Target
Tyrosine-protein kinase Yes
Ligand
BDBM50193874
Substrate
n/a
Meas. Tech.
ChEMBL_473236 (CHEMBL932927)
IC50
1.2±n/a nM
Citation
 Palanki, MSAkiyama, HCampochiaro, PCao, JChow, CPDellamary, LDoukas, JFine, RGritzen, CHood, JDHu, SKachi, SKang, XKlebansky, BKousba, ALohse, DMak, CCMartin, MMcPherson, APathak, VPRenick, JSoll, RUmeda, NYee, SYokoi, KZeng, BZhu, HNoronha, G Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration. J Med Chem 51:1546-59 (2008) [PubMed]  Article 
Target
Name:
Tyrosine-protein kinase Yes
Synonyms:
Proto-oncogene c-Yes | VHL/Tyrosine-protein kinase Yes | YES | YES1 | YES_HUMAN | p61-yes
Type:
Protein
Mol. Mass.:
60801.54
Organism:
Homo sapiens (Human)
Description:
P07947
Residue:
543
Sequence:
MGCIKSKENKSPAIKYRPENTPEPVSTSVSHYGAEPTTVSPCPSSSAKGTAVNFSSLSMTPFGGSSGVTPFGGASSSFSVVPSSYPAGLTGGVTIFVALYDYEARTTEDLSFKKGERFQIINNTEGDWWEARSIATGKNGYIPSNYVAPADSIQAEEWYFGKMGRKDAERLLLNPGNQRGIFLVRESETTKGAYSLSIRDWDEIRGDNVKHYKIRKLDNGGYYITTRAQFDTLQKLVKHYTEHADGLCHKLTTVCPTVKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTKVAIKTLKPGTMMPEAFLQEAQIMKKLRHDKLVPLYAVVSEEPIYIVTEFMSKGSLLDFLKEGDGKYLKLPQLVDMAAQIADGMAYIERMNYIHRDLRAANILVGENLVCKIADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILQTELVTKGRVPYPGMVNREVLEQVERGYRMPCPQGCPESLHELMNLCWKKDPDERPTFEYIQSFLEDYFTATEPQYQPGENL
  
Inhibitor
Name:
BDBM50193874
Synonyms:
7-(2,6-dimethylphenyl)-5-methyl-N-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)benzo[e][1,2,4]triazin-3-amine | 7-(2,6-dimethylphenyl)-5-methyl-N-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-1,2,4-benzotriazin-3-amine | CHEMBL436137 | US8481536, 322
Type:
Small organic molecule
Emp. Form.:
C28H31N5O
Mol. Mass.:
453.5786
SMILES:
Cc1cccc(C)c1-c1cc(C)c2nc(Nc3ccc(OCCN4CCCC4)cc3)nnc2c1
Structure:
Search PDB for entries with ligand similarity: