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Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Ligand
BDBM50357666
Substrate
n/a
Meas. Tech.
ChEMBL_786049 (CHEMBL1921659)
Ki
0.900000±n/a nM
Citation
Nishimura, N; Siegmund, A; Liu, L; Yang, K; Bryan, MC; Andrews, KL; Bo, Y; Booker, SK; Caenepeel, S; Freeman, D; Liao, H; McCarter, J; Mullady, EL; San Miguel, T; Subramanian, R; Tamayo, N; Wang, L; Whittington, DA; Zalameda, L; Zhang, N; Hughes, PE; Norman, MH Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives. J Med Chem 54:4735-51 (2011) [PubMed] Article
More Info.:
Target
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:
Human
Description:
P42336
Residue:
1068
Sequence:
MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKEARKYPLHQLLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFAIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLKLCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPMDCFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHCPLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVIEEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPLSEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAMELLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRSCAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDFLIVISKGAQECTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYFMKQMNDAHHGGWTTKMDWIFHTIKQHALN