Target
Platelet-derived growth factor receptor alpha
Ligand
BDBM50510917
Substrate
n/a
Meas. Tech.
ChEMBL_1842659 (CHEMBL4343086)
IC50
36±n/a nM
Citation
 ?ezní?ková, EGucký, TKová?ová, VAjani, HJorda, RKry?tof, V Activity of 2,6,9-trisubstituted purines as potent PDGFR? kinase inhibitors with antileukaemic activity. Eur J Med Chem 182:0 (2019) [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:
BDBM50510917
Synonyms:
CHEMBL4530087
Type:
Small organic molecule
Emp. Form.:
C28H34N8O
Mol. Mass.:
498.6226
SMILES:
COc1ccccc1-c1ccc(Nc2nc(N[C@H]3CC[C@H](N)CC3)nc3n(cnc23)C2CCCC2)cn1 |r,wU:20.21,wD:17.17,(51.16,-37.92,;49.82,-37.16,;49.81,-35.62,;51.13,-34.84,;51.12,-33.3,;49.77,-32.55,;48.45,-33.33,;48.47,-34.86,;47.16,-35.64,;45.81,-34.87,;44.48,-35.65,;44.49,-37.19,;43.16,-37.96,;43.17,-39.5,;41.83,-40.27,;41.83,-41.82,;40.5,-42.58,;39.16,-41.82,;39.16,-40.27,;37.84,-39.49,;36.5,-40.26,;35.17,-39.48,;36.5,-41.8,;37.83,-42.58,;43.17,-42.59,;44.5,-41.81,;45.97,-42.28,;46.87,-41.03,;45.97,-39.78,;44.5,-40.27,;46.45,-43.75,;45.55,-45,;46.45,-46.24,;47.91,-45.76,;47.91,-44.22,;45.83,-37.95,;47.16,-37.18,)|
Structure:
Search PDB for entries with ligand similarity: