| Assay ID | Title | Year | Journal | Article |
|---|
| AID699595 | Drug metabolism in mouse plasma after 24 hrs by HPLC analysis | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
| AID699593 | Half life in mouse liver homogenate by HPLC analysis at pH 7.4 | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
| AID641892 | Inhibition of hypoxia-induced HIF1alpha accumulation in human LN229 cells at 20 uM after 1 hr preincubation measured after 24 hrs by Western blot analysis | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Design and synthesis of novel small-molecule inhibitors of the hypoxia inducible factor pathway. |
| AID672172 | Aqueous solubility of the compound at pH 7.4 | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Structure-activity relationship of 2,2-dimethyl-2H-chromene based arylsulfonamide analogs of 3,4-dimethoxy-N-[(2,2-dimethyl-2H-chromen-6-yl)methyl]-N-phenylbenzenesulfonamide, a novel small molecule hypoxia inducible factor-1 (HIF-1) pathway inhibitor and |
| AID1443391 | Inhibition of HIF-1 pathway in human LN229 cells harboring HRE-AP assessed sa reduction in VEGF transcription pretreated for 1 hr under normoxic condition followed by 24 hrs incubation under hypoxic condition by HRE-luciferase reporter gene assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Examining the structure-activity relationship of benzopyran-based inhibitors of the hypoxia inducible factor-1 pathway. |
| AID617386 | Inhibition of hypoxia-induced HIF1 activation in human LN229 cells expressing HRE-AP reporter gene at 5 uM preincubated for 1 hr under normoxia condition followed by 24 hrs incubation under hypoxia condition by HRE-luciferase reporter assay relative to co | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors. |
| AID1443389 | Inhibition of HIF-1 pathway in human LN229 cells harboring HRE-AP by alkaline phosphatase reporter gene assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Examining the structure-activity relationship of benzopyran-based inhibitors of the hypoxia inducible factor-1 pathway. |
| AID672169 | Inhibition of HIF1 transcriptional activity in human LN229 cells expressing VEGF-HRE-V6R and coexpressing luciferase, lac Z gene incubated for 1 hr in normoxia condition followed by 24 hrs in hypoxia condition by reporter gene assay | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Structure-activity relationship of 2,2-dimethyl-2H-chromene based arylsulfonamide analogs of 3,4-dimethoxy-N-[(2,2-dimethyl-2H-chromen-6-yl)methyl]-N-phenylbenzenesulfonamide, a novel small molecule hypoxia inducible factor-1 (HIF-1) pathway inhibitor and |
| AID699450 | Inhibition of P300 CH1 domain-mediated HIF1 transcriptional activity in human LN229-V6R cells assessed as reduction in luciferase activity at 2.5 to 10 uM incubated for 1 hr under normoxia followed by 24 hrs under hypoxia by reporter gene assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
| AID672171 | Downregulation of HIF1alpha protein level in human LN229 cells expressing VEGF-HRE-V6R at 10 uM incubated for 1 hr in normoxia condition followed by 24 hrs in hypoxia condition by Western blot analysis relative to control | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Structure-activity relationship of 2,2-dimethyl-2H-chromene based arylsulfonamide analogs of 3,4-dimethoxy-N-[(2,2-dimethyl-2H-chromen-6-yl)methyl]-N-phenylbenzenesulfonamide, a novel small molecule hypoxia inducible factor-1 (HIF-1) pathway inhibitor and |
| AID699588 | 1-Octanol-phosphate buffer distribution coefficient, log P of the compound at pH 7.4 by HPLC analysis | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
| AID1639062 | Inhibition of HIF-1alpha (unknown origin)/p300 (unknown origin) protein-protein interaction | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
| Advances in inhibition of protein-protein interactions targeting hypoxia-inducible factor-1 for cancer therapy. |
| AID617384 | Inhibition of hypoxia-induced HIF1 activation in human LN229 cells expressing HRE-AP reporter gene assessed as HRE remaining activity at 10 uM preincubated for 1 hr under normoxia condition followed by 24 hrs incubation under hypoxia condition by alkaline | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors. |
| AID699452 | Inhibition of luciferase activity in human LN229-Lux cells at 2.5 to 10 uM incubated for 1 hr under normoxia followed by 24 hrs under hypoxia by reporter gene assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
| AID617480 | Inhibition of HIF1alpha expression in human LN229 cells assessed as reduction of HIF-1alpha accumulation at <10 uM preincubated for 1 hr under normoxia condition followed by 24 hrs incubation under hypoxia condition by Western blotting | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors. |
| AID699594 | Inhibition of P300 CH1 domain-mediated HIF1 transcriptional activity in human LN229-V6R cells assessed as remaining activity at 2.5 uM incubated for 1 hr under normoxia followed by 24 hrs under hypoxia by luciferase reporter gene assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
| AID617385 | Inhibition of hypoxia-induced HIF1 activation in human LN229 cells expressing HRE-AP reporter gene at 2.5 uM preincubated for 1 hr under normoxia condition followed by 24 hrs incubation under hypoxia condition by HRE-luciferase reporter assay relative to | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors. |
| AID699449 | Aqueous solubility of the compound | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
| AID617387 | Inhibition of hypoxia-induced HIF1 activation in human LN229 cells expressing HRE-AP reporter gene at 10 uM preincubated for 1 hr under normoxia condition followed by 24 hrs incubation under hypoxia condition by HRE-luciferase reporter assay relative to c | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors. |
| AID699589 | Aqueous solubility of the compound after 30 mins by HPLC analysis | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
| AID1443390 | Antitumor activity against human LN229 cells xenografted in nude mouse assessed as tumor growth inhibition at 60 mg/kg administered for 5 days in a week for 10 to 12 weeks relative to control | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Examining the structure-activity relationship of benzopyran-based inhibitors of the hypoxia inducible factor-1 pathway. |
| AID700953 | Binding affinity to HIF1alpha in human LN229 cell nuclear extracts by Western blot analysis | 2012 | ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
| Binding Model for the Interaction of Anticancer Arylsulfonamides with the p300 Transcription Cofactor. |
| AID700950 | Binding affinity to recombinant P300 CH1 domain assessed as dissociation constant by surface plasmon resonance analysis | 2012 | ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
| Binding Model for the Interaction of Anticancer Arylsulfonamides with the p300 Transcription Cofactor. |
| AID641891 | Inhibition of HIF1 in human LN229 cells at 10 uM after 1 hr preincubation under hypoxic condition measured after 24 hrs by luciferase reporter gene assay | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Design and synthesis of novel small-molecule inhibitors of the hypoxia inducible factor pathway. |
| AID699591 | Aqueous solubility of the compound at pH 5 after 90 mins by laser nephelometric analysis | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
| AID672170 | Inhibition of HIF1 transcriptional activity in human LN229 cells expressing VEGF-HRE-V6R and coexpressing lac Z gene at 10 uM incubated for 1 hr in normoxia condition followed by 24 hrs in hypoxia condition by luciferase reporter gene assay relative to co | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Structure-activity relationship of 2,2-dimethyl-2H-chromene based arylsulfonamide analogs of 3,4-dimethoxy-N-[(2,2-dimethyl-2H-chromen-6-yl)methyl]-N-phenylbenzenesulfonamide, a novel small molecule hypoxia inducible factor-1 (HIF-1) pathway inhibitor and |
| AID700952 | Binding affinity to P300 in human LN229 cell nuclear extracts by Western blot analysis | 2012 | ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
| Binding Model for the Interaction of Anticancer Arylsulfonamides with the p300 Transcription Cofactor. |
| AID699592 | Aqueous solubility of the compound at pH 3 after 90 mins by laser nephelometric analysis | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
| AID617478 | Inhibition of HIF1alpha expression in human LN229 cells assessed as reduction of HIF-1alpha accumulation at 20 uM preincubated for 1 hr under normoxia condition followed by 24 hrs incubation under hypoxia condition by Western blotting | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors. |
| AID617477 | Inhibition of hypoxia-induced HIF1 activation in human LN229 cells expressing VEGF reporter gene assessed as VEGF expression at 10 uM preincubated for 1 hr under normoxia condition followed by 24 hrs incubation under hypoxia condition by luciferase report | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors. |
| AID699590 | Aqueous solubility of the compound at pH 7.4 after 90 mins by laser nephelometric analysis | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents. |
| AID617481 | Inhibition of hypoxia-induced HIF1 activation in human LN229 cells expressing VEGF reporter gene assessed as VEGF expression at 10 uM after 24 hrs incubation under hypoxia condition by luciferase reporter assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors. |
| AID617388 | Inhibition of hypoxia-induced HIF1 activation in human LN229 cells expressing HRE-AP reporter gene preincubated for 1 hr under normoxia condition followed by 24 hrs incubation under hypoxia condition by HRE-luciferase reporter assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |