| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| 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. |
| 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. |
| 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. |
| AID1737268 | Inhibition of PAK1 in human MDA-MB-231 cells assessed as reduction in MAPK-ERK signaling measured after 24 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. |
| AID1242474 | Inhibition of recombinant human PAK4 by Z'-LYTE assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
| Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. |
| AID1721849 | Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
| Design, synthesis and biological evaluation of 2-indolinone derivatives as PAK1 inhibitors in MDA-MB-231 cells. |
| AID1326058 | Selectivity ratio of IC50 for FGFR1 (unknown origin) to IC50 for PAK1 (unknown origin) | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. |
| AID1737266 | Inhibition of PAK1 phosphorylation at Ser199 residues in human MDA-MB-231 cells at 2.5 to 10 uM measured after 24 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. |
| AID1737274 | Inhibition of PAK1 in human MDA-MB-231 cells assessed as reduction in c-Raf phosphorylation at Ser259 residues at 2.5 to 10 uM measured after 24 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. |
| AID1326062 | Distribution coefficient, logD of the compound | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. |
| AID1721848 | Inhibition of PAK1 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
| Design, synthesis and biological evaluation of 2-indolinone derivatives as PAK1 inhibitors in MDA-MB-231 cells. |
| AID1737273 | Inhibition of PAK1 in human MDA-MB-231 cells assessed as reduction in ERK expression at 2.5 to 10 uM measured after 24 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. |
| AID1326059 | Selectivity ratio of IC50 for KDR (unknown origin) to IC50 for PAK1 (unknown origin) | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. |
| AID1737259 | Inhibition of PAK1 (unknown origin) using lipid substrate measured after 40 mins by ADP-glo kinase assay | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. |
| AID1424468 | Inhibition of GST-tagged recombinant human PAK1 by Z'-LYTE functional biochemical assay | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | From bench (laboratory) to bed (hospital/home): How to explore effective natural and synthetic PAK1-blockers/longevity-promoters for cancer therapy. |
| AID1242471 | Inhibition of recombinant human PAK1 by Z'-LYTE assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
| Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. |
| AID1737275 | Inhibition of PAK1 in human MDA-MB-231 cells assessed as reduction in MEK1/2 phosphorylation at ser217/221 residues at 2.5 to 10 uM measured after 24 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. |
| AID1737263 | Down regulation of PAK1 expression in human MDA-MB-231 cells at 5 uM measured after 24 hrs by immunofluorescence analysis | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. |
| AID1242473 | Inhibition of recombinant human PAK3 by Z'-LYTE assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
| Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. |
| AID1737276 | Inhibition of PAK1 in human MDA-MB-231 cells assessed as reduction in ERK1/2 phosphorylation at Thr202/Tyr204 residues at 2.5 to 10 uM measured after 24 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. |
| AID1737261 | Inhibition of PAK3 (unknown origin) using lipid substrate measured after 40 mins by ADP-glo kinase assay | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. |
| AID1326055 | Inhibition of PAK1 phosphorylation in human MCF10A cells | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. |
| AID1737260 | Inhibition of PAK2 (unknown origin) using lipid substrate measured after 40 mins by ADP-glo kinase assay | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. |
| AID1326054 | Inhibition of PAK1 (unknown origin) by ATP-kinaseGlo assay | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. |
| AID1737267 | Inhibition of PAK1 phosphorylation at Thr212 residues in human MDA-MB-231 cells at 2.5 to 10 uM measured after 24 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. |
| AID1326060 | Selectivity ratio of IC50 for PAK4 (unknown origin) to IC50 for PAK1 (unknown origin) | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. |
| AID1326061 | Selectivity ratio of IC50 for SRC (unknown origin) to IC50 for PAK1 (unknown origin) | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. |
| AID1242472 | Inhibition of recombinant human PAK2 by Z'-LYTE assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
| Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. |
| AID1802401 | Z'-LYTEBiochemical Assay from Article 10.1074/jbc.M113.510933: \\FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas.\\ | 2013 | The Journal of biological chemistry, Oct-04, Volume: 288, Issue:40
| FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. |
| AID1345771 | Human p21 (RAC1) activated kinase 2 (PAKA subfamily) | 2013 | The Journal of biological chemistry, Oct-04, Volume: 288, Issue:40
| FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. |
| AID1345767 | Human p21 (RAC1) activated kinase 3 (PAKA subfamily) | 2013 | The Journal of biological chemistry, Oct-04, Volume: 288, Issue:40
| FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. |
| AID1345729 | Human p21 (RAC1) activated kinase 4 (PAKB subfamily) | 2013 | The Journal of biological chemistry, Oct-04, Volume: 288, Issue:40
| FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. |
| AID1345761 | Human p21 (RAC1) activated kinase 1 (PAKA subfamily) | 2013 | The Journal of biological chemistry, Oct-04, Volume: 288, Issue:40
| FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |