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Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Ligand
BDBM346175
Substrate
n/a
Meas. Tech.
Cellular Assays for PI3Kalpha, Beta and Delta
IC50
434±n/a nM
Citation
 Fairhurst, RA; Furet, P; Kalthoff, FS; Lerchner, A; Rueeger, H Oxazolidin-2-one-pyrimidine derivatives and the use thereof as phosphatidylinositol-3-kinase inhibitors US Patent  US10202371 Publication Date 2/12/2019 
Target
Name:
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Synonyms:
PI3-kinase subunit alpha | PI3K-alpha | PI3Kalpha | PK3CA_RAT | Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha | Phosphoinositide-3-kinase catalytic alpha polypeptide | Pik3ca | PtdIns-3-kinase subunit alpha | PtdIns-3-kinase subunit p110-alpha | Serine/threonine protein kinase PIK3CA | p110alpha
Type:
Enzyme Catalytic Domain
Mol. Mass.:
124363.80
Organism:
Rattus norvegicus (Rat)
Description:
A0A0G2K344
Residue:
1068
Sequence:
MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLVTIKHELFKEARKYPLHQLLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFVIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLKLCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPIDSFTMPSYSRRISTATPYMNGETATKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHCPLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVIEEHANWSVSREAGFSYSHTGLSNRLARDNELRENDKEQLRALCTRDPLSEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAMELLDCNYPDPMVRSFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRQPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRSCAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDFLIVISKGAQEYTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYFTKQMNDAHHGGWTTKMDWIFHTIKQHALN
  
Inhibitor
Name:
BDBM346175
Synonyms:
US10202371, Example 5
Type:
Small organic molecule
Emp. Form.:
C23H22F3N7O3
Mol. Mass.:
501.4611
SMILES:
C[C@H]1[C@@H](OC(=O)N1c1cc(nc(n1)N1CCOCC1)-c1cnc(N)nc1C(F)(F)F)c1ccccc1 |r|
Structure:
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