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Target
Platelet-derived growth factor receptor alpha
Ligand
BDBM50260917
Substrate
n/a
Meas. Tech.
ChEMBL_555675 (CHEMBL955829)
IC50
9±n/a nM
Citation
 Hu, E; Tasker, A; White, RD; Kunz, RK; Human, J; Chen, N; Bürli, R; Hungate, R; Novak, P; Itano, A; Zhang, X; Yu, V; Nguyen, Y; Tudor, Y; Plant, M; Flynn, S; Xu, Y; Meagher, KL; Whittington, DA; Ng, GY Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. J Med Chem 51:3065-8 (2008) [PubMed]  Article 
Target
Name:
Platelet-derived growth factor receptor alpha
Synonyms:
Alpha-type platelet-derived growth factor receptor | PDGFR2 | PDGFRA | PDGFRalpha | PGFRA_HUMAN | Platelet-derived growth factor receptor alpha (PDGFR-alpha) | Platelet-derived growth factor receptor alpha (PDGFRA) | Platelet-derived growth factor receptor, alpha polypeptid | RHEPDGFRA
Type:
Protein
Mol. Mass.:
122633.38
Organism:
Homo sapiens (Human)
Description:
P16234
Residue:
1089
Sequence:
MGTSHPAFLVLGCLLTGLSLILCQLSLPSILPNENEKVVQLNSSFSLRCFGESEVSWQYPMSEEESSDVEIRNEENNSGLFVTVLEVSSASAAHTGLYTCYYNHTQTEENELEGRHIYIYVPDPDVAFVPLGMTDYLVIVEDDDSAIIPCRTTDPETPVTLHNSEGVVPASYDSRQGFNGTFTVGPYICEATVKGKKFQTIPFNVYALKATSELDLEMEALKTVYKSGETIVVTCAVFNNEVVDLQWTYPGEVKGKGITMLEEIKVPSIKLVYTLTVPEATVKDSGDYECAARQATREVKEMKKVTISVHEKGFIEIKPTFSQLEAVNLHEVKHFVVEVRAYPPPRISWLKNNLTLIENLTEITTDVEKIQEIRYRSKLKLIRAKEEDSGHYTIVAQNEDAVKSYTFELLTQVPSSILDLVDDHHGSTGGQTVRCTAEGTPLPDIEWMICKDIKKCNNETSWTILANNVSNIITEIHSRDRSTVEGRVTFAKVEETIAVRCLAKNLLGAENRELKLVAPTLRSELTVAAAVLVLLVIVIISLIVLVVIWKQKPRYEIRWRVIESISPDGHEYIYVDPMQLPYDSRWEFPRDGLVLGRVLGSGAFGKVVEGTAYGLSRSQPVMKVAVKMLKPTARSSEKQALMSELKIMTHLGPHLNIVNLLGACTKSGPIYIITEYCFYGDLVNYLHKNRDSFLSHHPEKPKKELDIFGLNPADESTRSYVILSFENNGDYMDMKQADTTQYVPMLERKEVSKYSDIQRSLYDRPASYKKKSMLDSEVKNLLSDDNSEGLTLLDLLSFTYQVARGMEFLASKNCVHRDLAARNVLLAQGKIVKICDFGLARDIMHDSNYVSKGSTFLPVKWMAPESIFDNLYTTLSDVWSYGILLWEIFSLGGTPYPGMMVDSTFYNKIKSGYRMAKPDHATSEVYEIMVKCWNSEPEKRPSFYHLSEIVENLLPGQYKKSYEKIHLDFLKSDHPAVARMRVDSDNAYIGVTYKNEEDKLKDWEGGLDEQRLSADSGYIIPLPDIDPVPEEEDLGKRNRHSSQTSEESAIETGSSSSTFIKREDETIEDIDMMDDIGIDSSDLVEDSFL
  
Inhibitor
Name:
BDBM50260917
Synonyms:
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one | 3-(2-aminoquinazolin-6-yl)-4-methyl-1-[3-(trifluoromethyl)phenyl]pyridin-2(1H)-one | CHEMBL504805
Type:
Small organic molecule
Emp. Form.:
C21H15F3N4O
Mol. Mass.:
396.3652
SMILES:
Cc1ccn(-c2cccc(c2)C(F)(F)F)c(=O)c1-c1ccc2nc(N)ncc2c1
Structure:
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