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Target
Tyrosine-protein kinase Mer
Ligand
BDBM50384590
Substrate
n/a
Meas. Tech.
ChEMBL_820659 (CHEMBL2037930)
IC50
210±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:
BDBM50384590
Synonyms:
CHEMBL2036626
Type:
Small organic molecule
Emp. Form.:
C19H23N5O
Mol. Mass.:
337.4188
SMILES:
CNc1ncc2c(nn(C[C@H]3CC[C@H](O)CC3)c2n1)-c1ccccc1 |r,wU:10.9,wD:13.13,(55.74,2.99,;57.07,2.22,;58.4,2.99,;58.41,4.53,;59.73,5.3,;61.07,4.54,;62.54,5.02,;63.46,3.76,;62.55,2.51,;63.02,1.05,;61.99,-.1,;62.47,-1.55,;61.43,-2.69,;59.92,-2.37,;58.89,-3.51,;59.45,-.9,;60.48,.23,;61.07,2.99,;59.74,2.22,;63.02,6.48,;64.53,6.8,;65.01,8.26,;63.98,9.41,;62.47,9.08,;62,7.62,)|
Structure:
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