BindingDB BDBM92862 US9284315, BEZ-235::mTOR Inhibitor, BEZ235

BDBM92862 US9284315, BEZ-235::mTOR Inhibitor, BEZ235

SMILES Cn1c2cnc3ccc(cc3c2n(-c2ccc(cc2)C(C)(C)C#N)c1=O)-c1cnc2ccccc2c1

InChI Key InChIKey=JOGKUKXHTYWRGZ-UHFFFAOYSA-N

Data 2 KI 132 IC50 8 EC50

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 5 hits for monomerid = 92862

Serine/threonine-protein kinase mTOR(Human)
Northeastern University

Curated by ChEMBL

BDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)

IC50: 5nMAssay Description:Inhibition of human recombinant mTOR assessed as inhibition of 4EBP1 phosphorylation after 30 mins by TR-FRET analysisMore data for this Ligand-Target Pair

PDB MMDB NCI pathway Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar

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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Northeastern University

Curated by ChEMBL

BDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)

IC50: 20nMAssay Description:Inhibition of human PI3K-alpha assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysisMore data for this Ligand-Target Pair

PDB MMDB NCI pathway Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar

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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Human)
Northeastern University

Curated by ChEMBL

BDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)

IC50: 316nMAssay Description:Inhibition of human PI3K-beta assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysisMore data for this Ligand-Target Pair

PDB MMDB NCI pathway Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar

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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Human)
Northeastern University

Curated by ChEMBL

BDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)

IC50: 100nMAssay Description:Inhibition of human PI3K-gamma assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysisMore data for this Ligand-Target Pair

PDB MMDB NCI pathway Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar

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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Human)
Northeastern University

Curated by ChEMBL

BDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)

IC50: 13nMAssay Description:Inhibition of human PI3K-delta assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysisMore data for this Ligand-Target Pair

PDB MMDB NCI pathway Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar

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Filter my 140 hits

Targets 20▿
- Serine/threonine-protein kinase mTOR 26
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 22
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 22
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 21
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 20
- Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit delta isoform 6
- Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 6
- Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform 5
- ATP-binding cassette sub-family C member 3 1
- Serine-protein kinase ATM 1
- Phosphatidylinositol 3-kinase catalytic subunit type 3 1
- ATP-binding cassette sub-family C member 4 1
- Tyrosine-protein kinase JAK3 1
- ATP-binding cassette sub-family C member 2 1
- Histone deacetylase 6 1
- FKBP12A/mTOR 1
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform/Phosphoinositide 3-kinase regulatory subunit 5 1
- Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta 1
- Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha 1
- Bile salt export pump 1
- ...
Publications 39▿
- Bioorg Med Chem 26: 4537-4543 (2018) 6
- J Med Chem 65: 12781-12801 (2022) 5
- Eur J Med Chem 182: (2019) 5
- J Med Chem 57: 4834-48 (2014) 5
- Eur J Med Chem 228: (2022) 5
- Eur J Med Chem 208: (2020) 5
- ACS Med Chem Lett 7: 762-7 (2016) 5
- J Med Chem 60: 47-65 (2017) 5
- Eur J Med Chem 127: 509-520 (2017) 5
- Bioorg Med Chem Lett 22: 6788-93 (2012) 5
- Bioorg Med Chem Lett 29: 1313-1319 (2019) 5
- J Med Chem 65: 16033-16061 (2022) 5
- Bioorg Med Chem 23: 7765-76 (2015) 5
- Bioorg Med Chem 23: 5662-71 (2015) 5
- Eur J Med Chem 122: 731-743 (2016) 5
- Eur J Med Chem 178: 667-686 (2019) 5
- Bioorg Med Chem 23: 6477-85 (2015) 4
- Bioorg Med Chem 26: 3982-3991 (2018) 4
- Eur J Med Chem 158: 707-719 (2018) 4
- Toxicol Sci 136: 216-41 (2013) 4
- Bioorg Med Chem Lett 26: 4408-4413 (2016) 4
- Eur J Med Chem 208: (2020) 4
- Eur J Med Chem 157: 37-49 (2018) 4
- Eur J Med Chem 146: 460-470 (2018) 4
- Bioorg Med Chem 26: 1675-1685 (2018) 4
- J Med Chem 65: 8345-8379 (2022) 4
- Bioorg Med Chem 27: (2019) 3
- US Patent US9284315 (2016) 2
- Biochemistry 49: 8488-98 (2010) 2
- ACS Med Chem Lett 6: 434-8 (2015) 2
- Bioorg Med Chem Lett 47: (2021) 2
- Eur J Med Chem 199: (2020) 1
- Eur J Med Chem 164: 304-316 (2019) 1
- J Med Chem 65: 893-921 (2022) 1
- Bioorg Med Chem 26: 3992-4000 (2018) 1
- J Med Chem 56: 6991-7002 (2013) 1
- Bioorg Med Chem 23: 7585-96 (2015) 1
- J Med Chem 59: 559-77 (2016) 1
- J Med Chem 63: 10135-10157 (2020) 1
Institutions 26▿
- Xi'An Jiaotong University 21
- Shenyang Pharmaceutical University 12
- China Pharmaceutical University 12
- West China Hospital of Sichuan University 10
- Novartis Institutes For Biomedical Research 9
- Chongqing University 8
- Csir-Indian Institute of Integrative Medicine 6
- Jilin University 5
- Zydus Research Centre 5
- Hangzhou Xixi Hospital 5
- Montclair State University 5
- South China University of Technology 5
- School of Traditional Chinese Pharmacy 5
- Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory) 5
- Curtin University 5
- Northeastern University 5
- Amgen 4
- Zuanzhu Pharma 2
- Pfizer 2
- Harbin Medical University 2
- Pkucare Pharmaceutical R & D Center 2
- Eli Lilly 1
- Duke University School of Medicine 1
- Sichuan University 1
- Nanjing University of Chinese Medicine 1
- Zhejiang University 1
Affinity: 1.4 to 1.3E+5 nM▿
- Ki 2
- IC50 132
- EC50 8
- Affinity ≤ nM
Xtal structures: 0
Docked structures: 0
Catalog Cmpds: 1