Target
Platelet-derived growth factor receptor alpha [D842V]
Ligand
BDBM472779
Substrate
n/a
Meas. Tech.
Biochemical Enzymatic Activity
IC50
<0.30±n/a nM
Citation
 Dineen, TA Compositions and methods for treating KIT- and PDGFRA-mediated diseases US Patent  US10829493 Publication Date 11/10/2020 
Target
Name:
Platelet-derived growth factor receptor alpha [D842V]
Synonyms:
PDGFR2 | PDGFRA | PGFRA_HUMAN | Platelet-derived growth factor receptor (D842V) | Platelet-derived growth factor receptor alpha (PDGFR)(D842V) | Platelet-derived growth factor receptor alpha (PDGFRα)(D842V) | RHEPDGFRA
Type:
Protein
Mol. Mass.:
122618.43
Organism:
Homo sapiens (Human)
Description:
P16234 (D842V)
Residue:
1089
Sequence:
MGTSHPAFLVLGCLLTGLSLILCQLSLPSILPNENEKVVQLNSSFSLRCFGESEVSWQYPMSEEESSDVEIRNEENNSGLFVTVLEVSSASAAHTGLYTCYYNHTQTEENELEGRHIYIYVPDPDVAFVPLGMTDYLVIVEDDDSAIIPCRTTDPETPVTLHNSEGVVPASYDSRQGFNGTFTVGPYICEATVKGKKFQTIPFNVYALKATSELDLEMEALKTVYKSGETIVVTCAVFNNEVVDLQWTYPGEVKGKGITMLEEIKVPSIKLVYTLTVPEATVKDSGDYECAARQATREVKEMKKVTISVHEKGFIEIKPTFSQLEAVNLHEVKHFVVEVRAYPPPRISWLKNNLTLIENLTEITTDVEKIQEIRYRSKLKLIRAKEEDSGHYTIVAQNEDAVKSYTFELLTQVPSSILDLVDDHHGSTGGQTVRCTAEGTPLPDIEWMICKDIKKCNNETSWTILANNVSNIITEIHSRDRSTVEGRVTFAKVEETIAVRCLAKNLLGAENRELKLVAPTLRSELTVAAAVLVLLVIVIISLIVLVVIWKQKPRYEIRWRVIESISPDGHEYIYVDPMQLPYDSRWEFPRDGLVLGRVLGSGAFGKVVEGTAYGLSRSQPVMKVAVKMLKPTARSSEKQALMSELKIMTHLGPHLNIVNLLGACTKSGPIYIITEYCFYGDLVNYLHKNRDSFLSHHPEKPKKELDIFGLNPADESTRSYVILSFENNGDYMDMKQADTTQYVPMLERKEVSKYSDIQRSLYDRPASYKKKSMLDSEVKNLLSDDNSEGLTLLDLLSFTYQVARGMEFLASKNCVHRDLAARNVLLAQGKIVKICDFGLARVIMHDSNYVSKGSTFLPVKWMAPESIFDNLYTTLSDVWSYGILLWEIFSLGGTPYPGMMVDSTFYNKIKSGYRMAKPDHATSEVYEIMVKCWNSEPEKRPSFYHLSEIVENLLPGQYKKSYEKIHLDFLKSDHPAVARMRVDSDNAYIGVTYKNEEDKLKDWEGGLDEQRLSADSGYIIPLPDIDPVPEEEDLGKRNRHSSQTSEESAIETGSSSSTFIKREDETIEDIDMMDDIGIDSSDLVEDSFL
  
Inhibitor
Name:
BDBM472779
Synonyms:
US10829493, Example 5
Type:
Small organic molecule
Emp. Form.:
C12H14N6O
Mol. Mass.:
258.2792
SMILES:
C[C@H](CO)n1cc(cn1)-c1cc2c(N)ncnn2c1 |r|
Structure:
Search PDB for entries with ligand similarity: