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TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform
LigandBDBM340346
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2057575 (CHEMBL4712576)
Ki 1.7±n/a nM
Citation Cheng, H; Orr, STM; Bailey, S; Brooun, A; Chen, P; Deal, JG; Deng, YL; Edwards, MP; Gallego, GM; Grodsky, N; Huang, B; Jalaie, M; Kaiser, S; Kania, RS; Kephart, SE; Lafontaine, J; Ornelas, MA; Pairish, M; Planken, S; Shen, H; Sutton, S; Zehnder, L; Almaden, CD; Bagrodia, S; Falk, MD; Gukasyan, HJ; Ho, C; Kang, X; Kosa, RE; Liu, L; Spilker, ME; Timofeevski, S; Visswanathan, R; Wang, Z; Meng, F; Ren, S; Shao, L; Xu, F; Kath, JC Structure-Based Drug Design and Synthesis of PI3K?-Selective Inhibitor (PF-06843195). J Med Chem64:644-661 (2021) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform
Name:Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform
Synonyms:PI3-kinase subunit p110 beta/p85 alpha | PI3K p110 beta/p85 alpha | PI3K p110beta/p85alpha (Human) | Phosphoinositide 3-Kinase (PI3K), beta | p110β/p85α | p110beta/p85alpha
Type:Protein
Mol. Mass.:n/a
Description:n/a
Components:This complex has 2 components.
Component 1
Name:Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
Synonyms:PI3-kinase p110 subunit beta | PI3-kinase subunit p110-beta | PI3Kbeta | PIK3C1 | PIK3CB | PK3CB_HUMAN | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta (PI3Kbeta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PI3K beta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PI3K) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PI3K-beta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PI3Kbeta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PI3Kÿ²) | Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta isoform | Phosphoinositide 3-Kinase (PI3K), beta | Phosphoinositide 3-Kinase (PI3K), beta Chain A | Phosphoinositide-3-kinase (PI3K beta) | PtdIns-3-kinase p110
Type:Enzyme Subunit
Mol. Mass.:122769.00
Organism:Homo sapiens (Human)
Description:P42338
Residue:1070
Sequence:
MCFSFIMPPAMADILDIWAVDSQIASDGSIPVDFLLPTGIYIQLEVPREATISYIKQMLW
KQVHNYPMFNLLMDIDSYMFACVNQTAVYEELEDETRRLCDVRPFLPVLKLVTRSCDPGE
KLDSKIGVLIGKGLHEFDSLKDPEVNEFRRKMRKFSEEKILSLVGLSWMDWLKQTYPPEH
EPSIPENLEDKLYGGKLIVAVHFENCQDVFSFQVSPNMNPIKVNELAIQKRLTIHGKEDE
VSPYDYVLQVSGRVEYVFGDHPLIQFQYIRNCVMNRALPHFILVECCKIKKMYEQEMIAI
EAAINRNSSNLPLPLPPKKTRIISHVWENNNPFQIVLVKGNKLNTEETVKVHVRAGLFHG
TELLCKTIVSSEVSGKNDHIWNEPLEFDINICDLPRMARLCFAVYAVLDKVKTKKSTKTI
NPSKYQTIRKAGKVHYPVAWVNTMVFDFKGQLRTGDIILHSWSSFPDELEEMLNPMGTVQ
TNPYTENATALHVKFPENKKQPYYYPPFDKIIEKAAEIASSDSANVSSRGGKKFLPVLKE
ILDRDPLSQLCENEMDLIWTLRQDCREIFPQSLPKLLLSIKWNKLEDVAQLQALLQIWPK
LPPREALELLDFNYPDQYVREYAVGCLRQMSDEELSQYLLQLVQVLKYEPFLDCALSRFL
LERALGNRRIGQFLFWHLRSEVHIPAVSVQFGVILEAYCRGSVGHMKVLSKQVEALNKLK
TLNSLIKLNAVKLNRAKGKEAMHTCLKQSAYREALSDLQSPLNPCVILSELYVEKCKYMD
SKMKPLWLVYNNKVFGEDSVGVIFKNGDDLRQDMLTLQMLRLMDLLWKEAGLDLRMLPYG
CLATGDRSGLIEVVSTSETIADIQLNSSNVAAAAAFNKDALLNWLKEYNSGDDLDRAIEE
FTLSCAGYCVASYVLGIGDRHSDNIMVKKTGQLFHIDFGHILGNFKSKFGIKRERVPFIL
TYDFIHVIQQGKTGNTEKFGRFRQCCEDAYLILRRHGNLFITLFALMLTAGLPELTSVKD
IQYLKDSLALGKSEEEALKQFKQKFDEALRESWTTKVNWMAHTVRKDYRS
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Component 2
Name:Phosphatidylinositol 3-kinase regulatory subunit alpha
Synonyms:GRB1 | P85A_HUMAN | PI3-kinase class I | PI3-kinase p85 subunit alpha | PI3-kinase p85-alpha subunit | PI3-kinase p85-subunit alpha | PI3-kinase subunit p85-alpha | PI3K | PIK3CG/PIK3R1 | PIK3R1 | Phosphatidylinositol 3-kinase 85 kDa regulatory subunit alpha (PI3K alpha) | Phosphatidylinositol 3-kinase regulatory subunit alpha (PI3K p85-alpha) | Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) | Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3RI) | Phosphatidylinositol 3-kinase regulatory subunit alpha isoform 1 (PI3 Kinase alpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3Kalpha p85alpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3Kalpha) | Phosphoinositide 3-Kinase (PI3K) Chain B | PtdIns-3-kinase p85-alpha | p84 alpha | p85 alpha
Type:Protein
Mol. Mass.:83592.82
Organism:Homo sapiens (Human)
Description:P27986
Residue:724
Sequence:
MSAEGYQYRALYDYKKEREEDIDLHLGDILTVNKGSLVALGFSDGQEARPEEIGWLNGYN
ETTGERGDFPGTYVEYIGRKKISPPTPKPRPPRPLPVAPGSSKTEADVEQQALTLPDLAE
QFAPPDIAPPLLIKLVEAIEKKGLECSTLYRTQSSSNLAELRQLLDCDTPSVDLEMIDVH
VLADAFKRYLLDLPNPVIPAAVYSEMISLAPEVQSSEEYIQLLKKLIRSPSIPHQYWLTL
QYLLKHFFKLSQTSSKNLLNARVLSEIFSPMLFRFSAASSDNTENLIKVIEILISTEWNE
RQPAPALPPKPPKPTTVANNGMNNNMSLQDAEWYWGDISREEVNEKLRDTADGTFLVRDA
STKMHGDYTLTLRKGGNNKLIKIFHRDGKYGFSDPLTFSSVVELINHYRNESLAQYNPKL
DVKLLYPVSKYQQDQVVKEDNIEAVGKKLHEYNTQFQEKSREYDRLYEEYTRTSQEIQMK
RTAIEAFNETIKIFEEQCQTQERYSKEYIEKFKREGNEKEIQRIMHNYDKLKSRISEIID
SRRRLEEDLKKQAAEYREIDKRMNSIKPDLIQLRKTRDQYLMWLTQKGVRQKKLNEWLGN
ENTEDQYSLVEDDEDLPHHDEKTWNVGSSNRNKAENLLRGKRDGTFLVRESSKQGCYACS
VVVDGEVKHCVINKTATGYGFAEPYNLYSSLKELVLHYQHTSLVQHNDSLNVTLAYPVYA
QQRR
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BDBM340346
n/a
NameBDBM340346
Synonyms:US9758538, Example 34
TypeSmall organic molecule
Emp. Form.C19H26N8O4
Mol. Mass.430.4609
SMILESCOC(=O)N1CC[C@@](CO)(C1)Nc1cc(nc(n1)N1CCOCC1)-c1cnc(N)nc1 |r|
Structure
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