| 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 | BDBM291871 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | AlphaScreen |
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| pH | 8±n/a |
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| IC50 | 3.50±n/a nM |
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| Comments | extracted |
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| Citation |  Chan, HM; 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 Triazolopyrimidine compounds and uses thereof US Patent US9580437 Publication Date 2/28/2017 |
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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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| BDBM291871 |
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| n/a |
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| Name | BDBM291871 |
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| Synonyms: | (2R)-1-(4-(5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl)-3,5-dimethyl-1H-pyrazol-1-yl)propan-2-ol | US11207325, Example 186 | US9580437, Example 186 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H24FN7O2 |
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| Mol. Mass. | 437.4701 |
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| SMILES | C[C@@H](O)Cn1nc(C)c(c1C)-c1cnc(NCc2c3CCOc3ccc2F)n2cnnc12 |r,wD:1.1,(-5.91,-2.6,;-6.31,-4.09,;-7.79,-4.49,;-5.22,-5.18,;-3.73,-4.78,;-2.48,-5.68,;-1.24,-4.78,;.1,-5.55,;-1.71,-3.31,;-3.25,-3.31,;-4.02,-1.98,;-.63,-2.22,;.86,-2.62,;1.95,-1.53,;1.55,-.05,;2.64,1.04,;4.13,.64,;5.22,1.73,;4.82,3.22,;3.45,3.92,;3.69,5.44,;5.21,5.68,;5.91,4.31,;7.4,3.91,;7.79,2.42,;6.71,1.34,;7.1,-.15,;.06,.35,;-.63,1.73,;-2.16,1.48,;-2.4,-.04,;-1.02,-.74,)| |
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| Structure | 
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