| 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. |
| 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. |
| 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. |
| 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. |
| AID464829 | Volume of distribution in dog at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464852 | Toxicity in rat assessed as flushing-mediated vasodilation at 100 mg/kg, ip by laser doppler flowmetry | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464653 | Bioavailability in mouse at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464830 | Volume of distribution in mouse at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464652 | Bioavailability in dog at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464836 | Normalized AUC in rat at 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464840 | Drug level in NA-receptor null C57BL/6 mouse blood at 100 mg/kg, po after 15 mins | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464828 | Volume of distribution in rat at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464651 | Bioavailability in rat at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464848 | Antilipolytic activity in rat assessed as reduction plasma free fatty acids levels at 100 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464835 | Half life in rhesus monkey at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464862 | Antilipolytic activity in po dosed dog assessed as reduction plasma free fatty acids levels | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464850 | Toxicity in rat assessed as induction of flushing-mediated vasodilation in ears at >=3 mg/kg, sc by laser doppler flowmetry | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464857 | Antilipolytic activity in po dosed dog assessed as drug concentration causing maximum reduction plasma free fatty acids levels | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464867 | Inhibition of CYP2C9 | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464841 | Drug level in wild-type C57BL/6 mouse blood at 100 mg/kg, po after 15 mins | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464865 | Inhibition of CYP2D6 | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464866 | Inhibition of CYP3A4 | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464646 | Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464844 | Agonist activity at dog nicotinic acid receptor by [35S]GTPgammaS binding assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464825 | Clearance in dog at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464846 | Antilipolytic activity in wild-type C57BL/6 mouse assessed as reduction plasma free fatty acids levels at 100 mg/kg, po after 15 mins | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464839 | Normalized AUC in rhesus monkey at 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464851 | Toxicity in rat assessed as induction of induction of flushing-mediated vasodilation in ears at 100 mg/kg, sc by laser doppler flowmetry | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464834 | Half life in mouse at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464858 | Toxicity in po dosed dog assessed as threshold dose at which induction of flushing-mediated-vasodilation occurs in ears by spectrocolorimetry | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464831 | Volume of distribution in rhesus monkey at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464832 | Half life in rat at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464854 | Toxicity in ip dosed rat assessed as induction of induction of flushing-mediated vasodilation in ears by laser doppler flowmetry | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464655 | Clearance in rat at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464649 | Binding affinity to GPR81 | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464650 | Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464654 | Bioavailability in rhesus monkey at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464849 | Antilipolytic activity in po dosed rat assessed as reduction plasma free fatty acids levels | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464843 | Agonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464853 | Plasma concentration in rat at 100 mg/kg, ip | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464826 | Clearance in mouse at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464861 | Toxicity in po dosed dog assessed as Cmax at which threshold dose of vasodilation occurs in ears by spectrocolorimetry | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464647 | Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464859 | Therapeutic index, ratio of threshold dose of vasodilation in dog to drug concentration causing maximum free fatty acid reduction in dog | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464842 | Agonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464856 | Antilipolytic activity in dog assessed as reduction plasma free fatty acids levels at 100 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464838 | Normalized AUC in mouse at 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464855 | Therapeutic index, ratio of cutaneous vasodilation in rat to EC50 for free fatty acid reduction in rat | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464833 | Half life in dog at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464863 | Therapeutic index, ratio of Cmax for threshold dose of vasodilation in dog to EC50 for free fatty acid reduction in dog | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464845 | Ratio of Ki for human GPR109A in presence of human serum albumin to Ki for GPR109A in absence of human serum albumin | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464837 | Normalized AUC in dog at 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464827 | Clearance in rhesus monkey at 1.0 mg/kg, iv or 2 mg/kg, po | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464864 | Inhibition of CYP2C8 | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464648 | Binding affinity to GPR109B | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID464847 | Antilipolytic activity in NA-receptor null C57BL/6 mouse assessed as reduction plasma free fatty acids levels at 100 mg/kg, po after 15 mins | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| AID1346416 | Human HCA2 receptor (Hydroxycarboxylic acid receptors) | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |