Reaction Details |
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Target | Tyrosine-protein kinase Mer |
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Ligand | BDBM628989 |
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Substrate/Competitor | n/a |
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Meas. Tech. | MERTK, AXL, TYRO3 Kinase Homogeneous Time Resolved Fluorescence (HTRF) Assay |
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IC50 | 0.600±n/a nM |
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Citation | Tarby, CM; Norris, DJ; Lo, JC; Ahuja, VT; Seitz, SP; Gavai, AV; Tokarski, JS; Rajasagi, M; Wichroski, M; Broekema, M URACIL DERIVATIVES AS MER-AXL INHIBITORS US Patent US20230339891 Publication Date 10/26/2023 |
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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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BDBM628989 |
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n/a |
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Name | BDBM628989 |
Synonyms: | N-{3-fluoro-4-[(2-{[2-(pyrrolidin-1-yl)pyrimidin-4-yl]amino}pyridin-4-yl)oxy]phenyl}-3-(4-fluorophenyl)-2,4-dioxo-1-(propan-2-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide | US20230339891, Example 103 |
Type | Small organic molecule |
Emp. Form. | C33H30F2N8O4 |
Mol. Mass. | 640.6393 |
SMILES | CC(C)n1cc(C(=O)Nc2ccc(Oc3ccnc(Nc4ccnc(n4)N4CCCC4)c3)c(F)c2)c(=O)n(-c2ccc(F)cc2)c1=O |
Structure |
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