| 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 | BDBM50572990 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2118744 (CHEMBL4827810) |
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| IC50 | 7500±n/a nM |
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| Citation |  McKinney, DC; McMillan, BJ; Ranaghan, MJ; Moroco, JA; Brousseau, M; Mullin-Bernstein, Z; O'Keefe, M; McCarren, P; Mesleh, MF; Mulvaney, KM; Robinson, F; Singh, R; Bajrami, B; Wagner, FF; Hilgraf, R; Drysdale, MJ; Campbell, AJ; Skepner, A; Timm, DE; Porter, D; Kaushik, VK; Sellers, WR; Ianari, A Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction. J Med Chem64:11148-11168 (2021) [PubMed] Article |
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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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| BDBM50572990 |
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| n/a |
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| Name | BDBM50572990 |
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| Synonyms: | CHEMBL4859105 |
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| Type | Small organic molecule |
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| Emp. Form. | C21H22ClN5O4S |
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| Mol. Mass. | 475.948 |
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| SMILES | C[C@@H](C(=O)Nc1ccc(C)c(c1)S(=O)(=O)NCCc1ccccn1)n1ncc(Cl)cc1=O |r| |
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| Structure | 
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