Reaction Details |
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Target | Poly(ADP-ribose) glycohydrolase |
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Ligand | BDBM371049 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1793404 (CHEMBL4265323) |
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EC50 | 28±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 |
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: | MNAGPGCEPCTKRPRWGAATTSPAASDARSFPSRQRRVLDPKDAHVQFRVPPSSPACVPG
RAGQHRGSATSLVFKQKTITSWMDTKGIKTAESESLDSKENNNTRIESMMSSVQKDNFYQ
HNVEKLENVSQLSLDKSPTEKSTQYLNQHQTAAMCKWQNEGKHTEQLLESEPQTVTLVPE
QFSNANIDRSPQNDDHSDTDSEENRDNQQFLTTVKLANAKQTTEDEQAREAKSHQKCSKS
CDPGEDCASCQQDEIDVVPESPLSDVGSEDVGTGPKNDNKLTRQESCLGNSPPFEKESEP
ESPMDVDNSKNSCQDSEADEETSPGFDEQEDGSSSQTANKPSRFQARDADIEFRKRYSTK
GGEVRLHFQFEGGESRTGMNDLNAKLPGNISSLNVECRNSKQHGKKDSKITDHFMRLPKA
EDRRKEQWETKHQRTERKIPKYVPPHLSPDKKWLGTPIEEMRRMPRCGIRLPLLRPSANH
TVTIRVDLLRAGEVPKPFPTHYKDLWDNKHVKMPCSEQNLYPVEDENGERTAGSRWELIQ
TALLNKFTRPQNLKDAILKYNVAYSKKWDFTALIDFWDKVLEEAEAQHLYQSILPDMVKI
ALCLPNICTQPIPLLKQKMNHSITMSQEQIASLLANAFFCTFPRRNAKMKSEYSSYPDIN
FNRLFEGRSSRKPEKLKTLFCYFRRVTEKKPTGLVTFTRQSLEDFPEWERCEKPLTRLHV
TYEGTIEENGQGMLQVDFANRFVGGGVTSAGLVQEEIRFLINPELIISRLFTEVLDHNEC
LIITGTEQYSEYTGYAETYRWSRSHEDGSERDDWQRRCTEIVAIDALHFRRYLDQFVPEK
MRRELNKAYCGFLRPGVSSENLSAVATGNWGCGAFGGDARLKALIQILAAAAAERDVVYF
TFGDSELMRDIYSMHIFLTERKLTVGDVYKLLLRYYNEECRNCSTPGPDIKLYPFIYHAV
ESCAETADHSGQRTGT
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BDBM371049 |
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n/a |
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Name | BDBM371049 |
Synonyms: | US10239843, Example 156 |
Type | Small organic molecule |
Emp. Form. | C21H24N4O4S2 |
Mol. Mass. | 460.57 |
SMILES | Cc1ncc(Cn2c(=O)n(CC3CC3)c3ccc(cc3c2=O)S(=O)(=O)NC2(C)CC2)s1 |
Structure |
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