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Target
Tyrosine-protein kinase Mer
Ligand
BDBM50384600
Substrate
n/a
Meas. Tech.
ChEMBL_820659 (CHEMBL2037930)
IC50
18±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:
BDBM50384600
Synonyms:
CHEMBL2036792 | US9744172, Compound UNC00000563A
Type:
Small organic molecule
Emp. Form.:
C23H32N8
Mol. Mass.:
420.5538
SMILES:
CNc1ncc2c(nn(CC3CCC(N)CC3)c2n1)-c1ccc(cc1)N1CCNCC1 |(53.41,-28.01,;54.75,-28.78,;56.08,-28.01,;56.08,-26.46,;57.41,-25.69,;58.74,-26.46,;60.22,-25.98,;61.13,-27.23,;60.22,-28.49,;60.7,-29.95,;59.67,-31.09,;58.16,-30.76,;57.13,-31.9,;57.6,-33.37,;56.56,-34.51,;59.11,-33.69,;60.14,-32.55,;58.75,-28.01,;57.41,-28.78,;60.69,-24.51,;62.2,-24.2,;62.68,-22.74,;61.65,-21.59,;60.13,-21.92,;59.67,-23.38,;62.12,-20.13,;63.62,-19.81,;64.1,-18.35,;63.07,-17.2,;61.56,-17.52,;61.08,-18.99,)|
Structure:
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