| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| AID705237 | Antagonist activity at human TRPV1 expressed in CHOK1 cells assessed as inhibition of pH-induced activity by FLIPR assay | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
| 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent transient receptor potential vanilloid 1 (TRPV1) antagonists: structure-activity relationships of 2-amino derivatives in the N-(6-trifluoromethylpyridin-3-ylmethyl) C-region. |
| AID351814 | Antagonist activity at TRPV1 in Sprague-Dawley rat DRG neuron assessed as reduction of capsaicin-stimulated 45Ca2+ uptake | 2009 | Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
| Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists. |
| AID255112 | Concentration required to inhibit [3H]RTX radioligand binding towards transient receptor potential cation channel (subfamily V, member 1) expressed in chinese hamster ovary cells | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents. |
| AID238266 | Antagonist activity for rat TRPV1 expressed in CHO cells | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
| Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists. |
| AID246449 | Agonist activity by [Ca2+] uptake in CHO cells expressing rat TRPV1 at 10-30 uM; NE = Not effective | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
| Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists. |
| AID255029 | Inhibitory effect on capsaicin (0.5 uM)-induced calcium uptake in rat DRG neurons upon incubation at RT for 10 minutes | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents. |
| AID454507 | Antagonist activity at TRPV1 in Sprague-Dawley rat DRG neurons assessed as inhibition of capsaicin-induced [45]Ca2+ uptake | 2009 | Bioorganic & medicinal chemistry, Dec-15, Volume: 17, Issue:24
| Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists. |
| AID179770 | In vitro inhibitory concentration was determined against [45Ca2+]- influx in rat DRG neurons | 2004 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7
| N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands. |
| AID238618 | In vitro inhibition of [3H]RTX binding to rat TRPV1 expressed in CHO cells | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
| Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists. |
| AID254649 | Concentration required to antagonized capsaicin-induced calcium uptake at the transient receptor potential cation channel (subfamily V member 1) expressed in chinese hamster ovary cells | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents. |
| AID180309 | Inhibition of [Ca2+] uptake in dorsal root ganglion (DRG) neurons from neonatal Sprague-Dawley rat | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects. |
| AID456197 | Agonist activity at TRPV1 in Sprague-Dawley rat DRG neuron assessed as intracellular 45Ca2+ influx by scintillation counting | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Silicon switch approach in TRPV1 antagonist MK-056 and its analogues. |
| AID227528 | In vivo analgesic activity | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
| Vanilloid receptor TRPV1 antagonists as the next generation of painkillers. Are we putting the cart before the horse? |
| AID705238 | Antagonist activity at human TRPV1 expressed in CHOK1 cells assessed as inhibition of capsaicin-induced activity by FLIPR assay | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
| 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent transient receptor potential vanilloid 1 (TRPV1) antagonists: structure-activity relationships of 2-amino derivatives in the N-(6-trifluoromethylpyridin-3-ylmethyl) C-region. |
| AID238267 | Antagonist activity towards rat TRPV1 expressed in CHO cells | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
| Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists. |
| AID668951 | Antagonist activity at rat TRPV1 receptor expressed in CHO cells assessed as decrease in capsaicin-induced intracellular 45Ca2+ uptake after 1 hr by fluorometric analysis | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
| N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region. |
| AID289351 | Antagonist activity at rat TRPV1 receptor expressed in CHO cells by Ca2+ uptake assay | 2007 | Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
| Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists. |
| AID175852 | In vitro induction of 45 [Ca2+] influx in rat DRG neurons (ineffective at 30 uM, partial activity) | 2004 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7
| N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands. |
| AID289350 | Agonist activity at rat TRPV1 receptor expressed in CHO cells by Ca2+ uptake assay | 2007 | Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
| Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists. |
| AID289349 | Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells | 2007 | Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
| Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists. |
| AID456198 | Antagonist activity at TRPV1 in Sprague-Dawley rat DRG neuron assessed as reduction of capsaicin-stimulated intracellular 45Ca2+ influx by scintillation counting | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Silicon switch approach in TRPV1 antagonist MK-056 and its analogues. |
| AID668947 | Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells after 60 mins by scintillation counting | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
| N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region. |
| AID238617 | In vitro binding affinity for rat TRPV1 expressed in CHO cells using [3H]-RTX | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
| Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists. |
| AID668949 | Agonist activity at rat TRPV1 receptor expressed in CHO cells assessed as increase in intracellular 45Ca2+ uptake after 1 hr by fluorometric analysis | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
| N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region. |
| AID246722 | Induction of [Ca2+] uptake in CHO cells expressing rat TRPV1 at 10-30 uM relative to 300 nM capsaicin; Not effective | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
| Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists. |
| AID1346643 | Rat TRPV1 (Transient Receptor Potential channels) | 2002 | Molecular pharmacology, Oct, Volume: 62, Issue:4
| High affinity antagonists of the vanilloid receptor. |
| AID1797968 | Competition Binding Assay and Inhibition of Ca2+ Uptake Assay from Article 10.1016/j.bmc.2007.06.041: \\Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.\\ | 2007 | Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
| Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |