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Target
ADP-ribosylhydrolase ARH3
Ligand
BDBM371049
Substrate
n/a
Meas. Tech.
ChEMBL_1793408 (CHEMBL4265327)
EC50
>100000±n/a nM
Citation
 Waszkowycz, B; Smith, KM; McGonagle, AE; Jordan, AM; Acton, B; Fairweather, EE; Griffiths, LA; Hamilton, NM; Hamilton, NS; Hitchin, JR; Hutton, CP; James, DI; Jones, CD; Jones, S; Mould, DP; Small, HF; Stowell, AIJ; Tucker, JA; Waddell, ID; Ogilvie, DJ Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides. J Med Chem 61:10767-10792 (2018) [PubMed]  Article 
Target
Name:
ADP-ribosylhydrolase ARH3
Synonyms:
ADP-ribose glycohydrolase ARH3 | ADP-ribosylhydrolase 3 | ADPRHL2 | ADPRS | ADPRS_HUMAN | ARH3 | O-acetyl-ADP-ribose deacetylase ARH3 | Poly(ADP-ribose) glycohydrolase ARH3 | [Protein ADP-ribosylarginine] hydrolase-like protein 2 | [Protein ADP-ribosylserine] hydrolase
Type:
Enzyme Catalytic Domain
Mol. Mass.:
38934.22
Organism:
Homo sapiens (Human)
Description:
Q9NX46
Residue:
363
Sequence:
MAAAAMAAAAGGGAGAARSLSRFRGCLAGALLGDCVGSFYEAHDTVDLTSVLRHVQSLEPDPGTPGSERTEALYYTDDTAMARALVQSLLAKEAFDEVDMAHRFAQEYKKDPDRGYGAGVVTVFKKLLNPKCRDVFEPARAQFNGKGSYGNGGAMRVAGISLAYSSVQDVQKFARLSAQLTHASSLGYNGAILQALAVHLALQGESSSEHFLKQLLGHMEDLEGDAQSVLDARELGMEERPYSSRLKKIGELLDQASVTREEVVSELGNGIAAFESVPTAIYCFLRCMEPDPEIPSAFNSLQRTLIYSISLGGDTDTIATMAGAIAGAYYGMDQVPESWQQSCEGYEETDILAQSLHRVFQKS
  
Inhibitor
Name:
BDBM371049
Synonyms:
US10239843, Example 156
Type:
Small organic molecule
Emp. Form.:
C21H24N4O4S2
Mol. Mass.:
460.57
SMILES:
Cc1ncc(Cn2c(=O)n(CC3CC3)c3ccc(cc3c2=O)S(=O)(=O)NC2(C)CC2)s1
Structure:
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