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TargetTyrosine-protein kinase Mer
LigandBDBM50469350
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1804040 (CHEMBL4276332)
IC50 4.9±n/a nM
Citation Zhao, JZhang, DZhang, WStashko, MADeRyckere, DVasileiadi, EParker, REHunter, DLiu, QZhang, YNorris-Drouin, JLi, BDrewry, DHKireev, DGraham, DKEarp, HSFrye, SVWang, X Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group. J Med Chem61:10242-10254 (2018) [PubMed]  Article
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:
BDBM50469350
n/a
NameBDBM50469350
Synonyms:CHEMBL4284846
TypeSmall organic molecule
Emp. Form.C24H31N5O3
Mol. Mass.437.5346
SMILESCCC[C@H](C)Nc1ncc2c(cn([C@H]3CC[C@H](O)CC3)c2n1)-c1ccnc(c1)C(=O)OC |r,wU:13.12,wD:16.16,3.3,(1.51,-9.85,;2.84,-9.08,;4.18,-9.86,;5.51,-9.09,;5.51,-7.55,;6.84,-9.86,;8.18,-9.09,;8.18,-7.54,;9.51,-6.77,;10.84,-7.54,;12.32,-7.06,;13.23,-8.31,;12.32,-9.57,;13.07,-10.91,;14.6,-10.93,;15.35,-12.29,;14.55,-13.61,;15.29,-14.96,;13.01,-13.57,;12.27,-12.23,;10.84,-9.09,;9.51,-9.86,;13.03,-5.69,;12.21,-4.4,;12.91,-3.04,;14.46,-2.97,;15.28,-4.27,;14.57,-5.63,;16.82,-4.21,;17.54,-2.84,;17.65,-5.51,;16.93,-6.87,)|
Structure
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