAPYDNYVPSAPERTCRATLINESPVLSYMDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLVKICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLGGTPYPELPMNEQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFEIRPPFSQLVLLLERLLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGFHGLRSPLDTSSVLYTAVQPNEGDNDYIIPLPDPKPEVADEGPLEGSPSLASSTLNEVNTSSTISCDSPLEPQDEPEPEPQLELQVEPEPELEQLPDSGCPAPRAEAEDSFL
  
Inhibitor
Name:
BDBM6416
Synonyms:
3-[(5-{6-[(3-chlorophenyl)amino]pyrazin-2-yl}pyridin-3-yl)amino]propan-1-ol | 3-[[5-[6-[(3-chlorophenyl)amino]pyrazinyl]-3-pyridinyl]amino]-1-propanol | Pyrazine-Pyridine Biheteroaryl 7 | Pyrazine-Pyridine deriv. 15
Type:
Small organic molecule
Emp. Form.:
C18H18ClN5O
Mol. Mass.:
355.821
SMILES:
OCCCNc1cncc(c1)-c1cncc(Nc2cccc(Cl)c2)n1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PDGFR Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2588.40
Organism:
n/a
Description:
n/a
Residue:
23
Sequence:
ITINKHKKLAEGSAYEEVAMIDE