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Target
Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma
Ligand
BDBM60631
Substrate
n/a
Meas. Tech.
ChEMBL_1289875 (CHEMBL3119545)
IC50
3812±n/a nM
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 Chem 57:903-20 (2014) [PubMed]  Article
Target
Name:
Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma
Synonyms:
P3C2G_HUMAN | PI3K-C2-gamma | PIK3C2G | Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit gamma | Phosphoinositide 3-kinase-C2-gamma | PtdIns-3-kinase C2 subunit gamma
Type:
PROTEIN
Mol. Mass.:
165726.35
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1447686
Residue:
1445
Sequence:
MAYSWQTDPNPNESHEKQYEHQEFLFVNQPHSSSQVSLGFDQIVDEISGKIPHYESEIDENTFFVPTAPKWDSTGHSLNEAHQISLNEFTSKSRELSWHQVSKAPAIGFSPSVLPKPQNTNKECSWGSPIGKHHGADDSRFSILAPSFTSLDKINLEKELENENHNYHIGFESSIPPTNSSFSSDFMPKEENKRSGHVNIVEPSLMLLKGSLQPGMWESTWQKNIESIGCSIQLVEVPQSSNTSLASFCNKVKKIRERYHAADVNFNSGKIWSTTTAFPYQLFSKTKFNIHIFIDNSTQPLHFMPCANYLVKDLIAEILHFCTNDQLLPKDHILSVCGSEEFLQNDHCLGSHKMFQKDKSVIQLHLQKSREAPGKLSRKHEEDHSQFYLNQLLEFMHIWKVSRQCLLTLIRKYDFHLKYLLKTQENVYNIIEEVKKICSVLGCVETKQITDAVNELSLILQRKGENFYQSSETSAKGLIEKVTTELSTSIYQLINVYCNSFYADFQPVNVPRCTSYLNPGLPSHLSFTVYAAHNIPETWVHRINFPLEIKSLPRESMLTVKLFGIACATNNANLLAWTCLPLFPKEKSILGSMLFSMTLQSEPPVEMITPGVWDVSQPSPVTLQIDFPATGWEYMKPDSEENRSNLEEPLKECIKHIARLSQKQTPLLLSEEKKRYLWFYRFYCNNENCSLPLVLGSAPGWDERTVSEMHTILRRWTFSQPLEALGLLTSSFPDQEIRKVAVQQLDNLLNDELLEYLPQLVQAVKFEWNLESPLVQLLLHRSLQSIQVAHRLYWLLKNAENEAYFKSWYQKLLAALQFCAGKALNDEFSKEQKLIKILGDIGERVKSASDHQRQEVLKKEIGRLEEFFQDVNTCHLPLNPALCIKGIDHDACSYFTSNALPLKITFINANPMGKNISIIFKAGDDLRQDMLVLQLIQVMDNIWLQEGLDMQMIIYRCLSTGKDQGLVQMVPDAVTLAKIHRHSGLIGPLKENTIKKWFSQHNHLKADYEKALRNFFYSCAGWCVVTFILGVCDRHNDNIMLTKSGHMFHIDFGKFLGHAQTFGGIKRDRAPFIFTSEMEYFITEGGKNPQHFQDFVELCCRAYNIIRKHSQLLLNLLEMMLYAGLPELSGIQDLKYVYNNLRPQDTDLEATSHFTKKIKESLECFPVKLNNLIHTLAQMSAISPAKSTSQTFPQESCLLSTTRSIERATILGFSKKSSNLYLIQVTHSNNETSLTEKSFEQFSKLHSQLQKQFASLTLPEFPHWWHLPFTNSDHRRFRDLNHYMEQILNVSHEVTNSDCVLSFFLSEAVQQTVEESSPVYLGEKFPDKKPKVQLVISYEDVKLTILVKHMKNIHLPDGSAPSAHVEFYLLPYPSEVRRRKTKSVPKCTDPTYNEIVVYDEVTELQGHVLMLIVKSKTVFVGAINIRLCSVPLDKEKWYPLGNSII
  
Inhibitor
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:
Search PDB for entries with ligand similarity: