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TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform/gamma isoform
LigandBDBM50232430
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1647794
IC50 13±n/a nM
Citation Qin, LYRuan, ZCherney, RJDhar, TGMNeels, JWeigelt, CASack, JSSrivastava, ASCornelius, LAMTino, JAStefanski, KGu, XXie, JSusulic, VYang, XYarde-Chinn, MSkala, SBosnius, RGoldstein, CDavies, PRuepp, SSalter-Cid, LBhide, RSPoss, MA Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kd inhibitors. Bioorg Med Chem Lett27:855-861 (2017) [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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50232430
NameBDBM50232430
Synonyms:CHEMBL4061855 | US10214537, Example 262
TypeSmall organic molecule
Emp. Form.C28H34N8O2
Mol. Mass.514.622
SMILESC[C@H]1CN(C[C@@H](C)N1c1cccc(c1)-c1cc(-c2ccnn2C2CCOCC2)c2c(N)ncnn12)C(C)=O |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a