Assay ID | Title | Year | Journal | Article |
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. |
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. |
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. |
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. |
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. |
AID292018 | Oral bioavailability in Sprague-Dawley rat at 5 mg/kg | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID310509 | Aqueous solubility in PBS at pH 7 | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility. |
AID344596 | Oral bioavailability in Sprague-Dawley rat at 5 mg/kg | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID291980 | Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID384505 | Toxicity assessed as increase in body temperature in Sprague-Dawley rat at 0.1 to 3 mg/kg, po after 60 mins | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
| Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. |
AID384504 | Inhibition of capsaicin-induced flinching in po dosed rat | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
| Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. |
AID292015 | Half life in Sprague-Dawley rat at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID291979 | AUC (0-infinity) in Sprague-Dawley rat at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID291994 | Half life in dog at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID317249 | Clearance in iv dosed rat | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties. |
AID476740 | Inhibition of human TRPV1 | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists. |
AID291986 | AUC (0 to infinity) in rat at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID291991 | AUC (0-infinity) in dog at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID310510 | Aqueous solubility in fasted-state stimulated intestinal fluid at pH 6.8 | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility. |
AID384502 | Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced calcium influx | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
| Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. |
AID291975 | Metabolic stability in rat liver microsomes assessed as clearance | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID344594 | Elimination half life in Sprague-Dawley rat at 5 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID291993 | Volume of distribution at steady state in dog at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID317245 | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties. |
AID384508 | Ratio of drug level in brain to plasma in Sprague-Dawley rat at 5 mg/kg, iv | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
| Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. |
AID384507 | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced calcium influx | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
| Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. |
AID1866020 | Thermodynamic aqueous solubility of the compound | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Structural modification aimed for improving solubility of lead compounds in early phase drug discovery. |
AID344588 | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced 45Ca2+ influx by FLIPR assay | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID291988 | Volume of distribution at steady state at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID291970 | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID317248 | Solubility in simulated intestinal fluid at pH 6.8 | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties. |
AID291972 | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID291973 | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of heat-induced calcium influx | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID291977 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID291990 | Bioavailability in rat at 1 mg/kg, po | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID291998 | Volume of distribution at steady state in monkey at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID291992 | Clearance in dog at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID344590 | Solubility in 0.01N HCl | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID317246 | Solubility in aqueous 0.01 N HCL | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties. |
AID291978 | Half life in Sprague-Dawley rat at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID292000 | Bioavailability in monkey at 1 mg/kg, po | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID344597 | AUC (0 to infinity) in Sprague-Dawley rat at 5 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID344598 | Clearance in Sprague-Dawley rat at 5 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID291989 | Half life in rat at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID291976 | In vivo clearance in Sprague-Dawley rat at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID292002 | Inhibition of capsaicin-induced flinching in Sprague-Dawley rat at 3 mg/kg, po upto 24 hrs | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID292011 | Solubility in 0.01N HCl | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID291981 | Bioavailability in fasted Sprague-Dawley rat at 3 mg/kg, po | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID317250 | Half life in iv dosed rat | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties. |
AID291974 | Metabolic stability in human liver microsomes assessed as clearance | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID292016 | AUC (0 to infinity) in Sprague-Dawley rat at 3 mg/kg, po up to 8 hrs | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID384506 | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
| Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. |
AID317244 | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties. |
AID291995 | Bioavailability in dog at 1 mg/kg, po | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID344595 | Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID344592 | Solubility in simulated intestinal fluid | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID310507 | Antagonist activity at rat TRPV1 expressed in CHO cells assessed inhibition of acid induced calcium influx | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility. |
AID310506 | Antagonist activity at rat TRPV1 expressed in CHO cells assessed inhibition of capsaicin induced calcium influx | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility. |
AID292001 | Efficacy in capsaicin-induced flinching in po dosed Sprague-Dawley rat | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID292012 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv up to 6 hrs | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID291983 | Aqueous solubility in hydrochloric acid by high-throughput automated format | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID317251 | Bioavailability in rat at 3 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties. |
AID344600 | Agonist activity at rat TRPV1 expressed in CHO cells assessed as effect on pH 5 acid-induced 45Ca2+ influx by FLIPR assay | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID344589 | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced 45Ca2+ influx by FLIPR assay | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID291996 | AUC (0-infinity) in monkey at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID292003 | Inhibition of CFA-induced paw thermal hyperalgesia in po dosed Sprague-Dawley rat | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID292020 | Solubility in SIF | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID292010 | Inhibition of rat TRPV1 expressed in CHO cells assessed as acid-induced Ca2+ influx | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID291985 | Solubility in simulated intestinal fluid by high-throughput automated format | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID344591 | Solubility in phosphate buffered saline at pH 7 | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID292004 | Inhibition of CFA-induced paw thermal hyperalgesia in Sprague-Dawley rat at 10 mg/kg, po relative to control | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID317253 | AUC in rat at 3 mg/kg, po | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties. |
AID291969 | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID292014 | Volume of distribution in Sprague-Dawley rat at 1 mg/kg, iv up to 6 hrs | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID292013 | AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, iv up to 6 hrs | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID344599 | Agonist activity at rat TRPV1 expressed in CHO cells assessed as effect on capsaicin-induced 45Ca2+ influx by FLIPR assay | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. |
AID292009 | Inhibition of rat TRPV1 expressed in CHO cells assessed as capsaicin-induced Ca2+ influx | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID291999 | Half life in monkey at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID1866046 | Antagonist activity at TRPV1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Structural modification aimed for improving solubility of lead compounds in early phase drug discovery. |
AID291997 | Clearance in monkey at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID292019 | Solubility in PBS | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID291984 | Solubility in PBS by high-throughput automated format | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID310508 | Aqueous solubility in 0.01N HCl | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility. |
AID384503 | Antagonist activity at human TRPV1 assessed as inhibition of low pH-induced calcium influx | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
| Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. |
AID291971 | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID317247 | Solubility in phosphate buffered saline at pH 7.4 | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties. |
AID291987 | Clearance in rat at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID1797982 | Proton Antagonist Assay from Article 10.1021/jm070190p: \\Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.\\ | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID1797987 | Capsaicin Antagonist Assay from Article 10.1021/jm070191h: \\Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.\\ | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. |
AID1797981 | Capsaicin Antagonist Assay from Article 10.1021/jm070190p: \\Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.\\ | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
AID1346617 | Human TRPV1 (Transient Receptor Potential channels) | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |