| Reaction Details |
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 | Report a problem with these data |
| Target | Histone-binding protein RBBP4/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 |
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| Ligand | BDBM513693 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | Enzymatic Activity Assay |
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| IC50 | <100±n/a nM |
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| Citation |  Marx, MA; Lee, MR; Bobinski, TP; Burns, AC; Arora, N; Christensen, JG; Ketcham, JM Substituted imidazo[1,2-c]pyrimidines as PRC2 inhibitors US Patent US11485738 Publication Date 11/1/2022 |
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| More Info.: | Get all data from this article, Assay Method |
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| Histone-binding protein RBBP4/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 |
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| Name: | Histone-binding protein RBBP4/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 |
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| Synonyms: | Human PRC2 complex |
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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 5 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: | 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: | Zinc finger protein AEBP2 |
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| Synonyms: | AEBP2 | AEBP2_HUMAN | Adipocyte enhancer-binding protein 2 (AEBP2) | Zinc finger protein AEBP2 |
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| Type: | Protein |
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| Mol. Mass.: | 54448.84 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q6ZN18 |
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| Residue: | 517 |
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| Sequence: | MAAAITDMADLEELSRLSPLPPGSPGSAARGRAEPPEEEEEEEEEEEEAEAEAVAALLLN
GGSGGGGGGGGGGVGGGEAETMSEPSPESASQAGEDEDEEEDDEEEEDESSSSGGGEEES
SAESLVGSSGGSSSDETRSLSPGAASSSSGDGDGKEGLEEPKGPRGSQGGGGGGSSSSSV
VSSGGDEGYGTGGGGSSATSGGRRGSLEMSSDGEPLSRMDSEDSISSTIMDVDSTISSGR
STPAMMNGQGSTTSSSKNIAYNCCWDQCQACFNSSPDLADHIRSIHVDGQRGGVFVCLWK
GCKVYNTPSTSQSWLQRHMLTHSGDKPFKCVVGGCNASFASQGGLARHVPTHFSQQNSSK
VSSQPKAKEESPSKAGMNKRRKLKNKRRRSLPRPHDFFDAQTLDAIRHRAICFNLSAHIE
SLGKGHSVVFHSTVIAKRKEDSGKIKLLLHWMPEDILPDVWVNESERHQLKTKVVHLSKL
PKDTALLLDPNIYRTMPQKRLKRTLIRKVFNLYLSKQ
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| BDBM513693 |
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| n/a |
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| Name | BDBM513693 |
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| Synonyms: | US11091495, Example 54 | US11220509, Example 54 | US11485738, Example 54 |
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| Type | Small organic molecule |
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| Emp. Form. | C27H24F2N6O |
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| Mol. Mass. | 486.5159 |
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| SMILES | FC1CCN(Cc2ccc(cc2)-c2cnc(NCc3c4CCOc4ccc3F)n3cc(nc23)C#N)C1 |
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| Structure | 
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