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Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Ligand
BDBM50315907
Substrate
n/a
Meas. Tech.
ChEMBL_790077 (CHEMBL1925467)
IC50
4±n/a nM
Citation
Sutherlin, DP; Bao, L; Berry, M; Castanedo, G; Chuckowree, I; Dotson, J; Folks, A; Friedman, L; Goldsmith, R; Gunzner, J; Heffron, T; Lesnick, J; Lewis, C; Mathieu, S; Murray, J; Nonomiya, J; Pang, J; Pegg, N; Prior, WW; Rouge, L; Salphati, L; Sampath, D; Tian, Q; Tsui, V; Wan, NC; Wang, S; Wei, B; Wiesmann, C; Wu, P; Zhu, BY; Olivero, A Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. J Med Chem 54:7579-87 (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:
Homo sapiens (Human)
Description:
P42336
Residue:
1068
Sequence:
MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKEARKYPLHQLLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFAIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLKLCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPMDCFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHCPLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVIEEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPLSEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAMELLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRSCAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDFLIVISKGAQECTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYFMKQMNDAHHGGWTTKMDWIFHTIKQHALN
Inhibitor
Name:
BDBM50315907
Synonyms:
5-(7-methyl-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine | CHEMBL1091978
Type:
Small organic molecule
Emp. Form.:
C21H28N8O3S2
Mol. Mass.:
504.629
SMILES:
Cc1c(CN2CCN(CC2)S(C)(=O)=O)sc2c(nc(nc12)-c1cnc(N)nc1)N1CCOCC1