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Target
Tyrosine-protein kinase Mer
Ligand
BDBM50384598
Substrate
n/a
Meas. Tech.
ChEMBL_820659 (CHEMBL2037930)
IC50
56±n/a nM
Citation
 Liu, J; Yang, C; Simpson, C; Deryckere, D; Van Deusen, A; Miley, MJ; Kireev, D; Norris-Drouin, J; Sather, S; Hunter, D; Korboukh, VK; Patel, HS; Janzen, WP; Machius, M; Johnson, GL; Earp, HS; Graham, DK; Frye, SV; Wang, X Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia. ACS Med Chem Lett 3:129-134 (2012) [PubMed]  Article 
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:
BDBM50384598
Synonyms:
CHEMBL2036788 | US9744172, Compound UNC00000393A
Type:
Small organic molecule
Emp. Form.:
C25H28N6
Mol. Mass.:
412.53
SMILES:
CNc1ncc2c(nn(CC3CCC(N)CC3)c2n1)-c1ccc(cc1)-c1ccccc1 |(2.22,-28.77,;3.55,-29.54,;4.89,-28.77,;4.89,-27.22,;6.22,-26.45,;7.55,-27.22,;9.03,-26.74,;9.94,-27.99,;9.03,-29.25,;9.5,-30.71,;8.47,-31.86,;6.96,-31.52,;5.94,-32.66,;6.41,-34.13,;5.37,-35.27,;7.91,-34.45,;8.95,-33.31,;7.55,-28.77,;6.22,-29.54,;9.5,-25.27,;11.01,-24.96,;11.49,-23.49,;10.45,-22.35,;8.94,-22.68,;8.47,-24.14,;10.92,-20.89,;12.43,-20.57,;12.91,-19.11,;11.87,-17.96,;10.36,-18.29,;9.89,-19.75,)|
Structure:
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