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TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
LigandBDBM272909
Substrate/Competitorn/a
Meas. Tech.p110alpha (alpha) PI3K Binding Assay
Ki<0.020±n/a nM
Citation Braun, MGarland, KHanan, EPurkey, HStaben, STHeald, RAKnight, JMacleod, CLu, AWu, GYeap, SK Tricyclic PI3K inhibitor compounds and methods of use US Patent US10065970 Publication Date 9/4/2018
More Info.:Get all data from this article,  Assay Method
 
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Name:Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Synonyms:P42336 | PI3-kinase p110 subunit alpha | PI3-kinase subunit p110-alpha | PI3K | PIK3CA | PK3CA_HUMAN | Phosphatidylinositol 3-kinase alpha (PI3Kalpha) | Phosphatidylinositol 4,5-biphosphate 3-kinase catalytic subunit alpha (PIK3CA) | Phosphatidylinositol 4,5-bisphosphate 3-kinase (PI3K) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit (PI3K-alpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha (PI3Kalpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform ( PI3K-alpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3-Ka) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3K alpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3K p110alpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3K) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3K-alpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3Ka) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3Kalpha p110alpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3Kalpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PIK3CA) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (p110alpha) | Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | Phosphoinositide 3-Kinase (PI3K), alpha | Phosphoinositide 3-Kinase (PI3K), alpha Chain A | Phosphoinositide 3-kinase alpha (PI3K-alpha) | Phosphoinositide 3-kinases (PI3K) | Phosphoinositide-3-kinase (PI3K alpha) | PtdIns-3-kinase p110 | p110 alpha
Type:Enzyme Subunit
Mol. Mass.:124294.87
Organism:Homo sapiens (Human)
Description:P42336
Residue:1068
Sequence:
MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKEARKYPLHQ
LLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFA
IGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKH
IYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLK
LCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPMD
CFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGI
YHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHC
PLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWF
SSVVKFPDMSVIEEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPL
SEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAME
LLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTN
QRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILK
QEKKDETQKVQMKFLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLW
LNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLS
IGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRS
CAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDF
LIVISKGAQECTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIA
YIRKTLALDKTEQEALEYFMKQMNDAHHGGWTTKMDWIFHTIKQHALN
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM272909
n/a
NameBDBM272909
Synonyms:(S)-2-((1-(2- aminobenzo[d]thiazol- 6-yl)-7,8,9,10- tetrahydro-6-oxa- 2,10a- diazacycloocta[cd]- inden-4-yl)amino)-2- cyclopropylacetamide | US10065970, Compound 214
TypeSmall organic molecule
Emp. Form.C23H24N6O2S
Mol. Mass.448.541
SMILESNC(=O)[C@@H](Nc1cc2OCCCCn3c(nc(c1)c23)-c1ccc2nc(N)sc2c1)C1CC1 |r|
Structure
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