idelalisib: an antineoplastic agent and p110delta inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
idelalisib : A member of the class of quinazolines that is 5-fluoro-3-phenylquinazolin-4-one in which the hydrogen at position 2 is replaced by a (1S)-1-(3H-purin-6-ylamino)propyl group. used for for the treatment of refractory indolent non-Hodgkin's lymphoma and relapsed chronic lymphocytic leukemia. [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]
| ID Source | ID |
|---|---|
| PubMed CID | 11625818 |
| CHEMBL ID | 2216870 |
| CHEBI ID | 82701 |
| SCHEMBL ID | 356400 |
| SCHEMBL ID | 16782604 |
| MeSH ID | M0592589 |
| Synonym |
|---|
| idelalisib |
| HY-13026 |
| chebi:82701 , |
| gs-11cal-101 |
| cal 101 |
| cal-101 , |
| 1146702-54-6 |
| BCP9000471 |
| cal-101 (idelalisib, gs-1101) |
| cal101 |
| gs-1101 , |
| zydelig |
| chembl2216870 , |
| bdbm50403068 |
| 870281-82-6 |
| BCPP000307 |
| NCGC00262603-01 |
| idelalisib [usan:inn] |
| 5-fluoro-3-phenyl-2-((s)-1-(9h-purin-6-ylamino)-propyl)-3h-quinazolin-4-one |
| yg57i8t5m0 , |
| hsdb 8408 |
| unii-yg57i8t5m0 |
| gs 1101 |
| CS-0256 |
| S2226 |
| (s)-2-(1-(9h-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3h)-one |
| c22h18fn7o |
| 5-fluoro-3-phenyl-2-((1s)-1-(9h-purin-6-ylamino)propyl)-4(3h)-quinazolinone |
| 5-fluoro-3-phenyl-2-[(1s)-1-(7h-purin-6-ylamino)propyl]quinazolin-4-one |
| cal-101/cal101 |
| gtpl6741 |
| BRD-K60866521-001-01-4 |
| idelalisib [mi] |
| idelalisib [orange book] |
| idelalisib [jan] |
| 4(3h)-quinazolinone, 5-fluoro-3-phenyl-2-((1s)-1-(1h-purin-6-ylamino)propyl)- |
| idelalisib [who-dd] |
| 4(3h)-quinazolinone, 5-fluoro-3-phenyl-2-((1s)-1-(9h-purin-6-ylamino)propyl)- |
| idelalisib [usan] |
| idelalisib [inn] |
| idelalisib [vandf] |
| SCHEMBL356400 |
| AKOS022186334 |
| MLS006010985 |
| smr004702787 |
| 5-fluoro-3-phenyl-2-[(1s)-1-(3h-purin-6-ylamino)propyl]quinazolin-4(3h)-one |
| 5-fluoro-3-phenyl-2-[(1s)-1-(7h-purin-6-ylamino)propyl]quinazolin-4(3h)-one |
| 40L , |
| IFSDAJWBUCMOAH-HNNXBMFYSA-N |
| (s)-5-fluoro-3-phenyl-2-[1-(9h-purin-6-ylamino)-propyl]-3h-quinazolin-4-one |
| zydelig (tn) |
| D10560 |
| idelalisib (jan/usan/inn) |
| (s)-2-(1-((9h-purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3h)-one |
| AC-28394 |
| DB09054 |
| cal-101 (gs-1101) , |
| J-517532 |
| mfcd19443647 |
| EX-A1242 |
| EX-A330 |
| idelalisib; cal-101 |
| SCHEMBL16782604 |
| A-1138 , |
| NCGC00262603-02 |
| SW219823-1 |
| idelalisib (cal-101,gs-1101) |
| Q5908266 |
| idelalisib (cal-101) |
| BCP02532 |
| 4(3h)-quinazolinone,5-fluoro-3-phenyl-2-[(1s)-1-(1h-purin-6-ylamino)propyl]- |
| AMY9239 |
| CCG-264949 |
| NCGC00262603-04 |
| 1453810-72-4 |
| DTXSID701007266 |
| nsc759224 |
| idealisib |
| nsc800771 |
| nsc-759224 |
| nsc762828 |
| nsc-762828 |
| nsc-800771 |
| ic489666 |
| 5-fluoro-3-phenyl-2-((1s)-1-((7h-purin-6-yl)amino)propyl)quinazolin-4(3h)-one |
| 5-fluoro-3-phenyl-2-((1s)-1-(3h-purin-6-ylamino)propyl)quinazolin-4(3h)-one |
| l01xx47 |
| phosphoinositide-3 kinase delta inhibitor cal-101 |
| idelalisibum |
| 5-fluoro-3-phenyl-2-[(1s)-1-[(9h-purin-6-yl)amino]propyl]-3,4-dihydroquinazolin-4-one |
| EN300-7412931 |
| AC-36641 |
| AKOS040744041 |
Ielalisib is an oral first-in-class phosphatidylinositol 3-kinase delta (PI3Kδ) inhibitor approved for chronic lymphocytic leukaemia (CLL) alongside rituximab. It is approved for the treatment of CLL in patients with relapsed/refractory disease or in those harboring 17p deletions or tp53 mutations.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Idelalisib is a specific inhibitor of phosphoinositide 3-kinase (PI3K) δ." | ( Idelalisib inhibits experimental proliferative vitroretinopathy. Dong, L; Fang, D; Han, H; Han, Z; Huang, X; Lei, H; Ma, G; Qi, H; Tian, J; Vanhaesebroeck, B; Wang, L; Zhang, G; Zhang, S, 2022) | 2.89 |
| "Idelalisib is a phosphatidylinositol 3-kinase inhibitor highly selective for the delta isoform that has shown good efficacy in treating chronic lymphocytic leukemia and follicular lymphoma. " | ( Identification of Candidate Risk Factor Genes for Human Idelalisib Toxicity Using a Collaborative Cross Approach. Cai, Y; Corty, RW; Eaddy, JS; Mosedale, M; Nautiyal, M; Valdar, W; Watkins, PB, 2019) | 2.2 |
| "Idelalisib is a very potent anti-lymphoma agent in CLL and other NHL. " | ( Efficacy and safety of idelalisib for the treatment of indolent B-cell malignancies. Rydygier, D; Smolewski, P, 2020) | 2.31 |
| "Idelalisib is an orally administered, highly selective inhibitor of phosphatidylinositol 3-kinase-δ. " | ( Phase 1b study to investigate the safety and tolerability of idelalisib in Japanese patients with relapsed/refractory follicular lymphoma and chronic lymphocytic leukemia. Bhargava, P; Fukuhara, N; Fukui, M; Humeniuk, R; Izutsu, K; Kinoshita, T; Mathias, A; Nagai, H; Rajakumaraswamy, N; Tobinai, K; Xing, G; Yamamoto, G; Yamamoto, K, 2020) | 2.24 |
| "Idelalisib is a phosphatidylinositol 3-kinase δ inhibitor approved for relapsed/refractory follicular lymphoma, a type of indolent non-Hodgkin lymphoma (iNHL), and chronic lymphocytic leukemia (CLL). " | ( Retrospective Analysis of the Impact of Adverse Event-Triggered Idelalisib Interruption and Dose Reduction on Clinical Outcomes in Patients With Relapsed/Refractory B-Cell Malignancies. Chan, RJ; Gu, L; Ma, S; Rajakumaraswamy, N; Ruzicka, BB; Wagner-Johnston, ND; Xing, G, 2021) | 2.3 |
| "Idelalisib is a highly selective inhibitor of the PI3K p110∂ isoform and is approved for the treatment of CLL in patients with relapsed/refractory disease or in those harboring 17p deletions or tp53 mutations." | ( The PI3K∂-Selective Inhibitor Idelalisib Induces T- and NK-Cell Dysfunction Independently of B-Cell Malignancy-Associated Immunosuppression. Brauchle, B; Bücklein, VL; Ogrinc Wagner, A; Rohrbacher, L; Subklewe, M; von Bergwelt-Baildon, M, 2021) | 1.63 |
| "Idelalisib (IDL) is an oral first-in-class phosphatidylinositol 3-kinase delta (PI3Kδ) inhibitor approved for chronic lymphocytic leukaemia (CLL) alongside rituximab (R) since 2014. " | ( A retrospective observational study to evaluate the clinical outcomes and routine management of patients with chronic lymphocytic leukaemia treated with idelalisib and rituximab in the UK and Ireland (RETRO-idel). Cursley, AP; Eyre, TA; Fegan, C; Gu, L; Islam, A; Kagdi, H; Nicholson, T; Preston, G; Rajakumaraswamy, N; Ramroth, H; Smith, HW; Xing, G, 2021) | 2.26 |
| "Idelalisib is a highly selective oral inhibitor of PI3Kδ indicated for the treatment of patients with relapsed chronic lymphocytic leukemia in combination with rituximab. " | ( The PI3Kδ-Selective Inhibitor Idelalisib Minimally Interferes with Immune Effector Function Mediated by Rituximab or Obinutuzumab and Significantly Augments B Cell Depletion In Vivo. Bacac, M; Carter, MJ; Cox, KL; Cragg, MS; Frey, CR; Grosmaire, L; Herter, S; Jones, R; Klein, C; Limani, F; Marshall, MJE; Oldham, RJ; Palazzo, A; Tannheimer, S; Turaj, AH; Umana, P, 2018) | 2.21 |
| "As idelalisib is a PI3K inhibitor in clinical use for the treatment of non-Hodgkin lymphomas, we asked whether this inhibitor affects PMN functionalities." | ( Idelalisib impairs TREM-1 mediated neutrophil inflammatory responses. Alflen, A; Aranda Lopez, P; Heß, G; Radsak, MP; Stadler, N; Teschner, D; Theobald, M, 2018) | 2.44 |
| "Idelalisib (ILB) is a selective phosphatidylinositol-3-kinase delta inhibitor approved for the treatment of hematological malignancies. " | ( Identification of Novel Pathways in Idelalisib Metabolism and Bioactivation. Bi, H; Lu, J; Ma, X; Shehu, AI; Wang, P; Zhu, J, 2018) | 2.2 |
| "Idelalisib acts as a phosphoinositide 3 kinase inhibitor, which has been approved by the US FDA for the treatment of certain hematological malignancies. " | ( Characterization of the in vitro metabolites of idelalisib in liver microsomes and interspecies comparison. Chen, CM; Chen, JF; Chen, Y; Wu, WB, 2019) | 2.21 |
| "Idelalisib is a potent and selective inhibitor of the PI3Kδ approved since September 2014 for the treatment of several types of B cell malignancies. " | ( Pulmonary adverse events related to idelalisib therapy: A single centre experience. Bani-Sadr, F; Delmer, A; Giltat, A; Julien, G; Lebargy, F; Lebrun, D; Migault, C; Nguyen, Y; Toubas, D; Toubas, O, 2018) | 2.2 |
| "Idelalisib is a novel, highly selective, small-molecule, tyrosine kinase inhibitor with potent activity against phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3Kδ). " | ( Idelalisib for the treatment of indolent non-Hodgkin's lymphoma. Jimeno, A; Lopez, JP, 2014) | 3.29 |
| "Idelalisib (Zydelig(®)) is a highly specific small-molecule phosphatidylinositol-3-kinase (PI3Kδ) inhibitor that has been developed as an oral treatment for B cell haematological cancers.It has received its first approval in the US in July 2014 for the treatment of relapsed chronic lymphocytic leukaemia(CLL), relapsed follicular B-cell non-Hodgkin lymphoma(NHL) and relapsed small lymphocytic lymphoma (SLL) [corrected]. " | ( Idelalisib: first global approval. Markham, A, 2014) | 3.29 |
| "Idelalisib (Zydelig®) is a first-in-class, orally administered, phosphatidylinositol 3-kinase-δ inhibitor that was recently approved for the treatment of relapsed chronic lymphocytic leukaemia (CLL), relapsed follicular B-cell non-Hodgkin's lymphoma (NHL) and relapsed small lymphocytic lymphoma (SLL) in the USA and for the treatment of CLL and refractory follicular lymphoma in the EU. " | ( Idelalisib: a review of its use in chronic lymphocytic leukaemia and indolent non-Hodgkin's lymphoma. Keating, GM, 2015) | 3.3 |
| "Idelalisib is an orally bioavailable ATP-competitive kinase inhibitor that targets the PI3K p110 isoform δ (PI3Kδ) with high potency and selectivity." | ( Idelalisib: First-in-Class PI3K Delta Inhibitor for the Treatment of Chronic Lymphocytic Leukemia, Small Lymphocytic Leukemia, and Follicular Lymphoma. Gandhi, V; Modi, P; Newcomb, T; Quéva, C; Yang, Q, 2015) | 2.58 |
| "Idelalisib is a promising new therapy for relapsed indolent B-cell malignancies." | ( Idelalisib- a PI3Kδ targeting agent for B-cell malignancies. Hewett, YG; Shah, BK; Uprety, D, 2016) | 2.6 |
| "Idelalisib is a first-in-class selective, oral, phosphatidylinositol 3-kinase delta (PI3Kδ) inhibitor approved for the treatment of several types of blood cancer. " | ( Management of adverse events associated with idelalisib treatment: expert panel opinion. Barrientos, JC; Brown, JR; Coutré, SE; de Vos, S; Furman, RR; Keating, MJ; Li, D; O'Brien, SM; Pagel, JM; Poleski, MH; Sharman, JP; Yao, NS; Zelenetz, AD, 2015) | 2.12 |
| "Idelalisib is a potent, first-in-class selective inhibitor of phosphatidylinositol-3-kinaseδ (PI3Kδ) approved by the FDA in July 2014 for the treatment of relapsed CLL, in combination with rituximab, in patients for whom rituximab monotherapy would be considered appropriate due to other comorbidities. " | ( Idelalisib: A Novel PI3Kδ Inhibitor for Chronic Lymphocytic Leukemia. Mangaonkar, A; Shah, A, 2015) | 3.3 |
| "Idelalisib is a potent and selective phosphatidylinositol 3-kinase-δ inhibitor, which is a first-in-class agent to be approved for the treatment of relapsed chronic lymphocytic leukaemia, follicular B cell non-Hodgkin's lymphoma and small lymphocytic lymphoma. " | ( Clinical Pharmacokinetic and Pharmacodynamic Profile of Idelalisib. Jin, F; Kearney, BP; Ramanathan, S; Sharma, S, 2016) | 2.12 |
| "Idelalisib is an oral PI3Kδ inhibitor approved in 2014 in the USA and the EU as monotherapy in relapsed follicular lymphoma or relapsed small lymphocytic lymphoma previously treated with two or more prior systemic therapies, or as part of combination therapy with rituximab in patients with chronic lymphocytic leukemia, for whom rituximab monotherapy would be considered appropriate due to the presence of comorbidities." | ( Idelalisib for relapsed/refractory indolent B-cell non-Hodgkin's lymphoma: an overview of pharmacokinetics and clinical trial outcomes. Davies, A, 2015) | 2.58 |
| "Idelalisib is a highly specific small-molecule phosphoinositide-3-kinase δ inhibitor that was recently approved by the Food and Drug Administration for the treatment of chronic lymphocytic leukemia/small lymphocytic lymphoma and follicular lymphoma. " | ( Idelalisib-associated Enterocolitis: Clinicopathologic Features and Distinction From Other Enterocolitides. Berry, GJ; Coutre, SE; DiMaio, MA; Longacre, TA; Louie, CY; Matsukuma, KE, 2015) | 3.3 |
| "Idelalisib is an inhibitor of the PI3Kδ isoform approved for treatment of patients with relapsed chronic lymphocytic leukemia and indolent non-Hodgkin lymphoma. " | ( Idelalisib-associated Colitis: Histologic Findings in 14 Patients. Bhavsar, EB; Furman, RR; Geyer, JT; Jessurun, J; Leonard, JP; Panarelli, NC; Weidner, AS; Yantiss, RK, 2015) | 3.3 |
| "Idelalisib is a first-in-class oral inhibitor of PI3Kδ that has shown substantial activity in patients with relapsed/refractory chronic lymphocytic leukemia (CLL). " | ( A phase 2 study of idelalisib plus rituximab in treatment-naïve older patients with chronic lymphocytic leukemia. Burger, JA; Coutre, SE; Dansey, RD; Dubowy, RL; Flinn, I; Holes, L; Johnson, DM; Keating, M; Kim, Y; Kipps, TJ; Lamanna, N; Miller, LL; Mitra, S; O'Brien, SM; Yu, AS; Zelenetz, AD, 2015) | 2.19 |
| "Idelalisib is a novel, potent inhibitor of phosphatidylinositol 3-kinase delta (PI3Kδ), which is prominently expressed in cells of hematopoietic origin. " | ( The pharmacokinetics and safety of idelalisib in subjects with severe renal impairment. Hisoire, G; Jin, F; Ramanathan, S; Robeson, M; Zhou, H, 2015) | 2.14 |
| "Idelalisib is a potent PI3Kδ inhibitor that was recently approved for treating hematologic malignancies. " | ( Population pharmacokinetic modeling of idelalisib, a novel PI3Kδ inhibitor, in healthy subjects and patients with hematologic malignancies. Fang, L; Gao, Y; Jin, F; Li, X; Ramanathan, S; Zhou, H, 2016) | 2.15 |
| "Idelalisib is a potent, selective inhibitor of the delta isoform of phosphatidylinositol-3-kinase (PI3K), a lipid kinase whose over-activity in B-NHL drives disease progression." | ( Idelalisib for the treatment of non-Hodgkin lymphoma. Gopal, AK; Graf, SA, 2016) | 2.6 |
| "Idelalisib is a well-tolerated and effective treatment for patients with relapsed or refractory CLL or indolent NHL, providing a novel targeted therapeutic option for the management of these hematologic malignancies." | ( Idelalisib for treatment of B-cell malignancies. Do, B; Mace, M; Rexwinkle, A, 2016) | 3.32 |
| "Idelalisib is a first-in-class inhibitor of the PI3K delta isoform that shows near complete inhibition of AKT phosphorylation in CLL cells in vitro and in vivo." | ( The PI3K pathway: clinical inhibition in chronic lymphocytic leukemia. Brown, JR, 2016) | 1.16 |
| "Idelalisib is a small-molecule inhibitor of PI3Kδ with demonstrated efficacy for the treatment of relapsed/refractory chronic lymphocytic leukemia (CLL). " | ( Idelalisib given front-line for treatment of chronic lymphocytic leukemia causes frequent immune-mediated hepatotoxicity. Abramson, JS; Armand, P; Arnason, JE; Brown, JR; Davids, MS; Fein, J; Fernandes, S; Fisher, DC; Freedman, AS; Hanna, J; Jacobson, CA; Kasar, SN; Kim, HT; Kipps, TJ; Lampson, BL; Matos, TR; Morgan, EA; Rassenti, L; Ritz, J, 2016) | 3.32 |
| "Idelalisib is a first-in-class selective oral PI3Kδ inhibitor for the treatment of patients with relapsed chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma, a predominantly elderly population with high comorbidity. " | ( Idelalisib for the treatment of chronic lymphocytic leukemia/small lymphocytic lymphoma. Barrientos, JC, 2016) | 3.32 |
| "Idelalisib is a selective inhibitor of the delta isoform of phosphatidylinositol 3-kinase which was approved by the United States Federal Drug Administration in 2014 for the treatment of relapsed chronic lymphocytic leukemia and indolent non-Hodgkin lymphoma. " | ( Idelalisib-induced colitis and skin eruption mimicking graft-versus-host disease. Al-Taee, A; Cao, D; Fesler, M; Hammami, MB; Hurley, MY; Lai, JP; Meeks, M, 2017) | 3.34 |
| "Idelalisib is a PI3Kδ inhibitor that has been approved for the treatment of lymphoma and chronic lymphocytic leukemia in the relapsed/refractory setting, and several other PI3K inhibitors are being developed targeting other isoforms of the PI3K enzyme, which results in distinct toxicities and variable efficacy in the clinical setting." | ( Clinical use of PI3K inhibitors in B-cell lymphoid malignancies: today and tomorrow. Blum, KA; Cohen, JB; Flowers, CR; Greenwell, IB, 2017) | 1.18 |
| "Idelalisib is a targeted agent that potently inhibits PI3Kδ which is exclusively expressed in hematological cells. " | ( Idelalisib and bendamustine combination is synergistic and increases DNA damage response in chronic lymphocytic leukemia cells. Balakrishnan, K; Gandhi, V; Keating, MJ; Modi, P; Wierda, WG; Yang, Q, 2017) | 3.34 |
Ielalisib has shown efficacy with acceptable safety as monotherapy and combination therapy in relapsed/refractory CLL. It is currently approved for use in combination with rituximab.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Idelalisib has shown efficacy in the relapsed setting and is currently approved by the FDA for use in combination with rituximab." | ( Three newly approved drugs for chronic lymphocytic leukemia: incorporating ibrutinib, idelalisib, and obinutuzumab into clinical practice. Burger, JA; Keating, MJ; O'Brien, SM; Sanford, DS; Wierda, WG, 2015) | 1.36 |
| "Idelalisib has shown efficacy with acceptable safety as monotherapy and combination therapy in relapsed/refractory CLL." | ( Idelalisib for the treatment of chronic lymphocytic leukemia/small lymphocytic lymphoma. Barrientos, JC, 2016) | 2.6 |
Idelalisib (IDELA) treatment is associated with diarrhea/colitis (incidence of ∼15% grade ≥3). IdelalisIB treatment resulted in nodal responses in 81% of patients. Treatment was well tolerated in patients with allergic rhinitis and appears to reduce allergic responses after an environmental allergen challenge.
Pulmonary adverse events related to idelalisib are an emerging serious adverse event. Expert panel convened to review the pathology of these treatment-emergent adverse events (TEAEs) Panel was able to shape recommendations which may assist hematologist.
The objective of this analysis was to develop a population pharmacokinetic model for idelalisib and its inactive metabolite GS-563117. No meaningful impact on idelaliib pharmacokinetics was noted for any of the covariates tested.
| Excerpt | Reference | Relevance |
|---|---|---|
| " In a population pharmacokinetic model, no meaningful impact on idelalisib pharmacokinetics was noted for any of the covariates tested." | ( Clinical Pharmacokinetic and Pharmacodynamic Profile of Idelalisib. Jin, F; Kearney, BP; Ramanathan, S; Sharma, S, 2016) | 0.92 |
| " The objective of this analysis was to develop a population pharmacokinetic model for idelalisib and its inactive metabolite GS-563117 and to evaluate the impact of covariates on idelalisib/GS-563117 PK." | ( Population pharmacokinetic modeling of idelalisib, a novel PI3Kδ inhibitor, in healthy subjects and patients with hematologic malignancies. Fang, L; Gao, Y; Jin, F; Li, X; Ramanathan, S; Zhou, H, 2016) | 0.93 |
| " Here, we review the available literature on the pharmacokinetic and pharmacodynamic properties of these novel agents to guide the reader in the appropriate use of ibrutinib, idelalisib, and venetoclax." | ( Pharmacokinetic and Pharmacodynamic Considerations in the Treatment of Chronic Lymphocytic Leukemia: Ibrutinib, Idelalisib, and Venetoclax. Hill, BT; Waldron, M; Winter, A, 2017) | 0.86 |
Tirabrutinib in combination with idelalisib or entospletinib was well tolerated in patients with CLL. Study established an acceptable safety profile for concurrent selective inhibition of BTK with either PI3Kδ or SYK.
Ielalisib is an orally bioavailable ATP-competitive kinase inhibitor that targets the PI3K p110 isoform δ (PI3Kδ) with high potency and selectivity.
The recommended dosage of idelalisib is 150 mg orally twice daily; the medication can be taken without regard to mealtimes. The pharmacology, pharmacokinetics, clinical efficacy, safety and tolerability, dosing and administration, and place in therapy are reviewed.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Analysis of anti-CD20 mediated activation of natural killer cells isolated from patients on continued oral ibrutinib treatment suggested that repeated drug dosing inhibits these cells in vivo." | ( Ibrutinib interferes with the cell-mediated anti-tumor activities of therapeutic CD20 antibodies: implications for combination therapy. Beurskens, FJ; Breij, EC; Da Roit, F; Engelberts, PJ; Golay, J; Gritti, G; Introna, M; Parren, PW; Rambaldi, A; Taylor, RP, 2015) | 0.42 |
| " Idelalisib may be administered without regard to food on the basis of the absence of clinically relevant food effects, and was accordingly dosed in primary efficacy/safety studies." | ( Clinical Pharmacokinetic and Pharmacodynamic Profile of Idelalisib. Jin, F; Kearney, BP; Ramanathan, S; Sharma, S, 2016) | 1.59 |
| " Idelalisib dosing was generally well tolerated with most treatment-emergent adverse events and laboratory abnormalities assessed as grade 1 or 2 in severity." | ( The pharmacokinetics and safety of idelalisib in subjects with severe renal impairment. Hisoire, G; Jin, F; Ramanathan, S; Robeson, M; Zhou, H, 2015) | 1.6 |
| "The pharmacology, pharmacokinetics, clinical efficacy, safety and tolerability, dosing and administration, and place in therapy of idelalisib, a targeted therapy for certain types of non-Hodgkin's lymphoma (NHL), are reviewed." | ( Idelalisib for treatment of B-cell malignancies. Do, B; Mace, M; Rexwinkle, A, 2016) | 2.08 |
| " The recommended dosage of idelalisib is 150 mg orally twice daily; the medication can be taken without regard to mealtimes." | ( Idelalisib for treatment of B-cell malignancies. Do, B; Mace, M; Rexwinkle, A, 2016) | 2.17 |
| " The results showed that compound 11 exhibited good antibacterial activity against Serratia marcescens compared to the positive control ampicillin at a dosage of 100 μg/disk." | ( Halogenated Sesquiterpenoids from the Red Alga Laurencia tristicha Collected in Taiwan. Chen, JY; Chiou, SF; Huang, CY; Hwang, TL; Lin, YS; Sheu, JH; Wang, WL, 2016) | 0.43 |
| " The main challenge of the optimization process was to identify an orally available compound with a good pharmacokinetic profile in preclinical species that predicted a suitable dosing regimen in humans." | ( Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. Armengol, C; Bernal, FJ; Bravo, M; Cabedo, J; Calama, E; Caturla, JF; Domínguez, M; Erra, M; Gràcia, J; Gréco, A; Hernández, B; Lehner, MD; Miralpeix, M; Paris, S; Sabaté, M; Soria, S; Taltavull, J, 2017) | 0.46 |
| " We randomised patients in a 2:1 ratio using a web-based interactive system that generated a unique treatment code, and assigned patients to receive either idelalisib plus ofatumumab (oral idelalisib 150 mg twice daily continuously plus ofatumumab 300 mg intravenously in week 1, then 1000 mg intravenously weekly for 7 weeks, and every 4 weeks for 16 weeks) or ofatumumab alone (ofatumumab dosing as per the combination group, except 2000 mg was substituted for the 1000 mg dose)." | ( Efficacy and safety of idelalisib in combination with ofatumumab for previously treated chronic lymphocytic leukaemia: an open-label, randomised phase 3 trial. Awan, FT; Badoux, X; Brown, JR; Coutre, S; Dreiling, L; Dubowy, R; Flinn, IW; Jones, JA; Loscertales, J; Owen, C; Robak, T; Taylor, K; Vandenberghe, E; Wach, M; Wagner-Johnston, N; Xing, G; Ysebaert, L, 2017) | 0.96 |
| " Alternative dosing regimens and new PI3K inhibitors should be explored, particularly in patients who are double-refractory to inhibitors of BTK and Bcl-2." | ( Idelalisib (PI3Kδ inhibitor) therapy for patients with relapsed/refractory chronic lymphocytic leukemia: A Swedish nation-wide real-world report on consecutively identified patients. Axelsson, P; Ellin, F; Hansson, L; Johansson, H; Kjellander, C; Larsson, K; Lauri, B; Lewerin, C; Mattsson, A; Österborg, A; Scharenberg, C; Sylvan, SE; Tätting, L, 2023) | 2.35 |
| Role | Description |
|---|---|
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| apoptosis inducer | Any substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms. |
| EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | An inhibitor of phosphatidylinositol 3-kinase, EC 2.7.1.137, a family of related enzymes capable of phosphorylating the 3 position hydroxy group of the inositol ring of a phosphatidylinositol. |
| [role 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] | |
| Class | Description |
|---|---|
| purines | A class of imidazopyrimidines that consists of purine and its substituted derivatives. |
| organofluorine compound | An organofluorine compound is a compound containing at least one carbon-fluorine bond. |
| quinazolines | Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives. |
| aromatic amine | An amino compound in which the amino group is linked directly to an aromatic system. |
| secondary amino compound | A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups. |
| [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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 2.7242 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 1.4125 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Bone morphogenetic protein receptor type-1B | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.1413 | 3.7000 | AID1424922 |
| Membrane-associated progesterone receptor component 1 | Homo sapiens (human) | Kd | 30.0000 | 0.2040 | 0.2040 | 0.2040 | AID1425109 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform | Homo sapiens (human) | EC50 (µMol) | 0.0080 | 0.0080 | 0.0428 | 0.0930 | AID1894167 |
| Serine/threonine-protein kinase PLK4 | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.5144 | 9.0000 | AID1425121 |
| ATP-dependent RNA helicase DDX3X | Homo sapiens (human) | Kd | 30.0000 | 0.4350 | 0.4350 | 0.4350 | AID1424975 |
| Pyridoxal kinase | Homo sapiens (human) | Kd | 30.0000 | 0.2860 | 5.0765 | 16.4040 | AID1425106 |
| Citron Rho-interacting kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 3.0646 | 48.8760 | AID1424954 |
| Serine/threonine-protein kinase Chk1 | Homo sapiens (human) | Kd | 30.0000 | 0.0028 | 1.4744 | 8.7000 | AID1424953 |
| Aurora kinase A | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.7342 | 9.3000 | AID1424917 |
| Cyclin-G-associated kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 0.9086 | 28.6510 | AID1425009 |
| Ephrin type-B receptor 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 1.0768 | 9.0000 | AID1424995 |
| Peroxisomal acyl-coenzyme A oxidase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 1.3140 | 2.6020 | AID1424896 |
| Receptor-interacting serine/threonine-protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6212 | 11.4330 | AID1425155 |
| Mitotic checkpoint serine/threonine-protein kinase BUB1 | Homo sapiens (human) | Kd | 30.0000 | 0.0940 | 1.3910 | 3.5070 | AID1424926 |
| Dynamin-like 120 kDa protein, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 0.3610 | 0.7050 | AID1425097 |
| Eukaryotic translation initiation factor 5B | Homo sapiens (human) | Kd | 30.0000 | 0.2320 | 0.2320 | 0.2320 | AID1424986 |
| Rho-associated protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.7105 | 56.0660 | AID1425158 |
| Serine/threonine-protein kinase ULK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.8410 | 23.2730 | AID1425208 |
| Serine/threonine-protein kinase/endoribonuclease IRE1 | Homo sapiens (human) | Kd | 30.0000 | 0.0057 | 2.0095 | 12.2010 | AID1424997 |
| Ribosomal protein S6 kinase alpha-5 | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 1.9737 | 29.9570 | AID1425162 |
| U5 small nuclear ribonucleoprotein 200 kDa helicase | Homo sapiens (human) | Kd | 30.0000 | 1.3820 | 1.3820 | 1.3820 | AID1425174 |
| Ribosomal protein S6 kinase alpha-4 | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 1.6396 | 7.2000 | AID1425161 |
| Serine/threonine-protein kinase 16 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.2483 | 9.9690 | AID1425179 |
| Cyclin-dependent kinase-like 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.4788 | 7.3000 | AID1424951 |
| Serine/threonine-protein kinase 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 2.9234 | 57.4530 | AID1425177 |
| Serine/threonine-protein kinase D3 | Homo sapiens (human) | Kd | 30.0000 | 0.0089 | 2.2738 | 23.3410 | AID1425137 |
| Structural maintenance of chromosomes protein 2 | Homo sapiens (human) | Kd | 30.0000 | 0.2090 | 0.6575 | 1.1060 | AID1425173 |
| Mitogen-activated protein kinase kinase kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 1.5781 | 8.0000 | AID1425050 |
| Mitogen-activated protein kinase kinase kinase kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0082 | 2.3645 | 62.7720 | AID1425054 |
| Serine/threonine-protein kinase LATS1 | Homo sapiens (human) | Kd | 30.0000 | 0.0140 | 1.8393 | 10.7330 | AID1425033 |
| Serine/threonine-protein kinase PAK 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0027 | 2.5694 | 30.3710 | AID1425100 |
| Tyrosine-protein kinase ABL1 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 1.0411 | 13.4530 | AID1424890 |
| Epidermal growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.3514 | 20.8270 | AID1424983 |
| High affinity nerve growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.3484 | 9.2000 | AID1425094 |
| Guanine nucleotide-binding protein G(i) subunit alpha-2 | Homo sapiens (human) | Kd | 30.0000 | 0.1840 | 0.1840 | 0.1840 | AID1425011 |
| ADP/ATP translocase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.4510 | 0.4510 | 0.4510 | AID1425169 |
| Protein kinase C beta type | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 2.7081 | 26.3240 | AID1425130 |
| Insulin receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.0823 | 7.9060 | AID1425026 |
| Tyrosine-protein kinase Lck | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1174 | 24.2210 | AID1425034 |
| Tyrosine-protein kinase Fyn | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.4238 | 8.4000 | AID1425008 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.2880 | 1.4952 | 3.0490 | AID1424937 |
| Glycogen phosphorylase, liver form | Homo sapiens (human) | Kd | 30.0000 | 2.1210 | 2.1210 | 2.1210 | AID1425146 |
| Tyrosine-protein kinase Fes/Fps | Homo sapiens (human) | Kd | 30.0000 | 0.0048 | 1.0986 | 7.4000 | AID1425003 |
| Adenine phosphoribosyltransferase | Homo sapiens (human) | Kd | 30.0000 | 0.0290 | 0.0290 | 0.0290 | AID1424914 |
| Tyrosine-protein kinase Yes | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.3708 | 17.1520 | AID1425212 |
| Tyrosine-protein kinase Lyn | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.0485 | 5.7000 | AID1425037 |
| Proto-oncogene tyrosine-protein kinase receptor Ret | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 0.8642 | 27.5420 | AID1425154 |
| Insulin-like growth factor 1 receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.9211 | 19.2170 | AID1425022 |
| Signal recognition particle receptor subunit alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 0.0080 | 0.0080 | AID1425176 |
| Cytochrome c1, heme protein, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.2020 | 0.2020 | 0.2020 | AID1424969 |
| Hepatocyte growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.6297 | 8.5000 | AID1425076 |
| Tyrosine-protein kinase HCK | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.0343 | 15.9930 | AID1425017 |
| Platelet-derived growth factor receptor beta | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.0050 | 11.1070 | AID1425104 |
| Tyrosine-protein kinase Fgr | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.0721 | 7.8000 | AID1425005 |
| Serine/threonine-protein kinase A-Raf | Homo sapiens (human) | Kd | 30.0000 | 0.0470 | 9.6832 | 33.6550 | AID1424915 |
| Glycogen phosphorylase, brain form | Homo sapiens (human) | Kd | 30.0000 | 3.5690 | 3.5690 | 3.5690 | AID1425145 |
| Breakpoint cluster region protein | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.2196 | 17.3640 | AID1424919 |
| Serine/threonine-protein kinase pim-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.1393 | 19.3160 | AID1425111 |
| Fibroblast growth factor receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.5581 | 6.2000 | AID1425004 |
| DNA topoisomerase 2-alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0640 | 0.2750 | 0.4860 | AID1425202 |
| Cyclin-dependent kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0033 | 1.6050 | 8.6000 | AID1424946 |
| ADP/ATP translocase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 0.2505 | 0.4950 | AID1425170 |
| Proto-oncogene tyrosine-protein kinase Src | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.5077 | 9.6000 | AID1425175 |
| cAMP-dependent protein kinase type II-alpha regulatory subunit | Homo sapiens (human) | Kd | 30.0000 | 0.0520 | 1.7535 | 3.4550 | AID1425128 |
| Serine/threonine-protein kinase B-raf | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.6258 | 26.0180 | AID1424924 |
| Phosphorylase b kinase gamma catalytic chain, liver/testis isoform | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.0569 | 9.5000 | AID1425110 |
| Ribosyldihydronicotinamide dehydrogenase [quinone] | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 6.7556 | 88.9030 | AID1425093 |
| Tyrosine-protein kinase Fer | Homo sapiens (human) | Kd | 30.0000 | 0.0014 | 1.3604 | 8.8000 | AID1425002 |
| Protein kinase C alpha type | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.7922 | 21.3520 | AID1425129 |
| cAMP-dependent protein kinase catalytic subunit alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0039 | 2.9479 | 23.2450 | AID1425123 |
| General transcription and DNA repair factor IIH helicase subunit XPD | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6906 | 12.0220 | AID1424996 |
| Casein kinase II subunit alpha' | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 2.5309 | 28.8720 | AID1424968 |
| Ras-related protein Rab-6A | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 0.0330 | 0.0330 | AID1425150 |
| Ephrin type-A receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0041 | 1.8000 | 9.8000 | AID1424987 |
| Multifunctional protein ADE2 | Homo sapiens (human) | Kd | 30.0000 | 5.4810 | 5.4810 | 5.4810 | AID1425098 |
| cAMP-dependent protein kinase catalytic subunit gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 8.5577 | 49.2780 | AID1425125 |
| cAMP-dependent protein kinase catalytic subunit beta | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 0.7408 | 4.1000 | AID1425124 |
| Ferrochelatase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.2430 | 6.4343 | 67.9140 | AID1425001 |
| Ribosomal protein S6 kinase beta-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 1.1805 | 4.8000 | AID1425164 |
| Tyrosine-protein kinase JAK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0016 | 1.2166 | 7.8000 | AID1425030 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.5179 | 10.4870 | AID1424944 |
| Beta-adrenergic receptor kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 5.5791 | 22.4940 | AID1424908 |
| Probable ATP-dependent RNA helicase DDX6 | Homo sapiens (human) | Kd | 30.0000 | 4.1030 | 4.1030 | 4.1030 | AID1424977 |
| Mitogen-activated protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.4300 | 5.2743 | 9.8000 | AID1425061 |
| MAP/microtubule affinity-regulating kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 3.9689 | 58.2400 | AID1425069 |
| Deoxycytidine kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 1.0875 | 2.1630 | AID1424970 |
| Mitogen-activated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.7441 | 7.3000 | AID1425056 |
| Ephrin type-A receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.0752 | 8.1980 | AID1424988 |
| Ephrin type-B receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 3.1536 | 53.1980 | AID1424992 |
| Non-receptor tyrosine-protein kinase TYK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.5575 | 8.7000 | AID1425207 |
| Phosphatidylethanolamine-binding protein 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0030 | 0.0030 | AID1425107 |
| Wee1-like protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0014 | 3.5389 | 65.1580 | AID1425210 |
| Heme oxygenase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.1190 | 0.1190 | 0.1190 | AID1425018 |
| DnaJ homolog subfamily A member 1 | Homo sapiens (human) | Kd | 30.0000 | 0.9620 | 0.9620 | 0.9620 | AID1424980 |
| RAC-alpha serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.0621 | 4.4000 | AID1424910 |
| RAC-beta serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0021 | 1.6196 | 8.7000 | AID1424911 |
| DNA replication licensing factor MCM4 | Homo sapiens (human) | Kd | 30.0000 | 0.6290 | 0.6290 | 0.6290 | AID1425072 |
| Dual specificity mitogen-activated protein kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0039 | 1.6429 | 9.6000 | AID1425039 |
| Receptor-type tyrosine-protein kinase FLT3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 0.9559 | 9.9000 | AID1425006 |
| Bone morphogenetic protein receptor type-1A | Homo sapiens (human) | Kd | 30.0000 | 0.0600 | 1.5010 | 7.0000 | AID1424921 |
| Activin receptor type-1B | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 1.5110 | 15.2580 | AID1424901 |
| TGF-beta receptor type-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 2.2785 | 9.6000 | AID1425196 |
| TGF-beta receptor type-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0800 | 1.8351 | 6.9000 | AID1425197 |
| Electron transfer flavoprotein subunit beta | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 0.0120 | 0.0120 | AID1424999 |
| Tyrosine-protein kinase CSK | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 3.4578 | 39.5530 | AID1424960 |
| Glycine--tRNA ligase | Homo sapiens (human) | Kd | 30.0000 | 0.0400 | 0.0400 | 0.0400 | AID1425010 |
| Protein kinase C iota type | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 9.3316 | 51.0180 | AID1425133 |
| Exosome RNA helicase MTR4 | Homo sapiens (human) | Kd | 30.0000 | 2.6070 | 2.6070 | 2.6070 | AID1425168 |
| Tyrosine-protein kinase Tec | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.0095 | 8.7000 | AID1425193 |
| Tyrosine-protein kinase ABL2 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1249 | 14.9240 | AID1424891 |
| Tyrosine-protein kinase FRK | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.2424 | 10.8370 | AID1425007 |
| G protein-coupled receptor kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 1.1890 | 1.4020 | 1.6150 | AID1425012 |
| Tyrosine-protein kinase SYK | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 2.0052 | 9.2260 | AID1425188 |
| 26S proteasome regulatory subunit 6B | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 0.0050 | 0.0050 | AID1425141 |
| Mitogen-activated protein kinase 8 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 2.0965 | 26.0590 | AID1425063 |
| Mitogen-activated protein kinase 9 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.4596 | 8.1000 | AID1425064 |
| Dual specificity mitogen-activated protein kinase kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0038 | 1.6264 | 9.9000 | AID1425041 |
| Dual specificity mitogen-activated protein kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 2.0462 | 6.6000 | AID1425040 |
| Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha | Homo sapiens (human) | Kd | 30.0000 | 0.2080 | 3.6125 | 7.0170 | AID1425113 |
| Casein kinase I isoform alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 2.5756 | 19.3520 | AID1424961 |
| Casein kinase I isoform delta | Homo sapiens (human) | Kd | 30.0000 | 0.0150 | 2.2270 | 18.3960 | AID1424962 |
| MAP kinase-activated protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.0274 | 14.7420 | AID1425065 |
| Elongation factor Tu, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.4640 | 0.4640 | 0.4640 | AID1425206 |
| Cysteine--tRNA ligase, cytoplasmic | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 0.3320 | 0.6520 | AID1424932 |
| Casein kinase I isoform epsilon | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 1.4086 | 12.4090 | AID1424963 |
| Very long-chain specific acyl-CoA dehydrogenase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 1.6890 | 1.6890 | 1.6890 | AID1424894 |
| Dual specificity protein kinase CLK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.8791 | 29.8810 | AID1424955 |
| Dual specificity protein kinase CLK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.1384 | 6.5000 | AID1424956 |
| Glycogen synthase kinase-3 alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 2.4754 | 22.5430 | AID1425013 |
| Glycogen synthase kinase-3 beta | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.0057 | 6.1680 | AID1425014 |
| Cyclin-dependent kinase 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.6783 | 7.7000 | AID1424949 |
| Cyclin-dependent kinase 9 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.6166 | 9.9010 | AID1424950 |
| Ras-related protein Rab-27A | Homo sapiens (human) | Kd | 30.0000 | 4.4930 | 4.4930 | 4.4930 | AID1425149 |
| Interleukin-1 receptor-associated kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0061 | 1.5252 | 8.5000 | AID1425027 |
| Ribosomal protein S6 kinase alpha-3 | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 2.8896 | 37.6050 | AID1425160 |
| Serine/threonine-protein kinase Nek2 | Homo sapiens (human) | Kd | 30.0000 | 0.1100 | 1.5649 | 6.5000 | AID1425086 |
| Serine/threonine-protein kinase Nek3 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 5.9368 | 38.0880 | AID1425087 |
| Dual specificity mitogen-activated protein kinase kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0034 | 2.3943 | 6.5000 | AID1425043 |
| Serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.5711 | 5.0000 | AID1425120 |
| LIM domain kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 1.7840 | 21.0890 | AID1425035 |
| LIM domain kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0570 | 4.9717 | 52.0560 | AID1425036 |
| Mitogen-activated protein kinase 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.6354 | 5.9000 | AID1425057 |
| Tyrosine--tRNA ligase, cytoplasmic | Homo sapiens (human) | Kd | 30.0000 | 3.3160 | 3.3160 | 3.3160 | AID1425211 |
| 5'-AMP-activated protein kinase subunit gamma-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.4681 | 10.2120 | AID1425126 |
| Ephrin type-B receptor 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0069 | 2.1713 | 6.4100 | AID1424993 |
| Ephrin type-A receptor 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.2100 | 5.9000 | AID1424990 |
| Ephrin type-B receptor 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.1678 | 26.3990 | AID1424994 |
| Ephrin type-A receptor 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 3.1525 | 43.9420 | AID1424989 |
| Adenylate kinase 2, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 1.0360 | 1.0360 | 1.0360 | AID1424909 |
| Adenosine kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 1.8368 | 3.4930 | AID1424907 |
| Ras-related protein Rab-10 | Homo sapiens (human) | Kd | 30.0000 | 1.3480 | 1.3480 | 1.3480 | AID1425148 |
| Actin-related protein 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0360 | 2.7735 | 5.5110 | AID1424899 |
| Actin-related protein 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 0.0040 | 0.0040 | AID1424898 |
| GTP-binding nuclear protein Ran | Homo sapiens (human) | Kd | 30.0000 | 0.7590 | 0.7590 | 0.7590 | AID1425153 |
| Casein kinase I isoform gamma-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0460 | 1.4506 | 6.6000 | AID1424965 |
| Cyclin-dependent kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 3.0602 | 63.6140 | AID1424945 |
| Cyclin-dependent kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0320 | 1.2007 | 3.3560 | AID1424948 |
| Cyclin-dependent-like kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0430 | 1.3757 | 8.3000 | AID1424947 |
| Cyclin-dependent kinase 16 | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.5855 | 10.0000 | AID1424941 |
| Cyclin-dependent kinase 17 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 0.8233 | 5.6000 | AID1424942 |
| ATP-dependent 6-phosphofructokinase, platelet type | Homo sapiens (human) | Kd | 30.0000 | 0.9830 | 0.9830 | 0.9830 | AID1425108 |
| Dual specificity mitogen-activated protein kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1386 | 8.7730 | AID1425038 |
| DNA topoisomerase 2-beta | Homo sapiens (human) | Kd | 30.0000 | 0.1480 | 1.2270 | 2.5970 | AID1425203 |
| Protein kinase C theta type | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 1.6140 | 7.2000 | AID1425134 |
| Activin receptor type-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 1.4853 | 16.1210 | AID1424900 |
| Macrophage-stimulating protein receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 2.0718 | 8.4000 | AID1425078 |
| Focal adhesion kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.2255 | 13.0390 | AID1425142 |
| Protein kinase C delta type | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1261 | 9.2060 | AID1425131 |
| Tyrosine-protein kinase BTK | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.5299 | 10.1530 | AID1424925 |
| Activated CDC42 kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.7138 | 9.6000 | AID1425201 |
| Epithelial discoidin domain-containing receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.6314 | 71.4840 | AID1424972 |
| Mitogen-activated protein kinase kinase kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0031 | 1.4681 | 14.0430 | AID1425052 |
| Serine/threonine-protein kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.7120 | 25.9020 | AID1425185 |
| 5'-AMP-activated protein kinase catalytic subunit alpha-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0037 | 1.8913 | 15.3890 | AID1425122 |
| Dual specificity mitogen-activated protein kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.6590 | 65.6770 | AID1425042 |
| Mitogen-activated protein kinase 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0420 | 2.0073 | 9.9000 | AID1425062 |
| Serine/threonine-protein kinase PAK 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0031 | 2.3045 | 6.0000 | AID1425099 |
| Serine/threonine-protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.8602 | 17.5260 | AID1425182 |
| Mitogen-activated protein kinase kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0970 | 2.5995 | 12.4730 | AID1425044 |
| Integrin-linked protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0200 | 0.4603 | 1.3290 | AID1425024 |
| Rho-associated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.7555 | 13.4620 | AID1425157 |
| Non-receptor tyrosine-protein kinase TNK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0018 | 1.0064 | 11.2690 | AID1425200 |
| Calcium/calmodulin-dependent protein kinase type II subunit gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.0209 | 7.8000 | AID1424929 |
| Calcium/calmodulin-dependent protein kinase type II subunit delta | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.5044 | 20.3010 | AID1424928 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.1016 | 40.2910 | AID1424981 |
| Activin receptor type-2B | Homo sapiens (human) | Kd | 30.0000 | 0.0076 | 2.7328 | 9.9000 | AID1424902 |
| Bone morphogenetic protein receptor type-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0190 | 2.5917 | 14.3770 | AID1424923 |
| Protein-tyrosine kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0043 | 1.7430 | 9.0000 | AID1425144 |
| cGMP-dependent protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0016 | 0.7072 | 3.8000 | AID1425138 |
| Cyclin-dependent kinase 13 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.2571 | 4.5180 | AID1424940 |
| Inhibitor of nuclear factor kappa-B kinase subunit epsilon | Homo sapiens (human) | Kd | 30.0000 | 0.0051 | 1.1093 | 8.3000 | AID1425023 |
| Protein-tyrosine kinase 2-beta | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.9450 | 30.4140 | AID1425143 |
| Maternal embryonic leucine zipper kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0049 | 2.2835 | 29.9330 | AID1425074 |
| Structural maintenance of chromosomes protein 1A | Homo sapiens (human) | Kd | 30.0000 | 0.3650 | 0.3650 | 0.3650 | AID1425172 |
| Chromodomain-helicase-DNA-binding protein 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0030 | 0.0030 | AID1424952 |
| Peroxisomal acyl-coenzyme A oxidase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0140 | 0.1425 | 0.2710 | AID1424895 |
| Serine/threonine-protein kinase 38 | Homo sapiens (human) | Kd | 30.0000 | 0.0560 | 1.5651 | 9.4000 | AID1425183 |
| Ephrin type-A receptor 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.4445 | 6.5000 | AID1424991 |
| Delta(24)-sterol reductase | Homo sapiens (human) | Kd | 30.0000 | 0.4320 | 0.4320 | 0.4320 | AID1424978 |
| Ribosomal protein S6 kinase alpha-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0280 | 2.5286 | 22.7260 | AID1425159 |
| Dual specificity testis-specific protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 1.7568 | 5.6000 | AID1425194 |
| Myosin light chain kinase, smooth muscle | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.2088 | 7.9000 | AID1425081 |
| Mitogen-activated protein kinase 11 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.4610 | 3.7430 | AID1425058 |
| Serine/threonine-protein kinase STK11 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.9949 | 5.9000 | AID1425178 |
| Serine/threonine-protein kinase N1 | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 3.1729 | 49.8130 | AID1425117 |
| Serine/threonine-protein kinase N2 | Homo sapiens (human) | Kd | 30.0000 | 0.0018 | 1.7527 | 9.9000 | AID1425118 |
| Mitogen-activated protein kinase 14 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 0.5036 | 8.5000 | AID1425059 |
| Calcium/calmodulin-dependent protein kinase type IV | Homo sapiens (human) | Kd | 30.0000 | 0.0300 | 1.9215 | 5.4600 | AID1424930 |
| Mitogen-activated protein kinase kinase kinase 11 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 1.5639 | 17.9840 | AID1425045 |
| MAP kinase-activated protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 0.0170 | 0.0260 | AID1425066 |
| Discoidin domain-containing receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.9888 | 42.2800 | AID1424973 |
| AP2-associated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 1.3707 | 13.7110 | AID1424889 |
| Myosin light chain kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6184 | 10.4240 | AID1425082 |
| Uncharacterized aarF domain-containing protein kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.2020 | 0.4990 | 0.7960 | AID1424906 |
| Putative heat shock protein HSP 90-beta 2 | Homo sapiens (human) | Kd | 30.0000 | 2.5660 | 2.5660 | 2.5660 | AID1425019 |
| Rab-like protein 3 | Homo sapiens (human) | Kd | 30.0000 | 4.8300 | 4.8300 | 4.8300 | AID1425151 |
| Serine/threonine-protein kinase MRCK alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0570 | 4.5547 | 14.0200 | AID1424933 |
| Serine/threonine-protein kinase MRCK gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0370 | 1.9625 | 9.5000 | AID1424935 |
| Acyl-CoA dehydrogenase family member 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0780 | 1.6997 | 3.9570 | AID1424892 |
| Serine/threonine-protein kinase N3 | Homo sapiens (human) | Kd | 30.0000 | 0.0990 | 0.7365 | 1.3740 | AID1425119 |
| Serine/threonine-protein kinase ULK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 1.3350 | 9.9000 | AID1425209 |
| Uncharacterized protein FLJ45252 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.2292 | 9.3110 | AID1425147 |
| Acyl-CoA dehydrogenase family member 11 | Homo sapiens (human) | Kd | 30.0000 | 1.9160 | 3.0730 | 4.1470 | AID1424893 |
| Serine/threonine-protein kinase/endoribonuclease IRE2 | Homo sapiens (human) | Kd | 30.0000 | 0.1160 | 0.7604 | 1.5000 | AID1424998 |
| Serine/threonine-protein kinase MARK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.8425 | 11.1030 | AID1425068 |
| ATP-dependent RNA helicase DHX30 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 0.0060 | 0.0060 | AID1424979 |
| Serine/threonine-protein kinase TAO1 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 2.1612 | 18.7570 | AID1425189 |
| STE20-related kinase adapter protein alpha | Homo sapiens (human) | Kd | 30.0000 | 0.3160 | 1.7208 | 3.6720 | AID1425186 |
| AarF domain-containing protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0230 | 3.1137 | 22.7470 | AID1424904 |
| Mitogen-activated protein kinase kinase kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0051 | 1.6413 | 15.4350 | AID1425053 |
| MAP kinase-activated protein kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 1.1241 | 3.1180 | AID1425067 |
| Misshapen-like kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.1425 | 8.9000 | AID1425077 |
| Atypical kinase COQ8A, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0940 | 5.1673 | 65.3020 | AID1424905 |
| Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 2.7522 | 8.8000 | AID1425115 |
| Mitogen-activated protein kinase 15 | Homo sapiens (human) | Kd | 30.0000 | 0.0049 | 0.6880 | 4.5000 | AID1425060 |
| Serine/threonine-protein kinase Nek9 | Homo sapiens (human) | Kd | 30.0000 | 0.0160 | 2.7428 | 19.6170 | AID1425089 |
| ATP-dependent RNA helicase DDX1 | Homo sapiens (human) | Kd | 30.0000 | 0.0860 | 0.0860 | 0.0860 | AID1424974 |
| Mitogen-activated protein kinase kinase kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 0.9378 | 5.5000 | AID1425051 |
| Aurora kinase B | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.0614 | 22.8520 | AID1424918 |
| MAP/microtubule affinity-regulating kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0054 | 1.1029 | 4.9000 | AID1425070 |
| Serine/threonine-protein kinase Nek1 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 2.4294 | 8.3000 | AID1425085 |
| PAS domain-containing serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 1.0670 | 1.0670 | 1.0670 | AID1425102 |
| Calcium/calmodulin-dependent protein kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 3.2331 | 52.8470 | AID1424931 |
| EKC/KEOPS complex subunit TP53RK | Homo sapiens (human) | Kd | 30.0000 | 0.3110 | 1.9519 | 3.8400 | AID1425204 |
| Dual specificity testis-specific protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 0.0020 | 0.0020 | AID1425195 |
| Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0440 | 0.9285 | 2.9000 | AID1425116 |
| Mitogen-activated protein kinase kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0700 | 6.5647 | 50.5360 | AID1425049 |
| Mitogen-activated protein kinase kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.5331 | 9.9000 | AID1425047 |
| Eukaryotic translation initiation factor 2-alpha kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0580 | 1.9224 | 4.8360 | AID1424984 |
| Nucleolar GTP-binding protein 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0090 | 4.1035 | 8.1980 | AID1425016 |
| Serine/threonine-protein kinase D2 | Homo sapiens (human) | Kd | 30.0000 | 0.0081 | 2.3723 | 25.0190 | AID1425136 |
| NUAK family SNF1-like kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.6774 | 4.6000 | AID1425095 |
| RNA cytidine acetyltransferase | Homo sapiens (human) | Kd | 30.0000 | 1.2400 | 1.2400 | 1.2400 | AID1425083 |
| Serine/threonine-protein kinase SIK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.8165 | 41.7950 | AID1425166 |
| STE20-like serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 3.8573 | 99.2320 | AID1425171 |
| Serine/threonine-protein kinase TAO3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.7131 | 14.1960 | AID1425191 |
| dCTP pyrophosphatase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.5730 | 1.7403 | 3.0540 | AID1424971 |
| Dual specificity protein kinase CLK4 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.4122 | 8.3000 | AID1424958 |
| Casein kinase I isoform gamma-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0530 | 2.0622 | 5.7000 | AID1424964 |
| Serine/threonine-protein kinase PAK 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 1.9194 | 9.7000 | AID1425101 |
| Phenylalanine--tRNA ligase beta subunit | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0045 | 0.0060 | AID1425000 |
| BMP-2-inducible protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0022 | 2.4097 | 56.0320 | AID1424920 |
| Interleukin-1 receptor-associated kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 3.4719 | 34.1450 | AID1425029 |
| Mitogen-activated protein kinase kinase kinase 20 | Homo sapiens (human) | Kd | 30.0000 | 0.0023 | 1.7034 | 13.6380 | AID1425213 |
| Cyclin-dependent kinase 12 | Homo sapiens (human) | Kd | 30.0000 | 0.0320 | 1.8032 | 5.6350 | AID1424939 |
| NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 | Homo sapiens (human) | Kd | 30.0000 | 3.9200 | 3.9200 | 3.9200 | AID1425084 |
| Serine/threonine-protein kinase 26 | Homo sapiens (human) | Kd | 30.0000 | 0.0074 | 1.7380 | 8.3000 | AID1425181 |
| Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 0.0070 | 0.0070 | AID1425187 |
| Serine/threonine-protein kinase NLK | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.0226 | 4.4000 | AID1425090 |
| 5'-AMP-activated protein kinase subunit gamma-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 1.1581 | 9.1280 | AID1425127 |
| Serine/threonine-protein kinase TBK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.7674 | 49.6010 | AID1425192 |
| Septin-9 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 0.2430 | 0.6350 | AID1425165 |
| Ribosomal protein S6 kinase alpha-6 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 2.4153 | 23.7620 | AID1425163 |
| TRAF2 and NCK-interacting protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0047 | 1.3935 | 10.0000 | AID1425199 |
| Serine/threonine-protein kinase TAO2 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 2.0176 | 12.9420 | AID1425190 |
| Long-chain-fatty-acid--CoA ligase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 0.6353 | 1.6900 | AID1424897 |
| Serine/threonine-protein kinase ICK | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 1.4717 | 9.3000 | AID1425021 |
| RAC-gamma serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.7646 | 6.2000 | AID1424912 |
| Serine/threonine-protein kinase 38-like | Homo sapiens (human) | Kd | 30.0000 | 0.0280 | 1.4692 | 6.9000 | AID1425184 |
| Serine/threonine-protein kinase SIK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.5086 | 10.3180 | AID1425167 |
| Mitogen-activated protein kinase kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0024 | 1.3298 | 6.9000 | AID1425046 |
| Thyroid hormone receptor-associated protein 3 | Homo sapiens (human) | Kd | 30.0000 | 2.7460 | 2.7460 | 2.7460 | AID1425198 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1B | Homo sapiens (human) | Kd | 30.0000 | 0.0280 | 1.8129 | 9.5000 | AID1424982 |
| Mitogen-activated protein kinase kinase kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.9494 | 50.2140 | AID1425055 |
| Receptor-interacting serine/threonine-protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 1.4797 | 6.7000 | AID1425156 |
| Serine/threonine-protein kinase MRCK beta | Homo sapiens (human) | Kd | 30.0000 | 0.0340 | 3.6252 | 50.0050 | AID1424934 |
| Interleukin-1 receptor-associated kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.7137 | 25.5810 | AID1425028 |
| Serine/threonine-protein kinase 24 | Homo sapiens (human) | Kd | 30.0000 | 0.0065 | 0.8920 | 4.0840 | AID1425180 |
| Casein kinase I isoform gamma-3 | Homo sapiens (human) | Kd | 30.0000 | 0.0970 | 2.3978 | 8.7000 | AID1424966 |
| Mitogen-activated protein kinase kinase kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0390 | 2.3970 | 8.4000 | AID1425048 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| 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. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347154 | Primary screen GU AMC 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. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Highly predictive and interpretable models for PAMPA permeability. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1 | Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
| 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. |
| AID1424904 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1177098 | Inhibition of human class 3 PI3K by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID1895256 | Inhibition of PI3Kdelta in conA-stimulated primary human T cell proliferation incubated for 1 hr by CellTiter-glo luminescent assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1424921 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1777384 | Antitumour activity against human MOLT-4 cells xenografted in Balb/c nude mouse assessed as inhibition of tumour growth at 10 mg/kg, po administered via gavage qd for 57 days | |||
| AID1722463 | Inhibition of recombinant human His-tagged PI3Kalpha expressed in insect cell expression system using PIP2:PS as substrate incubated for 1 hr by invitrogen adapta assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1424982 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID1534885 | Inhibition of PI3Kgamma (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Targeting the immunity protein kinases for immuno-oncology. |
| AID1587173 | Inhibition of His-tagged recombinant human PI3K p110delta/p85alpha using lipid substrate incubated for 2 hrs by ADP-Glo assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1605967 | Antiproliferative activity against human HOP62 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1425129 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1722465 | Inhibition of recombinant human His-tagged PI3Kgamma expressed in baculovirus expression system using PIP2:PS as substrate incubated for 1 hr by invitrogen adapta assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| 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. |
| AID1424985 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424952 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1335159 | AUC in Beagle dog at 1 mg/kg, iv through bolus administration | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1425196 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425040 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1317009 | Inhibition of human PI3Kdelta (R108 to Q1044 residues) expressed in mammalian expression system incubated for 60 mins by ADAPTA assay | |||
| AID1361701 | Inhibition of N-terminal GST-tagged recombinant human PIK3C2A catalytic domain expressed in Baculovirus expression system using PI as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in presence of 50 uM ATP by ADP-Gl | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1425195 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424974 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424977 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425185 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1781108 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at G2 phase at 5 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =14.7 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1777382 | Induction of apoptosis in human MOLT-4 cells assessed as late apoptotic cells at 20 uM measured after 24 hrs by AnnexinV-FITC/PI staining based flowcytometry method (Rvb = 2.17%) | |||
| AID1459890 | Inhibition of recombinant human full length His-tagged PI3Kgamma expressed in insect cells | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1424915 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1328340 | Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c at 10 uM preincubated for 5 mins followed by fMLP/CB-inductio | 2016 | Journal of natural products, 09-23, Volume: 79, Issue:9 | Halogenated Sesquiterpenoids from the Red Alga Laurencia tristicha Collected in Taiwan. |
| AID1459868 | Antiproliferative activity against human WSU-DLCL2 cells measured after 72 hrs by alamar blue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1177095 | Inhibition of human PI3KC2beta by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID1425013 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1361698 | Inhibition of PI3Kbeta (unknown origin) using PIP2:PS as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in presence of 50 uM ATP by ADP-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1425154 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1628350 | Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of elastase release preincubated for 5 mins followed by FMLP/CB stimulation for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Bioactive Isoprenoid-Derived Natural Products from a Dongsha Atoll Soft Coral Sinularia erecta. |
| AID1606007 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability at 2.5 to 5 uM after 72 hrs by tryphan blue assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1587177 | Selectivity ratio of IC50 for His6-tagged recombinant full length human N-terminal PI3Kbeta to IC50 for His-tagged recombinant human PI3K p110delta/p85alpha | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1390806 | Inhibition of PI3K p110delta (unknown origin) at 100 nM using lipid substrate after 40 mins by kinase-Glo assay relative to control | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1700587 | Selectivity index, ratio of IC50 for human PI3Kalpha to IC50 for human PI3Kdelta | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Discovery of ( |
| AID1425120 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1593850 | Antiproliferative activity against human TMD8 cells | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1424920 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424908 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425041 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1903029 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| 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. |
| AID1718772 | Half life in Beagle dog at 1 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425061 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1361716 | Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1425172 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID1777392 | Inhibition of PI3Kdelta in human SU-DHL-5 cells assessed as inhibition of AKT phosphorylation at Thr308 residue at 1 to 5 uM measured after 3 hrs by western blot assay | |||
| AID1425133 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1872691 | Antitumor activity against human DOHH-2 cells xenografted in CB17/SCID mouse assessed as reduction in tumor growth at 25 mg/kg, po administered twice daily in combination with ibrutinib at 15 mg/kg for 30 days and measured twice a week relative to control | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Recent development of BTK-based dual inhibitors in the treatment of cancers. |
| AID1395213 | Selectivity index, ratio of IC50 for PI3Kgamma (unknown origin) to IC50 for PI3Kdelta (unknown origin) | |||
| AID1425164 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425199 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718790 | Tmax in Beagle dog at 1 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1718783 | Clearance in Sprague-Dawley rat at 3 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1459887 | Inhibition of human full length His-tagged PI3Kdelta expressed in baculovirus expression system | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1605970 | Antiproliferative activity against human KM12 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1593855 | Inhibition of human PI3Kgamma using PIP2 as substrate after 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1459889 | Inhibition of recombinant human full length His-tagged PI3Kbeta expressed in insect cells | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1425064 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1587178 | Selectivity ratio of IC50 for His-tagged recombinant human full length PI3K p110gamma to IC50 for His-tagged recombinant human PI3K p110delta/p85alpha | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1722458 | Antiproliferative activity against human JeKo-1 assessed as reduction in cell growth by MTS assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1722464 | Inhibition of recombinant human His-tagged PI3Kbeta expressed in insect cell expression system using PIP2:PS as substrate incubated for 1 hr by invitrogen adapta assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1605978 | Antiproliferative activity against human Caki1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1425192 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425051 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1389909 | Inhibition of human recombinant PI3K-delta | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6 | Design and synthesis of 1,4-substituted 1H-1,2,3-triazolo-quinazolin-4(3H)-ones by Huisgen 1,3-dipolar cycloaddition with PI3Kγ isoform selective activity. |
| AID1424953 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1722453 | Inhibition of PI3Kbeta (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1895253 | Inhibition of PI3Kdelta in anti-IgM-stimulated human Raji cells assessed as reduction in AKT phosphorylation at S473 residue incubated for 30 mins | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1425212 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425010 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1722461 | Cytotoxicity against human HEK293 cells assessed as reduction in cell viability by MTS assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1722459 | Cytotoxicity against monkey Vero cells assessed as reduction in cell viability by MTS assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1425024 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425200 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1777376 | Induction of apoptosis in human SU-DHL-10 cells assessed as viable cells at 20 uM measured after 24 hrs by AnnexinV-FITC/PI staining based flowcytometry method (Rvb = 90%) | |||
| AID1781112 | Induction of apoptosis in human MOLM16 cells assessed as necrotic cells at 1 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 0.44 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1425072 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718754 | Plasma concentration in CB.17 SCID mouse xenografted with TMD-8 cells at 3 mg/kg, po once daily for 19 days | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425175 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1917537 | Inhibition of PI3Kalpha (unknown origin) measured by ADP-Glo assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1481748 | Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9 | Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors. |
| AID1448833 | Inhibition of PI3Kgamma (unknown origin) | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders. |
| 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. |
| AID1448835 | Inhibition of PI3Kbeta (unknown origin) | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders. |
| AID1425206 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1600807 | Inhibition of PI3K delta (unknown origin) using phosphatidyl inositol as substrate measured after 60 mins in presence of ATP by Kinase-Glo Plus reagent-based luminescence assay | |||
| AID1587185 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg by LC/MS/MS analysis | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1425044 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424930 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424976 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1777385 | Toxicity in Balb/c nude mouse xenografted with human MOLT-4 cells assessed as changes in body weight at 10 mg/kg, po administered via gavage qd for 57 days | |||
| AID1425177 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425193 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425123 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425049 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425209 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1777386 | AUC (last) in Sprague-Dawley rat at 3 mg/kg, po measured for 24 hrs by LC-MS/MS analysis | |||
| AID1390811 | Antiproliferative activity against human Raji cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1781115 | Induction of apoptosis in human MOLM16 cells assessed as late apoptotic cells at 2 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 6.77 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1587176 | Inhibition of His-tagged recombinant human full length PI3K p110gamma expressed in baculovirus expression system using lipid substrate incubated for 2 hrs by ADP-Glo assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID719947 | Antitumor activity in Non-Hodgkin Lymphoma patient assessed as clinical response rate at 50 to 350 mg, bid | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID1600812 | Antiproliferative activity against human Ramos cells by MTT assay | |||
| AID1425105 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1903020 | Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1781098 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at G1 phase at 1 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =46.8 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1425168 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID719934 | Toxicity in healthy human administered bid up to 7 days | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID1425174 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424989 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1781105 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at subG1 phase at 5 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =4.02 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1390820 | AUC in Sprague-Dawley rat at 3 mg/kg, po by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1425028 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718669 | Clearance in BALB/C mouse at 10 mg/kg, iv measured upto 24 hrs by LC-MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425023 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425125 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425211 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424911 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1509602 | Selectivity ratio of IC50 for inhibition of PI3K beta (unknown origin) to IC50 for inhibition of PI3K delta (unknown origin) | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1587172 | Inhibition of His6-tagged recombinant full length human N-terminal PI3Kbeta expressed in baculovirus infected Sf21 cells using lipid substrate incubated for 2 hrs by ADP-Glo assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1605969 | Antiproliferative activity against human HCC2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1553489 | Cytotoxicity against basophil derived from B-cell malignant patient by cell-titer aqueous one solution cell proliferation assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1424928 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424962 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1917530 | Inhibition of HDAC1 (unknown origin) measured by fluorescence based assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1424969 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1469862 | Inhibition of PI3Kdelta (unknown origin) after 60 mins using fluorescein-labeled kinase tracer by HTRF assay | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Identification of highly potent and selective PI3Kδ inhibitors. |
| AID1605976 | Antiproliferative activity against human OVCAR3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1328343 | Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release at 20 uM using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate preincubated for 5 mins followed by fMLP/CB-induction | 2016 | Journal of natural products, 09-23, Volume: 79, Issue:9 | Halogenated Sesquiterpenoids from the Red Alga Laurencia tristicha Collected in Taiwan. |
| AID1317033 | Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay | |||
| AID1379445 | Growth inhibition of human T47D cells after 72 hrs by SRB assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1425078 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1781085 | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate in presence of ATP measured after 60 mins by ADP-Glo assay | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1459858 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 30 mins by HTRF assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1777377 | Induction of apoptosis in human SU-DHL-10 cells assessed as early apoptotic cells at 20 uM measured after 24 hrs by AnnexinV-FITC/PI staining based flowcytometry method (Rvb = 6.32%) | |||
| AID1718800 | Volume of distribution at steady state in BALB/C mouse at 10 mg/kg, iv measured upto 24 hrs by LC-MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1424896 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425093 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1390804 | Inhibition of PI3Kdelta (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1425118 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425187 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1587180 | AUC (0 to t) in Sprague-Dawley rat at 2 mg/kg, iv by LC/MS/MS analysis | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1718718 | Antitumor activity against human OCI-LY10 cells xenografted in CB.17 SCID mouse assessed as tumor weight at 3 mg/kg, po once daily for 24 days (Rvb = 0.86 +/- 0.26 g) | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1361717 | Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1424889 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424939 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1361703 | Inhibition of PI4K3A (unknown origin) using PI:PS as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in presence of 50 uM ATP by ADP-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1425062 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1895245 | Inhibition of PI3Kbeta (unknown origin) | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1718785 | Tmax in Sprague-Dawley rat at 3 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425046 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425042 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1617136 | Inhibition of PI3Kbeta (unknown origin) using biotin-PIP3 as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence polarization assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of |
| AID1903026 | Antiproliferative activity against human HepG2 cells assessed as inhibition rate at 10 uM incubated for 72 hrs by SRB assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1718758 | Antitumor activity against human SUDHL-6 cells xenografted in CB.17 SCID mouse assessed as tumor volume at 5 mg/kg, po once daily for 15 days (Rvb = 1982 +/- 289.04 mm3) | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1605980 | Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID719923 | Selectivity ratio of IC50 for PI3Kgamma to IC50 for PI3Kdelta | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID1425111 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1917538 | Inhibition of PI3Kgamma (unknown origin) measured by ADP-Glo assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1571683 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate after 2 hrs by ADP-Glo assay | 2019 | MedChemComm, Mar-01, Volume: 10, Issue:3 | Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation. |
| AID1390809 | Inhibition of PI3K p110gamma (unknown origin) using lipid substrate after 40 mins by kinase-Glo assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1895246 | Metabolic stability in human liver microsome assessed as half life at 10 uM in presence of NADPH incubated up to 60 hrs | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1425076 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1872693 | Antitumor activity against human DOHH-2 cells xenografted in CB17/SCID mouse assessed as reduction in tumor growth at 50 mg/kg, po administered twice daily in combination with ibrutinib at 30 mg/kg for 30 days and measured twice a week relative to control | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Recent development of BTK-based dual inhibitors in the treatment of cancers. |
| AID1425053 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424892 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1317025 | Inhibition of p110delta in HMEC assessed as reduction in Akt phosphorylation at Ser-473 residue at 10 nM after 1 hr by Western blot analysis | |||
| AID1459856 | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate measured after 30 mins by HTRF assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1777371 | Inhibition of PI3Kdelta in human MOLT-4 cells assessed as inhibition of AKT phosphorylation at Ser473 residue at 1 to 5 uM measured after 3 hrs by western blot assay | |||
| AID1317026 | Inhibition of p110delta in HMEC assessed as reduction in Akt phosphorylation at Thr-308 residue at 10 nM after 1 hr by Western blot analysis | |||
| AID1362214 | Antitumor activity against human MOLM14 cells xenografted in nu/nu mouse assessed as inhibition of tumor proliferation 100 mg/kg, po administered daily via gavage dosed for 14 days and measured daily during compound dosing by Ki-67 labelling based immunoh | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1424980 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424951 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425073 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1917535 | Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1425210 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1895250 | Inhibition of PI3Kalpha in human SK-OV-3 cells assessed as reduction in AKT phosphorylation at S473 residue incubated for 30 mins | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1425126 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1903039 | Induction of cell cycle arrest in human Bel-7402 cells assessed as accumulation of cells in subG1 phase at 50 uM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb=2.15+/-0.70%) | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1424983 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1395211 | Selectivity index, ratio of IC50 for PI3Kalpha (unknown origin) to IC50 for PI3Kdelta (unknown origin) | |||
| AID1469863 | Inhibition of PI3Kgamma (unknown origin) after 60 mins using fluorescein-labeled kinase tracer by HTRF assay | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Identification of highly potent and selective PI3Kδ inhibitors. |
| AID1379443 | Growth inhibition of human NCI-H460 cells after 72 hrs by SRB assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1390813 | Antiproliferative activity against human SUDHL6 cells after 72 hrs by CCK8 assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1605981 | Antiproliferative activity against human T47D cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1424988 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425202 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424919 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1177100 | Inhibition of human PI3KCdelta by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID1777368 | Inhibition of recombinant human full length His-tagged p110delta/p85alpha expressed in baculovirus expression system measured after 60 mins in presence of ATP by ATP-competitive binding assay | |||
| AID1425148 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1335160 | Clearance in Beagle dog at 1 mg/kg, iv through bolus administration | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1424967 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1605975 | Antiproliferative activity against human IGROV1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1424931 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1486992 | Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide oxide dismutase inhibitable reduction of ferricytochrome c incubated for 5 mins | 2017 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15 | Bioactive new withanolides from the cultured soft coral Sinularia brassica. |
| AID1571685 | Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate after 2 hrs by ADP-Glo assay | 2019 | MedChemComm, Mar-01, Volume: 10, Issue:3 | Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation. |
| AID1425208 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1361715 | Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1722454 | Inhibition of PI3Kgamma (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1605972 | Antiproliferative activity against human U251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1424997 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1617135 | Inhibition of PI3Kdelta (unknown origin) using biotin-PIP3 as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence polarization assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of |
| AID1424955 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425181 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425095 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718759 | Antitumor activity against human SUDHL-6 cells xenografted in CB.17 SCID mouse assessed as tumor growth inhibition at 5 mg/kg, po once daily for 15 days relative to control | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1459870 | Antiproliferative activity against human Pfeiffer cells measured after 72 hrs by alamar blue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1379446 | Growth inhibition of human U87MG cells after 72 hrs by SRB assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1425117 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1486995 | Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release at 10 uM incubated for 5 mins in presence of MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide | 2017 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15 | Bioactive new withanolides from the cultured soft coral Sinularia brassica. |
| AID1424991 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1335140 | Clearance in Wistar rat at 1 mg/kg, iv | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1321981 | Inhibition of his-tagged human recombinant PIK3CD/PIK3R1 by Select-screen kinase inhibitor assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1 | Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
| AID1587171 | Selectivity ratio of IC50 for His-tagged recombinant human full length PI3K p110alpha/p85alpha to IC50 for His-tagged recombinant human PI3K p110delta/p85alpha | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1425034 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425022 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1587186 | Half life in Sprague-Dawley rat at 10 mg/kg, po by LC/MS/MS analysis | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1335145 | Half life in Wistar rat at 1 mg/kg, iv | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1424994 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1558396 | Inhibition of His-tagged recombinant human PI3K p110delta/p85alpha expressed in Baculovirus expression system | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | The Exploration of Chirality for Improved Druggability within the Human Kinome. |
| AID1509589 | Inhibition of PI3K gamma (unknown origin) using lipid substrate measured after 40 mins in presence of ATP by Kinase-Glo plus reagent based luminescence assay | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1718780 | Tmax in Sprague-Dawley rat at 3 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1534886 | Inhibition of PI3Kdelta (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Targeting the immunity protein kinases for immuno-oncology. |
| AID1895247 | Metabolic stability in human liver microsome assessed as intrinsic clearance at 10 uM in presence of NADPH incubated up to 60 hrs | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1425197 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1903059 | Antitumor activity against human Bel-7402 cells xenografted in Balb/c (nu/nu) mouse assessed as relative tumor volume at 40 mg/kg, po qd after 14 days (Rvb=25.69+/-2.73 No_unit) | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1192864 | Inhibition of PI3Kalpha (unknown origin) by biochemical Alphascreen assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Synthesis and SAR study of potent and selective PI3Kδ inhibitors. |
| AID1718760 | Antitumor activity against human SUDHL-6 cells xenografted in CB.17 SCID mouse assessed as tumor weight at 5 mg/kg, po once daily for 15 days (Rvb = 1.69 +/- 0.32 g) | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425026 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718762 | Drug uptake in CB.17 SCID mouse tumor xenografted with SUDHL-6 cells assessed as effect on body weight at 5 mg/kg, po once daily for 15 days | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425009 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425094 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID719935 | Toxicity in healthy human | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID1425134 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424907 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID729013 | Inhibition of PI3K p110delta (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors. |
| AID1425036 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424917 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID728998 | Selectivity ratio of IC50 for PI3Kgamma (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors. |
| AID1424941 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1177096 | Inhibition of human PI3KC2gamma by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID1425054 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718788 | Oral bioavailability in Sprague-Dawley rat at 3 mg/kg measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425203 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425008 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1781111 | Induction of apoptosis in human MOLM16 cells assessed as late apoptotic cells at 1 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 6.77 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1424932 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424912 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1628349 | Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of elastase release at 10 uM preincubated for 5 mins followed by FMLP/CB stimulation for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate relative t | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Bioactive Isoprenoid-Derived Natural Products from a Dongsha Atoll Soft Coral Sinularia erecta. |
| AID1379447 | Growth inhibition of human KARPAS422 cells by CCK8 assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1424944 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1777363 | Antiproliferative activity against human SU-DHL-5 cells assessed as cell viability at 10 uM by CellTiter-Glo luminescent cell viability assay (Rvb = 100%) | |||
| AID1395210 | Inhibition of PI3Kgamma (unknown origin) using Biotin-S11S12 as substrate after 60 mins in presence of ATP by ADPGlo luminescence assay | |||
| AID1335142 | Drug metabolism in rat liver microsomes assessed as disappearance of parent compound at 5 uM after 30 mins in presence of NADPH by UPLC-MS/MS analysis | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1459888 | Inhibition of recombinant human full length His-tagged PI3Kalpha expressed in baculovirus expression system | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1903046 | Antitumor activity against human Bel-7402 cells xenografted in BAlb/c (nu/nu) mouse assessed as T/C ratio at 40 mg/kg, po daily measured after 14 days | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1718738 | Antitumor activity against human TMD-8 cells xenografted in CB.17 SCID mouse assessed as tumor growth inhibition at 3 mg/kg, po once daily for 19 days relative to control | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1553485 | Inhibition of PI3Kdelta in basophil derived from B-cell malignant patient | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1424945 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425004 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1777364 | Antiproliferative activity against human MOLT-4 cells assessed as cell viability at 20 uM by CellTiter-Glo luminescent cell viability assay (Rvb = 100%) | |||
| AID1425065 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425016 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425141 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424979 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718668 | Terminal Half life in BALB/C mouse at 10 mg/kg, iv measured upto 24 hrs by LC-MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1321983 | Inhibition of human recombinant DNA-PK by Select-screen kinase inhibitor assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1 | Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
| AID729000 | Selectivity ratio of IC50 for PI3Kalpha (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors. |
| AID1327613 | Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate preincubated for 5 mins followed by fMLP/CB-induction | 2016 | Journal of natural products, 08-26, Volume: 79, Issue:8 | Chemical Constituents of the Rhizomes of Bletilla formosana and Their Potential Anti-inflammatory Activity. |
| AID1903049 | Antitumor activity against human Bel-7402 cells xenografted in BAlb/c (nu/nu) mouse assessed as inhibition rate at 40 mg/kg, po daily measured after 14 days | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1425055 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1605965 | Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1628348 | Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of superoxide generation preincubated for 5 mins followed by cytochalasin B and FMLP stimulation for 3 mins and 10 mins respectively by ferricytochrome c reduction b | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Bioactive Isoprenoid-Derived Natural Products from a Dongsha Atoll Soft Coral Sinularia erecta. |
| AID1718784 | Volume of distribution at steady state in Sprague-Dawley rat at 3 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425039 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1335157 | Anti-inflammatory activity in Brown Norway rat assessed as reduction in OVA-induced eosinophil infilteration to bronchoalveolar lavage administered orally bid 1 hr prior to OVA challenge on day 14 and 6 hrs post OVA challenge on day 21 measured 24 hrs pos | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1718675 | Cmax in BALB/C mouse at 30 mg/kg,po measured upto 24 hrs by LC-MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1448728 | Selectivity ratio of IC50 for PI3Kgamma (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders. |
| AID1438033 | Inhibition of human full length PI3K p110alpha/p85 alpha using PIP2/ATP as substrate after 30 mins by TR-FRET assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856. |
| AID1424996 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1395214 | Growth inhibition of human SU-DHL6 cells by CellTiter-Glo assay | |||
| AID1424902 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425106 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1558397 | Inhibition of His-tagged recombinant human PIK3CA/PIK3R1 expressed in Baculovirus expression system | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | The Exploration of Chirality for Improved Druggability within the Human Kinome. |
| AID1424984 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424893 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1690216 | Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | Structurally novel PI3Kδ/γ dual inhibitors characterized by a seven-membered spirocyclic spacer: The SARs investigation and PK evaluation. |
| AID1425045 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1438036 | Inhibition of human full length PI3Kgamma using PIP2/ATP as substrate after 30 mins by TR-FRET assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856. |
| AID1424963 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424981 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1395208 | Inhibition of PI3Kalpha (unknown origin) using Biotin-S11S12 as substrate after 60 mins in presence of ATP by Kinase Glo luminescence assay | |||
| AID1424934 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425098 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424895 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424942 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425122 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718730 | Plasma concentration in CB.17 SCID mouse xenografted with OCI-LY10 cells at 3 mg/kg, po once daily for 24 days | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1600808 | Inhibition of PI3K alpha (unknown origin) using phosphatidyl inositol as substrate measured after 60 mins in presence of ATP by Kinase-Glo Plus reagent-based luminescence assay | |||
| AID1425171 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425083 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1605977 | Antiproliferative activity against human A498 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1777370 | Inhibition of PI3Kdelta in human SU-DHL-5 cells assessed as inhibition of AKT phosphorylation at Ser473 residue at 1 to 5 uM measured after 3 hrs by western blot assay | |||
| 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. |
| AID1459869 | Antiproliferative activity against human HT cells measured after 72 hrs by alamar blue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1424987 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424914 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1192866 | Activation of human PXR at 2 uM relative to rifampicin | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Synthesis and SAR study of potent and selective PI3Kδ inhibitors. |
| AID1425151 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1903027 | Antiproliferative activity against human Hep3B cells assessed as inhibition rate at 10 uM incubated for 72 hrs by SRB assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1781100 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at G2 phase at 1 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =14.7 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1335136 | AUC in Wistar rat at 1 mg/kg, iv | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1425017 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424990 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1321982 | Inhibition of human recombinant Vps34 by Select-screen kinase inhibitor assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1 | Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
| AID1361742 | Antitumor activity against human MOLM14 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 100 mg/kg, po administered daily via gavage dosed for 14 days and measured daily during compound dosing relative to control | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1424933 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1781104 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at G2 phase at 2 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =14.7 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1773367 | Inhibition of recombinant full-length human His-tagged PI3Kgamma expressed in baculovirus expression system by Selectscreen kinase assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ. |
| AID1509590 | Inhibition of PI3K delta (unknown origin) using lipid substrate measured after 40 mins in presence of ATP by Kinase-Glo plus reagent based luminescence assay | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1425142 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1192862 | Inhibition of PI3Kgamma (unknown origin) by biochemical Alphascreen assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Synthesis and SAR study of potent and selective PI3Kδ inhibitors. |
| AID1424947 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1534884 | Inhibition of human full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Targeting the immunity protein kinases for immuno-oncology. |
| AID1781102 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at G1 phase at 2 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =46.8 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1600811 | Antiproliferative activity against human SUDHL6 cells by MTT assay | |||
| AID1425157 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1722450 | Inhibition of PI3Kdelta (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1390825 | Oral bioavailability in Sprague-Dawley rat at 3 mg/kg by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1425027 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425063 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1895254 | Inhibition of PI3Kdelta in anti-FceRI-stimulated human Basophil cells degranulation incubated for 30 mins | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1424899 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1777390 | Cytotoxicity against human MRC5 cells assessed as inhibition of cell viability at 20 uM measured after 48 hrs by MTT assay | |||
| AID1917533 | Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1390808 | Inhibition of PI3K p110beta (unknown origin) using lipid substrate after 40 mins by kinase-Glo assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1777367 | Inhibition of recombinant human full length His-tagged p110gamma expressed in baculovirus expression system measured after 60 mins in presence of ATP by ATP-competitive binding assay | |||
| AID1424929 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1361700 | Inhibition of PI3Kdelta (unknown origin) using PIP2:PS as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in presence of 50 uM ATP by ADP-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1553487 | Selectivity ratio of IC50 for PI3Kalpha in basophil derived from B-cell malignant patient to IC50 for PI3Kdelta in basophil derived from B-cell malignant patient | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1425018 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718722 | Toxicity in CB.17 SCID mouse xenografted with OCI-LY10 cells assessed as effect on body weight at 3 mg/kg, po once daily for 24 days (Rvb = 22.6 +/- 0.34 g) | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| 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. |
| AID1718678 | Oral bioavailability in BALB/C mouse at 30 mg/kg measured upto 24 hrs by LC-MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425050 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425115 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1722462 | Inhibition of recombinant human His-tagged PI3Kdelta expressed in baculovirus expression system using PIP2:PS as substrate incubated for 1 hr by invitrogen adapta assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1424909 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1192865 | Inhibition of PI3Kdelta (unknown origin) assessed as inhibition of AKT phosphorylation by cell-based HTRF assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Synthesis and SAR study of potent and selective PI3Kδ inhibitors. |
| AID1777388 | Tmax in Sprague-Dawley rat at 3 mg/kg, po measured for 24 hrs by LC-MS/MS analysis | |||
| AID1425138 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718782 | Half life in Sprague-Dawley rat at 3 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1773365 | Inhibition of recombinant full-length human His-tagged PI3Kalpha expressed in insect cells by Selectscreen kinase assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ. |
| AID1425070 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1777369 | Selectivity ratio of IC50 for recombinant human full length His-tagged p110gamma expressed in baculovirus expression system to IC50 for recombinant human full length His-tagged p110delta/p85alpha expressed in baculovirus expression system | |||
| AID1425158 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1509604 | Selectivity ratio of IC50 for inhibition of PI3K gamma (unknown origin) to IC50 for inhibition of PI3K delta (unknown origin) | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1424986 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425029 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424918 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1722451 | Selectivity index, ratio of IC50 for PI3Kalpha (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1425057 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1903021 | Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1605968 | Antiproliferative activity against human HOP92 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1395207 | Inhibition of PI3Kdelta (unknown origin) at 1 uM using Biotin-S11S12 as substrate after 120 mins in presence of ATP by ADPGlo luminescence assay | |||
| AID1425116 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425149 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424956 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425153 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424905 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1335141 | Drug metabolism in human liver microsomes assessed as disappearance of parent compound at 5 uM after 30 mins in presence of NADPH by UPLC-MS/MS analysis | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1425163 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718691 | Anticancer activity against human TMD8 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1424966 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425213 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425084 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1317030 | Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay | |||
| AID1718710 | Antitumor activity against human OCI-LY10 cells xenografted in CB.17 SCID mouse assessed as tumor volume at 3 mg/kg, po once daily for 24 days (Rvb = 1430.74 +/- 363.89 mm3) | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1328342 | Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release at 10 uM using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate preincubated for 5 mins followed by fMLP/CB-induction | 2016 | Journal of natural products, 09-23, Volume: 79, Issue:9 | Halogenated Sesquiterpenoids from the Red Alga Laurencia tristicha Collected in Taiwan. |
| AID1425173 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1335170 | Apparent volume of distribution in Wistar rat at 1 mg/kg, iv | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1425160 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1917532 | Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1425102 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424940 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718786 | Cmax in Sprague-Dawley rat at 3 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425131 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1587183 | Cmax in Sprague-Dawley rat at 10 mg/kg, po by LC/MS/MS analysis | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1379444 | Growth inhibition of human MCF7 cells after 72 hrs by SRB assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1718746 | Toxicity in CB.17 SCID mouse xenografted with TMD-8 cells assessed as effect on body weight at 3 mg/kg, po once daily for 19 days (Rvb = 28.66 +/- 0.83 g) | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1781103 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at S phase at 2 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =31.8 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1469865 | Inhibition of PI3Kbeta (unknown origin) after 60 mins using fluorescein-labeled kinase tracer by HTRF assay | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Identification of highly potent and selective PI3Kδ inhibitors. |
| AID1425146 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1605979 | Antiproliferative activity against human RXF393 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1718677 | Half life in BALB/C mouse at 30 mg/kg, po measured upto 24 hrs by LC-MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425082 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425007 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1534883 | Inhibition of human N-terminal His-tagged PI3Kalpha/p85alpha expressed in Spodoptera frugiperda using phosphatidylinositol as substrate | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Targeting the immunity protein kinases for immuno-oncology. |
| AID1777381 | Induction of apoptosis in human MOLT-4 cells assessed as early apoptotic cells at 20 uM measured after 24 hrs by AnnexinV-FITC/PI staining based flowcytometry method (Rvb = 2.04%) | |||
| AID719910 | Inhibition of PI3Kdelta | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID1718763 | Plasma concentration in CB.17 SCID mouse tumor xenografted with SUDHL-6 cells assessed as effect on body weight at 5 mg/kg, po once daily for 15 days | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1424924 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718792 | Half life in Beagle dog at 1 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1177094 | Inhibition of human PI3KC2alpha by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID1700586 | Inhibition of human PI3Kdelta using substrate PIP2:PS and ATP incubated for 1 hr by ADP-Glo assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Discovery of ( |
| AID1777391 | Cytotoxicity against human MRC5 cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay | |||
| AID1903065 | Induction of apoptosis in human Bel-7402 cells xenografted in Balb/c (nu/nu) mouse assessed as increase in expression of cleaved PARP at 40 mg/kg, po daily after 14 days by western blot analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1617134 | Inhibition of PI3Kalpha (unknown origin) using biotin-PIP3 as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence polarization assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of |
| AID1361697 | Inhibition of PI3Kalpha (unknown origin) using PIP2:PS as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in presence of 10 uM ATP by ADP-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1571686 | Selectivity ratio of IC50 for PI3Kalpha (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2019 | MedChemComm, Mar-01, Volume: 10, Issue:3 | Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation. |
| AID1424992 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1917529 | Inhibition of HDAC6 (unknown origin) measured by fluorescence based assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1390824 | Half life in Sprague-Dawley rat at 3 mg/kg, po by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1425188 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425167 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1917528 | Inhibition of PI3Kdelta (unknown origin) measured by ADP-Glo assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1525547 | Inhibition of PIK3CD (unknown origin) | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Why Some Targets Benefit from beyond Rule of Five Drugs. |
| AID1628347 | Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of superoxide generation at 10 uM preincubated for 5 mins followed by cytochalasin B and FMLP stimulation for 3 mins and 10 mins respectively by ferricytochrome c re | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Bioactive Isoprenoid-Derived Natural Products from a Dongsha Atoll Soft Coral Sinularia erecta. |
| AID1425161 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425000 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424973 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424968 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425156 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1481746 | Inhibition of PI3K p110delta/p85alpha (unknown origin) using lipid substrate after 40 mins by kinase-glo luminescence assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9 | Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors. |
| AID1722452 | Inhibition of PI3Kalpha (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1425069 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1509588 | Inhibition of PI3K beta (unknown origin) using lipid substrate measured after 40 mins in presence of ATP by Kinase-Glo plus reagent based luminescence assay | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1425006 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1777383 | Induction of apoptosis in human MOLT-4 cells assessed as necrotic cells at 20 uM measured after 24 hrs by AnnexinV-FITC/PI staining based flowcytometry method (Rvb = 0.51%) | |||
| AID1424972 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1177104 | Inhibition of human DNA-PK by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID1425189 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425150 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1438034 | Inhibition of N-terminal His6-tagged recombinant full-length human PI3K p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2/ATP as substrate after 30 mins by TR-FRET assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856. |
| AID1718793 | Oral bioavailability in Beagle dog at 1 mg/kg measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID719962 | Inhibition of PI3Kdelta in B-cells by proliferation assay | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID1425130 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1593856 | Inhibition of mTOR (unknown origin) assessed as reduction in p70S6K phosphorylation | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1425207 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1700589 | Selectivity index, ratio of IC50 for human PI3Kgamma to IC50 for human PI3Kdelta | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Discovery of ( |
| AID1895273 | Antiarthritic activity in collagen-induced rheumatoid arthritis DBA1/J mouse model assessed as reduction in disease severity at 20 mg/kg, po qd measured once daily for 24 to 27 days | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1424901 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1390812 | Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1600815 | Antiproliferative activity against human MCF7 cells by MTT assay | |||
| AID1718742 | Antitumor activity against human TMD-8 cells xenografted in CB.17 SCID mouse xenografted with OCI-LY10 cells assessed as tumor weight at 3 mg/kg, po once daily for 19 days (Rvb = 1.3 +/- 0.3 g) | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1481747 | Antiproliferative activity against human RPMI8266 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9 | Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors. |
| AID1425033 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID1425025 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425059 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID719925 | Selectivity ratio of IC50 for PI3Kbeta to IC50 for PI3Kdelta | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID1425191 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1459874 | Antiproliferative activity against human SU-DHL10 cells measured after 72 hrs by alamar blue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1424922 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424998 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424906 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425162 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1390807 | Inhibition of PI3K p110alpha (unknown origin) using lipid substrate after 40 mins by kinase-Glo assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1718734 | Antitumor activity against human TMD-8 cells xenografted in CB.17 SCID mouse assessed as tumor volume at 3 mg/kg, po once daily for 19 days (Rvb = 1811.14 +/- 301.55 mm3) | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1895243 | Inhibition of PI3Kgamma (unknown origin) | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1425074 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425198 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425067 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1605971 | Antiproliferative activity against human SNB75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1593852 | Inhibition of human PI3Kdelta using PIP2 as substrate after 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1917534 | Antiproliferative activity against human T47D cells incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1903025 | Antiproliferative activity against human Bel-7402 cells assessed as inhibition rate at 10 uM incubated for 72 hrs by SRB assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1425104 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424949 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425038 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425085 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1781106 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at G1 phase at 5 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =46.8 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1917540 | Selectivity ratio, ratio IC50 for inhibition of PI3Kgamma (unknown origin) to IC50 for inhibition of PI3Kdelta (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1718726 | Drug uptake in CB.17 SCID mouse tumor xenografted with OCI-LY10 cells at 3 mg/kg, po once daily for 24 days | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1722460 | Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTS assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1327612 | Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/cytochalasin B-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c preincubated for 5 mins followed by FMLP/cytochal | 2016 | Journal of natural products, 08-26, Volume: 79, Issue:8 | Chemical Constituents of the Rhizomes of Bletilla formosana and Their Potential Anti-inflammatory Activity. |
| AID1558392 | Inhibition of His-tagged recombinant human PIK3CB | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | The Exploration of Chirality for Improved Druggability within the Human Kinome. |
| AID729014 | Inhibition of PI3K p110beta (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors. |
| AID1425144 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1903064 | Induction of apoptosis in human Bel-7402 cells xenografted in Balb/c (nu/nu) mouse assessed as decrease in phosphorylation of Akt at serine 473 residue at 40 mg/kg, po daily after 14 days by western blot analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1425190 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425077 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1593854 | Inhibition of human PI3Kbeta using PIP2 as substrate after 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| 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. |
| AID1781119 | Induction of apoptosis in human MOLM16 cells assessed as late apoptotic cells at 5 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 6.77 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1425014 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424923 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1895251 | Inhibition of PI3Kbeta in human 786-0 cells assessed as reduction in AKT phosphorylation at S473 residue incubated for 30 mins | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1718674 | Tmax in BALB/C mouse at 30 mg/kg, po measured upto 24 hrs by LC-MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1718761 | Toxicity in CB.17 SCID mouse xenografted with SUDHL-6 cells assessed as effect on body weight at 5 mg/kg, po once daily for 15 days (Rvb = 28.13 +/- 0.65 g) | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1553486 | Inhibition of PI3Kgamma in basophil derived from B-cell malignant patient | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1781097 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at subG1 phase at 1 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =4.02 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1425099 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1558398 | Inhibition of His-tagged recombinant human PIK3CG expressed in Baculovirus expression system | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | The Exploration of Chirality for Improved Druggability within the Human Kinome. |
| AID1425124 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1571681 | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate after 2 hrs by ADP-Glo assay | 2019 | MedChemComm, Mar-01, Volume: 10, Issue:3 | Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation. |
| AID1605973 | Antiproliferative activity against human LOXIMVI cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1317034 | Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay | |||
| AID1425140 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID729012 | Inhibition of PI3K p110gamma (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors. |
| AID1425100 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425184 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425143 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1390815 | Cmax in Sprague-Dawley rat at 3 mg/kg, po by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1424900 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1903066 | Induction of apoptosis in human Bel-7402 cells xenografted in Balb/c (nu/nu) mouse assessed as increase in expression of cleaved caspase-3 at 40 mg/kg, po daily after 14 days by western blot analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1690215 | Inhibition of human full-length recombinant His-tagged PI3K p110delta/p85alpha expressed in baculovirus expression system using PIP2 as substrate measured after 2 hrs by ADP-Glo luminescence assay | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | Structurally novel PI3Kδ/γ dual inhibitors characterized by a seven-membered spirocyclic spacer: The SARs investigation and PK evaluation. |
| AID1773366 | Inhibition of recombinant full-length human His-tagged PI3Kbeta expressed in insect cells by Selectscreen kinase assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ. |
| AID1425097 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1509603 | Selectivity ratio of IC50 for inhibition of PI3K alpha (unknown origin) to IC50 for inhibition of PI3K delta (unknown origin) | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1361718 | Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1317035 | Antiproliferative activity against patient-derived IgM-stimulated CLL cells after 3 days by CellTiter-Glo assay | |||
| AID1390805 | Inhibition of PI3K p110delta (unknown origin) using lipid substrate after 40 mins by kinase-Glo assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1425101 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425056 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425043 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1335138 | Oral bioavailability in Wistar rat at 1 mg/kg administered via gavage | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1571682 | Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | MedChemComm, Mar-01, Volume: 10, Issue:3 | Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation. |
| AID1361719 | Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1425204 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424891 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1571684 | Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate after 2 hrs by ADP-Glo assay | 2019 | MedChemComm, Mar-01, Volume: 10, Issue:3 | Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation. |
| AID1777365 | Inhibition of recombinant human full length N-terminal His-tagged p110alpha/p85alpha expressed in baculovirus expression system measured after 60 mins in presence of ATP by ATP-competitive binding assay | |||
| AID1424970 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID1587179 | Half life in Sprague-Dawley rat at 2 mg/kg, iv by LC/MS/MS analysis | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1722455 | Antiproliferative activity against human OCILY3 assessed as reduction in cell growth by MTS assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1553488 | Selectivity ratio of IC50 for PI3Kbeta in basophil derived from B-cell malignant patient to IC50 for PI3Kdelta in basophil derived from B-cell malignant patient | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1605974 | Antiproliferative activity against human M14 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1424978 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1895244 | Inhibition of PI3Kalpha (unknown origin) | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1781114 | Induction of apoptosis in human MOLM16 cells assessed as early apoptotic cells at 2 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 16.4 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1425081 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1395206 | Inhibition of PI3Kdelta (unknown origin) using Biotin-S11S12 as substrate after 120 mins in presence of ATP by ADPGlo luminescence assay | |||
| AID1424948 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1777378 | Induction of apoptosis in human SU-DHL-10 cells assessed as late apoptotic cells at 20 uM measured after 24 hrs by AnnexinV-FITC/PI staining based flowcytometry method (Rvb = 3.48%) | |||
| AID1773368 | Inhibition of PI3Kdelta (unknown origin) by Selectscreen kinase assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ. |
| AID1425169 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1469864 | Inhibition of PI3Kalpha (unknown origin) after 60 mins using fluorescein-labeled kinase tracer by HTRF assay | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Identification of highly potent and selective PI3Kδ inhibitors. |
| AID1361704 | Inhibition of PI4K3B (unknown origin) using PI:PS as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in presence of 50 uM ATP by ADP-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1903055 | Antitumor activity against human Bel-7402 cells xenografted in Balb/c (nu/nu) mouse assessed as tumor weight at 40 mg/kg, po qd after 14 days (Rvb=0.65 +/- 0.06 g) | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1425048 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424946 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425155 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425186 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424995 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425003 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718750 | Drug uptake in CB.17 SCID mouse tumor xenografted with TMD-8 cells at 3 mg/kg, po once daily for 19 days | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1718781 | Cmax in Sprague-Dawley rat at 3 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1361696 | Inhibition of GST-tagged full length recombinant human VPS34 expressed in Baculovirus expression system using PI:PS as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in presence of 50 uM ATP by ADP-Glo luminescence | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1425179 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425005 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1593851 | Inhibition of human PI3Kdelta using PIP2 as substrate at 100 nM after 1 hr relative to control | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1425019 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424925 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1587174 | Growth inhibition of human SU-DHL6 cells incubated for 72 hrs by CellTiter-Glo assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1777393 | Inhibition of PI3Kdelta in human MOLT-4 cells assessed as inhibition of AKT phosphorylation at Thr308 residue at 1 to 5 uM measured after 3 hrs by western blot assay | |||
| AID1424971 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425090 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425165 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425060 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425128 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID1903041 | Induction of apoptosis in human Bel-7402 cells assessed as increase in apoptotic cells at 50 uM for 24 hrs by TUNEL staining method | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1425127 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1509587 | Inhibition of PI3K alpha (unknown origin) using lipid substrate measured after 40 mins in presence of ATP by Kinase-Glo plus reagent based luminescence assay | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1718687 | Anticancer activity against human SUDHL-6 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1781120 | Induction of apoptosis in human MOLM16 cells assessed as necrotic cells at 5 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 0.44 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1553514 | Inhibition of Vps34 (unknown origin) | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases. |
| AID1424916 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425058 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1361743 | Antitumor activity against human MOLM14 cells xenografted in nu/nu mouse assessed as induction of apoptosis at 100 mg/kg, po administered daily via gavage dosed for 14 days and measured daily during compound dosing by TUNEL based assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1459854 | Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate measured after 30 mins by HTRF assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1425159 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425178 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424999 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425194 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1895255 | Inhibition of PI3Kdelta in anti-IgM-stimulated human whole blood B cell degranulation incubated for 60 mins by flow cytometry | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1424950 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425201 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425137 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1390810 | Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1718676 | AUClast in BALB/C mouse at 30 mg/kg, po measured upto 24 hrs by LC-MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1335161 | Apparent volume of distribution in Beagle dog at 1 mg/kg, iv through bolus administration | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1192861 | Inhibition of PI3Kdelta (unknown origin) by biochemical Alphascreen assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Synthesis and SAR study of potent and selective PI3Kδ inhibitors. |
| AID1328341 | Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c at 20 uM preincubated for 5 mins followed by fMLP/CB-inductio | 2016 | Journal of natural products, 09-23, Volume: 79, Issue:9 | Halogenated Sesquiterpenoids from the Red Alga Laurencia tristicha Collected in Taiwan. |
| AID1425021 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID1917539 | Selectivity ratio, ratio IC50 for inhibition of PI3Kalpha (unknown origin) to IC50 for inhibition of PI3Kdelta (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1459859 | Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate measured after 30 mins by HTRF assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| 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. |
| AID1425037 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425086 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1481749 | Antiproliferative activity against human Raji cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9 | Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors. |
| AID1425108 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424954 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425035 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424890 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425182 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1459867 | Antiproliferative activity against human KARPAS422 cells measured after 72 hrs by alamar blue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1425030 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425176 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424937 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424961 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425002 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1722456 | Antiproliferative activity against human OCILY10 assessed as reduction in cell growth by MTS assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1425012 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1438035 | Inhibition of human full length PI3K p110delta/p85 alpha using PIP2/ATP as substrate after 30 mins by TR-FRET assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856. |
| AID1587181 | Volume of distribution at steady state in Sprague-Dawley rat at 2 mg/kg, iv by LC/MS/MS analysis | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1395212 | Selectivity index, ratio of IC50 for PI3Kbeta (unknown origin) to IC50 for PI3Kdelta (unknown origin) | |||
| AID1600810 | Inhibition of PI3K gamma (unknown origin) using phosphatidyl inositol as substrate measured after 60 mins in presence of ATP by Kinase-Glo Plus reagent-based luminescence assay | |||
| AID1571688 | Selectivity ratio of IC50 for PI3Kgamma (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2019 | MedChemComm, Mar-01, Volume: 10, Issue:3 | Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation. |
| AID1425166 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718688 | Anticancer activity against human OCILY10 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1448831 | Inhibition of PI3Kdelta (unknown origin) | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders. |
| AID1317010 | Inhibition of human PI3Kgamma (S144 to A1102 residues) expressed in mammalian expression system incubated for 60 mins by ADAPTA assay | |||
| AID1777366 | Inhibition of recombinant human full length His-tagged p110beta expressed in baculovirus expression system measured after 60 mins in presence of ATP by ATP-competitive binding assay | |||
| AID1781099 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at S phase at 1 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =31.8 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1718667 | AUClast in BALB/C mouse at 10 mg/kg, iv measured upto 24 hrs by LC-MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1481745 | Inhibition of PI3K p110delta/p85alpha (unknown origin) at 100 nM using lipid substrate after 40 mins by kinase-glo luminescence assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9 | Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors. |
| AID1424964 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1361699 | Inhibition of PI3Kgamma (unknown origin) using PIP2:PS as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in presence of 50 uM ATP by ADP-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1425001 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718789 | Tmax in Beagle dog at 1 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1424894 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425170 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425180 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425113 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1321980 | Inhibition of human recombinant PI3KC2beta by Select-screen kinase inhibitor assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1 | Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
| AID1903019 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1425121 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424960 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1781101 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at subG1 phase at 2 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =4.02 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1424910 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424897 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1777387 | Cmax in Sprague-Dawley rat at 3 mg/kg, po measured for 24 hrs by LC-MS/MS analysis | |||
| AID1425107 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1781118 | Induction of apoptosis in human MOLM16 cells assessed as early apoptotic cells at 5 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 16.4 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1587175 | Inhibition of His-tagged recombinant human full length PI3K p110alpha/p85alpha expressed in baculovirus expression system using lipid substrate incubated for 60 mins by kinase-Glo reagent based luminescence assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1317006 | Inhibition of p110delta in HMEC assessed as reduction in S6RP phosphorylation at Ser-235/236 residue at 10 nM after 1 hr by Western blot analysis | |||
| AID1459875 | Antiproliferative activity against human MOLT4 cells measured after 72 hrs by alamar blue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1379448 | Growth inhibition of human Pfeiffer cells by CCK8 assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1600813 | Antiproliferative activity against human Raji cells by MTT assay | |||
| AID1600809 | Inhibition of PI3K beta (unknown origin) using phosphatidyl inositol as substrate measured after 60 mins in presence of ATP by Kinase-Glo Plus reagent-based luminescence assay | |||
| AID1425119 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718714 | Antitumor activity against human OCI-LY10 cells xenografted in CB.17 SCID mouse assessed as tumor growth inhibition at 3 mg/kg, po once daily for 24 days relative to control | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1781113 | Induction of apoptosis in human MOLM16 cells assessed as viable cells at 2 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 76.3 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1777379 | Induction of apoptosis in human SU-DHL-10 cells assessed as necrotic cells at 20 uM measured after 24 hrs by AnnexinV-FITC/PI staining based flowcytometry method (Rvb = 0.2%) | |||
| AID1718791 | Cmax in Beagle dog at 1 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425047 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1317032 | Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay | |||
| AID1718773 | Clearance in Beagle dog at 1 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1425011 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID729015 | Inhibition of PI3K p110alpha (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors. |
| AID1781107 | Induction of cell cycle arrest in human MOLM16 cells assessed as accumulation at S phase at 5 uM incubated for 24 hrs by propidium iodide /RNase staining based flow cytometry(Rvb =31.8 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1424993 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1781109 | Induction of apoptosis in human MOLM16 cells assessed as viable cells at 1 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 76.3 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| 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. |
| AID1486993 | Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide oxide dismutase inhibitable reduction of ferricytochrome c at 10 uM incubated for 5 mins | 2017 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15 | Bioactive new withanolides from the cultured soft coral Sinularia brassica. |
| AID1486994 | Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release incubated for 5 mins in presence of MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide | 2017 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15 | Bioactive new withanolides from the cultured soft coral Sinularia brassica. |
| AID1425109 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1781116 | Induction of apoptosis in human MOLM16 cells assessed as necrotic cells at 2 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 0.44 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1777380 | Induction of apoptosis in human MOLT-4 cells assessed as viable cells at 20 uM measured after 24 hrs by AnnexinV-FITC/PI staining based flowcytometry method (Rvb = 95.3%) | |||
| AID1425068 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1192863 | Inhibition of PI3Kbeta (unknown origin) by biochemical Alphascreen assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Synthesis and SAR study of potent and selective PI3Kδ inhibitors. |
| AID1617137 | Inhibition of PI3Kgamma (unknown origin) using biotin-PIP3 as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence polarization assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of |
| AID1425087 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID1903028 | Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1593853 | Inhibition of human PI3Kalpha using PIP2 as substrate after 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1459873 | Antiproliferative activity against human SU-DHL4 cells measured after 72 hrs by alamar blue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| 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. |
| AID1425110 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1605937 | Antiproliferative activity against human Hs578T cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1424975 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1600814 | Antiproliferative activity against human HCT116 cells by MTT assay | |||
| AID1722457 | Antiproliferative activity against human SU-DHL-6 assessed as reduction in cell growth by MTS assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors. |
| AID1424958 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425136 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425145 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425052 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424935 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1459857 | Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by alamar blue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1448834 | Inhibition of PI3Kalpha (unknown origin) | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders. |
| AID728999 | Selectivity ratio of IC50 for PI3Kbeta (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors. |
| AID1917536 | Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1777389 | Half life in Sprague-Dawley rat at 3 mg/kg, po measured for 24 hrs by LC-MS/MS analysis | |||
| AID1424965 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1395209 | Inhibition of PI3Kbeta (unknown origin) using Biotin-S11S12 as substrate after 60 mins in presence of ATP by ADPGlo luminescence assay | |||
| AID1425089 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1895242 | Inhibition of PI3Kdelta (unknown origin) | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1317031 | Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay | |||
| AID1781117 | Induction of apoptosis in human MOLM16 cells assessed as viable cells at 5 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 76.3 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1606026 | Binding affinity to PI3Kdelta in human MV4-11 cells assessed as increase in cellular protein stabilization at 1 uL preincubated for 1 hr followed by heating at 52 degree C for 3.5 mins by CETSA | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1335156 | In vivo inhibition of PI3Kdelta in Wistar rat assessed as reduction in ConA-induced increase in plasma IL2 production administered through oral gavage 1 hr prior to ConA measured 90 mins post ConA challenge by ELISA | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1425066 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1718787 | Half life in Sprague-Dawley rat at 3 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Discovery of a Potent and Selective PI3Kδ Inhibitor ( |
| AID1895252 | Inhibition of PI3Kgamma in c5a-stimulated mouse RAW264.7 cells assessed as reduction in AKT phosphorylation at S473 residue incubated for 30 mins | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases. |
| AID1459872 | Antiproliferative activity against human SU-DHL1 cells measured after 72 hrs by alamar blue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID1700588 | Selectivity index, ratio of IC50 for human PI3Kbeta to IC50 for human PI3Kdelta | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Discovery of ( |
| AID1335158 | Half life in Beagle dog at 1 mg/kg, iv through bolus administration | 2017 | ACS medicinal chemistry letters, Jan-12, Volume: 8, Issue:1 | Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. |
| AID1587182 | Clearance in Sprague-Dawley rat at 2 mg/kg, iv by LC/MS/MS analysis | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1903030 | Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. |
| AID1425183 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1361702 | Inhibition of N-terminal GST-tagged recombinant human PIK3C2B catalytic domain expressed in Baculovirus expression system using PI as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in presence of 50 uM ATP by ADP-Gl | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID1425147 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425071 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424898 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1872689 | Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Recent development of BTK-based dual inhibitors in the treatment of cancers. |
| AID1781110 | Induction of apoptosis in human MOLM16 cells assessed as early apoptotic cells at 1 uM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 16.4 %) | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1459871 | Antiproliferative activity against human NAMALWA cells measured after 72 hrs by alamar blue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. |
| AID719924 | Selectivity ratio of IC50 for PI3Kalpha to IC50 for PI3Kdelta | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID1571687 | Selectivity ratio of IC50 for PI3Kbeta (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2019 | MedChemComm, Mar-01, Volume: 10, Issue:3 | Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation. |
| AID1587184 | AUC (0 to t) in Sprague-Dawley rat at 10 mg/kg, po by LC/MS/MS analysis | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| 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. |
| AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
| AID1345749 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (Phosphatidylinositol kinases) | 2011 | Blood, Jan-13, Volume: 117, Issue:2 | CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. |
| AID1345786 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma (Phosphatidylinositol kinases) | 2011 | Blood, Jan-13, Volume: 117, Issue:2 | CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. |
| AID1345748 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta (Phosphatidylinositol kinases) | 2011 | Blood, Jan-13, Volume: 117, Issue:2 | CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. |
| AID1345778 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta (Phosphatidylinositol kinases) | 2011 | Blood, Jan-13, Volume: 117, Issue:2 | CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| 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 | 311 (76.23) | 24.3611 |
| 2020's | 97 (23.77) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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 very strong demand-to-supply ratio for research on this compound.
| This Compound (54.53) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 46 (11.17%) | 5.53% |
| Reviews | 91 (22.09%) | 6.00% |
| Case Studies | 33 (8.01%) | 4.05% |
| Observational | 4 (0.97%) | 0.25% |
| Other | 238 (57.77%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Phase Ib /II Trial of Pembrolizumab and Idelalisib in Patients With Non-small Cell Lung Cancer (NSCLC) Who Have Failed Immune Checkpoint Inhibitor [NCT03257722] | Phase 1/Phase 2 | 40 participants (Anticipated) | Interventional | 2017-09-26 | Recruiting | ||
| A Randomized, Multicenter, Open-Label, Phase 3 Study of Acalabrutinib (ACP-196) Versus Investigator's Choice of Either Idelalisib Plus Rituximab or Bendamustine Plus Rituximab in Subjects With R/R Chronic Lymphocytic Leukemia [NCT02970318] | Phase 3 | 310 participants (Actual) | Interventional | 2017-02-02 | Active, not recruiting | ||
| A Prospective, Open-Label, Multicenter, Phase 2 Trial to Evaluate the Safety and Efficacy of the Combination of Tirabrutinib (GS-4059) and Idelalisib With and Without Obinutuzumab in Subjects With Chronic Lymphocytic Leukemia [NCT02968563] | Phase 2 | 35 participants (Actual) | Interventional | 2016-12-13 | Completed | ||
| Idelalisib Plus Obinutuzumab in Patients With Relapsed/Refractory Follicular Lymphoma: a Phase 2, Single-arm, Multicentric Study [NCT03890289] | Phase 2 | 5 participants (Actual) | Interventional | 2019-10-18 | Terminated(stopped due to Study was halted prematurely due to safety, since tocity stopping rules have been met) | ||
| A Phase II, Two-Cohort, Open-Label, Multicenter Study to Evaluate the Safety and Preliminary Efficacy of MOR00208 Combined With Idelalisib or Venetoclax in Patients With Relapsed or Refractory CLL/SLL Previously Treated With Bruton's Tyrosine Kinase (BTK) [NCT02639910] | Phase 2 | 24 participants (Actual) | Interventional | 2016-11-30 | Completed | ||
| "An Open Label Non-randomized Phase II Study Exploring Chemo-free Treatment Association With Idelalisib + Obinutuzumab in Patient With Relapsed/Refractory Waldenstrom's Macroglobulinemia" [NCT02962401] | Phase 2 | 50 participants (Actual) | Interventional | 2017-03-07 | Completed | ||
| Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) Trial: PRIME [NCT03878524] | Phase 1 | 2 participants (Actual) | Interventional | 2020-04-01 | Active, not recruiting | ||
| Study of Phosphatidylinositol-3-kinase (PI3K) Inhibitor, Idelalisib (GS-1101), in IgM-Associated AL Amyloid [NCT02590588] | Phase 2 | 1 participants (Actual) | Interventional | 2016-01-31 | Terminated(stopped due to Poor accrual) | ||
| An Open Label, Roll Over Study to Provide Idelalisib to Subjects Previously Treated With the Investigational PI3Kδ Inhibitor, GS-9820 [NCT02739360] | Phase 4 | 3 participants (Actual) | Interventional | 2016-05-04 | Terminated | ||
| Phase 1b Trial Evaluating Idelalisib in Children and Adolescents With Relapsed or Refractory Diffuse Large B-cell Lymphoma or Mediastinal B-cell Lymphoma in Combination With RICE [NCT03349346] | Phase 1 | 0 participants (Actual) | Interventional | 2019-06-30 | Withdrawn(stopped due to The European Medical Agency granted a Paediatric Investigational Product-specific waiver on the grounds that idelalisib is likely to be unsafe in paediatrics) | ||
| Prospective, Open-label, Multicenter Phase-II Trial to Evaluate Efficacy and Safety of a Sequential Regimen of Bendamustine Followed by GA101 (Obinutuzumab) and CAL-101 (Idelalisib) Followed by CAL-101 and GA101 Maintenance in CLL Patients [NCT02445131] | Phase 2 | 48 participants (Actual) | Interventional | 2015-05-28 | Completed | ||
| A Phase 2 Randomized Study of Loncastuximab Tesirine Versus Idelalisib in Patients With Relapsed or Refractory Follicular Lymphoma (LOTIS-6) [NCT04699461] | Phase 2 | 6 participants (Actual) | Interventional | 2021-11-04 | Terminated(stopped due to Administrative decision (not due to safety reason)) | ||
| An Extension Study to Investigate the Safety and Durability of Clinical Activity of Idelalisib in Subjects With Hematologic Malignancies [NCT01090414] | Phase 1/Phase 2 | 202 participants (Actual) | Interventional | 2010-03-22 | Terminated | ||
| Single-agent Idelalisib for Previously Treated Low-grade Lymphoma: A Phase 1/2 Study of Safety, Efficacy, and Flow-cytometric Assessment of Tumor-cell Signaling Events [NCT01306643] | Phase 1/Phase 2 | 18 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
| A Phase 1b/2 Study of Idelalisib in Combination With BI 836826 in Subjects With Chronic Lymphocytic Leukemia [NCT02538614] | Phase 1 | 2 participants (Actual) | Interventional | 2015-12-29 | Terminated | ||
| An Expanded Access Protocol for Idelalisib in Combination With Rituximab for Relapsed, Previously Treated Subjects With Chronic Lymphocytic Leukemia [NCT02136511] | 0 participants | Expanded Access | Approved for marketing | ||||
| A Phase II, Non-Randomized, Single Institution, Clinical Trial of Signal Transduction Inhibitors, Ibrutinib or Idelalisib, to Treat Patients With Persistent or Relapsed B-Cell Malignancies Following Allogeneic Hematopoietic Cell Transplantation [NCT02662296] | Phase 2 | 0 participants (Actual) | Interventional | 2016-03-31 | Withdrawn(stopped due to Low enrollment) | ||
| A Phase Ib Feasibility Study of Personalized Kinase Inhibitor Therapy Combined With Induction in Acute Leukemias Who Exhibit In Vitro Kinase Inhibitor Sensitivity [NCT02779283] | Phase 1 | 7 participants (Actual) | Interventional | 2016-01-13 | Completed | ||
| Phase I-II Unmasked, Non-randomized Study Evaluating the Role of Idelalisib in Patients With Acute Lymphoblastic Leukemia (ALL) That is Relapsing or Refractory to Other Treatments, and in Older Patients With ALL for Whom Conventional Treatments Are Not Re [NCT03742323] | Phase 1/Phase 2 | 6 participants (Actual) | Interventional | 2018-07-01 | Terminated(stopped due to Because of low recruitment) | ||
| A Phase Ib Dose Escalation Study of BCL201 in Combination With Idelalisib in Patients With Follicular Lymphoma (FL) and Mantle Cell Lymphoma (MCL) [NCT02603445] | Phase 1 | 20 participants (Actual) | Interventional | 2015-11-16 | Completed | ||
| A Phase 1 Sequential Dose Escalation Study to Investigate the Safety, Pharmacokinetics, Pharmacodynamics, and Clinical Activity of CAL-101 in Patients With Select, Relapsed or Refractory Hematologic Malignancies [NCT00710528] | Phase 1 | 192 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| A Phase 1, Randomized, Double-Blind, Placebo-Controlled, Two-Period Crossover Study to Investigate the Safety of CAL-101 in Allergic Rhinitis Subjects and Effects on the Response to Environmental Chamber Allergen Challenge [NCT00836914] | Phase 1 | 41 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| A Phase 1b Dose Escalation and Dose Expansion Study of Tirabrutinib (ONO/GS-4059) in Combination With Other Targeted Anti-cancer Therapies in Subjects With B-cell Malignancies [NCT02457598] | Phase 1 | 203 participants (Actual) | Interventional | 2015-06-16 | Active, not recruiting | ||
| A Phase II Study of Anti-PD-1 Antibody (MK-3475) in Relapsed/Refractory Chronic Lymphocytic Leukemia (CLL) and Other Low Grade B Cell Non-Hodgkin Lymphoma (NHL) [NCT02332980] | Phase 2 | 65 participants (Actual) | Interventional | 2015-02-19 | Completed | ||
| A Phase 2 Study to Assess the Efficacy and Safety of Idelalisib in Subjects With Indolent B-Cell Non-Hodgkin Lymphomas Refractory to Rituximab and Alkylating Agents [NCT01282424] | Phase 2 | 125 participants (Actual) | Interventional | 2011-03-18 | Completed | ||
| A Phase Ib Study of ACY-1215 in Combination With BCR Pathway Inhibitors in Relapsed Chronic Lymphocytic Leukemia [NCT02787369] | Phase 1 | 3 participants (Actual) | Interventional | 2016-05-31 | Active, not recruiting | ||
| A Phase I Study to Investigate the Safety and Clinical Activity of Idelalisib in Combination With Chemotherapeutic Agents, Immunomodulatory Agents and Anti-CD20 mAb in Subjects With Relapsed or Refractory Indolent B-cell Non-Hodgkin Lymphoma, Mantle Cell [NCT01088048] | Phase 1 | 241 participants (Actual) | Interventional | 2010-03-25 | Completed | ||
| A Phase II Study of Idelalisib (GS1101, CAL101) + Ofatumumab in Previously Untreated Chronic Lymphocytic Leukemia (CLL) and Small Lymphocytic Leukemia (SLL) [NCT02135133] | Phase 2 | 50 participants (Anticipated) | Interventional | 2014-06-30 | Active, not recruiting | ||
| A Phase 2 Single Arm Study to Investigate the Safety and Clinical Activity of Idelalisib Alone and in Combination With Rituximab in Elderly Subjects With Previously Untreated Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma [NCT01203930] | Phase 2 | 105 participants (Actual) | Interventional | 2010-10-31 | Terminated | ||
| Idelalisib (GS-1101)-Associated Colitis - Molecular and Cellular Mechanisms Research Proposal [NCT02928510] | 1 participants (Actual) | Observational | 2016-02-01 | Terminated(stopped due to withdrawn by sponsor) | |||
| A Phase 3, Double-Blind Extension Study Evaluating the Efficacy and Safety of Two Different Dose Levels of Single-Agent Idelalisib (GS-1101) for Previously Treated Chronic Lymphocytic Leukemia A Companion Trial to Study GS-US-312-0116: A Phase 3, Randomiz [NCT01539291] | Phase 3 | 161 participants (Actual) | Interventional | 2012-10-03 | Terminated | ||
| A Phase 1b Open-Label Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Idelalisib in Subjects Receiving Ruxolitinib as Therapy for Primary, Post-Polycythemia Vera, or Post-Essential Thrombocythemia Myelofibrosis With Progressive or Rela [NCT02436135] | Phase 1 | 10 participants (Actual) | Interventional | 2015-06-05 | Terminated | ||
| A Phase 2 Study to Assess the Efficacy and Safety of GS-1101 (CAL-101) in Patients With Relapsed or Refractory Hodgkin Lymphoma [NCT01393106] | Phase 2 | 25 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| A Retrospective Observational Study to Evaluate the Clinical Outcomes and Routine Management of Patients With Chronic Lymphocytic Leukaemia Treated With Idelalisib and Rituximab in the United Kingdom (UK) and Ireland [NCT03582098] | 112 participants (Actual) | Observational | 2018-09-12 | Completed | |||
| A Phase II Proof-of-Concept Trial to Study Kinase Inhibition in Relapsed/Refractory Acute Leukemias: Using a Comprehensive In Vitro Kinase Inhibitor Panel to Select Individualized, Targeted Therapies [NCT01620216] | Phase 2 | 12 participants (Actual) | Interventional | 2012-05-11 | Terminated(stopped due to Unable to recruit enough eligible subjects) | ||
| Study to Investigate Outcome of Individualized Treatment Based on Pharmacogenomic Profiling & Ex Vivo Drug Sensitivity Testing of Patient-derived Organoids in Patients With Metastatic Colorectal Cancer [NCT05725200] | Phase 2 | 40 participants (Anticipated) | Interventional | 2022-09-27 | Recruiting | ||
| Phase 1b, Open Label Study to Evaluate Safety and Efficacy of TRU-016 in Combination With Rituximab, Obinutuzumab, Rituximab and Idelalisib, or Ibrutinib in Chronic Lymphocytic Leukemia and With Bendamustine in Peripheral T-cell Lymphoma [NCT01644253] | Phase 1 | 87 participants (Actual) | Interventional | 2012-09-30 | Terminated(stopped due to Business decision) | ||
| A Phase I Trial of Lenalidomide and Idelalisib in Recurrent Follicular Lymphoma [NCT01644799] | Phase 1 | 8 participants (Actual) | Interventional | 2013-07-31 | Completed | ||
| A Phase 2, Single-Arm, Open-Label Study Evaluating the Efficacy and Safety of Single Agent GS 1101 (CAL 101) as Therapy for Previously Treated Chronic Lymphocytic Leukemia [NCT01659047] | Phase 2 | 0 participants (Actual) | Interventional | 2012-08-31 | Withdrawn | ||
| A Phase I/Randomized Phase II Trial of Idelalisib and Lenalidomide in Patients With Relapsed/Refractory Mantle Cell Lymphoma [NCT01838434] | Phase 1 | 106 participants (Actual) | Interventional | 2013-07-31 | Completed | ||
| A Phase 3 Open-Label, Randomized Study of LOXO-305 Versus Investigator's Choice of Idelalisib Plus Rituximab or Bendamustine Plus Rituximab in BTK Inhibitor Pretreated Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (BRUIN CLL-321) [NCT04666038] | Phase 3 | 250 participants (Anticipated) | Interventional | 2021-03-09 | Recruiting | ||
| 1630GCC: A Pilot Study of Zydelig in Patients With B-cell Malignancies as Post-Autologous Transplant Remission Maintenance [NCT03133221] | Phase 2 | 34 participants (Anticipated) | Interventional | 2017-10-23 | Active, not recruiting | ||
| Idelalisib Post Allogeneic Hematopoietic Stem Cell Transplant (HSCT) in B Cell Derived Malignancies: A Phase 1 Double Blinded Randomized Placebo Toxicity Trial [NCT03151057] | Phase 1 | 18 participants (Actual) | Interventional | 2018-07-31 | Terminated(stopped due to Safety endpointreached) | ||
| A Phase 2, Single Arm Study Evaluating the Safety and Efficacy of Idelalisib in Combination With Rituximab for Previously Untreated Follicular Lymphoma and Small Lymphocytic Lymphoma [NCT02258529] | Phase 2 | 10 participants (Actual) | Interventional | 2015-09-14 | Terminated | ||
| A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy and Safety of Idelalisib in Combination With Bendamustine and Rituximab for Previously Untreated Chronic Lymphocytic Leukemia [NCT01980888] | Phase 3 | 311 participants (Actual) | Interventional | 2014-02-05 | Terminated | ||
| A Phase 1b Study to Investigate the Safety, Tolerability, and Pharmacokinetics of Idelalisib in Japanese Subjects With Relapsed or Refractory Indolent B-Cell Non-Hodgkin Lymphomas or Chronic Lymphocytic Leukemia [NCT02242045] | Phase 1 | 6 participants (Actual) | Interventional | 2014-10-01 | Completed | ||
| Dose Optimization Study of Idelalisib in Follicular Lymphoma [NCT02536300] | Phase 3 | 96 participants (Actual) | Interventional | 2016-01-14 | Terminated(stopped due to Gilead has made the decision to close the study due to enrollment challenges) | ||
| Efficacy and Safety in Patients With Chronic Lymphocytic Leukemia (CLL) Treated With Idelalisib and Rituximab in the Clinical Practice: a GIMEMA-ERIC Study [NCT03545035] | 104 participants (Actual) | Observational | 2019-02-06 | Completed | |||
| A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy and Safety of Idelalisib (GS-1101) in Combination With Bendamustine and Rituximab for Previously Treated Chronic Lymphocytic Leukemia [NCT01569295] | Phase 3 | 416 participants (Actual) | Interventional | 2012-06-15 | Completed | ||
| A Phase 3, Randomized, Controlled Study Evaluating the Efficacy and Safety of Idelalisib (GS-1101) in Combination With Ofatumumab for Previously Treated Chronic Lymphocytic Leukemia [NCT01659021] | Phase 3 | 261 participants (Actual) | Interventional | 2012-12-04 | Terminated | ||
| A Phase 2, Single Arm Study Evaluating the Efficacy and Safety of Idelalisib in Combination With Rituximab in Patients With Previously Untreated Chronic Lymphocytic Leukemia With 17p Deletion [NCT02044822] | Phase 2 | 102 participants (Actual) | Interventional | 2014-08-06 | Terminated | ||
| A Phase II Trial of Idelalisib in Patients With Relapsed/Refractory Diffuse Large B-cell Lymphoma [NCT03576443] | Phase 2 | 36 participants (Actual) | Interventional | 2017-07-07 | Completed | ||
| A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy and Safety of Idelalisib (GS-1101) in Combination With Rituximab for Previously Treated Chronic Lymphocytic Leukemia [NCT01539512] | Phase 3 | 220 participants (Actual) | Interventional | 2012-04-30 | Completed | ||
| Phase II Study of Phosphatidylinositol-3-kinase (PI3K) Inhibitor Idelalisib (GS-1101) in Waldenström Macroglobulinemia [NCT02439138] | Phase 2 | 5 participants (Actual) | Interventional | 2015-10-31 | Terminated(stopped due to Safety issues from trials in CLL) | ||
| A Phase 1b Study of Single Agent Idelalisib Followed by Idelalisib in Combination With Chemotherapy in Subjects With Metastatic Pancreatic Ductal Adenocarcinoma [NCT02468557] | Phase 1 | 16 participants (Actual) | Interventional | 2015-07-30 | Terminated | ||
| A Phase 3, Randomized, Open-Label Study Evaluating the Efficacy and Safety of Idelalisib in Combination With Obinutuzumab Compared to Chlorambucil in Combination With Obinutuzumab for Previously Untreated Chronic Lymphocytic Leukemia [NCT01980875] | Phase 3 | 57 participants (Actual) | Interventional | 2015-04-21 | Terminated | ||
| Efficacy of BCR Inhibitors in the Treatment of Autoimmune Cytopenias Associated With Chronic Lymphocytic Leukemia (CLL): A Retrospective Analysis of the French Innovative Leukemia Organization (FILO) [NCT03469895] | 40 participants (Actual) | Observational | 2017-07-21 | Active, not recruiting | |||
| A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy and Safety of Idelalisib (GS-1101) in Combination With Rituximab for Previously Treated Indolent Non-Hodgkin Lymphomas [NCT01732913] | Phase 3 | 295 participants (Actual) | Interventional | 2013-01-16 | Terminated | ||
| A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy and Safety of Idelalisib (GS-1101) in Combination With Bendamustine and Rituximab for Previously Treated Indolent Non-Hodgkin Lymphomas [NCT01732926] | Phase 3 | 475 participants (Actual) | Interventional | 2013-01-02 | Terminated | ||
| Non-interventional Study to Assess the Safety Profile of Idelalisib in Patients With Refractory Follicular Lymphoma (FL) [NCT03568929] | 257 participants (Actual) | Observational | 2018-05-25 | Completed | |||
| A Phase 2, Open-Label Study Evaluating the Efficacy, Safety, Tolerability, and Pharmacodynamics of GS-9973 in Combination With Idelalisib in Subjects With Relapsed or Refractory Hematologic Malignancies [NCT01796470] | Phase 2 | 66 participants (Actual) | Interventional | 2013-06-20 | Terminated(stopped due to Study was terminated due to safety measures.) | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||