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Inhibitory Activity Against KHK In Vitro from US Patent US20240067633: "KETOHEXOKINASE INHIBITOR AND USE THEREOF"
Assay data:9 Active, 9 Activity ≤ 1 µM, 9 Tested
SummaryRelated BioAssays by Target
Glosensor cAMP assay from US Patent US20240059655: "HETEROCYCLIC G-PROTEIN-COUPLED RECEPTOR 52 (GPR52) AGONISTS"
Assay data:69 Active, 62 Activity ≤ 1 µM, 69 Tested
cell-based NF-kB reporter assay from US Patent US11905258: "2-aminoaryl-5-aryloxazole analogs for the treatment of neurodegenerative diseases"
Assay data:29 Active, 10 Activity ≤ 1 µM, 36 Tested
DHODH Kinetic Analysis from US Patent US11903936: "Anti-malarial agents"
Assay data:13 Active, 13 Activity ≤ 1 µM, 13 Tested
Human P2X7 Channel Calcium-Influx Assay from US Patent US20240034737: "Heterocyclic Derivatives as P2X7 Receptor Antagonists"
Assay data:103 Active, 103 Activity ≤ 1 µM, 103 Tested
Antitumor activity against mouse MC38 tumor model administered as monotherapy
Assay data:1 Active, 1 Tested
Summary
[3H] 2-OG cleavage activity assay (mouse brain)
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Mouse GCS enzymatic assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
Interleukin IL-1 Eurofins Panlabs panel
Assay data:1 Tested
Nitric Oxide Synthetase, Inducible (iNOS) Eurofins Panlabs panel
Cellular PDE9A assay
Inhibition of M-1 water resorption
Enzymatic assay (mHSD17B13)
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 2 Tested
Antihypercholesterolemic activity against hApoB100/hCETP-dTg hypercholesterolemic mouse model assessed as serum non-HDL-C level at 3 mg/kg, po administered once daily for 8 days
Assay data:5 Tested
Antihypercholesterolemic activity against hApoB100/hCETP-dTg hypercholesterolemic mouse model assessed as serum total cholesterol level at 3 mg/kg, po administered once daily for 8 days
Antihypercholesterolemic activity against hApoB100/hCETP-dTg hypercholesterolemic mouse model assessed as serum HDL-C level at 3 mg/kg, po administered once daily for 8 days
Selectivity ratio of EC50 for agonist activity at Gal4-fused mouse PPAR-gamma ligand binding domain expressed in CHO-K1 cells to EC50 for agonist activity at Gal4-fused mouse PPAR-delta ligand binding domain expressed in CHO-K1 cells
Assay data:23 Tested
Agonist activity at Gal4-fused mouse PPAR-gamma ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay relative to control
Agonist activity at Gal4-fused mouse PPAR-gamma ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay
Assay data:20 Active, 14 Activity ≤ 1 µM, 23 Tested
Selectivity ratio of EC50 for agonist activity at Gal4-fused mouse PPAR-alpha ligand binding domain expressed in CHO-K1 cells to EC50 for agonist activity at Gal4-fused mouse PPAR-delta ligand binding domain expressed in CHO-K1 cells
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