| Reaction Details |
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 | Report a problem with these data |
| Target | Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12 |
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| Ligand | BDBM498166 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | TR-FRET Assay |
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| IC50 | 1.70±n/a nM |
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| Citation |  Zhou, B; Luo, C; Yang, Y; Zhang, Y; Du, D; Jiang, H; Qiao, G; Wang, X Triazolopyrimidine, triazolopyridine compounds, and the composition thereof for treating PRC2-mediated diseases US Patent US11013745 Publication Date 5/25/2021 |
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| More Info.: | Get all data from this article, Assay Method |
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| Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12 |
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| Name: | Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12 |
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| Synonyms: | 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 4 components. |
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| Component 1 |
| Name: | Polycomb protein EED [40-441] |
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| Synonyms: | EED | EED_HUMAN | Polycomb protein EED (EED) |
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| Type: | Protein |
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| Mol. Mass.: | 46101.42 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Human polycomb protein EED (40-441 aa) |
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| Residue: | 402 |
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| Sequence: | DAVSIESGTNTERPDTPTNTPNAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGV
QFNWHSKEGDPLVFATVGSNRVTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTS
HPLLAVAGSRGIIRIINPITMQCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWN
IQTDTLVAIFGGVEGHRDEVLSADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYD
YNPNKTNRPFISQKIHFPDFSTRDIHRNYVDCVRWLGDLILSKSCENAIVCWKPGKMEDD
IDKIKPSESNVTILGRFDYSQCDIWYMRFSMDFWQKMLALGNQVGKLYVWDLEVEDPHKA
KCTTLTHHKCGAAIRQTSFSRDSSILIAVCDDASIWRWDRLR
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| Component 2 |
| 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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| Component 3 |
| Name: | Histone-binding protein RBBP4 |
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| Synonyms: | RBAP48 | RBBP4 | RBBP4_HUMAN | Retinoblastoma-binding protein p48 (RBAP48) |
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| Type: | Protein |
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| Mol. Mass.: | 47627.91 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q09028 |
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| Residue: | 425 |
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| Sequence: | MADKEAAFDDAVEERVINEEYKIWKKNTPFLYDLVMTHALEWPSLTAQWLPDVTRPEGKD
FSIHRLVLGTHTSDEQNHLVIASVQLPNDDAQFDASHYDSEKGEFGGFGSVSGKIEIEIK
INHEGEVNRARYMPQNPCIIATKTPSSDVLVFDYTKHPSKPDPSGECNPDLRLRGHQKEG
YGLSWNPNLSGHLLSASDDHTICLWDISAVPKEGKVVDAKTIFTGHTAVVEDVSWHLLHE
SLFGSVADDQKLMIWDTRSNNTSKPSHSVDAHTAEVNCLSFNPYSEFILATGSADKTVAL
WDLRNLKLKLHSFESHKDEIFQVQWSPHNETILASSGTDRRLNVWDLSKIGEEQSPEDAE
DGPPELLFIHGGHTAKISDFSWNPNEPWVICSVSEDNIMQVWQMAENIYNDEDPEGSVDP
EGQGS
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| Component 4 |
| 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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| BDBM498166 |
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| n/a |
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| Name | BDBM498166 |
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| Synonyms: | US11013745, Compound SL-E14 |
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| Type | Small organic molecule |
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| Emp. Form. | C21H23FN6O3S |
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| Mol. Mass. | 458.509 |
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| SMILES | CS(=O)(=O)N1CCC=C(CC1)c1cnc(NCc2c3CCOc3ccc2F)n2cnnc12 |c:7| |
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| Structure | 
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