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Target
Methylosome protein 50/Protein arginine N-methyltransferase 5
Ligand
BDBM578819
Substrate
n/a
Meas. Tech.
PRMT5:MEP50 FlashPlate Assay with MTA
IC50
0.500±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  US11479551 Publication Date 10/25/2022 
Target
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:
MAAMAVGGAGGSRVSSGRDLNCVPEIADTLGAVAKQGFDFLCMPVFHPRFKREFIQEPAKNRPGPQTRSDLLLSGRDWNTLIVGKLSPWIRPDSKVEKIRRNSEAAMLQELNFGAYLGLPAFLLPLNQEDNTNLARVLTNHIHTGHHSSMFWMRVPLVAPEDLRDDIIENAPTTHTEEYSGEEKTWMWWHNFRTLCDYSKRIAVALEIGADLPSNHVIDRWLGEPIKAAILPTSIFLTNKKGFPVLSKMHQRLIFRLLKLEVQFIITGTNHHSEKEFCSYLQYLEYLSQNRPPPNAYELFAKGYEDYLQSPLQPLMDNLESQTYEVFEKDPIKYSQYQQAIYKCLLDRVPEEEKDTNVQVLMVLGAGRGPLVNASLRAAKQADRRIKLYAVEKNPNAVVTLENWQFEEWGSQVTVVSSDMREWVAPEKADIIVSELLGSFADNELSPECLDGAQHFLKDDGVSIPGEYTSFLAPISSSKLYNEVRACREKDRDPEAQFEMPYVVRLHNFHQLSAPQPCFTFSHPNRDPMIDNNRYCTLEFPVEVNTVLHGFAGYFETVLYQDITLSIRPETHSPGMFSWFPILFPIKQPITVREGQTICVRFWRCSNSKKVWYEWAVTAPVCSAIHNPTGRSYTIGL
  
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:
MRKETPPPLVPPAAREWNLPPNAPACMERQLEAARYRSDGALLLGASSLSGRCWAGSLWLFKDPCAAPNEGFCSAGVQTEAGVADLTWVGERGILVASDSGAVELWELDENETLIVSKFCKYEHDDIVSTVSVLSSGTQAVSGSKDICIKVWDLAQQVVLSSYRAHAAQVTCVAASPHKDSVFLSCSEDNRILLWDTRCPKPASQIGCSAPGYLPTSLAWHPQQSEVFVFGDENGTVSLVDTKSTSCVLSSAVHSQCVTGLVFSPHSVPFLASLSEDCSLAVLDSSLSELFRSQAHRDFVRDATWSPLNHSLLTTVGWDHQVVHHVVPTEPLPAPGPASVTE
  
Inhibitor
Name:
BDBM578819
Synonyms:
2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin-6-yl)-1-methyl-1H- pyrazol-5-yl)benzonitrile | US11479551, Example 4-100 | US11479551, Example 4-200 | US11492351, Example 4-100
Type:
Small organic molecule
Emp. Form.:
C20H16N6O
Mol. Mass.:
356.3806
SMILES:
Cn1ncc(c1-c1ccccc1C#N)-c1ccc2c(c1)c(CN)n[nH]c2=O |(-4.48,2.08,;-2.94,2.08,;-2.03,3.33,;-.57,2.85,;-.57,1.31,;-2.03,.84,;-2.43,-.65,;-1.34,-1.74,;-1.74,-3.23,;-3.23,-3.62,;-4.32,-2.54,;-3.92,-1.05,;-5.01,.04,;-6.1,1.13,;.76,.54,;.76,-1,;2.1,-1.77,;3.43,-1,;3.43,.54,;2.1,1.31,;4.76,1.31,;4.76,2.85,;3.43,3.62,;6.1,.54,;6.1,-1,;4.76,-1.77,;4.76,-3.31,)|
Structure:
Search PDB for entries with ligand similarity: