Target
Platelet-derived growth factor receptor alpha [D842V]
Ligand
BDBM469346
Substrate
n/a
Meas. Tech.
PDGFRA D842V assay at Km
IC50
<1.0±n/a nM
Citation
 Wilson, KJ Compositions useful for treating disorders related to kit US Patent  US10807985 Publication Date 10/20/2020 
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:
BDBM469346
Synonyms:
US10807985, Compound 121
Type:
Small organic molecule
Emp. Form.:
C28H29FN9O2
Mol. Mass.:
542.5874
SMILES:
C[C@](O)(c1ccc(F)cc1)c1cnc(nc1)N1CCN(CC1)C1=NC=N[N]2=CC(C=C12)c1cnn(c1)C1COC1 |r,c:27,t:25,29,32|
Structure:
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