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Target
Protein arginine N-methyltransferase 5
Ligand
BDBM50566339
Substrate
n/a
Meas. Tech.
ChEMBL_2100039 (CHEMBL4808435)
EC50
5.3±n/a nM
Citation
 Quiroz, RV; Reutershan, MH; Schneider, SE; Sloman, D; Lacey, BM; Swalm, BM; Yeung, CS; Gibeau, C; Spellman, DS; Rankic, DA; Chen, D; Witter, D; Linn, D; Munsell, E; Feng, G; Xu, H; Hughes, JME; Lim, J; Saurí, J; Geddes, K; Wan, M; Mansueto, MS; Follmer, NE; Fier, PS; Siliphaivanh, P; Daublain, P; Palte, RL; Hayes, RP; Lee, S; Kawamura, S; Silverman, S; Sanyal, S; Henderson, TJ; Ye, Y; Gao, Y; Nicholson, B; Machacek, MR The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer. J Med Chem 64:3911-3939 (2021) [PubMed]  Article 
Target
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
  
Inhibitor
Name:
BDBM50566339
Synonyms:
CHEMBL4854567
Type:
Small organic molecule
Emp. Form.:
C23H23BrN6O4
Mol. Mass.:
527.371
SMILES:
[H][C@]12O[C@H]([C@H](O)[C@@]1(O)CC[C@@H]2Oc1ccc2cc(Br)c(N)nc2c1)n1ccc2c(NC)ncnc12 |r|
Structure:
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