Reaction Details |
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Target | Tyrosine-protein kinase Mer |
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Ligand | BDBM308455 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1804040 (CHEMBL4276332) |
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IC50 | 4.4±n/a nM |
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Citation | Zhao, J; Zhang, D; Zhang, W; Stashko, MA; DeRyckere, D; Vasileiadi, E; Parker, RE; Hunter, D; Liu, Q; Zhang, Y; Norris-Drouin, J; Li, B; Drewry, DH; Kireev, D; Graham, DK; Earp, HS; Frye, SV; Wang, X Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group. J Med Chem61:10242-10254 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Tyrosine-protein kinase Mer |
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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: | MGPAPLPLLLGLFLPALWRRAITEAREEAKPYPLFPGPFPGSLQTDHTPLLSLPHASGYQ
PALMFSPTQPGRPHTGNVAIPQVTSVESKPLPPLAFKHTVGHIILSEHKGVKFNCSISVP
NIYQDTTISWWKDGKELLGAHHAITQFYPDDEVTAIIASFSITSVQRSDNGSYICKMKIN
NEEIVSDPIYIEVQGLPHFTKQPESMNVTRNTAFNLTCQAVGPPEPVNIFWVQNSSRVNE
QPEKSPSVLTVPGLTEMAVFSCEAHNDKGLTVSKGVQINIKAIPSPPTEVSIRNSTAHSI
LISWVPGFDGYSPFRNCSIQVKEADPLSNGSVMIFNTSALPHLYQIKQLQALANYSIGVS
CMNEIGWSAVSPWILASTTEGAPSVAPLNVTVFLNESSDNVDIRWMKPPTKQQDGELVGY
RISHVWQSAGISKELLEEVGQNGSRARISVQVHNATCTVRIAAVTRGGVGPFSDPVKIFI
PAHGWVDYAPSSTPAPGNADPVLIIFGCFCGFILIGLILYISLAIRKRVQETKFGNAFTE
EDSELVVNYIAKKSFCRRAIELTLHSLGVSEELQNKLEDVVIDRNLLILGKILGEGEFGS
VMEGNLKQEDGTSLKVAVKTMKLDNSSQREIEEFLSEAACMKDFSHPNVIRLLGVCIEMS
SQGIPKPMVILPFMKYGDLHTYLLYSRLETGPKHIPLQTLLKFMVDIALGMEYLSNRNFL
HRDLAARNCMLRDDMTVCVADFGLSKKIYSGDYYRQGRIAKMPVKWIAIESLADRVYTSK
SDVWAFGVTMWEIATRGMTPYPGVQNHEMYDYLLHGHRLKQPEDCLDELYEIMYSCWRTD
PLDRPTFSVLRLQLEKLLESLPDVRNQADVIYVNTQLLESSEGLAQGSTLAPLDLNIDPD
SIIASCTPRAAISVVTAEVHDSKPHEGRYILNGGSEEWEDLTSAPSAAVTAEKNSVLPGE
RLVRNGVSWSHSSMLPLGSSLPDELLFADDSSEGSEVLM
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BDBM308455 |
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n/a |
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Name | BDBM308455 |
Synonyms: | US9649309, Compound UNC2541A |
Type | Small organic molecule |
Emp. Form. | C24H34FN7O2 |
Mol. Mass. | 471.5709 |
SMILES | N[C@H]1CCCCNc2nc(NCCCCCCNC1=O)ncc2C(=O)NCc1ccc(F)cc1 |r| |
Structure |
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