| Assay ID | Title | Year | Journal | Article |
|---|
| AID1162883 | Thermodynamic solubility of the compound at pH 6.5 | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162877 | Volume of distribution at steady state in rat at 1 mg/kg, iv or 5 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162852 | Permeability from basolateral to apical side in MDCK cells | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162856 | Protein binding in mouse plasma | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162879 | Oral bioavailability in rat at 5 mg/kg | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162878 | Dose normalized AUC in rat at 5 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162850 | Free clearance in rat at 1 mg/kg, iv or 5 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162865 | Inhibition of CYP2C19 (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162875 | Total clearance in rat at 1 mg/kg, iv or 5 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162872 | Hepatic clearance in mouse liver microsomes | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162851 | Permeability from apical to basolateral side in MDCK cells | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162870 | Hepatic clearance in human liver microsomes | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162881 | Inhibition of human ERG by patch clamp assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162862 | Antiproliferative activity against human A375 cells assessed as inhibition of cell proliferation after 72 hrs | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162873 | Hepatic clearance in dog liver microsomes | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162855 | Protein binding in rat plasma | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162854 | Protein binding in human plasma | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162871 | Hepatic clearance in rat liver microsomes | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162853 | Efflux ratio in MDCK cells | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162864 | Inhibition of CYP2C9 (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162863 | Lipophilicity, logD of the compound at pH 7.4 | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162866 | Inhibition of CYP3A4 (unknown origin) using midazolam substrate | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162882 | Dissociation constant, pKa of the compound by Sirius based assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162868 | Inhibition of CYP2D6 (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162867 | Inhibition of CYP3A4 (unknown origin) using testosterone substrate | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162876 | Half life in rat at 1 mg/kg, iv or 5 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162869 | Inhibition of CYP1A2 (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162858 | Drug metabolism rat plasma assessed as metabolite formation at 5 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162857 | Stability in rat plasma at 5 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162861 | Antiproliferative activity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| AID1162874 | Hepatic clearance in cynomolgus monkey liver microsomes | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
| Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. |
| 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. |
| 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. |
| AID1345759 | Human mitogen-activated protein kinase kinase 1 (STE7 family) | 2013 | Nature, Sep-12, Volume: 501, Issue:7466
| Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |