| Reaction Details |
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 | Report a problem with these data |
| Target | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform [H1047R] |
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| Ligand | BDBM602676 |
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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] |
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| Synonyms: | PIK3CA | PK3CA_HUMAN | Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform mutant | Phosphoinositide 3-Kinase (PI3K), alpha Mutant (H1047R) Chain A |
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| Type: | Catalytic subunit |
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| Mol. Mass.: | 124314.42 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P42336 H1047R |
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| Residue: | 1068 |
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| Sequence: | MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKEARKYPLHQ
LLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFA
IGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKH
IYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLK
LCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPMD
CFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGI
YHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHC
PLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWF
SSVVKFPDMSVIEEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPL
SEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAME
LLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTN
QRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILK
QEKKDETQKVQMKFLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLW
LNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLS
IGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRS
CAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDF
LIVISKGAQECTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIA
YIRKTLALDKTEQEALEYFMKQMNDARHGGWTTKMDWIFHTIKQHALN
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| BDBM602676 |
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| n/a |
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| Name | BDBM602676 |
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| Synonyms: | 2-[1[2-(6,6-Difluoro-2- azaspiro[3.3]heptan-2-yl)-6- methyl-4-oxo-chromen-8- yl]ethylamino]benzoic acid 2,2,2-trifluoroacetic acid, Isomer 1 | US11649227, Example 222 | US20230286960, Example 222 |
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| Type | Small organic molecule |
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| Emp. Form. | C25H24F2N2O4 |
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| Mol. Mass. | 454.4659 |
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| SMILES | CC(Nc1ccccc1C(O)=O)c1cc(C)cc2c1oc(cc2=O)N1CC2(C1)CC(F)(F)C2 |
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| Structure | 
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