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Report error Found 21 Enz. Inhib. hit(s) for PDB: 8V8U

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 3nMAssay Description:Inhibition of PI3Kalpha H1047R mutant (unknown origin) using PI(4,5)P2:PS as substrate incubated in presence of ATP by ADP-Glo assayMore data for this Ligand-Target Pair

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Date in BDB:
12/22/2024
Entry Details
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Guizhou Medical University

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 3.90nMAssay Description:Inhibition of His-tagged human full length PI3Kalpha coexpressed with p85 alpha in baculovirus expression system using PIP2 peptide as substrate incu...More data for this Ligand-Target Pair

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Date in BDB:
3/29/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 4.60nMAssay Description:Inhibition of wild type PI3Kalpha (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
12/22/2024
Entry Details
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 4.60nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
12/19/2024
Entry Details
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 4.60nMAssay Description:Inhibition of recombinant PI3Kalpha (unknown origin) by KinaseGlo assayMore data for this Ligand-Target Pair

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Date in BDB:
7/14/2018
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 4.80nMAssay Description:Inhibition of PI3Kalpha H1047R mutant (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
12/22/2024
Entry Details
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 5nMAssay Description:Inhibition of PI3K alpha (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
12/19/2024
Entry Details
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 5nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
9/3/2020
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 5nMAssay Description:Inhibition of P13Kalpha (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
11/15/2019
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 5nMAssay Description:Inhibition of P110alpha (unknown origin) by Kinase-Glo assayMore data for this Ligand-Target Pair

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Date in BDB:
11/22/2016
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 5nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
3/28/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 5nMAssay Description:Inhibition of P110alpha (unknown origin) using L-a-phosphatidylinositol as substrate by luminescence assayMore data for this Ligand-Target Pair

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Date in BDB:
4/13/2014
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 9.5nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr by ADP-glo plus luminescence assayMore data for this Ligand-Target Pair

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Date in BDB:
3/27/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 18nMAssay Description:Inhibition of human PI3Kalpha using PIP2 as substrate in presence of ATP measured after 30 mins by HTRF assayMore data for this Ligand-Target Pair

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Date in BDB:
3/28/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Human)
Guizhou Medical University

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 72nMAssay Description:Inhibition of N-terminal His6-tagged human recombinant full length PI3Kdelta co-expressed with human recombinant full length P85alpha in baculovirus ...More data for this Ligand-Target Pair

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Date in BDB:
3/29/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 74nMAssay Description:Inhibition of myristoylated human P110alpha expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analy...More data for this Ligand-Target Pair

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Date in BDB:
11/22/2016
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 74nMAssay Description:Inhibition of N-terminal myristoylated P110alpha (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISAMore data for this Ligand-Target Pair

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Date in BDB:
4/13/2014
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Mirati Therapeutics

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 200nMAssay Description:Inhibition of recombinant human N-terminal Myr signal and C-terminal Flag-tagged PI3K p110alpha expressed in rat Rat1 cellsMore data for this Ligand-Target Pair

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Date in BDB:
3/26/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Human)
Guizhou Medical University

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 383nMAssay Description:Inhibition of human PI3K p110delta/p85alpha using PIP2 as substrate in presence of ATP measured after 40 mins by HTRF assayMore data for this Ligand-Target Pair

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Date in BDB:
3/28/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Human)
Guizhou Medical University

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 1.54E+3nMAssay Description:Inhibition of N-terminal His6-tagged human recombinant full length PI3Kbeta co-expressed with human recombinant full length P85alpha in baculovirus i...More data for this Ligand-Target Pair

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Date in BDB:
3/29/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Human)
Guizhou Medical University

Curated by ChEMBL

BDBM50436459(CHEMBL2396661)

IC50: 1.84E+3nMAssay Description:Inhibition of human PI3K p110beta/p85alpha using PIP2 as substrate incubated for 40 mins in presence of ATP measured after 40 mins by HTRF assayMore data for this Ligand-Target Pair

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Date in BDB:
3/28/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Filter my 21 hits

Targets 4▿
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 16
- Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit delta isoform 2
- Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform 2
- Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
Publications 13▿
- J Med Chem 67: 4936-4949 (2024) 3
- Eur J Med Chem 197: (2020) 3
- Eur J Med Chem 209: (2021) 3
- Bioorg Med Chem Lett 25: 3582-4 (2015) 2
- Bioorg Med Chem Lett 23: 3741-8 (2013) 2
- Bioorg Med Chem 29: (2021) 1
- J Med Chem 64: 644-661 (2021) 1
- Bioorg Med Chem Lett 94: (2023) 1
- Bioorg Med Chem 25: 2657-2665 (2017) 1
- ACS Med Chem Lett 14: 1266-1274 (2023) 1
- J Med Chem 60: 47-65 (2017) 1
- Bioorg Med Chem Lett 25: 3569-74 (2015) 1
- ACS Med Chem Lett 11: 2156-2164 (2020) 1
Institutions 11▿
- Novartis Institutes For Biomedical Research 5
- Chinese Academy of Sciences 3
- Mirati Therapeutics 3
- Guizhou Medical University 3
- Shenyang Pharmaceutical University 1
- Zhejiang Chinese Medical University 1
- Pfizer 1
- Temple University 1
- University of Oxford 1
- Curtin University 1
- Zhejiang University 1
Affinity: 3 to 1.8E+3 nM▿
- IC50 21
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1