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Target
Protein arginine N-methyltransferase 5
Ligand
BDBM578780
Substrate
n/a
Meas. Tech.
ChEMBL_2163192 (CHEMBL5048053)
IC50
910±n/a nM
Citation
 Smith, CR; Aranda, R; Bobinski, TP; Briere, DM; Burns, AC; Christensen, JG; Clarine, J; Engstrom, LD; Gunn, RJ; Ivetac, A; Jean-Baptiste, R; Ketcham, JM; Kobayashi, M; Kuehler, J; Kulyk, S; Lawson, JD; Moya, K; Olson, P; Rahbaek, L; Thomas, NC; Wang, X; Waters, LM; Marx, MA Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5?MTA Complex for the Treatment of  J Med Chem 65:1749-1766 (2022) [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:
BDBM578780
Synonyms:
4-(aminomethyl)-6-(pyridin-3-yl)phthalazin-1(2H)-one | US11479551, Example 1-5 | US11492351, Example 1-5
Type:
Small organic molecule
Emp. Form.:
C14H12N4O
Mol. Mass.:
252.2713
SMILES:
NCc1n[nH]c(=O)c2ccc(cc12)-c1cccnc1
Structure:
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