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Cytochrome P450 Family 3 Subfamily A Member 4 (CYP3A4) small molecule antagonists: luciferase reporter qHTS assay
Assay data:1792 Active, 248 Activity ≤ 1 µM, 9667 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Cytochrome P450 Family 2 Subfamily C Member 19 (CYP2C19) small molecule antagonists: luciferase reporter qHTS assay
Assay data:3508 Active, 4 Activity ≤ 1 nM, 319 Activity ≤ 1 µM, 9667 Tested
Maximum serum concentration in human at 500 mg, po
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: luciferase cell-based qHTS assay
Assay data:2147 Active, 1 Activity ≤ 1 nM, 377 Activity ≤ 1 µM, 5242 Tested
Displacement of [3H]FMZ from GABA-A receptor in rat brain assessed as Kd of [3H]-FMZ at 10 uM after 30 mins by autoradiography (Rvb = 0.66 +/- 0.12 nM)
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of LPS-stimulated TNFalpha production in human neutrophils at 50 uM after 24 hrs by ELISA
Assay data:2 Active, 2 Tested
Inhibition of LPS-stimulated IL-8 production in human neutrophils at 2.5 uM after 24 hrs by ELISA
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
Assay data:41 Active, 10 Activity ≤ 1 µM, 24161 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µM
Pharmacokinetic parameters for Clarithromycin evaluated after single oral administration of 1000 or 2 x 500 mg Clarithromycin extended-release tablets to 34 adult volunteers under fasting and feeding conditions.
SummaryCompounds, Active
Evaluation of pharmacokinetic parameters for Clarithromycin following multiple oral doses of Clarithromycin tablets.
pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells
Assay data:63 Active, 10 Activity ≤ 1 µM, 66 Tested
pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells
Assay data:64 Active, 21 Activity ≤ 1 µM, 67 Tested
TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
Assay data:14 Active, 2 Activity ≤ 1 µM, 24 Tested
TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
Assay data:14 Active, 1 Activity ≤ 1 µM, 27 Tested
A screen for compounds that inhibit the activity of LtaS in Staphylococcus aureus
Assay data:902 Active, 168808 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis
Assay data:105 Active, 107 Tested
Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins
Assay data:160 Active, 221 Tested
Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins
Assay data:141 Active, 221 Tested
Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins
Assay data:163 Active, 221 Tested
Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins
Assay data:162 Active, 221 Tested
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