Target
Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12
Ligand
BDBM498089
Substrate
n/a
Meas. Tech.
TR-FRET Assay
IC50
611±n/a nM
Citation
 Zhou, BLuo, CYang, YZhang, YDu, DJiang, HQiao, GWang, X Triazolopyrimidine, triazolopyridine compounds, and the composition thereof for treating PRC2-mediated diseases US Patent  US11013745 Publication Date 5/25/2021 
Target
Name:
Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12
Synonyms:
Polycomb Repressive Complex 2 (PRC2)
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 4 components.
Component 1
Name:
Polycomb protein EED [40-441]
Synonyms:
EED | EED_HUMAN | Polycomb protein EED (EED)
Type:
Protein
Mol. Mass.:
46101.42
Organism:
Homo sapiens (Human)
Description:
Human polycomb protein EED (40-441 aa)
Residue:
402
Sequence:
DAVSIESGTNTERPDTPTNTPNAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNRVTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIINPITMQCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLVAIFGGVEGHRDEVLSADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYDYNPNKTNRPFISQKIHFPDFSTRDIHRNYVDCVRWLGDLILSKSCENAIVCWKPGKMEDDIDKIKPSESNVTILGRFDYSQCDIWYMRFSMDFWQKMLALGNQVGKLYVWDLEVEDPHKAKCTTLTHHKCGAAIRQTSFSRDSSILIAVCDDASIWRWDRLR
  
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:
MAPQKHGGGGGGGSGPSAGSGGGGFGGSAAVAAATASGGKSGGGSCGGGGSYSASSSSSAAAAAGAAVLPVKKPKMEHVQADHELFLQAFEKPTQIYRFLRTRNLIAPIFLHRTLTYMSHRNSRTNIKRKTFKVDDMLSKVEKMKGEQESHSLSAHLQLTFTGFFHKNDKPSPNSENEQNSVTLEVLLVKVCHKKRKDVSCPIRQVPTGKKQVPLNPDLNQTKPGNFPSLAVSSNEFEPSNSHMVKSYSLLFRVTRPGRREFNGMINGETNENIDVNEELPARRKRNREDGEKTFVAQMTVFDKNRRLQLLDGEYEVAMQEMEECPISKKRATWETILDGKRLPPFETFSQGPTLQFTLRWTGETNDKSTAPIAKPLATRNSESLHQENKPGSVKPTQTIAVKESLTTDLQTRKEKDTPNENRQKLRIFYQFLYNNNTRQQTEARDDLHCPWCTLNCRKLYSLLKHLKLCHSRFIFNYVYHPKGARIDVSINECYDGSYAGNPQDIHRQPGFAFSRNGPVKRTPITHILVCRPKRTKASMSEFLESEDGEVEQQRTYSSGHNRLYFHSDTCLPLRPQEMEVDSEDEKDPEWLREKTITQIEEFSDVNEGEKEVMKLWNLHVMKHGFIADNQMNHACMLFVENYGQKIIKKNLCRNFMLHLVSMHDFNLISIMSIDKAVTKLREMQQKLEKGESASPANEEITEEQNGTANGFSEINSKEKALETDSVSGVSKQSKKQKL
  
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:
MADKEAAFDDAVEERVINEEYKIWKKNTPFLYDLVMTHALEWPSLTAQWLPDVTRPEGKDFSIHRLVLGTHTSDEQNHLVIASVQLPNDDAQFDASHYDSEKGEFGGFGSVSGKIEIEIKINHEGEVNRARYMPQNPCIIATKTPSSDVLVFDYTKHPSKPDPSGECNPDLRLRGHQKEGYGLSWNPNLSGHLLSASDDHTICLWDISAVPKEGKVVDAKTIFTGHTAVVEDVSWHLLHESLFGSVADDQKLMIWDTRSNNTSKPSHSVDAHTAEVNCLSFNPYSEFILATGSADKTVALWDLRNLKLKLHSFESHKDEIFQVQWSPHNETILASSGTDRRLNVWDLSKIGEEQSPEDAEDGPPELLFIHGGHTAKISDFSWNPNEPWVICSVSEDNIMQVWQMAENIYNDEDPEGSVDPEGQGS
  
Component 4
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:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
  
Inhibitor
Name:
BDBM498089
Synonyms:
US11013745, Compound E-Y5
Type:
Small organic molecule
Emp. Form.:
C15H15N5OS
Mol. Mass.:
313.378
SMILES:
C(Nc1ncc(C2=CCSCC2)c2nncn12)c1ccco1 |t:6|
Structure:
Search PDB for entries with ligand similarity: