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Target
Tyrosine-protein kinase Mer
Ligand
BDBM397014
Substrate
n/a
Meas. Tech.
TAM Enzymatic Assay
IC50
7.5±n/a nM
Citation
 Li, Y; Wang, X; He, C Pyrrolotriazine compounds as TAM inhibitors US Patent  US10844069 Publication Date 11/24/2020 
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:
BDBM397014
Synonyms:
US10442810, Example 76 | US10844069, Example 76 | US11591338, Example 76 | US9981975, Example 76
Type:
Small organic molecule
Emp. Form.:
C35H36F2N8O4
Mol. Mass.:
670.7083
SMILES:
CC(C)C(=O)N1CCC(CC1)c1cc(-c2ccc(NC(=O)c3cn(C(C)C)c(=O)n(-c4cc(F)ccc4F)c3=O)cc2)c2c(N)ncnn12 |(2.27,-10.37,;1.18,-11.46,;1.57,-12.95,;-.31,-11.06,;-1.4,-12.15,;-.71,-9.57,;-2.2,-9.17,;-2.6,-7.69,;-1.51,-6.6,;-.02,-7,;.38,-8.48,;-1.91,-5.11,;-1,-3.86,;-1.91,-2.62,;-1.51,-1.13,;-.02,-.73,;.38,.75,;-.71,1.84,;-.31,3.33,;1.18,3.73,;2.27,2.64,;1.57,5.22,;3.06,5.62,;3.46,7.1,;4.95,7.5,;5.35,8.99,;6.04,6.41,;2.37,8.19,;2.77,9.68,;.88,7.79,;-.2,8.88,;.19,10.37,;-.89,11.46,;-.5,12.95,;-2.38,11.06,;-2.78,9.57,;-1.69,8.48,;-2.09,7,;.49,6.31,;-1,5.91,;-2.2,1.45,;-2.6,-.04,;-3.37,-3.09,;-4.7,-2.32,;-4.7,-.78,;-6.04,-3.09,;-6.04,-4.63,;-4.7,-5.4,;-3.37,-4.63,)|
Structure:
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