Reaction Details Report a problem with these data
Target
Poly(ADP-ribose) glycohydrolase
Ligand
BDBM371067
Substrate
n/a
Meas. Tech.
ChEMBL_1793403 (CHEMBL4265322)
EC50
29±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
More Info.:
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