Target
Poly(ADP-ribose) glycohydrolase
Ligand
BDBM371292
Substrate
n/a
Meas. Tech.
PARG Assay
IC50
31.0±n/a nM
Citation
 McGonagle, AEJordan, AWaszkowycz, BHutton, CWaddell, IHitchin, JRSmith, KMHamilton, NM 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG US Patent  US10239843 Publication Date 3/26/2019 
Target
Name:
Poly(ADP-ribose) glycohydrolase
Synonyms:
PARG | PARG_HUMAN | Poly(ADP-ribose) glycohydrolase | poly(ADP-ribose) glycohydrolase (PARG)
Type:
Protein
Mol. Mass.:
111107.13
Organism:
Homo sapiens (Human)
Description:
Q86W56
Residue:
976
Sequence:
MNAGPGCEPCTKRPRWGAATTSPAASDARSFPSRQRRVLDPKDAHVQFRVPPSSPACVPGRAGQHRGSATSLVFKQKTITSWMDTKGIKTAESESLDSKENNNTRIESMMSSVQKDNFYQHNVEKLENVSQLSLDKSPTEKSTQYLNQHQTAAMCKWQNEGKHTEQLLESEPQTVTLVPEQFSNANIDRSPQNDDHSDTDSEENRDNQQFLTTVKLANAKQTTEDEQAREAKSHQKCSKSCDPGEDCASCQQDEIDVVPESPLSDVGSEDVGTGPKNDNKLTRQESCLGNSPPFEKESEPESPMDVDNSKNSCQDSEADEETSPGFDEQEDGSSSQTANKPSRFQARDADIEFRKRYSTKGGEVRLHFQFEGGESRTGMNDLNAKLPGNISSLNVECRNSKQHGKKDSKITDHFMRLPKAEDRRKEQWETKHQRTERKIPKYVPPHLSPDKKWLGTPIEEMRRMPRCGIRLPLLRPSANHTVTIRVDLLRAGEVPKPFPTHYKDLWDNKHVKMPCSEQNLYPVEDENGERTAGSRWELIQTALLNKFTRPQNLKDAILKYNVAYSKKWDFTALIDFWDKVLEEAEAQHLYQSILPDMVKIALCLPNICTQPIPLLKQKMNHSITMSQEQIASLLANAFFCTFPRRNAKMKSEYSSYPDINFNRLFEGRSSRKPEKLKTLFCYFRRVTEKKPTGLVTFTRQSLEDFPEWERCEKPLTRLHVTYEGTIEENGQGMLQVDFANRFVGGGVTSAGLVQEEIRFLINPELIISRLFTEVLDHNECLIITGTEQYSEYTGYAETYRWSRSHEDGSERDDWQRRCTEIVAIDALHFRRYLDQFVPEKMRRELNKAYCGFLRPGVSSENLSAVATGNWGCGAFGGDARLKALIQILAAAAAERDVVYFTFGDSELMRDIYSMHIFLTERKLTVGDVYKLLLRYYNEECRNCSTPGPDIKLYPFIYHAVESCAETADHSGQRTGT
  
Inhibitor
Name:
BDBM371292
Synonyms:
N-(1-Cyanocyclopropyl)-1-(cyclopropylmethyl)-3-[(2-methylthiazol-5-yl)methyl]-2,4-dioxo-quinazoline-6-sulfonamide | US10239843, Example 399
Type:
Small organic molecule
Emp. Form.:
C21H21N5O4S2
Mol. Mass.:
471.553
SMILES:
Cc1ncc(Cn2c(=O)n(CC3CC3)c3ccc(cc3c2=O)S(=O)(=O)NC2(CC2)C#N)s1
Structure:
Search PDB for entries with ligand similarity: