Reaction Details |
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Target | Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta |
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Ligand | BDBM50274638 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1714205 (CHEMBL4124254) |
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IC50 | 32±n/a nM |
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Citation | Pemberton, N; Mogemark, M; Arlbrandt, S; Bold, P; Cox, RJ; Gardelli, C; Holden, NS; Karabelas, K; Karlsson, J; Lever, S; Li, X; Lindmark, H; Norberg, M; Perry, MWD; Petersen, J; Rodrigo Blomqvist, S; Thomas, M; Tyrchan, C; Westin Eriksson, A; Zlatoidsky, P; ึster, L Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-? Inhibitors. J Med Chem61:5435-5441 (2018) [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 beta |
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Name: | Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta |
Synonyms: | C2-PI3K | P3C2B_HUMAN | PI3K-C2beta | PIK3C2B | Phosphatidylinositol 4-phosphate 3-kinase C2 beta (PIK3C2B) | Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide | Phosphoinositide 3-Kinase (PI3K), C2beta | Phosphoinositide 3-Kinase-C2-beta | PtdIns-3-kinase C2 beta |
Type: | Enzyme |
Mol. Mass.: | 184784.86 |
Organism: | Homo sapiens (Human) |
Description: | O00750 |
Residue: | 1634 |
Sequence: | MSSTQGNGEHWKSLESVGISRKELAMAEALQMEYDALSRLRHDKEENRAKQNADPSLISW
DEPGVDFYSKPAGRRTDLKLLRGLSGSDPTLNYNSLSPQEGPPNHSTSQGPQPGSDPWPK
GSLSGDYLYIFDGSDGGVSSSPGPGDIEGSCKKLSPPPLPPRASIWDTPPLPPRKGSPSS
SKISQPSDINTFSLVEQLPGKLLEHRILEEEEVLGGGGQGRLLGSVDYDGINDAITRLNL
KSTYDAEMLRDATRGWKEGRGPLDFSKDTSGKPVARSKTMPPQVPPRTYASRYGNRKNAT
PGKNRRISAAPVGSRPHTVANGHELFEVSEERDEEVAAFCHMLDILRSGSDIQDYFLTGY
VWSAVTPSPEHLGDEVNLKVTVLCDRLQEALTFTCNCSSTVDLLIYQTLCYTHDDLRNVD
VGDFVLKPCGLEEFLQNKHALGSHEYIQYCRKFDIDIRLQLMEQKVVRSDLARTVNDDQS
PSTLNYLVHLQERPVKQTISRQALSLLFDTYHNEVDAFLLADGDFPLKADRVVQSVKAIC
NALAAVETPEITSALNQLPPCPSRMQPKIQKDPSVLAVRENREKVVEALTAAILDLVELY
CNTFNADFQTAVPGSRKHDLVQEACHFARSLAFTVYATHRIPIIWATSYEDFYLSCSLSH
GGKELCSPLQTRRAHFSKYLFHLIVWDQQICFPVQVNRLPRETLLCATLYALPIPPPGSS
SEANKQRRVPEALGWVTTPLFNFRQVLTCGRKLLGLWPATQENPSARWSAPNFHQPDSVI
LQIDFPTSAFDIKFTSPPGDKFSPRYEFGSLREEDQRKLKDIMQKESLYWLTDADKKRLW
EKRYYCHSEVSSLPLVLASAPSWEWACLPDIYVLLKQWTHMNHQDALGLLHATFPDQEVR
RMAVQWIGSLSDAELLDYLPQLVQALKYECYLDSPLVRFLLKRAVSDLRVTHYFFWLLKD
GLKDSQFSIRYQYLLAALLCCCGKGLREEFNRQCWLVNALAKLAQQVREAAPSARQGILR
TGLEEVKQFFALNGSCRLPLSPSLLVKGIVPRDCSYFNSNAVPLKLSFQNVDPLGENIRV
IFKCGDDLRQDMLTLQMIRIMSKIWVQEGLDMRMVIFRCFSTGRGRGMVEMIPNAETLRK
IQVEHGVTGSFKDRPLADWLQKHNPGEDEYEKAVENFIYSCAGCCVATYVLGICDRHNDN
IMLKTTGHMFHIDFGRFLGHAQMFGNIKRDRAPFVFTSDMAYVINGGDKPSSRFHDFVDL
CCQAYNLIRKHTHLFLNLLGLMLSCGIPELSDLEDLKYVYDALRPQDTEANATTYFTRLI
ESSLGSVATKLNFFIHNLAQMKFTGSDDRLTLSFASRTHTLKSSGRISDVFLCRHEKIFH
PNKGYIYVVKVMRENTHEATYIQRTFEEFQELHNKLRLLFPSSHLPSFPSRFVIGRSRGE
AVAERRREELNGYIWHLIHAPPEVAECDLVYTFFHPLPRDEKAMGTSPAPKSSDGTWARP
VGKVGGEVKLSISYKNNKLFIMVMHIRGLQLLQDGNDPDPYVKIYLLPDPQKTTKRKTKV
ARKTCNPTYNEMLVYDGIPKGDLQQRELQLSVLSEQGFWENVLLGEVNIRLRELDLAQEK
TGWFALGSRSHGTL
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BDBM50274638 |
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n/a |
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Name | BDBM50274638 |
Synonyms: | CHEMBL4126156 | US10858355, Example 4 |
Type | Small organic molecule |
Emp. Form. | C20H23N3O4S2 |
Mol. Mass. | 433.544 |
SMILES | C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(C)(=O)=O)-c1sc(NC(C)=O)nc1C |r| |
Structure |
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