Reaction Details |
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Target | DNA (cytosine-5)-methyltransferase 1 (DNMT1) |
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Ligand | BDBM50448485 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1294384 |
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IC50 | 265000±n/a nM |
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Citation | Valente S; Liu Y; Schnekenburger M; Zwergel C; Cosconati S; Gros C; Tardugno M; Labella D; Florean C; Minden S; Hashimoto H; Chang Y; Zhang X; Kirsch G; Novellino E; Arimondo PB; Miele E; Ferretti E; Gulino A; Diederich M; Cheng X; Mai A Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells. J Med Chem 57:701-13 (2014) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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DNA (cytosine-5)-methyltransferase 1 (DNMT1) |
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Name: | DNA (cytosine-5)-methyltransferase 1 |
Synonyms: | CXXC-type zinc finger protein 9 | DNA (cytosine-5)-methyltransferase 1 | DNA (cytosine-5)-methyltransferase 1 isoform b | DNA MTase HsaI | DNA methyltransferase HsaI | Dnmt1 | M.HsaI | MCMT |
Type: | Enzyme |
Mol. Mass.: | 183184.85 |
Organism: | Homo sapiens (Human) |
Description: | P26358 |
Residue: | 1616 |
Sequence: | MPARTAPARVPTLAVPAISLPDDVRRRLKDLERDSLTEKECVKEKLNLLHEFLQTEIKNQ
LCDLETKLRKEELSEEGYLAKVKSLLNKDLSLENGAHAYNREVNGRLENGNQARSEARRV
GMADANSPPKPLSKPRTPRRSKSDGEAKPEPSPSPRITRKSTRQTTITSHFAKGPAKRKP
QEESERAKSDESIKEEDKDQDEKRRRVTSRERVARPLPAEEPERAKSGTRTEKEEERDEK
EEKRLRSQTKEPTPKQKLKEEPDREARAGVQADEDEDGDEKDEKKHRSQPKDLAAKRRPE
EKEPEKVNPQISDEKDEDEKEEKRRKTTPKEPTEKKMARAKTVMNSKTHPPKCIQCGQYL
DDPDLKYGQHPPDAVDEPQMLTNEKLSIFDANESGFESYEALPQHKLTCFSVYCKHGHLC
PIDTGLIEKNIELFFSGSAKPIYDDDPSLEGGVNGKNLGPINEWWITGFDGGEKALIGFS
TSFAEYILMDPSPEYAPIFGLMQEKIYISKIVVEFLQSNSDSTYEDLINKIETTVPPSGL
NLNRFTEDSLLRHAQFVVEQVESYDEAGDSDEQPIFLTPCMRDLIKLAGVTLGQRRAQAR
RQTIRHSTREKDRGPTKATTTKLVYQIFDTFFAEQIEKDDREDKENAFKRRRCGVCEVCQ
QPECGKCKACKDMVKFGGSGRSKQACQERRCPNMAMKEADDDEEVDDNIPEMPSPKKMHQ
GKKKKQNKNRISWVGEAVKTDGKKSYYKKVCIDAETLEVGDCVSVIPDDSSKPLYLARVT
ALWEDSSNGQMFHAHWFCAGTDTVLGATSDPLELFLVDECEDMQLSYIHSKVKVIYKAPS
ENWAMEGGMDPESLLEGDDGKTYFYQLWYDQDYARFESPPKTQPTEDNKFKFCVSCARLA
EMRQKEIPRVLEQLEDLDSRVLYYSATKNGILYRVGDGVYLPPEAFTFNIKLSSPVKRPR
KEPVDEDLYPEHYRKYSDYIKGSNLDAPEPYRIGRIKEIFCPKKSNGRPNETDIKIRVNK
FYRPENTHKSTPASYHADINLLYWSDEEAVVDFKAVQGRCTVEYGEDLPECVQVYSMGGP
NRFYFLEAYNAKSKSFEDPPNHARSPGNKGKGKGKGKGKPKSQACEPSEPEIEIKLPKLR
TLDVFSGCGGLSEGFHQAGISDTLWAIEMWDPAAQAFRLNNPGSTVFTEDCNILLKLVMA
GETTNSRGQRLPQKGDVEMLCGGPPCQGFSGMNRFNSRTYSKFKNSLVVSFLSYCDYYRP
RFFLLENVRNFVSFKRSMVLKLTLRCLVRMGYQCTFGVLQAGQYGVAQTRRRAIILAAAP
GEKLPLFPEPLHVFAPRACQLSVVVDDKKFVSNITRLSSGPFRTITVRDTMSDLPEVRNG
ASALEISYNGEPQSWFQRQLRGAQYQPILRDHICKDMSALVAARMRHIPLAPGSDWRDLP
NIEVRLSDGTMARKLRYTHHDRKNGRSSSGALRGVCSCVEAGKACDPAARQFNTLIPWCL
PHTGNRHNHWAGLYGRLEWDGFFSTTVTNPEPMGKQGRVLHPEQHRVVSVRECARSQGFP
DTYRLFGNILDKHRQVGNAVPPPLAKAIGLEIKLCMLAKARESASAKIKEEEAAKD
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BDBM50448485 |
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n/a |
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Name | BDBM50448485 |
Synonyms: | CHEMBL3126645 |
Type | Small organic molecule |
Emp. Form. | C27H23N7O |
Mol. Mass. | 461.5178 |
SMILES | Cc1cc(Nc2ccc(NC(=O)c3cccc(Nc4ccnc5ccccc45)c3)cc2)nc(N)n1 |
Structure |
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