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Target
Tyrosine-protein kinase Mer
Ligand
BDBM50444245
Substrate
n/a
Meas. Tech.
ChEMBL_1277932 (CHEMBL3094776)
IC50
6.7±n/a nM
Citation
 Zhang, W; McIver, AL; Stashko, MA; DeRyckere, D; Branchford, BR; Hunter, D; Kireev, D; Miley, MJ; Norris-Drouin, J; Stewart, WM; Lee, M; Sather, S; Zhou, Y; Di Paola, JA; Machius, M; Janzen, WP; Earp, HS; Graham, DK; Frye, SV; Wang, X Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem 56:9693-700 (2014) [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:
BDBM50444245
Synonyms:
CHEMBL3093752
Type:
Small organic molecule
Emp. Form.:
C26H38N6O3
Mol. Mass.:
482.6183
SMILES:
CCCCNc1ncc(C(=O)Nc2ccc(CN3CCOCC3)cc2)c(N[C@H]2CC[C@H](O)CC2)n1 |r,wU:27.28,wD:30.32,(21.61,-58.16,;22.95,-57.39,;24.28,-58.16,;25.61,-57.39,;26.95,-58.16,;28.28,-57.39,;29.62,-58.16,;30.95,-57.39,;30.95,-55.84,;32.28,-55.07,;32.27,-53.53,;33.61,-55.83,;34.95,-55.06,;36.28,-55.83,;37.61,-55.06,;37.6,-53.51,;38.93,-52.74,;40.27,-53.5,;40.27,-55.03,;41.6,-55.8,;42.93,-55.03,;42.93,-53.49,;41.59,-52.71,;36.26,-52.75,;34.93,-53.53,;29.61,-55.08,;29.61,-53.54,;28.27,-52.77,;26.94,-53.55,;25.6,-52.78,;25.6,-51.24,;24.27,-50.47,;26.94,-50.47,;28.26,-51.23,;28.28,-55.85,)|
Structure:
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