Reaction Details |
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Target | Methylosome protein 50/Protein arginine N-methyltransferase 5 |
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Ligand | BDBM50572974 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2118729 (CHEMBL4827795) |
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IC50 | 4200±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 |
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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BDBM50572974 |
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n/a |
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Name | BDBM50572974 |
Synonyms: | CHEMBL4853507 |
Type | Small organic molecule |
Emp. Form. | C21H21Cl2N5O4S |
Mol. Mass. | 510.394 |
SMILES | CCc1ccc(NC(=O)Cn2ncc(Cl)c(Cl)c2=O)cc1S(=O)(=O)NCCc1ccccn1 |
Structure |
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