| Reaction Details |
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 | Report a problem with these data |
| Target | Methylosome protein 50/Protein arginine N-methyltransferase 5 |
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| Ligand | BDBM578922 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | PRMT5:MEP50 FlashPlate Assay |
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| IC50 | 0.600±n/a nM |
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| Citation |  Bobinski, TP; Smith, CR; Marx, MA; Ketcham, JM; Burns, AC; Lawson, JD; Kulyk, S; Kuehler, J; Ivetac, A MTA-cooperative PRMT5 inhibitors US Patent US11492351 Publication Date 11/8/2022 |
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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 |
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| Synonyms: | PRMT5 | PRMT5/MEP50 | PRMT5/MEP50 Enzyme | PRMT5/MEP50 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 2 components. |
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| Component 1 |
| Name: | Protein arginine N-methyltransferase 5 |
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| 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 |
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| Type: | Enzyme |
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| Mol. Mass.: | 72679.99 |
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| Organism: | Homo sapiens (Human) |
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| Description: | O14744 |
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| Residue: | 637 |
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| Sequence: | MAAMAVGGAGGSRVSSGRDLNCVPEIADTLGAVAKQGFDFLCMPVFHPRFKREFIQEPAK
NRPGPQTRSDLLLSGRDWNTLIVGKLSPWIRPDSKVEKIRRNSEAAMLQELNFGAYLGLP
AFLLPLNQEDNTNLARVLTNHIHTGHHSSMFWMRVPLVAPEDLRDDIIENAPTTHTEEYS
GEEKTWMWWHNFRTLCDYSKRIAVALEIGADLPSNHVIDRWLGEPIKAAILPTSIFLTNK
KGFPVLSKMHQRLIFRLLKLEVQFIITGTNHHSEKEFCSYLQYLEYLSQNRPPPNAYELF
AKGYEDYLQSPLQPLMDNLESQTYEVFEKDPIKYSQYQQAIYKCLLDRVPEEEKDTNVQV
LMVLGAGRGPLVNASLRAAKQADRRIKLYAVEKNPNAVVTLENWQFEEWGSQVTVVSSDM
REWVAPEKADIIVSELLGSFADNELSPECLDGAQHFLKDDGVSIPGEYTSFLAPISSSKL
YNEVRACREKDRDPEAQFEMPYVVRLHNFHQLSAPQPCFTFSHPNRDPMIDNNRYCTLEF
PVEVNTVLHGFAGYFETVLYQDITLSIRPETHSPGMFSWFPILFPIKQPITVREGQTICV
RFWRCSNSKKVWYEWAVTAPVCSAIHNPTGRSYTIGL
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| Component 2 |
| Name: | Methylosome protein 50 |
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| Synonyms: | Androgen receptor cofactor p44 | MEP-50 | MEP50 | MEP50_HUMAN | Nbla10071 | WD repeat-containing protein 77 | WD45 | WDR77 | p44/Mep50 |
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| Type: | Enzyme |
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| Mol. Mass.: | 36713.38 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q9BQA1 |
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| Residue: | 342 |
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| Sequence: | MRKETPPPLVPPAAREWNLPPNAPACMERQLEAARYRSDGALLLGASSLSGRCWAGSLWL
FKDPCAAPNEGFCSAGVQTEAGVADLTWVGERGILVASDSGAVELWELDENETLIVSKFC
KYEHDDIVSTVSVLSSGTQAVSGSKDICIKVWDLAQQVVLSSYRAHAAQVTCVAASPHKD
SVFLSCSEDNRILLWDTRCPKPASQIGCSAPGYLPTSLAWHPQQSEVFVFGDENGTVSLV
DTKSTSCVLSSAVHSQCVTGLVFSPHSVPFLASLSEDCSLAVLDSSLSELFRSQAHRDFV
RDATWSPLNHSLLTTVGWDHQVVHHVVPTEPLPAPGPASVTE
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| BDBM578922 |
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| n/a |
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| Name | BDBM578922 |
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| Synonyms: | 4-(aminomethyl)-6-(3-(methoxymethyl)-1H- pyrrolo[2,3-b]pyridin-5-yl)phthalazin-1(2H)- one | US11479551, Example 4-46 | US11492351, Example 4-46 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H17N5O2 |
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| Mol. Mass. | 335.3599 |
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| SMILES | COCc1c[nH]c2ncc(cc12)-c1ccc2c(c1)c(CN)n[nH]c2=O |
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| Structure | 
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