Reaction Details |
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Target | Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha |
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Ligand | BDBM60631 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1289876 (CHEMBL3119546) |
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IC50 | >10000±n/a nM |
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Citation | Certal, V; Carry, JC; Halley, F; Virone-Oddos, A; Thompson, F; Filoche-Rommé, B; El-Ahmad, Y; Karlsson, A; Charrier, V; Delorme, C; Rak, A; Abecassis, PY; Amara, C; Vincent, L; Bonnevaux, H; Nicolas, JP; Mathieu, M; Bertrand, T; Marquette, JP; Michot, N; Benard, T; Perrin, MA; Lemaitre, O; Guerif, S; Perron, S; Monget, S; Gruss-Leleu, F; Doerflinger, G; Guizani, H; Brollo, M; Delbarre, L; Bertin, L; Richepin, P; Loyau, V; Garcia-Echeverria, C; Lengauer, C; Schio, L Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers. J Med Chem57:903-20 (2014) [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 |
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 |
Type: | Protein |
Mol. Mass.: | 190704.50 |
Organism: | Homo sapiens (Human) |
Description: | O00443 |
Residue: | 1686 |
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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BDBM60631 |
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n/a |
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Name | BDBM60631 |
Synonyms: | BDBM50447096 | US9133168, 19b |
Type | n/a |
Emp. Form. | C19H22N4O3 |
Mol. Mass. | 354.403 |
SMILES | C[C@H]1Cc2ccccc2N1C(=O)Cc1nc(cc(=O)[nH]1)N1CCOCC1 |r| |
Structure |
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