Reaction Details |
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Target | Methylosome protein 50/Protein arginine N-methyltransferase 5 |
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Ligand | BDBM515323 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Enzyme Methylation Assay |
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IC50 | 115±n/a nM |
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Citation | Machacek, MR; Witter, DJ; Reutershan, MH; Sloman, DL; Altman, MD PRMT5 inhibitors US Patent US11098059 Publication Date 8/24/2021 |
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More Info.: | Get all data from this article, Assay Method |
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Methylosome protein 50/Protein arginine N-methyltransferase 5 |
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Name: | Methylosome protein 50/Protein arginine N-methyltransferase 5 |
Synonyms: | PRMT5 | PRMT5/MEP50 | PRMT5/MEP50 Enzyme | PRMT5/MEP50 complex |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Protein arginine N-methyltransferase 5 |
Synonyms: | 72 kDa ICln-binding protein | ANM5_HUMAN | HRMT1L5 | Histone-arginine N-methyltransferase PRMT5 | IBP72 | JBP1 | Jak-binding protein 1 | PRMT5 | PRMT5/MEP50 complex | Protein arginine N-methyltransferase 5 (PRMT5) | Protein arginine methyltransferase 5 (PRMT5) | SKB1 | SKB1 homolog | SKB1Hs | Shk1 kinase-binding protein 1 homolog |
Type: | Enzyme |
Mol. Mass.: | 72679.99 |
Organism: | Homo sapiens (Human) |
Description: | O14744 |
Residue: | 637 |
Sequence: | MAAMAVGGAGGSRVSSGRDLNCVPEIADTLGAVAKQGFDFLCMPVFHPRFKREFIQEPAK
NRPGPQTRSDLLLSGRDWNTLIVGKLSPWIRPDSKVEKIRRNSEAAMLQELNFGAYLGLP
AFLLPLNQEDNTNLARVLTNHIHTGHHSSMFWMRVPLVAPEDLRDDIIENAPTTHTEEYS
GEEKTWMWWHNFRTLCDYSKRIAVALEIGADLPSNHVIDRWLGEPIKAAILPTSIFLTNK
KGFPVLSKMHQRLIFRLLKLEVQFIITGTNHHSEKEFCSYLQYLEYLSQNRPPPNAYELF
AKGYEDYLQSPLQPLMDNLESQTYEVFEKDPIKYSQYQQAIYKCLLDRVPEEEKDTNVQV
LMVLGAGRGPLVNASLRAAKQADRRIKLYAVEKNPNAVVTLENWQFEEWGSQVTVVSSDM
REWVAPEKADIIVSELLGSFADNELSPECLDGAQHFLKDDGVSIPGEYTSFLAPISSSKL
YNEVRACREKDRDPEAQFEMPYVVRLHNFHQLSAPQPCFTFSHPNRDPMIDNNRYCTLEF
PVEVNTVLHGFAGYFETVLYQDITLSIRPETHSPGMFSWFPILFPIKQPITVREGQTICV
RFWRCSNSKKVWYEWAVTAPVCSAIHNPTGRSYTIGL
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Component 2 |
Name: | Methylosome protein 50 |
Synonyms: | Androgen receptor cofactor p44 | MEP-50 | MEP50 | MEP50_HUMAN | Nbla10071 | WD repeat-containing protein 77 | WD45 | WDR77 | p44/Mep50 |
Type: | Enzyme |
Mol. Mass.: | 36713.38 |
Organism: | Homo sapiens (Human) |
Description: | Q9BQA1 |
Residue: | 342 |
Sequence: | MRKETPPPLVPPAAREWNLPPNAPACMERQLEAARYRSDGALLLGASSLSGRCWAGSLWL
FKDPCAAPNEGFCSAGVQTEAGVADLTWVGERGILVASDSGAVELWELDENETLIVSKFC
KYEHDDIVSTVSVLSSGTQAVSGSKDICIKVWDLAQQVVLSSYRAHAAQVTCVAASPHKD
SVFLSCSEDNRILLWDTRCPKPASQIGCSAPGYLPTSLAWHPQQSEVFVFGDENGTVSLV
DTKSTSCVLSSAVHSQCVTGLVFSPHSVPFLASLSEDCSLAVLDSSLSELFRSQAHRDFV
RDATWSPLNHSLLTTVGWDHQVVHHVVPTEPLPAPGPASVTE
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BDBM515323 |
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n/a |
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Name | BDBM515323 |
Synonyms: | 6-(hexahydro-3,6- epiminofuro[3,2-b]furan- 7-carbonyl)-2-((R)-2- hydroxy-2-((S)-1,2,3,4- tetrahydroisoquinolin-3- yl)ethyl)-4,4-dimethyl- 3,4-dihydroisoquinolin- 1(2H)-one | US11098059, Example 27 |
Type | Small organic molecule |
Emp. Form. | C29H33N3O5 |
Mol. Mass. | 503.5894 |
SMILES | CC1(C)CN(C[C@@H](O)[C@@H]2Cc3ccccc3CN2)C(=O)c2ccc(cc12)C(=O)N1C2COC3C1COC23 |r,TLB:26:28:30.31:36,30:29:32:34.35,31:32:28.29:34.35,THB:26:28:32:34.35,34:33:30.31:36,35:36:30.31:33.28| |
Structure |
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