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TargetTyrosine-protein kinase Mer
LigandBDBM50469354
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1804040 (CHEMBL4276332)
IC50 2.0±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:
BDBM50469354
n/a
NameBDBM50469354
Synonyms:CHEMBL4286701
TypeSmall organic molecule
Emp. Form.C30H41N5O
Mol. Mass.487.6794
SMILESCCC[C@H](C)Nc1ncc2c(cn([C@H]3CC[C@H](O)CC3)c2n1)-c1ccc(CN2C3CCC2CC3)cc1 |r,wU:13.12,wD:16.16,3.3,(1.56,-13,;2.9,-12.23,;4.23,-13,;5.56,-12.23,;5.57,-10.69,;6.9,-13,;8.23,-12.23,;8.23,-10.69,;9.56,-9.92,;10.9,-10.68,;12.37,-10.2,;13.29,-11.45,;12.37,-12.71,;13.12,-14.05,;14.66,-14.08,;15.4,-15.43,;14.6,-16.75,;15.34,-18.1,;13.06,-16.71,;12.32,-15.37,;10.9,-12.23,;9.57,-13,;13.09,-8.84,;14.63,-8.78,;15.34,-7.41,;14.51,-6.11,;15.23,-4.75,;16.76,-4.68,;19.39,-4.51,;20.2,-5.75,;19.01,-5.26,;18.13,-4.25,;18.77,-2.81,;19.88,-3.2,;12.97,-6.18,;12.26,-7.55,)|
Structure
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