Reaction Details |
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Target | Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 |
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Ligand | BDBM259341 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Scintillation Proximity Assay (SPA) |
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IC50 | 13±n/a nM |
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Citation | Blackledge, Jr., CW; Burgess, JL; Johnson, NW; Kasparec, J; Knight, SD; LaFrance, III, LV; Luengo, JI; Miller, WH; Newlander, KA; Romeril, SP; Schulz, M; Su, D; Tian, X Enhancer of zeste homolog 2 inhibitors US Patent US9505745 Publication Date 11/29/2016 |
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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/Polycomb protein SUZ12/Zinc finger protein AEBP2 |
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Name: | Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 |
Synonyms: | PRC2 complex | Polycomb Repressor Complex 2 (PRC2) |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 5 components. |
Component 1 |
Name: | Polycomb protein EED |
Synonyms: | EED | EED_HUMAN | WAIT-1 | WD protein associating with integrin cytoplasmic tails 1 | hEED |
Type: | Protein |
Mol. Mass.: | 50201.68 |
Organism: | Homo sapiens (Human) |
Description: | O75530 |
Residue: | 441 |
Sequence: | MSEREVSTAPAGTDMPAAKKQKLSSDENSNPDLSGDENDDAVSIESGTNTERPDTPTNTP
NAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNR
VTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIINPITM
QCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLVAIFGGVEGHRDEVL
SADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYDYNPNKTNRPFISQKIHFPDFS
TRDIHRNYVDCVRWLGDLILSKSCENAIVCWKPGKMEDDIDKIKPSESNVTILGRFDYSQ
CDIWYMRFSMDFWQKMLALGNQVGKLYVWDLEVEDPHKAKCTTLTHHKCGAAIRQTSFSR
DSSILIAVCDDASIWRWDRLR
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Component 2 |
Name: | Polycomb protein SUZ12 |
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 |
Type: | Protein |
Mol. Mass.: | 83080.09 |
Organism: | Homo sapiens (Human) |
Description: | Q15022 |
Residue: | 739 |
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 |
Synonyms: | RBAP48 | RBBP4 | RBBP4_HUMAN | Retinoblastoma-binding protein p48 (RBAP48) |
Type: | Protein |
Mol. Mass.: | 47627.91 |
Organism: | Homo sapiens (Human) |
Description: | Q09028 |
Residue: | 425 |
Sequence: | MADKEAAFDDAVEERVINEEYKIWKKNTPFLYDLVMTHALEWPSLTAQWLPDVTRPEGKD
FSIHRLVLGTHTSDEQNHLVIASVQLPNDDAQFDASHYDSEKGEFGGFGSVSGKIEIEIK
INHEGEVNRARYMPQNPCIIATKTPSSDVLVFDYTKHPSKPDPSGECNPDLRLRGHQKEG
YGLSWNPNLSGHLLSASDDHTICLWDISAVPKEGKVVDAKTIFTGHTAVVEDVSWHLLHE
SLFGSVADDQKLMIWDTRSNNTSKPSHSVDAHTAEVNCLSFNPYSEFILATGSADKTVAL
WDLRNLKLKLHSFESHKDEIFQVQWSPHNETILASSGTDRRLNVWDLSKIGEEQSPEDAE
DGPPELLFIHGGHTAKISDFSWNPNEPWVICSVSEDNIMQVWQMAENIYNDEDPEGSVDP
EGQGS
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Component 4 |
Name: | Zinc finger protein AEBP2 |
Synonyms: | AEBP2 | AEBP2_HUMAN | Adipocyte enhancer-binding protein 2 (AEBP2) | Zinc finger protein AEBP2 |
Type: | Protein |
Mol. Mass.: | 54448.84 |
Organism: | Homo sapiens (Human) |
Description: | Q6ZN18 |
Residue: | 517 |
Sequence: | MAAAITDMADLEELSRLSPLPPGSPGSAARGRAEPPEEEEEEEEEEEEAEAEAVAALLLN
GGSGGGGGGGGGGVGGGEAETMSEPSPESASQAGEDEDEEEDDEEEEDESSSSGGGEEES
SAESLVGSSGGSSSDETRSLSPGAASSSSGDGDGKEGLEEPKGPRGSQGGGGGGSSSSSV
VSSGGDEGYGTGGGGSSATSGGRRGSLEMSSDGEPLSRMDSEDSISSTIMDVDSTISSGR
STPAMMNGQGSTTSSSKNIAYNCCWDQCQACFNSSPDLADHIRSIHVDGQRGGVFVCLWK
GCKVYNTPSTSQSWLQRHMLTHSGDKPFKCVVGGCNASFASQGGLARHVPTHFSQQNSSK
VSSQPKAKEESPSKAGMNKRRKLKNKRRRSLPRPHDFFDAQTLDAIRHRAICFNLSAHIE
SLGKGHSVVFHSTVIAKRKEDSGKIKLLLHWMPEDILPDVWVNESERHQLKTKVVHLSKL
PKDTALLLDPNIYRTMPQKRLKRTLIRKVFNLYLSKQ
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Component 5 |
Name: | Histone-lysine N-methyltransferase EZH2 |
Synonyms: | ENX-1 | EZH2 | EZH2_HUMAN | Enhancer of zeste homolog 2 (EZH2) | Histone-lysine N-methyltransferase EZH2 | KMT6 | Lysine N-methyltransferase 6 |
Type: | Protein |
Mol. Mass.: | 85367.84 |
Organism: | Homo sapiens (Human) |
Description: | Q15910 |
Residue: | 746 |
Sequence: | MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
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BDBM259341 |
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n/a |
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Name | BDBM259341 |
Synonyms: | US9505745, 18 | US9790212, Example 18 |
Type | Small organic molecule |
Emp. Form. | C24H36N4O3S |
Mol. Mass. | 460.633 |
SMILES | CCN([C@H]1CC[C@@H](CC1)N(C)C)c1scc(C(=O)NCc2c(OC)cc(C)[nH]c2=O)c1C |r,wU:6.9,wD:3.2,(7.97,-10.65,;6.88,-9.56,;5.4,-9.96,;5,-11.45,;3.51,-11.84,;3.11,-13.33,;4.2,-14.42,;5.69,-14.02,;6.09,-12.53,;3.8,-15.91,;4.89,-17,;2.31,-16.31,;4.31,-8.87,;2.77,-8.87,;2.29,-7.4,;3.54,-6.5,;3.54,-4.96,;2.2,-4.19,;4.87,-4.19,;4.87,-2.65,;6.2,-1.88,;7.54,-2.65,;7.54,-4.19,;8.87,-4.96,;8.87,-1.88,;8.87,-.34,;10.21,.43,;7.54,.43,;6.2,-.34,;4.87,.43,;4.78,-7.4,;6.27,-7.01,)| |
Structure |
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