| Assay ID | Title | Year | Journal | Article |
|---|
| AID1363561 | Antagonist activity at TRPV1 in C57/BL6 mouse cerebellar granule cells assessed as inhibition of KCl-induced voltage dependent calcium entry at 10 uM by fura-2-based assay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1363557 | Inhibition of STIM1/STIM2/Orai1 (unknown origin) expressed in mouse BV2 cells assessed as reduction of store-operated calcium entry at 100 uM preincubated for 30 mins followed by tBhQ, mediated Ca2+ depletion and re-addition measured for 600 secs by Fluo- | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1578742 | Inhibition of ORAI (unknown origin) assessed as reduction in Ang2-induced NFAT translocation | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases. |
| AID1363551 | Modulation of STIM1/STIM2/Orai1 in mouse BV2 cells assessed as induction of store-operated calcium entry by measuring residual activity at 10 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular soluti | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1363563 | Antagonist activity at TRPV1 (unknown origin) expressed in HEK cells assessed as inhibition of capsaicin-induced calcium increase at 10 uM by fura-2-based assay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1363564 | Antagonist activity at TRPM8 (unknown origin) expressed in HEK cells assessed as inhibition of menthol -mediated calcium increase at 10 uM by fura-2-based assay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1363592 | Induction of store-operated calcium entry in human Jurkat cells assessed as induction of store-operated calcium entry by measuring residual activity at 100 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extrac | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1709646 | Neuroprotective activity in Sprague-Dawley rat primary hippocampal neurons assessed as reduction in Abeta-induced dendrites damage at 0.25 to 1 uM incubated for 16 hrs by MAP2 staining based assay | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1709642 | Metabolic stability in mouse liver microsomes assessed as half life at 10 mM measured up to 240 mins in presence of NADPH regeneration system by LC-MS analysis | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1709631 | Inhibition of human TRPC3 expressed in HEK293 cells assessed as inhibition of GSK170-induced current in presence of 2 mM extracellular calcium by whole cell patch-clamp method | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1363591 | Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring residual activity at 100 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solut | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1363552 | Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring residual activity at 10 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular soluti | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1363555 | Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring residual activity preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measur | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1363556 | Induction of store-operated calcium entry in human Jurkat cells assessed as induction of store-operated calcium entry by measuring residual activity preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular so | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1709574 | Cytotoxicity against HEK cells assessed as cell viability at 10 uM measured after 24 hrs by MTT assay relative to control | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| 1,2,4-Oxadiazole-Bearing Pyrazoles as Metabolically Stable Modulators of Store-Operated Calcium Entry. |
| AID1709632 | Inhibition of human TRPC3 expressed in HEK293 cells assessed as inhibition of OAG-induced current at 0.001 to 10 uM by whole cell patch-clamp method | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1363553 | Induction of store-operated calcium entry in human Jurkat cells assessed as induction of store-operated calcium entry by measuring residual activity at 10 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extrace | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1363565 | Metabolic stability in CD1 mouse plasma assessed as residual compound level at 50 uM after 30 mins by LC-UV analysis | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1363558 | Cytotoxicity against HEK cells assessed as cell viability at 10 uM by MTT assay relative to control | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1578741 | Inhibition of TRPC3 (unknown origin) | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases. |
| AID1363562 | Antagonist activity at TRPM8 in C57/BL6 mouse cerebellar granule cells assessed as inhibition of KCl-induced voltage dependent calcium entry at 10 uM by fura-2-based assay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1709639 | Inhibition of STIM/Orai1 (unknown origin) expressed in HEK293 cells assessed as reduction in thapsigargin-induced Ca2+ influx at 10 uM in presence of Ca2+ by whole cell patch clamp method | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1709575 | Inhibition of SOCE channel in tBhQ-treated HEK cells assessed as reduction in calcium entry preincubated for 600 secs followed by calcium addition by Fura-2 AM by fluorescence microscopic analysis | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| 1,2,4-Oxadiazole-Bearing Pyrazoles as Metabolically Stable Modulators of Store-Operated Calcium Entry. |
| AID1709645 | Toxicity in NSG/ICR mouse assessed as body weight loss at 200 mg/kg, ip administered once daily for 5 days | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1709643 | Metabolic stability in rat liver microsomes assessed as half life at 10 mM measured up to 240 mins in presence of NADPH regeneration system by LC-MS analysis | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1709647 | Inhibition of mouse TRPC3 expressed in HEK293 cells assessed as inhibition of Ca2+ influx by whole cell patch-clamp method | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1578743 | Inhibition of YFP-tagged TRPC3 (unknown origin) expressed in HEK293 cells assessed as reduction carbhocol-induced receptor operated Calcium influx after 5 mins by fura-2-AM dye based assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases. |
| AID1578744 | Inhibition of ORAI/STIM1 in thapsigargin treated rat RBL2H3 cells assessed as reduction in store-operated calcium entry after 5 mins by fura-2-AM dye based assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases. |
| AID1709630 | Inhibition of human TRPC3 expressed in HEK293 cells assessed as inhibition of GSK170-induced current in absence of extracellular calcium by whole cell patch-clamp method | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1709641 | Metabolic stability in human liver microsomes assessed as half life at 10 mM measured up to 240 mins in presence of NADPH regeneration system by LC-MS analysis | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1363590 | Modulation of STIM1/STIM2/Orai1 in mouse BV2 cells assessed as induction of store-operated calcium entry by measuring residual activity at 100 uM preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solut | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis. |
| AID1709577 | Stability in CD-1 mouse liver S9 fraction assessed as parent compound remaining at 50 uM measured after 60 mins by HPLC-UV analysis | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| 1,2,4-Oxadiazole-Bearing Pyrazoles as Metabolically Stable Modulators of Store-Operated Calcium Entry. |
| AID1709629 | Inhibition of human TRPC3 expressed in HEK293 cells assessed as inhibition of GSK170-induced current at 10 uM in absence of extracellular calcium by whole cell patch-clamp method relative to control | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1709648 | Toxicity in NSG/ICR mouse assessed as survival at 200 mg/kg, ip administered once daily for 5 days | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. |
| AID1709573 | Inhibition of SOCE channel in tBhQ-treated HEK cells assessed as reduction in calcium entry by measuring residual activity at 10 uM preincubated for 600 secs followed by calcium addition by Fura-2 AM by fluorescence microscopic analysis relative to contro | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
| 1,2,4-Oxadiazole-Bearing Pyrazoles as Metabolically Stable Modulators of Store-Operated Calcium Entry. |
| 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. |
| 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. |
| 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. |
| AID1346581 | Human TRPC3 (Transient Receptor Potential channels) | 2009 | Proceedings of the National Academy of Sciences of the United States of America, Mar-31, Volume: 106, Issue:13
| Selective and direct inhibition of TRPC3 channels underlies biological activities of a pyrazole compound. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |