Reaction Details | |||
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Target | Methylosome protein 50/Protein arginine N-methyltransferase 5 | ||
Ligand | BDBM578829 | ||
Substrate/Competitor | n/a | ||
Meas. Tech. | PRMT5:MEP50 FlashPlate Assay | ||
IC50 | 816±n/a nM | ||
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 | ||
More Info.: | Get all data from this article, Assay Method | ||
Methylosome protein 50/Protein arginine N-methyltransferase 5 | |||
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: |
| ||
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: |
| ||
BDBM578829 | |||
n/a | |||
Name | BDBM578829 | ||
Synonyms: | 2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin-6-yl)-1-methyl-1H- pyrazol-5-yl)-5-methylbenzonitrile | US11479551, Example 4-106 | US11492351, Example 4-106 | ||
Type | Small organic molecule | ||
Emp. Form. | C21H18N6O | ||
Mol. Mass. | 370.4072 | ||
SMILES | Cc1ccc(-c2c(cnn2C)-c2ccc3c(c2)c(CN)n[nH]c3=O)c(c1)C#N |(-3.63,-4.37,;-3.23,-2.88,;-1.74,-2.48,;-1.34,-.99,;-2.43,.09,;-2.03,1.58,;-.57,2.06,;-.57,3.6,;-2.03,4.07,;-2.94,2.83,;-4.48,2.83,;.76,1.29,;.76,-.25,;2.1,-1.02,;3.43,-.25,;3.43,1.29,;2.1,2.06,;4.76,2.06,;4.76,3.6,;6.1,4.37,;6.1,1.29,;6.1,-.25,;4.76,-1.02,;4.76,-2.56,;-3.92,-.3,;-4.32,-1.79,;-5.01,.78,;-6.1,1.87,)| | ||
Structure |