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Target
Methylosome protein 50/Protein arginine N-methyltransferase 5
Ligand
BDBM343824
Substrate
n/a
Meas. Tech.
ChEMBL_2026542 (CHEMBL4680700)
IC50
33±n/a nM
Citation
 Duncan, KW; Rioux, N; Boriack-Sjodin, PA; Munchhof, MJ; Reiter, LA; Majer, CR; Jin, L; Johnston, LD; Chan-Penebre, E; Kuplast, KG; Porter Scott, M; Pollock, RM; Waters, NJ; Smith, JJ; Moyer, MP; Copeland, RA; Chesworth, R Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. ACS Med Chem Lett 7:162-6 (2016) [PubMed]  Article 
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:
BDBM343824
Synonyms:
1-(3,4-Dihydroisoquinolin-2(1H)-yl)-3-((4-(1-methyl-1H-benzo[d]imidazol-6-yl)pyridin-2-yl)amino)propan-2-ol | US9777008, Compound 118
Type:
Small organic molecule
Emp. Form.:
C25H27N5O
Mol. Mass.:
413.5148
SMILES:
Cn1cnc2ccc(cc12)-c1ccnc(NCC(O)CN2CCc3ccccc3C2)c1
Structure:
Search PDB for entries with ligand similarity: