Page last updated: 2024-11-13
ipi-145
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 50905713 |
| CHEMBL ID | 3039502 |
| CHEBI ID | 131169 |
| SCHEMBL ID | 153543 |
| SCHEMBL ID | 18343557 |
| SCHEMBL ID | 19670020 |
| SCHEMBL ID | 20580104 |
| MeSH ID | M0591924 |
Synonyms (66)
| Synonym |
|---|
| duvelisib , |
| HY-17044 |
| CHEBI:131169 |
| SJVQHLPISAIATJ-ZDUSSCGKSA-N |
| CS-0888 |
| S7028 |
| ink-1147 |
| CHEMBL3039502 |
| ipi-145 |
| ink-1197 |
| unii-610v23s0ji |
| 8-chloro-2-phenyl-3-((1s)-1-(7h-purin-6-ylamino)ethyl)isoquinolin-1(2h)-one |
| duvelisib [usan:inn] |
| 1201438-56-3 |
| 610v23s0ji , |
| 1(2h)-isoquinolinone, 8-chloro-2-phenyl-3-((1s)-1-(9h-purin-6-ylamino)ethyl)- |
| 8-chloro-2-phenyl-3-((1s)-1-(9h-purin-6-ylamino)ethyl)-1(2h)-isoquinolinone |
| gtpl7795 |
| (s)-3-(1-((9h-purin-6-yl)amino)ethyl)-8-chloro-2-phenylisoquinolin-1(2h)-one |
| compound 4904 [patent us8193182] |
| AKOS022186370 |
| SCHEMBL153543 |
| duvelisib [orange book] |
| duvelisib [who-dd] |
| duvelisib [usan] |
| duvelisib [mi] |
| duvelisib [inn] |
| (s)-3-(1-(9h-purin-6-ylamino)ethyl)-8-chloro-2-phenylisoquinolin-1(2h)-one |
| ipi145 |
| ipi-145 (ink1197) |
| ipi 145 |
| duvelisib (usan/inn) |
| D10555 |
| AC-30239 |
| ipi-145;ink1197 |
| DTXSID80152697 , |
| ink1197 |
| SCHEMBL18343557 |
| mfcd15144635 |
| SCHEMBL19670020 |
| NCGC00351482-01 |
| bdbm50193013 |
| SW219822-1 |
| duvelisib (ipi-145, ink1197) |
| DB11952 |
| SCHEMBL20580104 |
| BCP07042 |
| ipi-145 pound>>ink1197; ipi 145; ipi145; ink-1197; ink 1197 |
| EX-A1562 |
| ipi-145, ink 1197, duvelisib |
| Q27077129 |
| AS-16309 |
| AMY24208 |
| 1(2h)-isoquinolinone, 8-chloro-2-phenyl-3-[(1s)-1-(9h-purin-6-ylamino)ethyl]- |
| CCG-268854 |
| 8-chloro-2-phenyl-3-[(1s)-1-(7h-purin-6-ylamino)ethyl]isoquinolin-1-one |
| AKOS037515795 |
| nsc772469 |
| nsc-772469 |
| duvelisib (ipi-145) |
| EN300-18167128 |
| 8-chloro-2-phenyl-3-[(1s)-1-[(9h-purin-6-yl)amino]ethyl]-1,2-dihydroisoquinolin-1-one |
| compound 4904 (patent us8193182) |
| duvelisibum |
| dtxcid2075188 |
| 8-chloro-2-phenyl-3-[(1s)-1-[(9h-purin-6-yl)amino]ethyl]isoquinolin-1-one |
Research Excerpts
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " Primary safety outcomes included risk of grade ≥ 3 treatment-emergent adverse events (TEAEs); primary efficacy outcomes included objective response rate (ORR)." | ( A Matching-Adjusted Indirect Comparison of Single-Arm Trials in Patients with Relapsed or Refractory Follicular Lymphoma Who Received at Least Two Prior Systemic Treatments: Tazemetostat was Associated with a Lower Risk for Safety Outcomes Versus the PI3- Adib, D; Gupta, D; Mamlouk, K; Nellesen, D; Proudman, D; Yang, J, 2022) | 0.72 |
| " For safety analysis, the incidences of any grade and grade ≥3 adverse events (AEs), serious AEs, and treatment-related discontinuation and death were evaluated." | ( Safety and efficacy of dual PI3K-δ, γ inhibitor, duvelisib in patients with relapsed or refractory lymphoid neoplasms: A systematic review and meta-analysis of prospective clinical trials. Niu, T; Wang, J; Wang, Z; Xu, J; Zhou, H, 2022) | 0.72 |
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " In literature, there is no method valid for quantitation of DUV in human plasma for its therapeutic monitoring and pharmacokinetic studies." | ( A Highly Sensitive Nonextraction-Assisted HPLC Method with Fluorescence Detection for Quantification of Duvelisib in Plasma Samples and its Application to Pharmacokinetic Study in Rats. Almehizia, AA; Almomen, A; Alzoman, NZ; Darwish, IA; Khalil, NY; Sayed, AY, 2021) | 0.62 |
| "The purpose of this study is the establishment of a highly sensitive HPLC method with fluorescence detection for quantitation of DUV in plasma for its therapeutic monitoring and pharmacokinetic studies of DUV." | ( A Highly Sensitive Nonextraction-Assisted HPLC Method with Fluorescence Detection for Quantification of Duvelisib in Plasma Samples and its Application to Pharmacokinetic Study in Rats. Almehizia, AA; Almomen, A; Alzoman, NZ; Darwish, IA; Khalil, NY; Sayed, AY, 2021) | 0.62 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " IPI-145 significantly reduced arthritis severity in both RA models using dosing regimens initiated before onset of clinical disease." | ( Novel phosphoinositide 3-kinase δ,γ inhibitor: potent anti-inflammatory effects and joint protection in models of rheumatoid arthritis. Bartok, B; Boyle, DL; Firestein, GS; Kim, HR; Topolewski, K, 2014) | 1.31 |
| " Duvelisib represents a highly active agent, and ongoing investigations, including fixed-duration drug combinations and alternative dosing schedules, are aimed at reducing immune-mediated toxicities." | ( Duvelisib for CLL/SLL and follicular non-Hodgkin lymphoma. Danilov, AV; Pagel, JM; Patel, K, 2019) | 0.51 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (1)
| Class | Description |
|---|---|
| isoquinolines | A class of organic heteropolycyclic compound consisting of isoquinoline and its substitution derivatives. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
Protein Targets (12)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 1.8557 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 2.3919 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 0.7564 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Interferon beta | Homo sapiens (human) | Potency | 1.5809 | 0.0033 | 9.1582 | 39.8107 | AID1347411; AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 0.7564 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 0.7564 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 0.7564 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
Biological Processes (184)
Molecular Functions (46)
Ceullar Components (34)
Bioassays (73)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1869969 | Inhibition of N-terminal His6-tagged recombinant full length human PI3Kdelta expressed in baculovirus infected Sf21 insect cells at 1 uM by HTRF assay relative to control | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1555068 | Inhibition of PI3Kdelta in human whole blood assessed as reduction in fMLP-stimulated CD63 expression in basophils preincubated for 30 mins followed by fMLP stimulation | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1317009 | Inhibition of human PI3Kdelta (R108 to Q1044 residues) expressed in mammalian expression system incubated for 60 mins by ADAPTA assay | |||
| AID1555055 | Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells at 1 uM using PIP2 as substrate measured after 80 mins by transcreener fluores | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1869964 | Inhibition of N-terminal His6-tagged recombinant full length human PI3Kgamma expressed in baculovirus infected Sf21 insect cells at 0.1 uM by HTRF assay relative to control | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1870047 | Inhibition of N-terminal His6-tagged recombinant full length human PI3Kdelta expressed in baculovirus infected Sf21 insect cells incubated for 30 mins by HTRF assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1555052 | Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence po | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1553531 | Selectivity ratio of IC50 for PI3Kalpha in human Raji cells to IC50 for PI3Kdelta in human Raji cells | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1869970 | Inhibition of N-terminal His6-tagged recombinant full length human PI3Kdelta expressed in baculovirus infected Sf21 insect cells at 0.1 uM by HTRF assay relative to control | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1555050 | Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence pol | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1317034 | Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay | |||
| AID1636709 | Inhibition of PI3Kgamma/delta in human whole blood assessed as inhibition of FcepsilonR1/fMLP-stimulated basophil degranulation by measuring CD63+ cells | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
| AID1553532 | Selectivity ratio of IC50 for PI3Kbeta in human Raji cells to IC50 for PI3Kdelta in human Raji cells | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1869968 | Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1317027 | Inhibition of p110beta in HMEC assessed as reduction in Akt phosphorylation at Ser-473 residue at 0.01 to 1 uM after 1 hr by Western blot analysis | |||
| AID1870035 | Selectivity ratio of IC50 for N-terminal His6-tagged recombinant full length human PI3Kalpha expressed in baculovirus infected Sf21 insect cells to IC50 for N-terminal His6-tagged recombinant full length human PI3Kgamma expressed in baculovirus infected S | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1553529 | Inhibition of PI3Kdelta in human Raji cells | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1870037 | Antiproliferative activity against human SUDHL2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1555064 | Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-IgM-stimulated CD69 expression on B-cells preincubated for 60 mins followed by anti-IgM stimulation and measured after overnight incubation by flow cytometry | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1869965 | Inhibition of N-terminal His6-tagged recombinant full length human PI3Kgamma expressed in baculovirus infected Sf21 insect cells at 1 uM by HTRF assay relative to control | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1317035 | Antiproliferative activity against patient-derived IgM-stimulated CLL cells after 3 days by CellTiter-Glo assay | |||
| AID1317031 | Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay | |||
| AID1534886 | Inhibition of PI3Kdelta (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Targeting the immunity protein kinases for immuno-oncology. |
| AID1317030 | Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay | |||
| AID1421361 | Inhibition of PI3KCgamma (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Piperidinyl-embeded chalcones possessing anti PI3Kδ inhibitory properties exhibit anti-atopic properties in preclinical models. |
| AID1555059 | Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in antihuman IgM-stimulated AKT phosphorylation at Ser473 residue preincubated for 60 mins followed by antihuman IgM stimulation and measured after 15 mins | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1317028 | Inhibition of p110beta in HMEC assessed as reduction in Akt phosphorylation at Thr-308 residue at 0.01 to 1 uM after 1 hr by Western blot analysis | |||
| AID1421359 | Inhibition of PI3KCbeta/PIK3R1 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Piperidinyl-embeded chalcones possessing anti PI3Kδ inhibitory properties exhibit anti-atopic properties in preclinical models. |
| AID1525582 | Antifibrotic activity against mouse Mlg2908 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Discovery of 4-Methylquinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis. |
| AID1869972 | Inhibition of N-terminal His6-tagged recombinant full length human PI3Kbeta expressed in baculovirus infected Sf21 insect cells at 1 uM by HTRF assay relative to control | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1553533 | Cytotoxicity against in human Raji cells | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1894167 | Inhibition of p110delta (unknown origin) | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
| AID1870039 | Selectivity ratio of IC50 for human SKOV-3 cells over expressing PI3Kalpha to IC50 for human SUDHL-6 cells | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1534890 | Inhibition of PI3Kalpha (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Targeting the immunity protein kinases for immuno-oncology. |
| AID1555067 | Inhibition of PI3Kgamma in human whole blood assessed as reduction in anti-IgE-stimulated CD63 expression in basophils preincubated for 30 mins followed by anti-IgE stimulation | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1869967 | Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1421360 | Inhibition of PI3KCdelta/PIK3R1 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Piperidinyl-embeded chalcones possessing anti PI3Kδ inhibitory properties exhibit anti-atopic properties in preclinical models. |
| AID1555056 | Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells at 1 uM using PIP2 as substrate measured after 80 mins by transcreener fluoresc | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1870038 | Selectivity ratio of IC50 for human 786-O cells over expressing PI3Kbeta to IC50 for human SU-DHL-6 cells | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1534885 | Inhibition of PI3Kgamma (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Targeting the immunity protein kinases for immuno-oncology. |
| AID1421358 | Inhibition of PI3KCalpha/PIK3R1 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Piperidinyl-embeded chalcones possessing anti PI3Kδ inhibitory properties exhibit anti-atopic properties in preclinical models. |
| AID1553492 | Selectivity ratio of IC50 for PI3Kalpha (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1317033 | Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay | |||
| AID1553493 | Selectivity ratio of IC50 for PI3Kbeta (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1555051 | Inhibition of recombinant human full-length His-tagged PI3K p110gamma expressed in baculovirus expression system using PIP2 as substrate measured after 80 mins by transcreener fluorescence polarization assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1870046 | Inhibition of N-terminal His6-tagged recombinant full length human PI3Kgamma expressed in baculovirus infected Sf21 insect cells incubated for 30 mins by HTRF assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1869966 | Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1317010 | Inhibition of human PI3Kgamma (S144 to A1102 residues) expressed in mammalian expression system incubated for 60 mins by ADAPTA assay | |||
| AID1555065 | Inhibition of PI3Kdelta in rat whole blood assessed as reduction in anti-IgD-stimulated CD86 expression on B-cells preincubated for 60 mins followed by anti-IgD stimulation and measured after overnight incubation by flow cytometry | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1870036 | Selectivity ratio of IC50 for N-terminal His6-tagged recombinant full length human PI3Kbeta expressed in baculovirus infected Sf21 insect cells to IC50 for N-terminal His6-tagged recombinant full length human PI3Kgamma expressed in baculovirus infected Sf | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1317029 | Inhibition of p110beta in HMEC assessed as reduction in S6RP phosphorylation at Ser-235/236 residue at 0.01 to 1 uM after 1 hr by Western blot analysis | |||
| AID1555061 | Stability in human liver microsomes assessed as parent compound remaining at 1 uM measured after 30 mins in presence of NADPH generating system | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1317032 | Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay | |||
| AID1869971 | Inhibition of N-terminal His6-tagged recombinant full length human PI3Kalpha expressed in baculovirus infected Sf21 insect cells at 1 uM by HTRF assay relative to control | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1894168 | Inhibition of p110gamma (unknown origin) | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
| AID1534891 | Inhibition of PI3Kbeta (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Targeting the immunity protein kinases for immuno-oncology. |
| AID1555054 | Inhibition of recombinant human full-length His-tagged PI3K p110gamma expressed in baculovirus expression system at 1 uM using PIP2 as substrate measured after 80 mins by transcreener fluorescence polarization assay relative to control | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1869973 | Metabolic stability in human liver microsomes assessed as clearance at 1 uM measured upto 60 mins in presence of NADPH by measuring protein | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
| AID1555058 | Inhibition of PI3Kgamma in rat RAW264.7 cells assessed as reduction in C5a-stimulated AKT phosphorylation at Ser473 residue preincubated for 30 mins followed by C5a-stimulation and measured after 5 mins | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1555060 | Stability in rat liver microsomes assessed as parent compound remaining at 1 uM measured after 30 mins in presence of NADPH generating system | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. |
| AID1553530 | Inhibition of PI3Kgamma in human Raji cells | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1345778 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta (Phosphatidylinositol kinases) | 2013 | Chemistry & biology, Nov-21, Volume: 20, Issue:11 | PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. |
| AID1345786 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma (Phosphatidylinositol kinases) | 2013 | Chemistry & biology, Nov-21, Volume: 20, Issue:11 | PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. |
| AID1345748 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta (Phosphatidylinositol kinases) | 2013 | Chemistry & biology, Nov-21, Volume: 20, Issue:11 | PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. |
| AID1345749 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (Phosphatidylinositol kinases) | 2013 | Chemistry & biology, Nov-21, Volume: 20, Issue:11 | PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (78)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 47 (60.26) | 24.3611 |
| 2020's | 31 (39.74) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 20.68
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (20.68) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 14 (17.95%) | 5.53% |
| Reviews | 12 (15.38%) | 6.00% |
| Case Studies | 5 (6.41%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 47 (60.26%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||