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Target
Platelet-derived growth factor receptor alpha
Ligand
BDBM50191975
Substrate
n/a
Meas. Tech.
ChEMBL_1613237 (CHEMBL3855037)
IC50
0.530000±n/a nM
Citation
 Shaw, DE; Baig, F; Bruce, I; Chamoin, S; Collingwood, SP; Cross, S; Dayal, S; Drückes, P; Furet, P; Furminger, V; Haggart, D; Hussey, M; Konstantinova, I; Loren, JC; Molteni, V; Roberts, S; Reilly, J; Saunders, AM; Stringer, R; Sviridenko, L; Thomas, M; Thomson, CG; Tomlins, C; Wen, B; Yeh, V; Pearce, AC Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension. J Med Chem 59:7901-14 (2016) [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:
BDBM50191975
Synonyms:
CHEMBL3975580
Type:
Small organic molecule
Emp. Form.:
C26H27FN6O3
Mol. Mass.:
490.5294
SMILES:
Cn1nccc1-c1ccn2c(cnc2c1)C(=O)Nc1cc(ccc1F)C(=O)NCC1CCC(C)(C)O1
Structure:
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