Target
Poly(ADP-ribose) glycohydrolase
Ligand
BDBM371352
Substrate
n/a
Meas. Tech.
PARG Assay
IC50
333±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:
BDBM371352
Synonyms:
N-[1-(Difluoromethyl)cyclopropyl]-1-[(4-fluorophenyl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-quinazoline-6-sulfonamide | US10239843, Example 460
Type:
Small organic molecule
Emp. Form.:
C24H22F3N5O4S
Mol. Mass.:
533.523
SMILES:
Cn1cc(Cn2c(=O)n(Cc3ccc(F)cc3)c3ccc(cc3c2=O)S(=O)(=O)NC2(CC2)C(F)F)cn1
Structure:
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