Target
Hepatocyte growth factor receptor
Ligand
BDBM28024
Substrate
poly(Glu/Tyr)
Meas. Tech.
Met Kinase Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
5.9±0.8 nM
Citation
 Schroeder, GMAn, YCai, ZWChen, XTClark, CCornelius, LADai, JGullo-Brown, JGupta, AHenley, BHunt, JTJeyaseelan, RKamath, AKim, KLippy, JLombardo, LJManne, VOppenheimer, SSack, JSSchmidt, RJShen, GStefanski, KTokarski, JSTrainor, GLWautlet, BSWei, DWilliams, DKZhang, YZhang, YFargnoli, JBorzilleri, RM Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily. J Med Chem 52:1251-4 (2009) [PubMed]  Article 
Target
Name:
Hepatocyte growth factor receptor
Synonyms:
Hepatocyte growth factor receptor | Hepatocyte growth factor receptor (MET) | Hepatocyte growth factor receptor (c-MET) | Hepatocyte growth factor receptor (cMET) | MET | MET_HUMAN | Met proto-oncogene (hepatocyte growth factor receptor) | Proto-oncogene c-Met | Tyrosine-protein kinase Met (c-Met) | Tyrosine-protein kinase Met (cMet) | c-Met kinase
Type:
Protein
Mol. Mass.:
155559.73
Organism:
Homo sapiens (Human)
Description:
P08581
Residue:
1390
Sequence:
MKAPAVLAPGILVLLFTLVQRSNGECKEALAKSEMNVNMKYQLPNFTAETPIQNVILHEHHIFLGATNYIYVLNEEDLQKVAEYKTGPVLEHPDCFPCQDCSSKANLSGGVWKDNINMALVVDTYYDDQLISCGSVNRGTCQRHVFPHNHTADIQSEVHCIFSPQIEEPSQCPDCVVSALGAKVLSSVKDRFINFFVGNTINSSYFPDHPLHSISVRRLKETKDGFMFLTDQSYIDVLPEFRDSYPIKYVHAFESNNFIYFLTVQRETLDAQTFHTRIIRFCSINSGLHSYMEMPLECILTEKRKKRSTKKEVFNILQAAYVSKPGAQLARQIGASLNDDILFGVFAQSKPDSAEPMDRSAMCAFPIKYVNDFFNKIVNKNNVRCLQHFYGPNHEHCFNRTLLRNSSGCEARRDEYRTEFTTALQRVDLFMGQFSEVLLTSISTFIKGDLTIANLGTSEGRFMQVVVSRSGPSTPHVNFLLDSHPVSPEVIVEHTLNQNGYTLVITGKKITKIPLNGLGCRHFQSCSQCLSAPPFVQCGWCHDKCVRSEECLSGTWTQQICLPAIYKVFPNSAPLEGGTRLTICGWDFGFRRNNKFDLKKTRVLLGNESCTLTLSESTMNTLKCTVGPAMNKHFNMSIIISNGHGTTQYSTFSYVDPVITSISPKYGPMAGGTLLTLTGNYLNSGNSRHISIGGKTCTLKSVSNSILECYTPAQTISTEFAVKLKIDLANRETSIFSYREDPIVYEIHPTKSFISGGSTITGVGKNLNSVSVPRMVINVHEAGRNFTVACQHRSNSEIICCTTPSLQQLNLQLPLKTKAFFMLDGILSKYFDLIYVHNPVFKPFEKPVMISMGNENVLEIKGNDIDPEAVKGEVLKVGNKSCENIHLHSEAVLCTVPNDLLKLNSELNIEWKQAISSTVLGKVIVQPDQNFTGLIAGVVSISTALLLLLGFFLWLKKRKQIKDLGSELVRYDARVHTPHLDRLVSARSVSPTTEMVSNESVDYRATFPEDQFPNSSQNGSCRQVQYPLTDMSPILTSGDSDISSPLLQNTVHIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLAARNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQTQKFTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVKCVAPYPSLLSSEDNADDEVDTRPASFWETS
  
Inhibitor
Name:
BDBM28024
Synonyms:
2-aminopyridine analogue, 3 | N-[4-({2-amino-3-[(4-methylpiperazin-1-yl)methyl]pyridin-4-yl}oxy)-3-fluorophenyl]-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
Type:
Small organic molecule
Emp. Form.:
C29H28F2N6O3
Mol. Mass.:
546.5678
SMILES:
CN1CCN(Cc2c(N)nccc2Oc2ccc(NC(=O)c3cccn(-c4ccc(F)cc4)c3=O)cc2F)CC1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
poly(Glu/Tyr)
Synonyms:
n/a
Type:
Random copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA