| Assay ID | Title | Year | Journal | Article |
|---|
| AID1345787 | Human mitogen-activated protein kinase 15 (Erk7 subfamily) | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1345612 | Human cyclin dependent kinase 2 (CDK1 subfamily) | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1345684 | Human cyclin dependent kinase 9 (CDK9 subfamily) | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1345677 | Human cyclin dependent kinase 5 (CDK5 subfamily) | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1345652 | Human cyclin dependent kinase 7 (CDK7 subfamily) | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| 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. |
| AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| 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. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| 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. |
| AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| AID604839 | Elimination half life in mouse at 10 mg/kg, iv | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604650 | Cell cycle arrest in human HCT116 cells assessed as reduction in cells at G1 phase at 1 to 10 umol/L after 24 hrs by propidium iodide staining based flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604777 | Toxicity in nude BALB/c mouse assessed as adverse effect on weight at 5 mg/kg, ip bid for 14 days | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604847 | Inhibition of cyclin-dependent kinase substrate RNA pol3 phosphorylation at Ser5 in nude BALB/c mouse PBMC at 25 mg/kg, po measured after 6 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604492 | Inhibition of DYRK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604833 | Elimination half life in mouse at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604690 | Inhibition of CDK9-mediated phosphorylation at Ser2 in C-terminal domain of RNA polymerase 2 in human HCT116 cells after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604774 | Antitumor activity against human MCF7 cells xenografted in ip dosed nude BALB/c mouse assessed as decrease in tumor volume measured after 14 days relative to control on day 1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604555 | Inhibition of MST4 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604484 | Inhibition of okadaic acid-activated PLK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604408 | Inhibition of p38-gamma MAPK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604830 | Tmax in mouse at 10 mg/kg, ip | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604695 | Inhibition of CDK6-mediated phosphorylation of RB protein in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1753548 | Inhibition of human CDK2 expressed in baculovirus infected Sf9 cells using Histone H1 as substrate incubated for 10 mins by scintillation counting method | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Mechanistic selectivity investigation and 2D-QSAR study of some new antiproliferative pyrazoles and pyrazolopyridines as potential CDK2 inhibitors. |
| AID604573 | Inhibition of DYRK1A | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604565 | Inhibition of CAMKKbeta at 0.1 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604552 | Inhibition of FGFR1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1609445 | Competitive reversible inhibition of CDK7 (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
| Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID604544 | Inhibition of EFK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604686 | Inhibition of CDK2-mediated phosphorylation of RB at Thr821 in human HCT116 cells after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604478 | Inhibition of PHK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604411 | Inhibition of RSK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604420 | Inhibition of PRK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604644 | Antiproliferative activity against human PC3 cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604925 | Inhibition of cyclin-dependent kinase substrate RB phosphorylation at Ser807/811 in HCT116 xenografted nude BALB/c mouse at 25 mg/kg/day, po measured after 14 days by immunostaining and flow cytometric analysis relative to control | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604760 | Inhibition of CDK7-mediated phosphorylation of RNA pol3 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604424 | Inhibition of MSK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604494 | Inhibition of NEK2a assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604658 | Inhibition of CDK2-mediated phosphorylation of RB at Ser780 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604570 | Inhibition of IRR at 0.1 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604843 | AUC (0 to last) in mouse at 10 mg/kg, iv | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID605638 | Inhibition of CDK9/cyclinT assessed as amount of ATP released by luciferase activity based PKLight assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604545 | Inhibition of HIPK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604821 | Lipophilicity, log D of the compound in n-octanol:PBS at pH 7.4 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604410 | Inhibition of ERK8 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604635 | Ratio of IC50 for CDK1/cyclinB1 to IC50 for ERK8 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604929 | Inhibition of cyclin-dependent kinase substrate RNA pol3 phosphorylation in nude BALB/c mouse PBMC at 75 to 100 mg/kg, po measured after 24 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604409 | Inhibition of p38sigma MAPK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604646 | Antiproliferative activity against human SKOV3 cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604758 | Inhibition of CDK6-mediated phosphorylation of RNA pol3 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604682 | Inhibition of CDK2-mediated phosphorylation of RB at Ser801 in human HCT116 cells after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604401 | Inhibition of MKK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604697 | Inhibition of CDK7-mediated phosphorylation of RB protein in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604638 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604701 | Inhibition of cyclin D1-mediated phosphorylation of RB protein in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604763 | Inhibition of cyclin B-mediated phosphorylation of RNA pol3 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604421 | Inhibition of PKCalpha assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604487 | Inhibition of BRSK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604836 | AUC (0 to last) in mouse at 10 mg/kg, ip | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604575 | Inhibition of ERK2 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604696 | Inhibition of phospho-CDK7-mediated phosphorylation of RB protein in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604688 | Inhibition of CDK1-mediated phosphorylation of PP1a at Thr320 in human HCT116 cells after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604844 | AUC (0 to infinity) in mouse at 10 mg/kg, iv | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604764 | Inhibition of cyclin D1-mediated phosphorylation of RNA pol3 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604407 | Inhibition of P38beta MAPK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604766 | Inhibition of cyclin B in human HCT116 cells assessed as decrease in protein level at 1 umol/L after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604475 | Inhibition of CAMKKbeta assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604641 | Antiproliferative activity against human HCT116 cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604425 | Inhibition of MNK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604415 | Inhibition of PKBbeta assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604822 | Apparent permeability from apical to basolateral side in monkey TC7 cells at 10 umol/L and pH 6.5/7.4 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1609446 | Competitive reversible inhibition of CDK2 (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
| Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID604574 | Inhibition of ERK1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604845 | Inhibition of cyclin-dependent kinase substrate RB phosphorylation at Thr 821 in nude BALB/c mouse PBMC at 25 mg/kg, po measured after 6 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604678 | Inhibition of CDK2-mediated phosphorylation of RB at Ser780 in human HCT116 cells after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604687 | Inhibition of CDK1-mediated phosphorylation of PP1a at Thr320 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1609441 | Competitive reversible inhibition of CDK6 (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
| Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID604413 | Inhibition of PDK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604568 | Inhibition of ERK1 at 0.1 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604849 | Inhibition of cyclin-dependent kinase substrate RNA pol3 phosphorylation in nude BALB/c mouse PBMC at 50 mg/kg, po measured after 6 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID605632 | Inhibition of CDK1/cyclinB1 assessed as amount of ATP released by luciferase activity based PKLight assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604685 | Inhibition of CDK2-mediated phosphorylation of RB at Thr821 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604767 | Inhibition of cyclin D1 in human HCT116 cells assessed as decrease in protein level at 1 umol/L after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID605639 | Ratio of IC50 for roscovitine to compound for CDK2/cyclinE by luciferase activity based PKLight assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604567 | Inhibition of DYRK1A at 0.1 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604648 | Antiproliferative activity against human NCI60 cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604559 | Inhibition of TBK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604684 | Inhibition of CDK2-mediated phosphorylation of RB at Ser807/811 in human HCT116 cells after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604403 | Inhibition of ERK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604692 | Inhibition of phospho-CDK2-mediated phosphorylation of RB protein in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604922 | Antitumor activity against human HCT116 cells xenografted in nude BALB/c mouse assessed as decrease in tumor volume at 25 mg/kg/day, po measured after 14 days relative to control on day 1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604414 | Inhibition of PKBalpha assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604423 | Inhibition of PKD1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604500 | Inhibition of SRPK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604572 | Inhibition of CK1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604558 | Inhibition of IKKepsilon assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604562 | Inhibition of BTK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604553 | Inhibition of IRR assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604647 | Antiproliferative activity against human HUVEC cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604418 | Inhibition of PKA assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604683 | Inhibition of CDK2-mediated phosphorylation of RB at Ser807/811 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604775 | Antitumor activity against human MCF7 cells xenografted in nude BALB/c mouse assessed as decrease in tumor volume at 5 mg/kg, ip bid for 14 days relative to control on day 1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604835 | AUC (0 to last) in mouse at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604405 | Inhibition of JNK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID605634 | Inhibition of CDK4/cyclinD1 assessed as amount of ATP released by luciferase activity based PKLight assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604557 | Inhibition of YES1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604759 | Inhibition of phospho-CDK7-mediated phosphorylation of RNA pol3 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604412 | Inhibition of RSK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604643 | Antiproliferative activity against human Saos2 cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1753546 | Cytotoxicity against human MCF7 cells | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Mechanistic selectivity investigation and 2D-QSAR study of some new antiproliferative pyrazoles and pyrazolopyridines as potential CDK2 inhibitors. |
| AID604416 | Inhibition of SGK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604481 | Inhibition of GSK3-beta assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604548 | Inhibition of PAK6 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604642 | Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604920 | Inhibition of cyclin-dependent kinase substrate RB phosphorylation at Thr 821 in nude BALB/c mouse PBMC at 75 mg/kg, po measured after 24 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604549 | Inhibition of Src assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604757 | Inhibition of CDK4-mediated phosphorylation of RNA pol3 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604496 | Inhibition of IKK-beta assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604485 | Inhibition of AMPK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604654 | Cell cycle arrest in human MCF7 cells assessed as concomitant increase in cells at S phase at 1 to 10 umol/L after 24 hrs by propidium iodide staining based flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604495 | Inhibition of NEK6 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604848 | Inhibition of cyclin-dependent kinase substrate RNA pol3 phosphorylation in nude BALB/c mouse PBMC at 100 mg/kg, po measured after 6 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604402 | Inhibition of ERK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604652 | Cell cycle arrest in human HCT116 cells assessed as concomitant increase in cells at G2/M phase at 1 to 10 umol/L after 24 hrs by propidium iodide staining based flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604680 | Inhibition of CDK2-mediated phosphorylation of RB at Ser795 in human HCT116 cells after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604651 | Cell cycle arrest in human HCT116 cells assessed as concomitant increase in cells at S phase at 1 to 10 umol/L after 24 hrs by propidium iodide staining based flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604640 | Antiproliferative activity against human COLO205 cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604498 | Inhibition of PIM2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604649 | Antiproliferative activity against human NCI60 cells assessed as lethal effect after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604639 | Antiproliferative activity against human MCF10A cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604829 | Tmax in mouse at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID605636 | Inhibition of CDK6/cyclinD1 assessed as amount of ATP released by luciferase activity based PKLight assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604930 | Inhibition of cyclin-dependent kinase substrate RB phosphorylation in nude BALB/c mouse PBMC at 75 to 100 mg/kg, po measured after 24 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604771 | Inhibition of CDK2 in human HCT116 cells assessed as decrease in protein level at 1 umol/L after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604488 | Inhibition of MELK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604489 | Inhibition of CK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604497 | Inhibition of PIM1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604569 | Inhibition of ERK2 at 0.1 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604778 | Toxicity in nude BALB/c mouse assessed as adverse effect on weight at 10 mg/kg, ip bid for 14 days | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604825 | Metabolic stability in human liver microsomes as compound remaining at 1 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604927 | Inhibition of cyclin-dependent kinase substrate RNA pol3 phosphorylation at Ser2 in po dosed nude BALB/c mouse PBMC measured after 6 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604547 | Inhibition of PAK5 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604490 | Inhibition of CK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604474 | Inhibition of PRAK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1753547 | Cytotoxicity against human HepG2 cells | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Mechanistic selectivity investigation and 2D-QSAR study of some new antiproliferative pyrazoles and pyrazolopyridines as potential CDK2 inhibitors. |
| AID604404 | Inhibition of JNK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID605637 | Inhibition of CDK7/cyclinH/MAT1 assessed as amount of ATP released by luciferase activity based PKLight assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1609442 | Competitive reversible inhibition of CDK8 (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
| Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID604828 | Bioavailability in mouse at 10 mg/kg, ip | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604765 | Inhibition of cyclin A in human HCT116 cells assessed as decrease in protein level at 1 umol/L after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604483 | Inhibition of PLK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604773 | Inhibition of CDK2 phosphorylation at Thr170 in human HCT116 cells after 24 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604576 | Inhibition of IRR | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604679 | Inhibition of CDK2-mediated phosphorylation of RB at Ser795 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604645 | Antiproliferative activity against human HepG2 cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604482 | Inhibition of CDK2/cyclin A assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604846 | Inhibition of cyclin-dependent kinase substrate RNA pol3 phosphorylation at Ser2 in nude BALB/c mouse PBMC at 25 mg/kg, po measured after 6 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604694 | Inhibition of CDK4-mediated phosphorylation of RB protein in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604841 | Apparent volume of distribution in mouse at 10 mg/kg, iv | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604473 | Inhibition of MAPKAPK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604426 | Inhibition of MNK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604826 | Metabolic stability in mouse liver microsomes as compound remaining at 1 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604563 | Inhibition of Histidine tagged-IR assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604422 | Inhibition of PKCzeta assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID605633 | Inhibition of CDK2/cyclinE assessed as amount of ATP released by luciferase activity based PKLight assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604551 | Inhibition of CSK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604834 | Elimination half life in mouse at 10 mg/kg, ip | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604842 | Volume of distribution at steady state in mouse at 10 mg/kg, iv | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID605635 | Inhibition of CDK5/cyclinT assessed as amount of ATP released by luciferase activity based PKLight assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604550 | Inhibition of Lck assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604923 | Toxicity in nude BALB/c mouse assessed as adverse effect on weight at 25 mg/kg/day, po for 14 days | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604491 | Inhibition of DYRK1A assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604633 | Inhibition of ERK8 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604924 | Inhibition of cyclin-dependent kinase substrate RB phosphorylation at Thr 821 in HCT116 xenografted nude BALB/c mouse at 25 mg/kg/day, po measured after 14 days by immunostaining and flow cytometric analysis relative to control | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604699 | Inhibition of cyclin A-mediated phosphorylation of RB protein in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604698 | Inhibition of CDK9-mediated phosphorylation of RB protein in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604921 | Antitumor activity against human HCT116 cells xenografted in po dosed nude BALB/c mouse assessed as decrease in tumor volume measured after 14 days relative to control on day 1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604493 | Inhibition of DYRK3 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604560 | Inhibition of IGF1R assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604480 | Inhibition of CHK2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604554 | Inhibition of EPH A2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604406 | Inhibition of p38alpha MAPK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604564 | Inhibition of EPHB3 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604656 | Induction of apoptosis in human HCT116 cells assessed as increase in sub-G1 population at 1 to 10 umol/L after 24 hrs by annexin V staining based flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604653 | Cell cycle arrest in human MCF7 cells assessed as reduction in cells at G1 phase at 1 to 10 umol/L after 24 hrs by propidium iodide staining based flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604926 | Decrease in RB protein level in HCT116 xenografted nude BALB/c mouse at 25 mg/kg/day, po measured after 14 days by immunostaining and flow cytometric analysis relative to control | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604546 | Inhibition of PAK4 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604566 | Inhibition of CK1 at 0.1 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604499 | Inhibition of PIM3 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604632 | Inhibition of ERK8 at 10 umol/L | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604776 | Antitumor activity against human MCF7 cells xenografted in nude BALB/c mouse assessed as decrease in tumor volume at 10 mg/kg, ip bid for 14 days relative to control on day 1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604832 | Cmax in mouse at 10 mg/kg, ip | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1609443 | Competitive reversible inhibition of CDK4 (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
| Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID604838 | AUC (0 to infinity) in mouse at 10 mg/kg, ip | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604837 | AUC (0 to infinity) in mouse at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604486 | Inhibition of MARK3 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604637 | Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604419 | Inhibition of ROCK 2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604702 | Inhibition of CDK1-mediated phosphorylation of RNA pol3 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604571 | Inhibition of CAMKKbeta | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604831 | Cmax in mouse at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604561 | Inhibition of VEGFR assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604636 | Ratio of IC50 for CDK5/cyclinT to IC50 for ERK8 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604655 | Cell cycle arrest in human MCF7 cells assessed as concomitant increase in cells at G2/M phase at 1 to 10 umol/L after 24 hrs by propidium iodide staining based flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604824 | Plasma protein binding in mouse at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604928 | Inhibition of cyclin-dependent kinase substrate RNA pol3 phosphorylation at Ser2 in nude BALB/c mouse PBMC at 50 to 100 mg/kg, po measured after 6 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604689 | Inhibition of CDK9-mediated phosphorylation at Ser2 in C-terminal domain of RNA polymerase 2 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604681 | Inhibition of CDK2-mediated phosphorylation of RB at Ser801 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID1609444 | Competitive reversible inhibition of CDK5 (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
| Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID604479 | Inhibition of CHK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604851 | Inhibition of cyclin-dependent kinase substrate RNA pol3 phosphorylation in nude BALB/c mouse PBMC at 50 mg/kg, po measured after 24 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604657 | Induction of apoptosis in human MCF7 cells assessed as increase in sub-G1 population at 1 to 10 umol/L after 24 hrs by annexin V staining based flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604691 | Inhibition of CDK1-mediated phosphorylation of RB protein in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604476 | Inhibition of CAMK1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604779 | Aqueous solubility of the compound in PBS as pH 7.4 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604417 | Inhibition of S6K1 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604477 | Inhibition of Smooth muscle MLCK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604761 | Inhibition of CDK9-mediated phosphorylation of RNA pol3 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604762 | Inhibition of cyclin A-mediated phosphorylation of RNA pol3 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604501 | Inhibition of MST2 assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604756 | Inhibition of CDK2-mediated phosphorylation of RNA pol3 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604850 | Inhibition of cyclin-dependent kinase substrate RB phosphorylation at Thr 821 in nude BALB/c mouse PBMC at 50 mg/kg, po measured after 24 hrs by immunostaining and flow cytometric analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604556 | Inhibition of SYK assessed as residual enzyme activity at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604700 | Inhibition of cyclin B-mediated phosphorylation of RB protein in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604840 | Clearance in mouse at 10 mg/kg, iv | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604634 | Ratio of IC50 for CDK2/cyclinE to IC50 for ERK8 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604755 | Inhibition of phospho-CDK2-mediated phosphorylation of RNA pol3 in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604827 | Oral bioavailability in mouse at 10 mg/kg | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604823 | Plasma protein binding in human at 10 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID604693 | Inhibition of CDK2-mediated phosphorylation of RB protein in human HCT116 cells after 4 hrs by immunoblotting analysis | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
| A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |