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Target
Protein arginine N-methyltransferase 5
Ligand
BDBM50572984
Substrate
n/a
Meas. Tech.
ChEMBL_2118741 (CHEMBL4827807)
Ki
78000±n/a nM
Citation
 McKinney, DC; McMillan, BJ; Ranaghan, MJ; Moroco, JA; Brousseau, M; Mullin-Bernstein, Z; O'Keefe, M; McCarren, P; Mesleh, MF; Mulvaney, KM; Robinson, F; Singh, R; Bajrami, B; Wagner, FF; Hilgraf, R; Drysdale, MJ; Campbell, AJ; Skepner, A; Timm, DE; Porter, D; Kaushik, VK; Sellers, WR; Ianari, A Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction. J Med Chem 64:11148-11168 (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:
BDBM50572984
Synonyms:
CHEMBL4874198
Type:
Small organic molecule
Emp. Form.:
C21H21Cl2N5O4S
Mol. Mass.:
510.394
SMILES:
C[C@H](C(=O)Nc1ccc(C)c(c1)S(=O)(=O)NCCc1ccccn1)n1ncc(Cl)c(Cl)c1=O |r|
Structure:
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