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TargetTyrosine-protein kinase Mer
LigandBDBM396967
Substrate/Competitorn/a
Meas. Tech.TAM Enzymatic Assay
IC50>100±n/a nM
Citation Li, YWang, XHe, C Pyrrolotriazine compounds as TAM inhibitors US Patent US11591338 Publication Date 2/28/2023
More Info.:Get all data from this article,  Assay Method
 
Tyrosine-protein kinase Mer
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:
MGPAPLPLLLGLFLPALWRRAITEAREEAKPYPLFPGPFPGSLQTDHTPLLSLPHASGYQ
PALMFSPTQPGRPHTGNVAIPQVTSVESKPLPPLAFKHTVGHIILSEHKGVKFNCSISVP
NIYQDTTISWWKDGKELLGAHHAITQFYPDDEVTAIIASFSITSVQRSDNGSYICKMKIN
NEEIVSDPIYIEVQGLPHFTKQPESMNVTRNTAFNLTCQAVGPPEPVNIFWVQNSSRVNE
QPEKSPSVLTVPGLTEMAVFSCEAHNDKGLTVSKGVQINIKAIPSPPTEVSIRNSTAHSI
LISWVPGFDGYSPFRNCSIQVKEADPLSNGSVMIFNTSALPHLYQIKQLQALANYSIGVS
CMNEIGWSAVSPWILASTTEGAPSVAPLNVTVFLNESSDNVDIRWMKPPTKQQDGELVGY
RISHVWQSAGISKELLEEVGQNGSRARISVQVHNATCTVRIAAVTRGGVGPFSDPVKIFI
PAHGWVDYAPSSTPAPGNADPVLIIFGCFCGFILIGLILYISLAIRKRVQETKFGNAFTE
EDSELVVNYIAKKSFCRRAIELTLHSLGVSEELQNKLEDVVIDRNLLILGKILGEGEFGS
VMEGNLKQEDGTSLKVAVKTMKLDNSSQREIEEFLSEAACMKDFSHPNVIRLLGVCIEMS
SQGIPKPMVILPFMKYGDLHTYLLYSRLETGPKHIPLQTLLKFMVDIALGMEYLSNRNFL
HRDLAARNCMLRDDMTVCVADFGLSKKIYSGDYYRQGRIAKMPVKWIAIESLADRVYTSK
SDVWAFGVTMWEIATRGMTPYPGVQNHEMYDYLLHGHRLKQPEDCLDELYEIMYSCWRTD
PLDRPTFSVLRLQLEKLLESLPDVRNQADVIYVNTQLLESSEGLAQGSTLAPLDLNIDPD
SIIASCTPRAAISVVTAEVHDSKPHEGRYILNGGSEEWEDLTSAPSAAVTAEKNSVLPGE
RLVRNGVSWSHSSMLPLGSSLPDELLFADDSSEGSEVLM
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM396967
n/a
NameBDBM396967
Synonyms:N-{4-[4-Amino-7-(cis-4-cyanocyclohexyl)pyrrolo[2,1-f][1,2,4]triazin-5-yl]phenyl}-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide | US10442810, Example 29 | US10844069, Example 29 | US11591338, Example 29 | US9981975, Example 29
TypeSmall organic molecule
Emp. Form.C31H26FN7O2
Mol. Mass.547.5822
SMILESNc1ncnn2c(cc(-c3ccc(NC(=O)c4cccn(-c5ccc(F)cc5)c4=O)cc3)c12)[C@@H]1CC[C@@H](CC1)C#N |r,wU:33.37,36.44,(-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,;-2.34,12.11,;-1.57,13.44,;-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,;-3.88,14.78,;-4.65,13.44,;-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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