Target
Tyrosine-protein kinase Mer
Ligand
BDBM401623
Substrate
n/a
Meas. Tech.
TAM Enzymatic Assay
IC50
300±n/a nM
Citation
 Li, YBurns, 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:
BDBM401623
Synonyms:
US10005788, 4 (2nd peak)
Type:
Small organic molecule
Emp. Form.:
C23H28N6O
Mol. Mass.:
404.508
SMILES:
CCCCNc1ncc2c(nc([C@@H]3CC[C@H](O)CC3)n2n1)-c1ccc2[nH]ccc2c1 |r,wU:12.11,15.15,(15.09,6.46,;13.58,6.14,;13.11,4.67,;11.6,4.35,;11.12,2.89,;9.62,2.57,;8.59,3.71,;7.08,3.39,;6.6,1.93,;5.2,1.3,;5.36,-.23,;6.87,-.55,;7.49,-1.96,;6.59,-3.2,;7.21,-4.61,;8.74,-4.77,;9.37,-6.18,;9.65,-3.52,;9.02,-2.12,;7.64,.78,;9.14,1.1,;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,;1.2,2.07,;2.53,1.3,)|
Structure:
Search PDB for entries with ligand similarity: