BS-181: a CDK7 inhibitor with antineoplastic activity [MeSH]
N5-(6-aminohexyl)-N7-(phenylmethyl)-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine : no description available [CHeBI]
| ID Source | ID |
|---|---|
| PubMed CID | 49867929 |
| CHEMBL ID | 1801932 |
| SCHEMBL ID | 10123390 |
| CHEBI ID | 95059 |
| MeSH ID | M000599671 |
| Synonym |
|---|
| HY-13266 |
| bs-181 |
| CHEMBL1801932 , |
| bs181 |
| bs 181 |
| bdbm50347389 |
| 1092443-52-1 |
| NCGC00346553-01 |
| CS-0490 |
| unii-75m620llbn |
| pyrazolo(1,5-a)pyrimidine-5,7-diamine, n5-(6-aminohexyl)-3-(1-methylethyl)-n7-(phenylmethyl)- |
| 75m620llbn , |
| SCHEMBL10123390 |
| n5-(6-aminohexyl)-n7-benzyl-3-isopropylpyrazolo[1,5-a]pyrimidine-5,7-diamine |
| gtpl9405 |
| 5-n-(6-aminohexyl)-7-n-benzyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine |
| J-523430 |
| AKOS026750277 |
| EX-A585 |
| CHEBI:95059 |
| n5-(6-aminohexyl)-3-(1-methylethyl)-n7-(phenylmethyl)pyrazolo[1,5-a]pyrimidine-5,7-diamine |
| mfcd22056527 |
| bs-181 free base |
| Q27166830 |
| BCP02853 |
| HMS3744E07 |
| A906301 |
| MS-26234 |
| DTXSID101025664 |
| n5-(6-aminohexyl)-3-(1-methylethyl)-n7-(phenylmethyl)-pyrazolo(1,5-a)pyrimidine-5,7-diamine |
| Class | Description |
|---|---|
| pyrazolopyrimidine |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Fumarate hydratase | Homo sapiens (human) | Potency | 33.1734 | AID1347053 |
| PPM1D protein | Homo sapiens (human) | Potency | 26.2123 | AID1347411 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 10.0674 | AID1259252; AID1259253; AID1259255; AID1259256 |
| polyprotein | Zika virus | Potency | 33.1734 | AID1347053 |
| Interferon beta | Homo sapiens (human) | Potency | 26.2123 | AID1347411 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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 ISSN: 1554-8937 | 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 ISSN: 1554-8937 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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 ISSN: 1949-2553 | 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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: 173ISSN: 1872-9096 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 ISSN: 2472-5560 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| 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 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | 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 ISSN: 2211-1247 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | 2022 | The Journal of biological chemistry, 08, Volume: 298, Issue:8 ISSN: 1083-351X | |
| 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 ISSN: 1949-2553 | 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: 173ISSN: 1872-9096 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| 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 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | 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: 173ISSN: 1872-9096 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| 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 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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 ISSN: 1949-2553 | 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 ISSN: 1949-2553 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID604399 | Ratio of IC50 for CDK5/cyclinT to IC50 for CDK7/cyclinH/MAT1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24 ISSN: 1520-4804 | 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. |
| AID1651617 | Inhibition of CDK9 (unknown origin) | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 ISSN: 1520-4804 | CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success? |
| AID1283430 | Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110ISSN: 1768-3254 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
| AID1771855 | Growth inhibition of human BT-549 cells assessed as cell viability measured after 4 days by WST8 assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 ISSN: 1520-4804 | Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer. |
| AID1609445 | Competitive reversible inhibition of CDK7 (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20 ISSN: 1464-3405 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID1651613 | Inhibition of CDK2 (unknown origin) | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 ISSN: 1520-4804 | CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success? |
| AID1283431 | Inhibition of CDK1 (unknown origin) | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110ISSN: 1768-3254 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
| AID1283433 | Inhibition of CDK5 (unknown origin) using histone H1 as substrate in presence of [gamma33P]-ATP | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110ISSN: 1768-3254 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
| AID1283446 | Inhibition of CDK7 (unknown origin) | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110ISSN: 1768-3254 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
| AID1651608 | Inhibition of CDK7 (unknown origin) | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 ISSN: 1520-4804 | CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success? |
| AID1651614 | Inhibition of CDK4 (unknown origin) | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 ISSN: 1520-4804 | CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success? |
| AID604398 | Ratio of IC50 for CDK4/cyclinD1 to IC50 for CDK7/cyclinH/MAT1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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. |
| AID1283429 | Inhibition of CDK4 (unknown origin) | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110ISSN: 1768-3254 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
| AID1277156 | Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108ISSN: 1768-3254 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
| AID1651612 | Inhibition of CDK1 (unknown origin) | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 ISSN: 1520-4804 | CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success? |
| AID1609444 | Competitive reversible inhibition of CDK5 (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20 ISSN: 1464-3405 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID1277161 | Inhibition of CDK9/Cyclin T1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108ISSN: 1768-3254 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
| AID1771856 | Growth inhibition of human MDA-MB-231 cells assessed as cell viability measured after 4 days by WST8 assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 ISSN: 1520-4804 | Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer. |
| AID1283447 | Inhibition of CDK9 (unknown origin) | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110ISSN: 1768-3254 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
| AID604400 | Ratio of IC50 for CDK6/cyclinD1 to IC50 for CDK7/cyclinH/MAT1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24 ISSN: 1520-4804 | 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. |
| AID1771854 | Growth inhibition of human MDA-MB-468 cells assessed as cell viability measured after 4 days by WST8 assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 ISSN: 1520-4804 | Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer. |
| AID1277160 | Inhibition of CDK7/Cyclin H/MAT1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108ISSN: 1768-3254 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
| AID1651615 | Inhibition of CDK5 (unknown origin) | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 ISSN: 1520-4804 | CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success? |
| AID1609441 | Competitive reversible inhibition of CDK6 (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20 ISSN: 1464-3405 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID605641 | Ratio of IC50 for CDK2/cyclinE to IC50 for CDK7/cyclinH/MAT1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24 ISSN: 1520-4804 | 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 ISSN: 1464-3405 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID1277158 | Inhibition of CDK4/Cyclin D1 (unknown origin) using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]ATP | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108ISSN: 1768-3254 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
| AID1609442 | Competitive reversible inhibition of CDK8 (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20 ISSN: 1464-3405 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID1277159 | Inhibition of CDK5/p35NCK (unknown origin) using histone H1 as substrate in presence of [gamma-33P]ATP | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108ISSN: 1768-3254 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
| AID1651616 | Inhibition of CDK6 (unknown origin) | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 ISSN: 1520-4804 | CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success? |
| AID605640 | Ratio of IC50 for CDK1/cyclinB1 to IC50 for CDK7/cyclinH/MAT1 | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24 ISSN: 1520-4804 | 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 ISSN: 1464-3405 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). |
| AID1345612 | Human cyclin dependent kinase 2 (CDK1 subfamily) | 2009 | Cancer research, Aug-01, Volume: 69, Issue:15 ISSN: 1538-7445 | The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. |
| AID1345652 | Human cyclin dependent kinase 7 (CDK7 subfamily) | 2009 | Cancer research, Aug-01, Volume: 69, Issue:15 ISSN: 1538-7445 | The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (5.00) | 29.6817 |
| 2010's | 11 (55.00) | 24.3611 |
| 2020's | 8 (40.00) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (10.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 18 (90.00%) | 84.16% |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| oxazoles | 1,3-oxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | ||
| thiazoles | 1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | ||
| cyc 202 | 2,6-diaminopurines | antiviral drug; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| bms 387032 | 1,3-oxazoles; 1,3-thiazoles; organic sulfide; piperidinecarboxamide; secondary carboxamide | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| ldc4297 | aromatic ether; piperidines; pyrazoles; pyrazolotriazine; secondary amino compound | antineoplastic agent; antiviral agent; apoptosis inducer; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 2014 | 2014 | 10.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Adjuvant Arthritis | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Arthritis, Rheumatoid | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Benign Neoplasms | 0 | 2014 | 2020 | 7.3 | medium | 0 | 0 | 0 | 0 | 3 | 0 | |
| Breast Cancer | 0 | 2009 | 2019 | 10.0 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
| Breast Neoplasms | 0 | 2009 | 2019 | 10.0 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
| Cancer of Stomach | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Disease Models, Animal | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| ER-Negative PR-Negative HER2-Negative Breast Cancer | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Experimental Neoplasms | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Inflammation | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Innate Inflammatory Response | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Neoplasms | 0 | 2014 | 2020 | 7.3 | medium | 0 | 0 | 0 | 0 | 3 | 0 | |
| Neuroblastoma | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Rheumatoid Arthritis | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Stomach Neoplasms | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Triple Negative Breast Neoplasms | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Article | Year |
|---|---|
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology, , Volume: 96, Issue:5 | 2019 |
| 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. Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24 | 2010 |
| Article | Year |
|---|---|
| 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. Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24 | 2010 |