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Cytochrome P450 family 3 subfamily A member 7 (CYP3A7) small molecule antagonists: luciferase cell-based qHTS assay
Assay data:2481 Active, 355 Activity ≤ 1 µM, 5246 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Depositor
Binding affinity towards human HRH3 in an in vitro assay with cellular components measured by scintillation counting
Assay data:41 Active, 7 Activity ≤ 1 µM, 993 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Compound was evaluated for inhibition of human KDR in an in vitro cell free assay measured by time-resolved fluorescence resonance energy transfer method
Assay data:12 Active, 3 Activity ≤ 1 nM, 7 Activity ≤ 1 µM, 101 Tested
Compound was evaluated for inhibition of human KCNH2 in an in vitro assay with cellular components measured by membrane filtration, radioactivity method
Assay data:353 Active, 116 Activity ≤ 1 µM, 1804 Tested
Compound was evaluated for inhibition of human ERBB2 in an in vitro cell free assay measured by Caliper microfluidic capillary electrophoresis, time-resolved fluorescence resonance energy transfer method
Assay data:6 Active, 5 Activity ≤ 1 µM, 83 Tested
Compound was evaluated for inhibition of human EGFR in an in vitro cell free assay measured by Caliper microfluidic capillary electrophoresis, time-resolved fluorescence resonance energy transfer method
Assay data:11 Active, 1 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 86 Tested
Anticancer activity against human HeLa cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Assay data:4 Active, 4 Tested
SummaryCompounds, ActivePubMed Citation
Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells harboring harboring EGFR L858R/T790M double mutant preincubated for 60 mins followed by EGF stimulation and measured after 8 mins by SULFO-TAG based electrochemiluminescent assay
Assay data:12 Active, 9 Activity ≤ 1 µM, 12 Tested
Inhibition of EGFR T790M/del (746 to 750 residues) mutant autophosphorylation in human PC-9/ER1 cells harboring harboring EGFR T790M/del (746 to 750 residues) mutant preincubated for 60 mins followed by EGF stimulation and measured after 8 mins by SULFO-TAG based electrochemiluminescent assay
Assay data:12 Active, 10 Activity ≤ 1 µM, 12 Tested
Inhibition of EGFR del (746 to 750) mutant autophosphorylation in human PC-9 cells harboring harboring EGFR del (746 to 750) mutant preincubated for 60 mins followed by EGF stimulation and measured after 8 mins by SULFO-TAG based electrochemiluminescent assay
Assay data:12 Active, 1 Activity ≤ 1 nM, 11 Activity ≤ 1 µM, 12 Tested
Inhibition of EGFR autophosphorylation in human NCI-H292 cells harboring harboring wild type EGFR preincubated for 60 mins followed by EGF stimulation and measured after 8 mins by SULFO-TAG based electrochemiluminescent assay
Assay data:11 Active, 9 Activity ≤ 1 µM, 12 Tested
Inhibition of human EGFR L858R mutant phosphorylation in human NSCLC cells
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of wild type EGFR (unknown origin) autophosphorylation by Kinase-Glo luminescent assay
Assay data:14 Active, 14 Activity ≤ 1 µM, 14 Tested
Inhibition of EGFR (unknown origin)
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Anticancer activity against human Panel NCI-60 (60 carcinoma cell lines) cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay
Assay data:7 Active, 11 Tested
Inhibition of human EGFR
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Antiproliferative activity against human PC-9 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of human EGFR L858R/T790M mutant using 5-FAM-EEPLYWSFPAKKKCONH2 as substrate incubated for 30 mins in presence of ATP
Inhibition of human EGFR L858R mutant using 5-FAM-EEPLYWSFPAKKKCONH2 as substrate incubated for 30 mins in presence of ATP
Inhibition of human EGFR d746-750 mutant using 5-FAM-EEPLYWSFPAKKKCONH2 as substrate incubated for 30 mins in presence of ATP
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