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Selectivity for human corpus cavernosum PDE5 over canine retina PDE6
Assay data:9 Tested
SummaryPubMed Citation
In Vitro Electrophysiological Analysis of the Human TASK-1 and TASK-3 Channels Via Two-Electrode Voltage Clamp Technique in Xenopus laevis Oocytes from US Patent US11208422: "Substituted bridged diazepane derivatives and use thereof as TASK-1 and TASK-3 inhibitors"
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
In Vitro Electrophysiological Assay from US Patent US11098063: "Diazabicyclic substituted imidazopyrimidines and their use for the treatment of breathing disorders"
Assay data:92 Active, 38 Activity ≤ 1 µM, 113 Tested
Inhibition of human INSR phosphorylation over expressed in CHOT cells after 60 mins by immunoblotting
Assay data:8 Active, 1 Activity ≤ 1 µM, 8 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human IGF1R phosphorylation expressed in IGF-1-stimulated knockout mouse R+ cells treated 30 mins before IGF-1 stimulation measured after 20 mins by immunoblotting
Assay data:7 Active, 1 Activity ≤ 1 µM, 8 Tested
Inhibition of human KDR phosphorylation expressed in VEGF-stimulated HUVEC treated 90 mins before VEGF stimulation measured after 5 mins by ELISA
Assay data:5 Active, 1 Activity ≤ 1 µM, 8 Tested
Inhibition of human FGFR1 phosphorylation expressed in COS1 cells after 1 hr by immunoblotting
Assay data:8 Active, 6 Activity ≤ 1 µM, 8 Tested
Inhibition of recombinant N terminal His6-tagged human IGF1R (959 to end) expressed in baculovirus infected Sf21 cells after 80 mins by caliper mobility shift assay
Assay data:17 Active, 3 Activity ≤ 1 µM, 30 Tested
Inhibition of recombinant N terminal GST-tagged human KDR (805 to 1356) expressed in baculovirus infected Sf9 cells after 90 mins by caliper mobility shift assay
Assay data:28 Active, 20 Activity ≤ 1 µM, 30 Tested
Inhibition of recombinant N terminal GST-tagged human FGFR1 (456 to 765) expressed in baculovirus infected Sf21 cells after 40 mins by caliper mobility shift assay
Assay data:30 Active, 29 Activity ≤ 1 µM, 30 Tested
Inhibition of canine retina PDE6 by scintillation proximity assay
Assay data:5 Active, 1 Activity ≤ 1 µM, 5 Tested
Inhibition of human corpus cavernosum PDE5 by scintillation proximity assay
Assay data:14 Active, 2 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 14 Tested
Inhibition constants against Met (L-methionine)P substrate site of M-T (Novikoff Ascitic Hepatoma form) variant of rat Methionine adenosyltransferase
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition constants against ATP substrate site of M-T (Novikoff Ascitic Hepatoma form) variant of rat Methionine adenosyltransferase
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
Inhibition constants against ATP substrate site of M-2 (kidney form) variant of rat Methionine adenosyltransferase
Ratio of permeability from apical to basolateral side over basolateral to apical side in human Caco-2 cells
Assay data:2 Tested
Permeability across human Caco-2 cells
Distribution coefficient, log D of the compound
Antidiabetic activity in rat hemidiaphragm assessed as glucose uptake at 2 mg after 45 mins in absence of insulin
Assay data:20 Tested
Immunostimulatory activity in C57BL/6 mouse assessed as maximum IL4 level in serum at 10 ug/ml, iv after 4 hrs by ELISA
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed Citation
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