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TargetTyrosine-protein kinase Mer
LigandBDBM628989
Substrate/Competitorn/a
Meas. Tech.MERTK, AXL, TYRO3 Kinase Homogeneous Time Resolved Fluorescence (HTRF) Assay
IC50 0.600±n/a nM
Citation Tarby, CMNorris, DJLo, JCAhuja, VTSeitz, SPGavai, AVTokarski, JSRajasagi, MWichroski, MBroekema, M URACIL DERIVATIVES AS MER-AXL INHIBITORS US Patent US20230339891 Publication Date 10/26/2023
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:
BDBM628989
n/a
NameBDBM628989
Synonyms:N-{3-fluoro-4-[(2-{[2-(pyrrolidin-1-yl)pyrimidin-4-yl]amino}pyridin-4-yl)oxy]phenyl}-3-(4-fluorophenyl)-2,4-dioxo-1-(propan-2-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide | US20230339891, Example 103
TypeSmall organic molecule
Emp. Form.C33H30F2N8O4
Mol. Mass.640.6393
SMILESCC(C)n1cc(C(=O)Nc2ccc(Oc3ccnc(Nc4ccnc(n4)N4CCCC4)c3)c(F)c2)c(=O)n(-c2ccc(F)cc2)c1=O
Structure
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