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TargetProtein arginine N-methyltransferase 5
LigandBDBM579047
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2163197 (CHEMBL5048058)
IC50 11±n/a nM
Citation Smith, CRAranda, RBobinski, TPBriere, DMBurns, ACChristensen, JGClarine, JEngstrom, LDGunn, RJIvetac, AJean-Baptiste, RKetcham, JMKobayashi, MKuehler, JKulyk, SLawson, JDMoya, KOlson, PRahbaek, LThomas, NCWang, XWaters, LMMarx, MA Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5?MTA Complex for the Treatment of  J Med Chem65:1749-1766 (2022) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Protein arginine N-methyltransferase 5
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:
MAAMAVGGAGGSRVSSGRDLNCVPEIADTLGAVAKQGFDFLCMPVFHPRFKREFIQEPAK
NRPGPQTRSDLLLSGRDWNTLIVGKLSPWIRPDSKVEKIRRNSEAAMLQELNFGAYLGLP
AFLLPLNQEDNTNLARVLTNHIHTGHHSSMFWMRVPLVAPEDLRDDIIENAPTTHTEEYS
GEEKTWMWWHNFRTLCDYSKRIAVALEIGADLPSNHVIDRWLGEPIKAAILPTSIFLTNK
KGFPVLSKMHQRLIFRLLKLEVQFIITGTNHHSEKEFCSYLQYLEYLSQNRPPPNAYELF
AKGYEDYLQSPLQPLMDNLESQTYEVFEKDPIKYSQYQQAIYKCLLDRVPEEEKDTNVQV
LMVLGAGRGPLVNASLRAAKQADRRIKLYAVEKNPNAVVTLENWQFEEWGSQVTVVSSDM
REWVAPEKADIIVSELLGSFADNELSPECLDGAQHFLKDDGVSIPGEYTSFLAPISSSKL
YNEVRACREKDRDPEAQFEMPYVVRLHNFHQLSAPQPCFTFSHPNRDPMIDNNRYCTLEF
PVEVNTVLHGFAGYFETVLYQDITLSIRPETHSPGMFSWFPILFPIKQPITVREGQTICV
RFWRCSNSKKVWYEWAVTAPVCSAIHNPTGRSYTIGL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM579047
n/a
NameBDBM579047
Synonyms:2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin-6-yl)-1-methyl-1H- pyrazol-5-yl)-1-naphthonitrile | US11479551, Example 4-147 | US11492351, Example 4-147
TypeSmall organic molecule
Emp. Form.C24H18N6O
Mol. Mass.406.4393
SMILESCn1ncc(c1-c1ccc2ccccc2c1C#N)-c1ccc2c(c1)c(CN)n[nH]c2=O |(-4.45,1.7,;-3.12,2.47,;-2.64,3.94,;-1.1,3.94,;-.63,2.47,;-1.87,1.57,;-2.27,.08,;-1.18,-1.01,;-1.58,-2.5,;-3.07,-2.9,;-3.47,-4.38,;-4.95,-4.78,;-6.04,-3.69,;-5.64,-2.21,;-4.16,-1.81,;-3.76,-.32,;-4.85,.77,;-5.94,1.86,;.71,1.7,;.71,.16,;2.04,-.61,;3.38,.16,;3.38,1.7,;2.04,2.47,;4.71,2.47,;4.71,4.01,;3.38,4.78,;6.04,1.7,;6.04,.16,;4.71,-.61,;4.71,-2.15,)|
Structure
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