Reaction Details Report a problem with these data
Target
Hepatocyte growth factor receptor
Ligand
BDBM24750
Substrate
biotinylated gastrin substrate
Meas. Tech.
HTRF Kinase Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
Ki
39±6 nM
Citation
 D'Angelo, ND; Bellon, SF; Booker, SK; Cheng, Y; Coxon, A; Dominguez, C; Fellows, I; Hoffman, D; Hungate, R; Kaplan-Lefko, P; Lee, MR; Li, C; Liu, L; Rainbeau, E; Reider, PJ; Rex, K; Siegmund, A; Sun, Y; Tasker, AS; Xi, N; Xu, S; Yang, Y; Zhang, Y; Burgess, TL; Dussault, I; Kim, TS Design, synthesis, and biological evaluation of potent c-Met inhibitors. J Med Chem 51:5766-79 (2008) [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:
BDBM24750
Synonyms:
2-benzyl-5-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-3-methyl-3,4-dihydropyrimidin-4-one | pyrimidone, 7
Type:
Small organic molecule
Emp. Form.:
C29H24FN3O4
Mol. Mass.:
497.517
SMILES:
COc1cc2nccc(Oc3ccc(cc3F)-c3cnc(Cc4ccccc4)n(C)c3=O)c2cc1OC
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated gastrin substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2100.22
Organism:
n/a
Description:
n/a
Residue:
17
Sequence:
ITINYLEEEEAYGWLDF