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TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
LigandBDBM50262139
Substrate/Competitorn/a
Meas. Tech.ChEMBL_514275 (CHEMBL979105)
IC50>10000±n/a nM
Citation Blois, JYuan, HSmith, APacold, MEWeissleder, RCantley, LCJosephson, L Slow self-activation enhances the potency of viridin prodrugs. J Med Chem51:4699-707 (2008) [PubMed]  Article
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:
BDBM50262139
n/a
NameBDBM50262139
Synonyms:2-acetamido-6-((5-acetoxy-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,7,10-trioxo-4,4a,6,6a,7,8,9,9a-octahydroindeno[4,5-h]isochromen-1(2H,5H,10H)-ylidene)methylamino)hexanoic acid | 2-acetamido-6-((Z)-((4S,4aR,5R,6aS,9aR)-5-acetoxy-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,7,10-trioxo-4,4a,6,6a,7,8,9,9a-octahydroindeno[4,5-h]isochromen-1(2H,5H,10H)-ylidene)methylamino)hexanoic acid | CHEMBL504715 | WmC20-lys, 2
TypeSmall organic molecule
Emp. Form.C31H40N2O11
Mol. Mass.616.6561
SMILESCOC[C@H]1OC(=O)C(=CNCCCCC(NC(C)=O)C(O)=O)C2C(=O)C(=O)C3=C([C@@H](C[C@@]4(C)[C@H]3CCC4=O)OC(C)=O)[C@@]12C |r,w:8.8,t:27|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: