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Target
Poly(ADP-ribose) glycohydrolase
Ligand
BDBM371476
Substrate
n/a
Meas. Tech.
PARG Assay
IC50
38.0±n/a nM
Citation
McGonagle, AE; Jordan, A; Waszkowycz, B; Hutton, C; Waddell, I; Hitchin, JR; Smith, KM; Hamilton, NM 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG US Patent US10239843 Publication Date 3/26/2019
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
Inhibitor
Name:
BDBM371476
Synonyms:
N-[1-(Fluoromethyl)cyclopropyl]-1-(isoxazol-5-ylmethyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-quinazoline-6-sulfonamide | US10239843, Example 585
Type:
Small organic molecule
Emp. Form.:
C21H21FN6O5S
Mol. Mass.:
488.492
SMILES:
Cn1cc(Cn2c(=O)n(Cc3ccno3)c3ccc(cc3c2=O)S(=O)(=O)NC2(CF)CC2)cn1