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Target
Protein arginine N-methyltransferase 5
Ligand
BDBM177909
Substrate
n/a
Meas. Tech.
PRMT5/MEP50 Enzyme Assay
IC50
<100±n/a nM
Citation
 Duncan, KW; Chesworth, R; Boriack-Sjodin, PA; Munchhof, MJ; Jin, L PRMT5 inhibitors and uses thereof US Patent  US9675614 Publication Date 6/13/2017 
Target
Name:
Protein arginine N-methyltransferase 5
Synonyms:
Human Flag-PRMT5/6His-MeP50 protein | PRMT5/MeP50
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Protein arginine N-methyltransferase 5
Synonyms:
ANM5_HUMAN | Flag-PRMT5 | HRMT1L5 | IBP72 | JBP1 | PRMT5 | Protein arginine N-methyltransferase 5 (Flag-PRMT5) | SKB1
Type:
Protein
Mol. Mass.:
72548.80
Organism:
Homo sapiens (Human)
Description:
Full-length PRMT5 with FLAG tag fused directly to Ala 2 (MDYKDDDDK removed)
Residue:
636
Sequence:
AAMAVGGAGGSRVSSGRDLNCVPEIADTLGAVAKQGFDFLCMPVFHPRFKREFIQEPAKNRPGPQTRSDLLLSGRDWNTLIVGKLSPWIRPDSKVEKIRRNSEAAMLQELNFGAYLGLPAFLLPLNQEDNTNLARVLTNHIHTGHHSSMFWMRVPLVAPEDLRDDIIENAPTTHTEEYSGEEKTWMWWHNFRTLCDYSKRIAVALEIGADLPSNHVIDRWLGEPIKAAILPTSIFLTNKKGFPVLSKMHQRLIFRLLKLEVQFIITGTNHHSEKEFCSYLQYLEYLSQNRPPPNAYELFAKGYEDYLQSPLQPLMDNLESQTYEVFEKDPIKYSQYQQAIYKCLLDRVPEEEKDTNVQVLMVLGAGRGPLVNASLRAAKQADRRIKLYAVEKNPNAVVTLENWQFEEWGSQVTVVSSDMREWVAPEKADIIVSELLGSFADNELSPECLDGAQHFLKDDGVSIPGEYTSFLAPISSSKLYNEVRACREKDRDPEAQFEMPYVVRLHNFHQLSAPQPCFTFSHPNRDPMIDNNRYCTLEFPVEVNTVLHGFAGYFETVLYQDITLSIRPETHSPGMFSWFPILFPIKQPITVREGQTICVRFWRCSNSKKVWYEWAVTAPVCSAIHNPTGRSYTIGL
  
Component 2
Name:
Protein arginine N-methyltransferase 5
Synonyms:
6His-MEP50 | ANM5_HUMAN | HRMT1L5 | IBP72 | JBP1 | Methylosome protein 50 (6His-MeP50) | PRMT5 | SKB1
Type:
Protein
Mol. Mass.:
37539.24
Organism:
Homo sapiens (Human)
Description:
Full-length MeP50 with His tag fused directly to Arg 2 of MEP50
Residue:
348
Sequence:
MHHHHHHRKETPPPLVPPAAREWNLPPNAPACMERQLEAARYRSDGALLLGASSLSGRCWAGSLWLFKDPCAAPNEGFCSAGVQTEAGVADLTWVGERGILVASDSGAVELWELDENETLIVSKFCKYEHDDIVSTVSVLSSGTQAVSGSKDICIKVWDLAQQVVLSSYRAHAAQVTCVAASPHKDSVFLSCSEDNRILLWDTRCPKPASQIGCSAPGYLPTSLAWHPQQSEVFVFGDENGTVSLVDTKSTSCVLSSAVHSQCVTGLVFSPHSVPFLASLSEDCSLAVLDSSLSELFRSQAHRDFVRDATWSPLNHSLLTTVGWDHQVVHHVVPTEPLPAPGPASVTE
  
Inhibitor
Name:
BDBM177909
Synonyms:
US10307413, Compound 163 | US10391089, Compound 163 | US10980794, Cmpd No 163 | US9675614, 163
Type:
Small organic molecule
Emp. Form.:
C25H34N4O2
Mol. Mass.:
422.5631
SMILES:
CN1CCN(Cc2ccc(cc2)C(=O)NCC(O)CN2CCc3ccccc3C2)CC1
Structure:
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