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Target
Poly(ADP-ribose) glycohydrolase
Ligand
BDBM205480
Substrate
n/a
Meas. Tech.
PARG Biochemical Assay
pH
7.4±n/a
IC50
40± 7 nM
Comments
extracted
Citation
 James, DI; Smith, KM; Jordan, AM; Fairweather, EE; Griffiths, LA; Hamilton, NS; Hitchin, JR; Hutton, CP; Jones, S; Kelly, P; McGonagle, AE; Small, H; Stowell, AI; Tucker, J; Waddell, ID; Waszkowycz, B; Ogilvie, DJ First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib. ACS Chem Biol 11:3179-3190 (2016) [PubMed]  Article 
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:
BDBM205480
Synonyms:
PDD00017238 (5) | US10508086, Example 90 | US10995073, Example 90
Type:
Small organic molecule
Emp. Form.:
C19H20N6O3S3
Mol. Mass.:
476.595
SMILES:
Cc1nc(C)c(Cn2c3ccc(cc3n(-c3ncns3)c2=O)S(=O)(=O)NC2(C)CC2)s1
Structure:
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