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Target
Tyrosine-protein kinase Mer
Ligand
BDBM50384579
Substrate
n/a
Meas. Tech.
ChEMBL_820659 (CHEMBL2037930)
IC50
13±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:
BDBM50384579
Synonyms:
CHEMBL2036794 | US9744172, Compound UNC00000343A
Type:
Small organic molecule
Emp. Form.:
C21H28N6
Mol. Mass.:
364.4872
SMILES:
CCCNc1ncc2c(nn(CC3CCC(N)CC3)c2n1)-c1ccccc1 |(4.32,-43.39,;5.65,-44.16,;5.65,-45.7,;6.98,-46.48,;8.32,-45.71,;8.32,-44.16,;9.65,-43.39,;10.98,-44.16,;12.46,-43.68,;13.37,-44.93,;12.46,-46.19,;12.94,-47.65,;11.91,-48.79,;10.4,-48.46,;9.37,-49.6,;9.84,-51.07,;8.8,-52.21,;11.34,-51.39,;12.38,-50.25,;10.98,-45.71,;9.65,-46.48,;12.93,-42.21,;14.44,-41.89,;14.92,-40.43,;13.89,-39.29,;12.37,-39.61,;11.91,-41.08,)|
Structure:
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