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Target
Tyrosine-protein kinase Mer
Ligand
BDBM401630
Substrate
n/a
Meas. Tech.
TAM Enzymatic Assay
IC50
<100±n/a nM
Citation
 Li, Y; Burns, DM Bicyclic fused pyrimidine compounds as TAM inhibitors US Patent  US10005788 Publication Date 6/26/2018 
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:
BDBM401630
Synonyms:
US10005788, 8 (1st peak)
Type:
Small organic molecule
Emp. Form.:
C22H29N5O2
Mol. Mass.:
395.498
SMILES:
CCCCNc1ncc2c(nc([C@H]3CC[C@H](O)CC3)n2n1)-c1cccc(CO)c1 |r,wU:15.15,wD:12.11,(10.53,1.3,;9.2,2.07,;7.87,1.3,;6.53,2.07,;5.2,1.3,;3.86,2.07,;3.86,3.61,;2.53,4.38,;1.2,3.61,;-.27,4.09,;-1.17,2.84,;-.27,1.6,;-.74,.13,;-2.25,-.19,;-2.73,-1.65,;-1.7,-2.8,;-2.17,-4.26,;-.19,-2.48,;.29,-1.01,;1.2,2.07,;2.53,1.3,;-.74,5.55,;.29,6.7,;-.19,8.16,;-1.7,8.48,;-2.73,7.34,;-4.23,7.66,;-5.26,6.51,;-2.25,5.87,)|
Structure:
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