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Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
Assay data:2 Activity ≤ 1 µM, 4307 Tested
SummaryCompounds, activity ≤ 1 µM
Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status
Assay data:929 Tested
SummaryPubMed Citation
Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index
Induction of stimulus generalization in Sprague-Dawley rat trained to discriminate S(-)MCAT assessed as appropriate responding level to training drug by two lever method
Assay data:5 Tested
Induction of stimulus generalization in Sprague-Dawley rat trained to discriminate S(+)AMPH assessed as appropriate responding level to training drug by two lever method
Induction of stimulus generalization in rat trained to discriminate S(+)methamphetamine assessed as appropriate responding level to training drug by two lever method
Assay data:6 Tested
Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis
Assay data:57 Active, 48 Activity ≤ 1 µM, 86 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay
Assay data:40 Active, 9 Activity ≤ 1 µM, 86 Tested
Ratio of Ki for displacement of [3H]DTBZ from VMAT2 in rat whole brain to Ki for inhibition of VMAT2-mediated [3H]DA uptake in rat brain synaptic vesicles
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of VMAT2-mediated [3H]DA uptake in rat brain synaptic vesicles by liquid scintillation spectrometry
Assay data:6 Active, 5 Activity ≤ 1 µM, 6 Tested
Displacement of [3H]DTBZ from VMAT2 in rat whole brain by liquid scintillation spectrometry
Assay data:5 Active, 5 Activity ≤ 1 µM, 6 Tested
Drug level in Homo sapiens (human) whole blood assessed as retention time by UPLC-TOF-MS analysis
Assay data:175 Tested
Summary
Selectivity ratio of EC50 for rat TAAR1 transmembrane domain 6 Met268(6.55)Thr mutant to EC50 for rat wild type TAAR1
Assay data:4 Tested
Activation of rat TAAR1 Asp102(3.32)Ala mutant expressed in HEK293 cells assessed as stimulation of cAMP production at 0.0001 to 100 uM after 1 hr by chemiluminescent assay relative to control
Activation of mouse TAAR1 Asp102(3.32)Ala mutant expressed in HEK293 cells assessed as stimulation of cAMP production at 0.0001 to 100 uM after 1 hr by chemiluminescent assay
Activation of rat wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
Activation of mouse wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay
Activation of rat TAAR1 transmembrane domain 6 Met268(6.55)Thr mutant expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay
Assay data:5 Active, 3 Activity ≤ 1 µM, 5 Tested
Activation of mouse TAAR1 transmembrane domain 6 Thr268(6.55)Met mutant expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay
Activation of rat TAAR1 transmembrane domain 7 Asn287(7.39)Tyr mutant expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay
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