| Assay ID | Title | Year | Journal | Article |
|---|
| AID1857478 | Microsomal stability in rat liver microsomes assessed as intrinsic clearance at 4 uM incubated for 30 mins in presence of NADPH by LCMS/MS analysis | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1857480 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv by LCMS/MS analysis | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1242478 | Inhibition of full length PAK4 (unknown origin) 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. |
| AID1857476 | Inhibition of LIMK1/LIMK2 in human SH-SY5Y cells assessed as effect on phospho cofilin serine 3 phosphorylation incubated for 2 hr by AlphaLISA SureFire assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1242476 | Inhibition of full length PAK2 (unknown origin) 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. |
| AID1857477 | Aqueous solubility of the compound at pH 7 | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1857483 | Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv by LCMS/MS analysis | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1857475 | Inhibition of recombinant LIMK2(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1857472 | Inhibition of PAK mediated recombinant LIMK1 phosphorylation (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1857486 | Half life in Sprague-Dawley rat at 1 mg/kg, iv by LCMS/MS analysis | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1242475 | Inhibition of full length PAK1 (unknown origin) 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. |
| AID1857470 | Inhibition of recombinant LIMK1 (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1857474 | Inhibition of recombinant LIMK1(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1242477 | Inhibition of full length PAK3 (unknown origin) 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. |
| AID1857471 | Inhibition of recombinant LIMK2 (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| 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. |
| AID1857473 | Inhibition of PAK mediated recombinant LIMK2 phosphorylation (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1857489 | Brain to plasma ratio in Sprague-Dawley rat by LCMS/MS analysis | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
| AID1857479 | Microsomal stability in human liver microsomes assessed as intrinsic clearance at 4 uM incubated for 30 mins in presence of NADPH by LCMS/MS analysis | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular 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
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1345729 | Human p21 (RAC1) activated kinase 4 (PAKB subfamily) | 2013 | Proceedings of the National Academy of Sciences of the United States of America, Apr-02, Volume: 110, Issue:14
| Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. |
| AID1345767 | Human p21 (RAC1) activated kinase 3 (PAKA subfamily) | 2013 | Proceedings of the National Academy of Sciences of the United States of America, Apr-02, Volume: 110, Issue:14
| Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. |
| AID1345761 | Human p21 (RAC1) activated kinase 1 (PAKA subfamily) | 2013 | Proceedings of the National Academy of Sciences of the United States of America, Apr-02, Volume: 110, Issue:14
| Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. |
| AID1345771 | Human p21 (RAC1) activated kinase 2 (PAKA subfamily) | 2013 | Proceedings of the National Academy of Sciences of the United States of America, Apr-02, Volume: 110, Issue:14
| Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |