Reaction Details |
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Target | Methylosome protein 50/Protein arginine N-methyltransferase 5 |
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Ligand | BDBM533482 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Biochemical Assay |
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IC50 | 0.330±n/a nM |
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Citation | Luengo, J; Leal, RA; Lin, H; Shetty, R; Vaddi, K Selective inhibitors of protein arginine methyltransferase 5 (PRMT5) US Patent US11220524 Publication Date 1/11/2022 |
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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 |
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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BDBM533482 |
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n/a |
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Name | BDBM533482 |
Synonyms: | (Z)-7-((1R,2S,3R,4S)-4-(2-(2- ((cyclopropylmethyl)amino)quinolin- 7-yl)ethyl)-2,3- dihydroxycyclopentyl)-1,7-dihydro- 4H-pyrrolo[2,3-d]pyrimidin-4-one oxime | US11220524, Example 87-B |
Type | Small organic molecule |
Emp. Form. | C26H30N6O3 |
Mol. Mass. | 474.5548 |
SMILES | O\N=c1/nc[nH]c2n(ccc12)[C@@H]1C[C@H](CCc2ccc3ccc(NCC4CC4)nc3c2)[C@@H](O)[C@H]1O |r| |
Structure |
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