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Target
Tyrosine-protein kinase Mer
Ligand
BDBM246868
Substrate
n/a
Meas. Tech.
TAM Enzymatic Assay
Temperature
298.15±n/a K
IC50
300±n/a nM
Comments
extracted
Citation
 Li, Y; Burns, DM Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors US Patent  US9708333 Publication Date 7/18/2017 
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:
BDBM246868
Synonyms:
US10053465, 7 | US10065963, Compound 7 | US10125150, Example 7 | US10336759, # 7 | US10479803, Example 7 | US10519163, Example 7 | US10675284, Example 7 | US10875847, Compound INCB39110 | US11084822, Example 7 | US11130767, # 7 | US11136326, Example 7 | US11285140, Example 364 | US11304949, Compound 1 | US11324749, Comp. No. 1 | US11406640, Comp. No. 1 | US11596632, Comp. No. 1 | US9732097, Example 7 | US9999619, Example 364 | {1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl] piperidin-4- yl}-3-[4-(7H- pyrrolo[2,3- d]pyrimidin-4-yl)- 1H-pyrazol-1- yl]azetidin-3- yl}acetonitrile
Type:
Small organic molecule
Emp. Form.:
C26H23F4N9O
Mol. Mass.:
553.5141
SMILES:
Fc1c(ccnc1C(F)(F)F)C(=O)N1CCC(CC1)N1CC(CC#N)(C1)n1cc(cn1)-c1ncnc2[nH]ccc12
Structure:
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