Reaction Details Report a problem with these data
Target
Hepatocyte growth factor receptor
Ligand
BDBM24440
Substrate
poly(Glu/Tyr)
Meas. Tech.
Met Kinase Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
1.8±0.7 nM
Citation
Kim, KS; Zhang, L; Schmidt, R; Cai, ZW; Wei, D; Williams, DK; Lombardo, LJ; Trainor, GL; Xie, D; Zhang, Y; An, Y; Sack, JS; Tokarski, JS; Darienzo, C; Kamath, A; Marathe, P; Zhang, Y; Lippy, J; Jeyaseelan R, Sr; Wautlet, B; Henley, B; Gullo-Brown, J; Manne, V; Hunt, JT; Fargnoli, J; Borzilleri, RM Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem 51:5330-41 (2008) [PubMed] Article
More Info.:
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:
BDBM24440
Synonyms:
2-pyridone analogue, 2 | JMC521251 Compound 1 | N-(3-fluoro-4-{1H-pyrrolo[2,3-b]pyridin-4-yloxy}phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
Type:
Small organic molecule
Emp. Form.:
C25H16F2N4O3
Mol. Mass.:
458.4163
SMILES:
Fc1ccc(cc1)-n1cccc(C(=O)Nc2ccc(Oc3ccnc4[nH]ccc34)c(F)c2)c1=O
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