Reaction Details |
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Target | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform |
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Ligand | BDBM50457968 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1761188 (CHEMBL4196435) |
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IC50 | 317±n/a nM |
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Citation | Ding, HW; Deng, CL; Li, DD; Liu, DD; Chai, SM; Wang, W; Zhang, Y; Chen, K; Li, X; Wang, J; Song, SJ; Song, HR Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3K?. Eur J Med Chem146:460-470 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform |
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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
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BDBM50457968 |
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n/a |
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Name | BDBM50457968 |
Synonyms: | CHEMBL4207750 |
Type | Small organic molecule |
Emp. Form. | C22H19ClFN5O3S |
Mol. Mass. | 487.934 |
SMILES | CCS(=O)(=O)Nc1cc(cnc1OC)-c1ccc2ncnc(Nc3ccc(F)c(Cl)c3)c2c1 |
Structure |
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