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Target
Tyrosine-protein kinase Mer
Ligand
BDBM50577089
Substrate
n/a
Meas. Tech.
ChEMBL_2129273 (CHEMBL4838702)
IC50
2.6±n/a nM
Citation
 Zheng, H; Zhao, J; Li, B; Zhang, W; Stashko, MA; Minson, KA; Huey, MG; Zhou, Y; Earp, HS; Kireev, D; Graham, DK; DeRyckere, D; Frye, SV; Wang, X UNC5293, a potent, orally available and highly MERTK-selective inhibitor. Eur J Med Chem 220:0 (2021) [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:
BDBM50577089
Synonyms:
CHEMBL4850498
Type:
Small organic molecule
Emp. Form.:
C22H35N5O
Mol. Mass.:
385.5462
SMILES:
CCC[C@H](C)Nc1ncc2c(cn([C@H]3CC[C@H](O)CC3)c2n1)C1CCNCC1 |r,wU:13.12,wD:16.16,3.3,(3.79,-11.34,;5.12,-10.57,;6.45,-11.34,;7.79,-10.57,;7.79,-9.03,;9.12,-11.34,;10.46,-10.57,;10.46,-9.03,;11.79,-8.26,;13.12,-9.02,;14.59,-8.55,;15.5,-9.79,;14.59,-11.04,;15.07,-12.51,;16.58,-12.81,;17.05,-14.29,;16.01,-15.43,;16.48,-16.9,;14.51,-15.1,;14.04,-13.64,;13.12,-10.57,;11.79,-11.34,;15.07,-7.09,;16.58,-6.77,;17.06,-5.31,;16.03,-4.16,;14.52,-4.48,;14.04,-5.95,)|
Structure:
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