Assay ID | Title | Year | Journal | Article |
AID365252 | Inhibition of human recombinant CYP3A4 in human liver microsomes using BzRes as a substrate | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID481242 | Inhibition of CYP3A4 assessed as dealkylation of 7-benzyloxy-4-trifluoromethylcoumarin | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one. |
AID466838 | Protein binding in human plasma | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. |
AID466833 | Inhibition of human recombinant IGF-1R tyrosine kinase expressed in baculovirus system assessed as [33gamma]ATP phosphorylation of poly(Glu/Tyr) substrate after 45 mins by scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. |
AID253684 | Steady-state volume of distribution in dog when administered intravenously at 2 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID254934 | Concentration required to inhibit cytochrome P450 isozyme CYP2C19 in vitro by 50% | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID253834 | Total clearance in monkey at 2 mg/kg intravenous dose | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID365255 | Protein binding in human plasma at 10 uM | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID253837 | Total clearance in dog when administered intravenously at 2 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID1191701 | Inhibition of NH2-terminal glutathione S-transferase fused human recombinant IGF-IR catalytic domain expressed in insect cells using poly(Glu:Tyr) substrate by ELISA-based assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
| Discovery of phenylpiperazine derivatives as IGF-1R inhibitor with potent antiproliferative properties in vitro. |
AID481244 | Solubility in phosphate buffer at pH 6.5 | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one. |
AID364772 | Increase in CYP3A4 mRNA expression level in human hepatocytes | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID255901 | In vitro inhibitory concentration against Geo (colon) cell line with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID254945 | In vitro inhibitory concentration against MEK with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID314564 | Inhibition of IGF1R expressed in SAL cells | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| 2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924. |
AID254987 | Concentration required to inhibit cytochrome P450 isozyme CYP2D6 in vitro by 50%; b = not determined | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID255905 | In vitro inhibitory concentration against MCF-7(breast) cell line with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID365251 | Induction of PXR transactivation at 10 uM relative to rifampicin | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID254797 | In vitro inhibitory concentration against IGF-1R kinase | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID364767 | Antiproliferative activity against transgenic mouse SAL cells overexpressing human IGF1R assessed as [3H]thymidine incorporation after 72 hrs | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID253832 | Bioavailability in dog at 5 mg/kg oral dose | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID254955 | Concentration required to inhibit cytochrome P450 isozyme CYP3A4-BzRes in vitro by 50% | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID254946 | In vitro inhibitory concentration against Met with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID314566 | Protein binding in mouse serum | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| 2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924. |
AID1191703 | Antiproliferative activity against human LS 174T cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
| Discovery of phenylpiperazine derivatives as IGF-1R inhibitor with potent antiproliferative properties in vitro. |
AID466836 | Antiproliferative activity against mouse Sal cells expressing human IGF-1R assessed as [3H]thymidine incorporation after 72 hrs by scintillation assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. |
AID255327 | In vitro kinase selectivity and cellular activity against MAPK2 kinase with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID430654 | Cytotoxicity against human MCF7 cells | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. |
AID253687 | Steady-state volume of distribution in rat when administered intravenously at 4 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID430647 | Inhibition of FAK | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. |
AID253688 | Steady-state volume of distribution in mouse when administered intravenously at 4 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID255909 | In vitro inhibitory concentration against COLO 205 (colon) cell line with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID364771 | AUC in mouse at 20 mg/kg after 4 hrs | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID481262 | Protein binding in mouse plasma assessed as fraction unbound at 10 uM by equilibrium dialysis | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one. |
AID466837 | AUC in mouse plasma at 20 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. |
AID466835 | Inhibition of CYP3A4 after 20 mins by BFC fluorescence assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. |
AID254920 | In vitro inhibitory concentration against HER2 with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID339683 | Inhibition of CYP3A4 | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors. |
AID314565 | Protein binding in human serum | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| 2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924. |
AID430645 | Inhibition of IGF1R | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. |
AID254919 | In vitro inhibitory concentration against FAK with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID364768 | Inhibition of human IGF1R expressed in transgenic mouse IGFSal cells | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID365247 | Inhibition of human recombinant CYP1A2 in human liver microsomes | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID254969 | In vitro inhibitory concentration against IGF-1R Sal kinase with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID365254 | Aqueous solubility of the compound | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID339685 | Metabolic stability in mouse liver microsomes | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors. |
AID481256 | In vivo antitumor activity against human COLO205 cells at 200 mg/kg, po qd for 21 days | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one. |
AID481259 | Protein binding in mouse plasma at 10 uM by equilibrium dialysis | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one. |
AID255926 | In vitro inhibitory concentration against RD1 (rhabdomyosarcoma) cell line with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID364769 | Inhibition of human recombinant CYP3A4 in human liver microsomes using BFC as a substrate | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID1191705 | Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
| Discovery of phenylpiperazine derivatives as IGF-1R inhibitor with potent antiproliferative properties in vitro. |
AID253838 | Total clearance in mouse when administered intravenously at 4 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID481240 | Inhibition of IGF1R | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one. |
AID339682 | Inhibition of IGF1R in mouse SAL cells assessed as thymidine incorporation | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors. |
AID254944 | Concentration required to inhibit cytochrome P450 isozyme CYP3A4-BFC in vitro by 50% | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID430651 | Cytotoxicity against human RD1 cells | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. |
AID481243 | AUC (0 to 4 hrs) in mouse at 20 mg/kg | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one. |
AID254913 | In vitro inhibitory concentration against LCK with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID339684 | AUC (0 to 4 hrs) in mouse plasma at 20 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors. |
AID481241 | In vivo antitumor activity against transgenic mouse Sal cells over expressing IGF1R | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one. |
AID430653 | Cytotoxicity against human COLO205 cells | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. |
AID253713 | Maximum concentration in dog administered orally at 5 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID255291 | In vitro inhibitory concentration against PDGFR with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID255921 | In vitro inhibitory concentration against MDA PCa-2b (prostate) cell line with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID365250 | Inhibition of human recombinant CYP2D6 in human liver microsomes | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID254931 | In vitro inhibitory concentration against VEGFR2 with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID253560 | Bioavailability in monkey at 5 mg/kg oral dose | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID255300 | In vitro inhibitory concentration against Akt1 with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID255318 | In vitro inhibitory concentration against CDK2/cyclin E kinase with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID466834 | Transactivation activity at human PXR assessed as induction of CYP3A4 activity at 10 uMol/l relative to rifampicin | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. |
AID314567 | AUC (0 to 4h) in mouse at 20 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| 2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924. |
AID430648 | Inhibition of MEK | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. |
AID365253 | Apparent permeability across human CaCo2 cells | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID481257 | In vivo antitumor activity against human RD1 cells at 150 mg/kg, po bid for 14 days | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one. |
AID314563 | Inhibition of IGF1R | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| 2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924. |
AID430652 | Cytotoxicity against human MDA PCa 2b cells | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. |
AID1191702 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
| Discovery of phenylpiperazine derivatives as IGF-1R inhibitor with potent antiproliferative properties in vitro. |
AID365249 | Inhibition of human recombinant CYP2C19 in human liver microsomes | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID253714 | Maximum concentration in rat administered orally at 50 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID254929 | Concentration required to inhibit cytochrome P450 isozyme CYP1A2 in vitro by 50% | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID1191704 | Antiproliferative activity against human SGC7901 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
| Discovery of phenylpiperazine derivatives as IGF-1R inhibitor with potent antiproliferative properties in vitro. |
AID254941 | In vitro inhibitory concentration against IR kinase with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID254930 | Concentration required to inhibit cytochrome P450 isozyme CYP2C9 in vitro by 50% | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID430646 | Inhibition of insulin receptor | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. |
AID253689 | Steady-state volume of distribution in monkey when administered intravenously at 2 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID253564 | Bioavailability in mouse administered perorally at 20 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID364773 | Protein binding in mouse plasma at 10 uM by equilibrium dialysis | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID253836 | Total clearance in rat when administered intravenously at 4 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID365248 | Inhibition of human recombinant CYP2C9 in human liver microsomes | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID254912 | In vitro inhibitory concentration EGF receptor with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID255302 | In vitro inhibitory concentration against MAPK1 kinase with ATP concentration at 1/2Km | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID1191706 | Cytotoxicity against human QSG7701 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
| Discovery of phenylpiperazine derivatives as IGF-1R inhibitor with potent antiproliferative properties in vitro. |
AID430650 | Inhibition of LCK | 2009 | Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
| Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. |
AID253716 | Maximum concentration in mouse administered orally at 20 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID253563 | Bioavailability in rat administered perorally at 50 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID253715 | Maximum concentration in monkey administered orally at 5 mg/kg | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
AID339681 | Inhibition of IGF1R | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors. |
AID364770 | Induction of PXR transactivation | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347167 | Vero cells viability qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347163 | 384 well plate NINDS AMC confirmatory qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347149 | Furin counterscreen qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347152 | Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347168 | HepG2 cells viability qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347153 | Confirmatory screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347161 | Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347169 | Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347158 | ZIKV-mCherry secondary qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
AID1347156 | DAPI mCherry counterscreen qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347164 | 384 well plate NINDS Rhodamine confirmatory qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1798842 | IGF-1R Inhibition Assay from Article 10.1021/jm800832q: \\Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
AID1798843 | CYP3A4 Enzyme Inhibition Assay from Article 10.1021/jm800832q: \\Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally effi | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |