| Reaction Details |
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 | Report a problem with these data |
| Target | Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha |
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| Ligand | BDBM50434806 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_962652 (CHEMBL2388230) |
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| IC50 | >10000±n/a nM |
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| Citation |  Ndubaku, CO; Heffron, TP; Staben, ST; Baumgardner, M; Blaquiere, N; Bradley, E; Bull, R; Do, S; Dotson, J; Dudley, D; Edgar, KA; Friedman, LS; Goldsmith, R; Heald, RA; Kolesnikov, A; Lee, L; Lewis, C; Nannini, M; Nonomiya, J; Pang, J; Price, S; Prior, WW; Salphati, L; Sideris, S; Wallin, JJ; Wang, L; Wei, B; Sampath, D; Olivero, AG Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): aß-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem56:4597-610 (2013) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha |
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| Name: | Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha |
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| Synonyms: | P3C2A_HUMAN | PI3K-C2-alpha | PIK3C2A | Phosphatidylinositol 4-phosphate 3-kinase C2 alpha (PIK3C2A) | Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha | Phosphoinositide 3-kinase-C2-alpha | PtdIns-3-kinase C2 subunit alpha |
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| Type: | Protein |
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| Mol. Mass.: | 190704.50 |
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| Organism: | Homo sapiens (Human) |
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| Description: | O00443 |
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| Residue: | 1686 |
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| Sequence: | MAQISSNSGFKECPSSHPEPTRAKDVDKEEALQMEAEALAKLQKDRQVTDNQRGFELSSS
TRKKAQVYNKQDYDLMVFPESDSQKRALDIDVEKLTQAELEKLLLDDSFETKKTPVLPVT
PILSPSFSAQLYFRPTIQRGQWPPGLPGPSTYALPSIYPSTYSKQAAFQNGFNPRMPTFP
STEPIYLSLPGQSPYFSYPLTPATPFHPQGSLPIYRPVVSTDMAKLFDKIASTSEFLKNG
KARTDLEITDSKVSNLQVSPKSEDISKFDWLDLDPLSKPKVDNVEVLDHEEEKNVSSLLA
KDPWDAVLLEERSTANCHLERKVNGKSLSVATVTRSQSLNIRTTQLAKAQGHISQKDPNG
TSSLPTGSSLLQEVEVQNEEMAAFCRSITKLKTKFPYTNHRTNPGYLLSPVTAQRNICGE
NASVKVSIDIEGFQLPVTFTCDVSSTVEIIIMQALCWVHDDLNQVDVGSYVLKVCGQEEV
LQNNHCLGSHEHIQNCRKWDTEIRLQLLTFSAMCQNLARTAEDDETPVDLNKHLYQIEKP
CKEAMTRHPVEELLDSYHNQVELALQIENQHRAVDQVIKAVRKICSALDGVETLAITESV
KKLKRAVNLPRSKTADVTSLFGGEDTSRSSTRGSLNPENPVQVSINQLTAAIYDLLRLHA
NSGRSPTDCAQSSKSVKEAWTTTEQLQFTIFAAHGISSNWVSNYEKYYLICSLSHNGKDL
FKPIQSKKVGTYKNFFYLIKWDELIIFPIQISQLPLESVLHLTLFGILNQSSGSSPDSNK
QRKGPEALGKVSLPLFDFKRFLTCGTKLLYLWTSSHTNSVPGTVTKKGYVMERIVLQVDF
PSPAFDIIYTTPQVDRSIIQQHNLETLENDIKGKLLDILHKDSSLGLSKEDKAFLWEKRY
YCFKHPNCLPKILASAPNWKWVNLAKTYSLLHQWPALYPLIALELLDSKFADQEVRSLAV
TWIEAISDDELTDLLPQFVQALKYEIYLNSSLVQFLLSRALGNIQIAHNLYWLLKDALHD
VQFSTRYEHVLGALLSVGGKRLREELLKQTKLVQLLGGVAEKVRQASGSARQVVLQRSME
RVQSFFQKNKCRLPLKPSLVAKELNIKSCSFFSSNAVPLKVTMVNADPMGEEINVMFKVG
EDLRQDMLALQMIKIMDKIWLKEGLDLRMVIFKCLSTGRDRGMVELVPASDTLRKIQVEY
GVTGSFKDKPLAEWLRKYNPSEEEYEKASENFIYSCAGCCVATYVLGICDRHNDNIMLRS
TGHMFHIDFGKFLGHAQMFGSFKRDRAPFVLTSDMAYVINGGEKPTIRFQLFVDLCCQAY
NLIRKQTNLFLNLLSLMIPSGLPELTSIQDLKYVRDALQPQTTDAEATIFFTRLIESSLG
SIATKFNFFIHNLAQLRFSGLPSNDEPILSFSPKTYSFRQDGRIKEVSVFTYHKKYNPDK
HYIYVVRILREGQIEPSFVFRTFDEFQELHNKLSIIFPLWKLPGFPNRMVLGRTHIKDVA
AKRKIELNSYLQSLMNASTDVAECDLVCTFFHPLLRDEKAEGIARSADAGSFSPTPGQIG
GAVKLSISYRNGTLFIMVMHIKDLVTEDGADPNPYVKTYLLPDNHKTSKRKTKISRKTRN
PTFNEMLVYSGYSKETLRQRELQLSVLSAESLRENFFLGGVTLPLKDFNLSKETVKWYQL
TAATYL
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| BDBM50434806 |
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| n/a |
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| Name | BDBM50434806 |
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| Synonyms: | 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide | CHEMBL2387080 | GDC 0032 | GDC-0032 | Roche RG7604 | Taselisib | US10851091, Compound taselisib | US8242104, Compound 196 |
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| Type | Small organic molecule |
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| Emp. Form. | C24H28N8O2 |
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| Mol. Mass. | 460.5315 |
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| SMILES | CC(C)n1nc(C)nc1-c1cn2CCOc3cc(ccc3-c2n1)-c1cnn(c1)C(C)(C)C(N)=O |
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| Structure | 
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