Reaction Details |
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Target | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform [H1047R] |
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Ligand | BDBM602619 |
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Substrate/Competitor | n/a |
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Meas. Tech. | PI3K-Alpha Kinase (PIK3CA) Activity, Wild-Type and H1047R Mutant and Determining IC50 Values for Inhibitors |
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IC50 | <500±n/a nM |
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Citation | ANDERSON, ED; ARONOW, SD; BOYLES, NA; DAHLGREN, MK; FENG, S; GERASYUTO, AI; HICKEY, ER; IRVIN, TC; KESICKI, EA; KLIPPEL-GIESE, A; KNIGHT, JL; KOLAKOWSKI, GR; KUMAR, M; LONG, KF; MAYNE, CG; MCELLIGOTT, DL; MCLEAN, JA; PUCA, L; RAVI, KK; SEVERANCE, DL; WELCH, MB; WIDJAJA, T ALLOSTERIC CHROMENONE INHIBITORS OF PHOSPHOINOSITIDE 3-KINASE (PI3K) FOR THE TREATMENT OF DISEASE US Patent US20230286960 Publication Date 9/14/2023 |
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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 [H1047R] |
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Name: | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform [H1047R] |
Synonyms: | PIK3CA | PK3CA_HUMAN | Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform mutant | Phosphoinositide 3-Kinase (PI3K), alpha Mutant (H1047R) Chain A |
Type: | Catalytic subunit |
Mol. Mass.: | 124314.42 |
Organism: | Homo sapiens (Human) |
Description: | P42336 H1047R |
Residue: | 1068 |
Sequence: | MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKEARKYPLHQ
LLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFA
IGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKH
IYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLK
LCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPMD
CFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGI
YHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHC
PLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWF
SSVVKFPDMSVIEEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPL
SEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAME
LLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTN
QRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILK
QEKKDETQKVQMKFLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLW
LNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLS
IGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRS
CAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDF
LIVISKGAQECTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIA
YIRKTLALDKTEQEALEYFMKQMNDARHGGWTTKMDWIFHTIKQHALN
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BDBM602619 |
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n/a |
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Name | BDBM602619 |
Synonyms: | 2-[1-[2-(4,4-Dimethyl-1-piperidyl)-6- methyl-4-oxo-chromen-8- yl]ethylamino]-N-methoxy-benzamide | US11649227, Example 19 | US20230286960, Example 19 |
Type | Small organic molecule |
Emp. Form. | C27H33N3O4 |
Mol. Mass. | 463.5686 |
SMILES | CONC(=O)c1ccccc1NC(C)c1cc(C)cc2c1oc(cc2=O)N1CCC(C)(C)CC1 |
Structure |
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