Reaction Details Report a problem with these data
Target
Hepatocyte growth factor receptor
Ligand
BDBM24477
Substrate
biotinylated gastrin substrate
Meas. Tech.
HTRF Kinase Inhibition Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
6±0.3 nM
Citation
 Albrecht, BK; Harmange, JC; Bauer, D; Berry, L; Bode, C; Boezio, AA; Chen, A; Choquette, D; Dussault, I; Fridrich, C; Hirai, S; Hoffman, D; Larrow, JF; Kaplan-Lefko, P; Lin, J; Lohman, J; Long, AM; Moriguchi, J; O'Connor, A; Potashman, MH; Reese, M; Rex, K; Siegmund, A; Shah, K; Shimanovich, R; Springer, SK; Teffera, Y; Yang, Y; Zhang, Y; Bellon, SF Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase. J Med Chem 51:2879-82 (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:
BDBM24477
Synonyms:
4-(3-{[(7-methoxyquinolin-4-yl)oxy]methyl}-[1,2,4]triazolo[4,3-a]pyridazin-6-yl)-N-methylbenzamide | Triazolopyridazine, 10g
Type:
Small organic molecule
Emp. Form.:
C24H20N6O3
Mol. Mass.:
440.454
SMILES:
CNC(=O)c1ccc(cc1)-c1ccc2nnc(COc3ccnc4cc(OC)ccc34)n2n1
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