| Reaction Details |
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 | Report a problem with these data |
| Target | Poly(ADP-ribose) glycohydrolase |
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| Ligand | BDBM371063 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1793404 (CHEMBL4265323) |
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| EC50 | 20±n/a nM |
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| 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 Chem61:10767-10792 (2018) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Poly(ADP-ribose) glycohydrolase |
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| Name: | Poly(ADP-ribose) glycohydrolase |
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| Synonyms: | PARG | PARG_HUMAN | Poly(ADP-ribose) glycohydrolase | poly(ADP-ribose) glycohydrolase (PARG) |
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| Type: | Protein |
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| Mol. Mass.: | 111107.13 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q86W56 |
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| Residue: | 976 |
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| Sequence: | MNAGPGCEPCTKRPRWGAATTSPAASDARSFPSRQRRVLDPKDAHVQFRVPPSSPACVPG
RAGQHRGSATSLVFKQKTITSWMDTKGIKTAESESLDSKENNNTRIESMMSSVQKDNFYQ
HNVEKLENVSQLSLDKSPTEKSTQYLNQHQTAAMCKWQNEGKHTEQLLESEPQTVTLVPE
QFSNANIDRSPQNDDHSDTDSEENRDNQQFLTTVKLANAKQTTEDEQAREAKSHQKCSKS
CDPGEDCASCQQDEIDVVPESPLSDVGSEDVGTGPKNDNKLTRQESCLGNSPPFEKESEP
ESPMDVDNSKNSCQDSEADEETSPGFDEQEDGSSSQTANKPSRFQARDADIEFRKRYSTK
GGEVRLHFQFEGGESRTGMNDLNAKLPGNISSLNVECRNSKQHGKKDSKITDHFMRLPKA
EDRRKEQWETKHQRTERKIPKYVPPHLSPDKKWLGTPIEEMRRMPRCGIRLPLLRPSANH
TVTIRVDLLRAGEVPKPFPTHYKDLWDNKHVKMPCSEQNLYPVEDENGERTAGSRWELIQ
TALLNKFTRPQNLKDAILKYNVAYSKKWDFTALIDFWDKVLEEAEAQHLYQSILPDMVKI
ALCLPNICTQPIPLLKQKMNHSITMSQEQIASLLANAFFCTFPRRNAKMKSEYSSYPDIN
FNRLFEGRSSRKPEKLKTLFCYFRRVTEKKPTGLVTFTRQSLEDFPEWERCEKPLTRLHV
TYEGTIEENGQGMLQVDFANRFVGGGVTSAGLVQEEIRFLINPELIISRLFTEVLDHNEC
LIITGTEQYSEYTGYAETYRWSRSHEDGSERDDWQRRCTEIVAIDALHFRRYLDQFVPEK
MRRELNKAYCGFLRPGVSSENLSAVATGNWGCGAFGGDARLKALIQILAAAAAERDVVYF
TFGDSELMRDIYSMHIFLTERKLTVGDVYKLLLRYYNEECRNCSTPGPDIKLYPFIYHAV
ESCAETADHSGQRTGT
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| BDBM371063 |
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| n/a |
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| Name | BDBM371063 |
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| Synonyms: | US10239843, Example 170 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H26N6O4S2 |
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| Mol. Mass. | 514.62 |
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| SMILES | Cc1nc(C)c(Cn2c3ccc(cc3c(=O)n(Cc3cnn(C)c3)c2=O)S(=O)(=O)NC2(C)CC2)s1 |
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| Structure | 
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