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TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform/gamma isoform
LigandBDBM50392138
Substrate/Competitorn/a
Meas. Tech.ChEMBL_851653
IC50 41±n/a nM
Citation Sutherlin DPBaker SBisconte ABlaney PMBrown AChan BKChantry DCastanedo GDePledge PGoldsmith PGoldstein DMHancox TKaur JKnowles DKondru RLesnick JLucas MCLewis CMurray JNadin AJNonomiya JPang JPegg NPrice SReif KSafina BSSalphati LStaben SSeward EMShuttleworth SSohal SSweeney ZKUltsch MWaszkowycz BWei B Potent and selective inhibitors of PI3Kd: obtaining isoform selectivity from the affinity pocket and tryptophan shelf. Bioorg Med Chem Lett 22:4296-302 (2012) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform/gamma isoform
Name:Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform/gamma isoform
Synonyms:PI3-kinase p110 subunit delta | PI3-kinase p110-delta subunit | PI3-kinase subunit p110-delta | PI3K | Phosphatidylinositol 4,5-biphosphate 3-kinase catalytic subunit delta (PIK3CD) | Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta | Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta (PI3K delta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic (PI3K) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta (PI3Kdelta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform ( PI3K-delta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3K delta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3K) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3K-delta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3Kd) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3Kdelta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3Kδ) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (p110 delta) | Phosphatidylinositol-4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta | Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta isoform | Phosphoinositide 3-Kinase (PI3K), delta | Phosphoinositide 3-Kinase (PI3K), delta Chain A | Phosphoinositide 3-kinases delta (PI3K delta) | Phosphoinositide-3-kinase (PI3K delta) | PtdIns-3-kinase p110 | p110delta | phosphatidylinositol 3-kinase (delta isoform)
Type:Enzyme Subunit
Mol. Mass.:119489.41
Organism:Homo sapiens (Human)
Description:O00329
Residue:1044
Sequence:
MPPGVDCPMEFWTKEENQSVVVDFLLPTGVYLNFPVSRNANLSTIKQLLWHRAQYEPLFH
MLSGPEAYVFTCINQTAEQQELEDEQRRLCDVQPFLPVLRLVAREGDRVKKLINSQISLL
IGKGLHEFDSLCDPEVNDFRAKMCQFCEEAAARRQQLGWEAWLQYSFPLQLEPSAQTWGP
GTLRLPNRALLVNVKFEGSEESFTFQVSTKDVPLALMACALRKKATVFRQPLVEQPEDYT
LQVNGRHEYLYGSYPLCQFQYICSCLHSGLTPHLTMVHSSSILAMRDEQSNPAPQVQKPR
AKPPPIPAKKPSSVSLWSLEQPFRIELIQGSKVNADERMKLVVQAGLFHGNEMLCKTVSS
SEVSVCSEPVWKQRLEFDINICDLPRMARLCFALYAVIEKAKKARSTKKKSKKADCPIAW
ANLMLFDYKDQLKTGERCLYMWPSVPDEKGELLNPTGTVRSNPNTDSAAALLICLPEVAP
HPVYYPALEKILELGRHSECVHVTEEEQLQLREILERRGSGELYEHEKDLVWKLRHEVQE
HFPEALARLLLVTKWNKHEDVAQMLYLLCSWPELPVLSALELLDFSFPDCHVGSFAIKSL
RKLTDDELFQYLLQLVQVLKYESYLDCELTKFLLDRALANRKIGHFLFWHLRSEMHVPSV
ALRFGLILEAYCRGSTHHMKVLMKQGEALSKLKALNDFVKLSSQKTPKPQTKELMHLCMR
QEAYLEALSHLQSPLDPSTLLAEVCVEQCTFMDSKMKPLWIMYSNEEAGSGGSVGIIFKN
GDDLRQDMLTLQMIQLMDVLWKQEGLDLRMTPYGCLPTGDRTGLIEVVLRSDTIANIQLN
KSNMAATAAFNKDALLNWLKSKNPGEALDRAIEEFTLSCAGYCVATYVLGIGDRHSDNIM
IRESGQLFHIDFGHFLGNFKTKFGINRERVPFILTYDFVHVIQQGKTNNSEKFERFRGYC
ERAYTILRRHGLLFLHLFALMRAAGLPELSCSKDIQYLKDSLALGKTEEEALKHFRVKFN
EALRESWKTKVNWLAHNVSKDNRQ
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  Blast E-value cutoff:
BDBM50392138
n/a
NameBDBM50392138
Synonyms:CHEMBL2152768
TypeSmall organic molecule
Emp. Form.C28H33FN6O2
Mol. Mass.504.599
SMILESCC(C)(O)C1CCN(Cc2ccc3nc(nc(N4CCOCC4)c3n2)-c2c(F)ccc3[nH]ccc23)CC1
Structure
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