| Reaction Details |
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 | Report a problem with these data |
| Target | Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12 |
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| Ligand | BDBM451074 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | EED-H3K27Me3 Peptide Competition Binding Assay by AlphaScreen |
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| IC50 | 3.00±n/a nM |
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| Citation |  Chan, HM; Fu, X; Gu, XJ; Huang, Y; Li, L; Mi, Y; Qi, W; Sendzik, M; Sun, Y; Wang, L; Yu, Z; Zhang, H; Zhang, JY; Zhang, M; Zhang, Q; Zhao, K Imidazolepyridine compounds and uses thereof US Patent US10676479 Publication Date 6/9/2020 |
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| More Info.: | Get all data from this article, Assay Method |
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| Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12 |
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| Name: | Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12 |
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| Synonyms: | EZH2/SUZ12/EED complex | Polycomb Repressive Complex 2 (PRC2) |
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| Type: | Protein |
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| Mol. Mass.: | n/a |
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| Description: | n/a |
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| Components: | This complex has 3 components. |
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| Component 1 |
| Name: | Polycomb protein EED |
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| Synonyms: | EED | EED_HUMAN | WAIT-1 | WD protein associating with integrin cytoplasmic tails 1 | hEED |
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| Type: | Protein |
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| Mol. Mass.: | 50201.68 |
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| Organism: | Homo sapiens (Human) |
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| Description: | O75530 |
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| Residue: | 441 |
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| Sequence: | MSEREVSTAPAGTDMPAAKKQKLSSDENSNPDLSGDENDDAVSIESGTNTERPDTPTNTP
NAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNR
VTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIINPITM
QCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLVAIFGGVEGHRDEVL
SADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYDYNPNKTNRPFISQKIHFPDFS
TRDIHRNYVDCVRWLGDLILSKSCENAIVCWKPGKMEDDIDKIKPSESNVTILGRFDYSQ
CDIWYMRFSMDFWQKMLALGNQVGKLYVWDLEVEDPHKAKCTTLTHHKCGAAIRQTSFSR
DSSILIAVCDDASIWRWDRLR
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| Component 2 |
| Name: | Histone-lysine N-methyltransferase EZH2 |
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| Synonyms: | ENX-1 | EZH2 | EZH2_HUMAN | Enhancer of zeste homolog 2 (EZH2) | Histone-lysine N-methyltransferase EZH2 | KMT6 | Lysine N-methyltransferase 6 |
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| Type: | Protein |
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| Mol. Mass.: | 85367.84 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q15910 |
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| Residue: | 746 |
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| Sequence: | MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
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| Component 3 |
| Name: | Polycomb protein SUZ12 |
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| Synonyms: | CHET9 | ChET 9 protein | Chromatin precipitated E2F target 9 protein | JJAZ1 | Joined to JAZF1 protein | KIAA0160 | Polycomb protein SUZ12 | Polycomb protein SUZ12 (SUZ12) | SUZ12 | SUZ12_HUMAN | Suppressor of zeste 12 protein homolog |
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| Type: | Protein |
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| Mol. Mass.: | 83080.09 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q15022 |
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| Residue: | 739 |
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| Sequence: | MAPQKHGGGGGGGSGPSAGSGGGGFGGSAAVAAATASGGKSGGGSCGGGGSYSASSSSSA
AAAAGAAVLPVKKPKMEHVQADHELFLQAFEKPTQIYRFLRTRNLIAPIFLHRTLTYMSH
RNSRTNIKRKTFKVDDMLSKVEKMKGEQESHSLSAHLQLTFTGFFHKNDKPSPNSENEQN
SVTLEVLLVKVCHKKRKDVSCPIRQVPTGKKQVPLNPDLNQTKPGNFPSLAVSSNEFEPS
NSHMVKSYSLLFRVTRPGRREFNGMINGETNENIDVNEELPARRKRNREDGEKTFVAQMT
VFDKNRRLQLLDGEYEVAMQEMEECPISKKRATWETILDGKRLPPFETFSQGPTLQFTLR
WTGETNDKSTAPIAKPLATRNSESLHQENKPGSVKPTQTIAVKESLTTDLQTRKEKDTPN
ENRQKLRIFYQFLYNNNTRQQTEARDDLHCPWCTLNCRKLYSLLKHLKLCHSRFIFNYVY
HPKGARIDVSINECYDGSYAGNPQDIHRQPGFAFSRNGPVKRTPITHILVCRPKRTKASM
SEFLESEDGEVEQQRTYSSGHNRLYFHSDTCLPLRPQEMEVDSEDEKDPEWLREKTITQI
EEFSDVNEGEKEVMKLWNLHVMKHGFIADNQMNHACMLFVENYGQKIIKKNLCRNFMLHL
VSMHDFNLISIMSIDKAVTKLREMQQKLEKGESASPANEEITEEQNGTANGFSEINSKEK
ALETDSVSGVSKQSKKQKL
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| BDBM451074 |
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| n/a |
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| Name | BDBM451074 |
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| Synonyms: | 8-(2,4-dimethylpyrimidin-5-yl)-1-(ethylsulfonyl)- | US10676479, Example 104 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H23FN6O3S |
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| Mol. Mass. | 482.531 |
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| SMILES | CCS(=O)(=O)c1ncn2c(NCc3c4CCOc4ccc3F)ncc(-c3cnc(C)nc3C)c12 |
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| Structure | 
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