Target
Hepatocyte growth factor receptor [D1228N]
Ligand
BDBM516966
Substrate
n/a
Meas. Tech.
Enzyme Assay
IC50
4.40±n/a nM
Citation
 Hinklin, RJAllen, SBarbour, PCook, ADahlke, JGaudino, JLaird, EMcNulty, OTZhao, Q Pyrazolo[3,4-b]pyridine compounds as inhibitors of TAM and MET kinases US Patent  US11104676 Publication Date 8/31/2021 
Target
Name:
Hepatocyte growth factor receptor [D1228N]
Synonyms:
Hepatocyte growth factor receptor (MET)(D1228N) | MET | MET_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
155559.76
Organism:
Homo sapiens (Human)
Description:
P08581[D1228N]
Residue:
1390
Sequence:
MKAPAVLAPGILVLLFTLVQRSNGECKEALAKSEMNVNMKYQLPNFTAETPIQNVILHEHHIFLGATNYIYVLNEEDLQKVAEYKTGPVLEHPDCFPCQDCSSKANLSGGVWKDNINMALVVDTYYDDQLISCGSVNRGTCQRHVFPHNHTADIQSEVHCIFSPQIEEPSQCPDCVVSALGAKVLSSVKDRFINFFVGNTINSSYFPDHPLHSISVRRLKETKDGFMFLTDQSYIDVLPEFRDSYPIKYVHAFESNNFIYFLTVQRETLDAQTFHTRIIRFCSINSGLHSYMEMPLECILTEKRKKRSTKKEVFNILQAAYVSKPGAQLARQIGASLNDDILFGVFAQSKPDSAEPMDRSAMCAFPIKYVNDFFNKIVNKNNVRCLQHFYGPNHEHCFNRTLLRNSSGCEARRDEYRTEFTTALQRVDLFMGQFSEVLLTSISTFIKGDLTIANLGTSEGRFMQVVVSRSGPSTPHVNFLLDSHPVSPEVIVEHTLNQNGYTLVITGKKITKIPLNGLGCRHFQSCSQCLSAPPFVQCGWCHDKCVRSEECLSGTWTQQICLPAIYKVFPNSAPLEGGTRLTICGWDFGFRRNNKFDLKKTRVLLGNESCTLTLSESTMNTLKCTVGPAMNKHFNMSIIISNGHGTTQYSTFSYVDPVITSISPKYGPMAGGTLLTLTGNYLNSGNSRHISIGGKTCTLKSVSNSILECYTPAQTISTEFAVKLKIDLANRETSIFSYREDPIVYEIHPTKSFISGGSTITGVGKNLNSVSVPRMVINVHEAGRNFTVACQHRSNSEIICCTTPSLQQLNLQLPLKTKAFFMLDGILSKYFDLIYVHNPVFKPFEKPVMISMGNENVLEIKGNDIDPEAVKGEVLKVGNKSCENIHLHSEAVLCTVPNDLLKLNSELNIEWKQAISSTVLGKVIVQPDQNFTGLIAGVVSISTALLLLLGFFLWLKKRKQIKDLGSELVRYDARVHTPHLDRLVSARSVSPTTEMVSNESVDYRATFPEDQFPNSSQNGSCRQVQYPLTDMSPILTSGDSDISSPLLQNTVHIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLAARNCMLDEKFTVKVADFGLARNMYDKEYYSVHNKTGAKLPVKWMALESLQTQKFTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVKCVAPYPSLLSSEDNADDEVDTRPASFWETS
  
Inhibitor
Name:
BDBM516966
Synonyms:
N-(3-fluoro-4-((3- (((1r,3r)-3- (hydroxymethyl)cyclobutyl) amino)-1H- pyrazolo[3,4-b]pyridin-4- yl)oxy)phenyl)-2-(4- fluorophenyl)-3-oxo-2,3- dihydropyridazine-4- carboxamide | US11104676, Example 36
Type:
Small organic molecule
Emp. Form.:
C28H23F2N7O4
Mol. Mass.:
559.5235
SMILES:
OC[C@H]1CC(C1)Nc1n[nH]c2nccc(Oc3ccc(NC(=O)c4ccnn(-c5ccc(F)cc5)c4=O)cc3F)c12 |r,wD:2.1,(-12.34,2.12,;-11.94,.63,;-10.45,.23,;-9.68,-1.1,;-8.35,-.33,;-9.12,1,;-6.86,-.73,;-6.46,-2.22,;-7.37,-3.47,;-6.46,-4.71,;-5,-4.23,;-3.67,-5,;-2.33,-4.23,;-2.33,-2.69,;-3.67,-1.93,;-3.67,-.38,;-2.33,.38,;-1,-.38,;.34,.38,;.34,1.93,;1.67,2.69,;3,1.93,;3,.38,;4.34,2.69,;4.34,4.23,;5.67,5,;7,4.23,;7,2.69,;8.34,1.93,;8.34,.38,;9.67,-.38,;11.01,.38,;12.34,-.38,;11.01,1.93,;9.67,2.69,;5.67,1.93,;5.67,.38,;-1,2.69,;-2.33,1.93,;-3.67,2.69,;-5,-2.69,)|
Structure:
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