| Assay ID | Title | Year | Journal | Article |
|---|
| AID262775 | Inhibition of DMN-induced collagen IA1 expression by TGF beta in Sprague-Dawley rat liver at 25 mg/kg, po | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. |
| AID262771 | Volume of distribution in Sprague-Dawley rat at 2 mg/kg, iv or 4 mg/kg, po | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. |
| AID262769 | Oral bioavailability in Sprague-Dawley rat at 2 mg/kg, iv and 4 mg/kg, po | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. |
| AID262767 | Inhibition of TGF beta-induced transcription of firefly luciferase reporter gene in HepG2 cells | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. |
| AID618727 | Inhibition of Activin A in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX at 1 uM after 16 hrs by luciferase reporter gene assay relative to control | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| 2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling. |
| AID262773 | Inhibition of DMN-induced collagen IA1 expression by TGF beta in Sprague-Dawley rat liver at 50 mg/kg, po | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. |
| AID262766 | Displacement of rhodamine green fluorescently labeled ATP from recombinant GST-ALK5 by FP assay | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. |
| AID447434 | Inhibition of TGFR1 | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
| Pharmacophore modeling and virtual screening for the discovery of new transforming growth factor-beta type I receptor (ALK5) inhibitors. |
| AID618725 | Inhibition of TGF-beta1 signaling expressed in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX at 1 uM after 16 hrs by luciferase reporter gene assay relative to control | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| 2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling. |
| AID262774 | Inhibition of DMN-induced collagen IA1 expression by TGF beta in Sprague-Dawley rat liver at 80 mg/kg, po | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. |
| AID262772 | Half life in Sprague-Dawley rat plasma | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. |
| AID618726 | Inhibition of TGF-beta1 signaling in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX at 100 nM after 16 hrs by luciferase reporter gene assay relative to control | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| 2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling. |
| AID262768 | Intrinsic clearance in Sprague-Dawley rat liver microsome | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. |
| AID618728 | Inhibition of Activin A in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX at 100 nM after 16 hrs by luciferase reporter gene assay relative to control | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| 2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling. |
| AID262770 | Plasma clearance in Sprague-Dawley rat at 2 mg/kg, iv or 4 mg/kg, po | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |