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Target
Tyrosine-protein kinase Mer
Ligand
BDBM396969
Substrate
n/a
Meas. Tech.
Enzymatic Assay
IC50
<5±n/a nM
Citation
 Li, Y; Wang, X; He, C Pyrrolotriazine compounds as tam inhibitors US Patent  US9981975 Publication Date 5/29/2018 
Target
Name:
Tyrosine-protein kinase Mer
Synonyms:
MER | MER intracellular domain/EGFR extracellular domain chimera | MERTK | MERTK_HUMAN | Proto-oncogene c-Mer | Proto-oncogene tyrosine-protein kinase MER | Receptor tyrosine kinase MerTK | Tyrosine-protein kinase Mer
Type:
PROTEIN
Mol. Mass.:
110234.77
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1498723
Residue:
999
Sequence:
MGPAPLPLLLGLFLPALWRRAITEAREEAKPYPLFPGPFPGSLQTDHTPLLSLPHASGYQPALMFSPTQPGRPHTGNVAIPQVTSVESKPLPPLAFKHTVGHIILSEHKGVKFNCSISVPNIYQDTTISWWKDGKELLGAHHAITQFYPDDEVTAIIASFSITSVQRSDNGSYICKMKINNEEIVSDPIYIEVQGLPHFTKQPESMNVTRNTAFNLTCQAVGPPEPVNIFWVQNSSRVNEQPEKSPSVLTVPGLTEMAVFSCEAHNDKGLTVSKGVQINIKAIPSPPTEVSIRNSTAHSILISWVPGFDGYSPFRNCSIQVKEADPLSNGSVMIFNTSALPHLYQIKQLQALANYSIGVSCMNEIGWSAVSPWILASTTEGAPSVAPLNVTVFLNESSDNVDIRWMKPPTKQQDGELVGYRISHVWQSAGISKELLEEVGQNGSRARISVQVHNATCTVRIAAVTRGGVGPFSDPVKIFIPAHGWVDYAPSSTPAPGNADPVLIIFGCFCGFILIGLILYISLAIRKRVQETKFGNAFTEEDSELVVNYIAKKSFCRRAIELTLHSLGVSEELQNKLEDVVIDRNLLILGKILGEGEFGSVMEGNLKQEDGTSLKVAVKTMKLDNSSQREIEEFLSEAACMKDFSHPNVIRLLGVCIEMSSQGIPKPMVILPFMKYGDLHTYLLYSRLETGPKHIPLQTLLKFMVDIALGMEYLSNRNFLHRDLAARNCMLRDDMTVCVADFGLSKKIYSGDYYRQGRIAKMPVKWIAIESLADRVYTSKSDVWAFGVTMWEIATRGMTPYPGVQNHEMYDYLLHGHRLKQPEDCLDELYEIMYSCWRTDPLDRPTFSVLRLQLEKLLESLPDVRNQADVIYVNTQLLESSEGLAQGSTLAPLDLNIDPDSIIASCTPRAAISVVTAEVHDSKPHEGRYILNGGSEEWEDLTSAPSAAVTAEKNSVLPGERLVRNGVSWSHSSMLPLGSSLPDELLFADDSSEGSEVLM
  
Inhibitor
Name:
BDBM396969
Synonyms:
N-{4-[4-Amino-7-(cis-4-cyanocyclohexyl)pyrrolo[2,1-f][1,2,4]triazin-5-yl]-3-fluorophenyl}-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide | US11591338, Example 31 | US9981975, Example 31
Type:
Small organic molecule
Emp. Form.:
C31H25F2N7O2
Mol. Mass.:
565.5727
SMILES:
Nc1ncnn2c(cc(-c3ccc(NC(=O)c4cccn(-c5ccc(F)cc5)c4=O)cc3F)c12)[C@@H]1CC[C@@H](CC1)C#N |r,wU:34.38,37.45,(-6.75,13.38,;-7.22,11.92,;-8.73,11.6,;-9.21,10.13,;-8.18,8.99,;-6.67,9.31,;-5.42,8.4,;-4.18,9.31,;-4.65,10.77,;-3.88,12.11,;-4.65,13.44,;-3.88,14.78,;-2.34,14.78,;-1.57,16.11,;-.03,16.11,;.74,14.78,;.74,17.44,;-.03,18.78,;.74,20.11,;2.28,20.11,;3.05,18.78,;4.59,18.78,;5.36,17.44,;6.9,17.44,;7.67,18.78,;9.21,18.78,;6.9,20.11,;5.36,20.11,;2.28,17.44,;3.05,16.11,;-1.57,13.44,;-2.34,12.11,;-1.57,10.77,;-6.19,10.77,;-5.42,6.86,;-6.76,6.09,;-6.76,4.55,;-5.42,3.78,;-4.09,4.55,;-4.09,6.09,;-5.42,2.24,;-5.42,.7,)|
Structure:
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