Reaction Details Report a problem with these data
Target
Platelet-derived growth factor receptor alpha [1-973]
Ligand
BDBM120816
Substrate
n/a
Meas. Tech.
HTRF kinase assay
pH
7.0000±n/a
Temperature
298.1500±n/a K
IC50
32.23±0.0 nM
Comments
extracted
Citation
 Zhou, S; Ren, J; Liu, M; Ren, L; Liu, Y; Gong, P Design, synthesis and pharmacological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents. Bioorg Chem 57:30-42 (2014) [PubMed]  Article 
Target
Name:
Platelet-derived growth factor receptor alpha [1-973]
Synonyms:
Alpha-type platelet-derived growth factor receptor | PGFRA_HUMAN | PDGFRA | PDGFR2 | RHEPDGFRA | Platelet-derived growth factor receptor alpha (PDGFR +-)
Type:
Protein
Mol. Mass.:
109689.70
Organism:
Human
Description:
P16234[1-973]
Residue:
973
Sequence:
MGTSHPAFLVLGCLLTGLSLILCQLSLPSILPNENEKVVQLNSSFSLRCFGESEVSWQYPMSEEESSDVEIRNEENNSGLFVTVLEVSSASAAHTGLYTCYYNHTQTEENELEGRHIYIYVPDPDVAFVPLGMTDYLVIVEDDDSAIIPCRTTDPETPVTLHNSEGVVPASYDSRQGFNGTFTVGPYICEATVKGKKFQTIPFNVYALKATSELDLEMEALKTVYKSGETIVVTCAVFNNEVVDLQWTYPGEVKGKGITMLEEIKVPSIKLVYTLTVPEATVKDSGDYECAARQATREVKEMKKVTISVHEKGFIEIKPTFSQLEAVNLHEVKHFVVEVRAYPPPRISWLKNNLTLIENLTEITTDVEKIQEIRYRSKLKLIRAKEEDSGHYTIVAQNEDAVKSYTFELLTQVPSSILDLVDDHHGSTGGQTVRCTAEGTPLPDIEWMICKDIKKCNNETSWTILANNVSNIITEIHSRDRSTVEGRVTFAKVEETIAVRCLAKNLLGAENRELKLVAPTLRSELTVAAAVLVLLVIVIISLIVLVVIWKQKPRYEIRWRVIESISPDGHEYIYVDPMQLPYDSRWEFPRDGLVLGRVLGSGAFGKVVEGTAYGLSRSQPVMKVAVKMLKPTARSSEKQALMSELKIMTHLGPHLNIVNLLGACTKSGPIYIITEYCFYGDLVNYLHKNRDSFLSHHPEKPKKELDIFGLNPADESTRSYVILSFENNGDYMDMKQADTTQYVPMLERKEVSKYSDIQRSLYDRPASYKKKSMLDSEVKNLLSDDNSEGLTLLDLLSFTYQVARGMEFLASKNCVHRDLAARNVLLAQGKIVKICDFGLARDIMHDSNYVSKGSTFLPVKWMAPESIFDNLYTTLSDVWSYGILLWEIFSLGGTPYPGMMVDSTFYNKIKSGYRMAKPDHATSEVYEIMVKCWNSEPEKRPSFYHLSEIVENLLPGQYKKSYEKIHLDFLKSD
  
Inhibitor
Name:
BDBM120816
Synonyms:
(Z)-4-(((3-fluoro-4-((6-methoxy-7-(3-morpholinopropoxy) quinolin-4-yl)oxy)phenyl)amino)methylene)-3-methyl-1-(2- (trifluoromethyl)phenyl)-1H-pyrazol-5(4H)-one (17)
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
COc1cc2c(Oc3ccc(cc3F)N=Cc3c(C)[nH]n(-c4ccccc4C(F)(F)F)c3=O)ccnc2cc1OCCCN1CCOCC1 |w:14.14|
Structure:
Search PDB for entries with ligand similarity: