Assay ID | Title | Year | Journal | Article |
AID527218 | Inhibition of tetrodotoxin-resistant NaV1.8 in rat DRG neuron by electrophysiology | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. |
AID312766 | Binding affinity to dopamine D1 receptor at 10 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318478 | Analgesic activity in ip dosed rat complete Freund's adjuvant-induced mechanical hyperalgesia model assessed as paw withdrawal latency after 2 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318445 | Inhibition of human Nav1.5 channel expressed in HEK293 cells at -90 mV by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID527224 | Oral bioavailability in rat at 3 mg/kg | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. |
AID318530 | Displacement of [3H]4DAMP from muscarinic M4 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318484 | Analgesic activity in ip dosed rat chronic constriction injury model of mechanical allodynia | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318443 | Inhibition of human Nav1.3 channel expressed in HEK293 cells at -60 mV by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312737 | Inhibition of human Nav1.3 channel at 10 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318441 | Inhibition of human Nav1.2 channel expressed in HEK293 cells at -60 mV by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318469 | Analgesic activity in rat formalin flinching inflammatory pain model at 300 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312754 | Cmax in Sprague-Dawley rat at 10 mg/kg, ip | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318473 | Analgesic activity in rat carrageenan-induced neuropathic pain model at 100 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318459 | Drug level in rat plasma at 10 to 100 mg/kg, ip after 45 mins | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312765 | Binding affinity to CCKAR at 10 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318498 | Analgesic activity in ip dosed rat colonic distension model | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318488 | Analgesic activity in ip dosed rat vincristine-induced mechanical allodynic neuropathic pain | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318481 | Analgesic activity in rat complete Freund's adjuvant-induced mechanical hyperalgesia model assessed as paw withdrawal latency at 100 mg/kg, ip after 4 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318452 | Inhibition of KCNQ2 channel | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312761 | Antinociceptive activity in ip dosed Sprague-Dawley rat assessed as reduction of mechanical allodynia in Bennett model of neuropathic pain | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318508 | Displacement of [125I]AB-MECA from adenosine A3 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318526 | Displacement of [125I]APT from histamine H2 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318529 | Displacement of [3H]4DAMP from muscarinic M3 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID536197 | Aqueous solubility of the compound | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
| Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain. |
AID318460 | Protein binding in rat plasma | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318548 | Inhibition of Nav1.8 channel in rat dorsal root ganglion neurons assessed as blockade of TTX-R current at -100 mV by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312740 | Inhibition of human Nav1.5 channel at 3 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318559 | Cmax in rat at 10 mg/kg, po | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318455 | Suppression of evoked action potential firing in rat DRG neurons at 0.1 uM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318466 | Analgesic activity in ip dosed rat acute mechanical stimulation nociception model assessed as paw withdrawal latency | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318480 | Analgesic activity in ip dosed rat complete Freund's adjuvant-induced mechanical hyperalgesia model assessed as paw withdrawal latency after 4 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318536 | Displacement of [3H]PACAP1-27 from PACAP PAC1 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318527 | Displacement of [3H]pirezepine from muscarinic M1 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID536192 | Inhibition of tetrodotoxin-resistant NaV1.8 in rat dorsal root ganglion neurons at holding potential -100 mV by whole-cell patch clamp electrophysiology assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
| Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain. |
AID318479 | Analgesic activity in rat complete Freund's adjuvant-induced mechanical hyperalgesia model assessed as paw withdrawal latency at 100 mg/kg, ip after 2 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318475 | Analgesic activity in rat complete Freund's adjuvant-induced thermal hyperalgesia model assessed as paw withdrawal latency at 100 mg/kg, ip after 2 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318525 | Displacement of [3H]pyrilamine from histamine H1 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318558 | Elimination half life in iv dosed rat | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318551 | Selectivity for human Nav1.8 channel over human Nav1.5 channel | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318545 | Displacement of [3H]LSD from 5HT6 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318470 | Analgesic activity in ip dosed rat capsaicn induced mechanical allodynia model | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318540 | Displacement of [3H]CYP from 5HT1B receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318437 | Inhibition of Nav1.8 channel in rat dorsal root ganglion neurons assessed as blockade of TTX-R current by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318519 | Displacement of [3H]spiperone from dopamine D4.4 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID536193 | Inhibition of mouse NaV1.8 expressed in HEK293 cells by isotopic efflux assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
| Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain. |
AID318456 | Bioavailability in rat at 10 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318504 | Motor effect in ip dosed rat assessed as latency to fall by edge balance test | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID313178 | Inhibition of inactivated human Nav1.5 sodium channel | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
| Sodium channel blockers. |
AID318533 | Displacement of [3H]U-69593 from opioid kappa receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318438 | Inhibition of human Nav1.8 channel expressed in HEK293 cells at -100 mV by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318544 | Displacement of [3H]LSD from 5HT5A receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID536198 | Clearance in rat microsomes | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
| Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain. |
AID318538 | Displacement of [35S]dATP-alpha-S from P2Y receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312699 | Activity at rat dorsal root ganglion in resting state with prepulse voltage of -100 mV assessed as blockade of TTx-resistant sodium current at 0.3 uM by whole-cell patch clamp technique | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318496 | Analgesic activity in ip dosed rat cyclophosphamide induced cyctitis model | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312772 | Binding affinity to melatonin receptor 1 | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318534 | Displacement of [3H]DAMGO from opioid mu receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318450 | Inhibition of P2X3 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID313183 | Effect on pain in rat by rotarod test | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
| Sodium channel blockers. |
AID312741 | Inhibition of human Nav1.5 channel at 1 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID312694 | Activity at rat dorsal root ganglion in inactivated state with prepulse voltage of -40 mV assessed as blockade of TTx-resistant sodium current at 0.1 uM by whole-cell patch clamp technique | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID313181 | Analgesic activity in ip dosed rat by CCI model of neuropathic pain | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
| Sodium channel blockers. |
AID318461 | Analgesic activity in rat spinal nerve ligation model at 200 to 300 nM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID527221 | Intrinsic clearance in rat microsomes after 1 hr | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. |
AID318474 | Analgesic activity in ip dosed rat complete Freund's adjuvant-induced thermal hyperalgesia model assessed as paw withdrawal latency after 2 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID536195 | Inhibition of human recombinant NaV1.2 by electrophysiology | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
| Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain. |
AID527223 | Aqueous solubility of the compound | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. |
AID313180 | Analgesic activity in ip dosed rat by chung model of neuropathic pain | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
| Sodium channel blockers. |
AID313179 | Inhibition of inactivated human Nav1.7 sodium channel | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
| Sodium channel blockers. |
AID318510 | Displacement of [3H]RX821002 from adrenergic alpha-2 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312752 | Clearance in Sprague-Dawley rat plasma | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318491 | Analgesic activity in rat skin incision model of post-operative pain at 100 mg/kg, ip after 2 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318446 | Inhibition of human Nav1.7 channel expressed in HEK293 cells at -120 mV by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318492 | Analgesic activity in ip dosed rat skin incision model of post-operative pain after 24 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318518 | Displacement of [3H]spiperone from dopamine D3 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312729 | Inhibition of human Nav1.2 channel at 3 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318539 | Displacement of [3H]8OH-DPAT from 5HT1A receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID313182 | Effect on locomotor activity in rat | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
| Sodium channel blockers. |
AID318486 | Analgesic activity in ip dosed rat chronic constriction injury model of cold allodynic neuropathic pain | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312731 | Inhibition of human Nav1.2 channel at 10 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID312762 | Antinociceptive activity in ip dosed Sprague-Dawley rat assessed as reduction of CFA-induced thermal hyperalgesia | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318523 | Displacement of [125I]TNFalpha from TNFalpha receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312773 | Binding affinity to 5HT2A receptor | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318522 | Displacement of [125I]IL8 from CXCR2 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318552 | Selectivity for human Nav1.8 channel over human Nav1.7 channel | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID527236 | Selectivity ratio of IC50 for NAv1.3 to IC50 for human Nav1.8 | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. |
AID318493 | Analgesic activity in rat skin incision model of post-operative pain at 100 mg/kg, ip after 24 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318502 | Motor effect in rat by rotarod test | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312723 | Inhibition of human recombinant Nav 1.8 channel expressed in HEK293 cells at 0.01 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318516 | Displacement of [3H]Win 55212-2 from cannabinoid CB2 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318442 | Inhibition of human Nav1.3 channel expressed in HEK293 cells at -120 mV by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312693 | Activity at rat dorsal root ganglion in inactivated state with prepulse voltage of -40 mV assessed as blockade of TTx-resistant sodium current at 0.3 uM by whole-cell patch clamp technique | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318542 | Displacement of [3H]mesulergine from 5HT2C receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318541 | Displacement of [3H]ketanserin from 5HT2A receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318547 | Displacement of [3H]pentazocine from sigma1 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID536194 | Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
| Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain. |
AID318535 | Displacement of [3H]nociceptin from ORL1 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318515 | Displacement of [3H]SCH-23390 from dopamine D1 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318457 | Cmax in rat at 10 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312757 | Protein binding in Sprague-Dawley rat plasma | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318467 | Analgesic activity in rat acute mechanical stimulation nociception model assessed as paw withdrawal latency at 100 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318554 | Suppression of spontaneous firing of rat DRG neurons at 0.3 uM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312758 | Oral bioavailability in Sprague-Dawley rat | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318487 | Analgesic activity in rat chronic constriction injury model of cold allodynic neuropathic pain at 100 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312768 | Binding affinity to 5HT2A receptor at 10 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318477 | Analgesic activity in rat complete Freund's adjuvant-induced thermal hyperalgesia model assessed as paw withdrawal latency at 100 mg/kg, ip after 4 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312770 | Binding affinity to CCKAR | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID312771 | Binding affinity to dopamine D1 receptor | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318550 | Selectivity for human Nav1.8 channel over human Nav1.3 channel | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312753 | Half life in Sprague-Dawley rat | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID312763 | Inhibition of human recombinant Nav 1.8 channel expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318509 | Displacement of [3H]prazosin from adrenergic alpha-1 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312756 | Ratio of drug level in brain to plasma in Sprague-Dawley rat | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318465 | Analgesic activity in rat acute thermal stimulation nociception model assessed as paw withdrawal latency at 100 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312755 | Volume of distribution at steady state in Sprague-Dawley rat | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318507 | Displacement of [3H]CGS-21680 from adenosine A2A receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318497 | Analgesic activity in ip dosed rat cyclophosphamide induced cyctitis model at 100 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312716 | Activity at human recombinant Nav 1.8 channel expressed in HEK293 cells in resting state with prepulse voltage of -100 mV assessed as blockade of TTx-resistant sodium current at 0.003 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318512 | Displacement of [3H](-)CGP-12177 from adrenergic beta2 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312748 | Inhibition of human Nav1.7 channel at 10 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID312751 | Inhibition of hERG potassium channel expressed in CHO cells by isotope efflux assay | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318546 | Displacement of [3H]LSD from 5HT7 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318436 | Inhibition of human Nav1.8 channel expressed in human HEK293 cells by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318531 | Displacement of [3H]4DAMP from muscarinic M5 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318471 | Analgesic activity in rat capsaicn induced mechanical allodynia model at 300 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318560 | Tmax in rat at 10 mg/kg, po | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318503 | Motor effect in rat by rotarod test at 300 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318463 | Antinociceptive activity in rat assessed as reduction of von Frey evoked firing of spinal dorsal horn wide dynamic range neurons at 20 mg/kg, iv | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312707 | Activity at human recombinant Nav 1.8 channel expressed in HEK293 cells in inactivated state with prepulse voltage of -40 mV assessed as blockade of TTx-resistant sodium current at 0.01 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318511 | Displacement of [3H](-)CGP-12177 from adrenergic beta-1 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318506 | Displacement of [3H]DPCPX from adenosine A1 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318556 | Clearance in rat plasma | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318458 | Tmax in rat at 10 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312708 | Activity at human recombinant Nav 1.8 channel expressed in HEK293 cells in inactivated state with prepulse voltage of -40 mV assessed as blockade of TTx-resistant sodium current at 0.003 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318462 | Antinociceptive activity in rat assessed as reduction of spontaneous firing of spinal dorsal horn wide dynamic range neurons at 20 mg/kg, iv | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318499 | Analgesic activity in rat colonic distension model at 100 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318513 | Displacement of [125I]endothelin-1 from endothelin ETA receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312735 | Inhibition of human Nav1.3 channel at 3 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318520 | Displacement of [3H]SCH23390 from dopamine D5 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318514 | Displacement of [3H]Win 55212-2 from cannabinoid CB1 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318439 | Inhibition of human Nav1.8 channel expressed in HEK293 cells at -40 mV by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312760 | Antinociceptive activity in ip dosed Sprague-Dawley rat assessed as attenuation of mechanical allodynia in chung model of neuropathic pain | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318500 | Motor effect in rat assessed as locomotory activity | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318532 | Displacement of [3H]DADLE from opioid delta receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318454 | Suppression of evoked action potential firing in rat DRG neurons at 0.3 uM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318448 | Inhibition of TRPV1 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318485 | Analgesic activity in rat chronic constriction injury model of mechanical allodynia at 100 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID313177 | Inhibition of inactivated human Nav1.3 sodium channel | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
| Sodium channel blockers. |
AID318521 | Displacement of [3H]GABA from GABA receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318490 | Analgesic activity in ip dosed rat skin incision model of post-operative pain after 2 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318451 | Inhibition of Cav2.2 channel | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318494 | Analgesic activity in ip dosed mouse visceral pain model assessed as acetic acid induced writhing | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318524 | Displacement of [125I]MIP1-alpha from CCR1 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312764 | Binding affinity to peripheral benzodiazepine receptor at 10 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318537 | Displacement of [3H]alpha,beta-methyl ATP from P2X receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318447 | Inhibition of human Nav1.7 channel expressed in HEK293 cells at -60 mV by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312700 | Activity at rat dorsal root ganglion in resting state with prepulse voltage of -100 mV assessed as blockade of TTx-resistant sodium current at 0.1 uM by whole-cell patch clamp technique | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID313176 | Inhibition of inactivated human Nav1.2 sodium channel | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
| Sodium channel blockers. |
AID318472 | Analgesic activity in ip dosed rat carrageenan-induced neuropathic pain model | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318476 | Analgesic activity in ip dosed rat complete Freund's adjuvant-induced thermal hyperalgesia model assessed as paw withdrawal latency after 4 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318453 | Inhibition of KCNQ3 channel | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318444 | Inhibition of human Nav1.5 channel expressed in HEK293 cells at -150 mV by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318501 | Motor effect in rat assessed as locomotory activity at 300 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318555 | Oral bioavailability in rat | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318553 | Inhibition of recombinant rat Nav1.8 sodium channel assessed as blockade of TTXR current by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312759 | Bioavailability in Sprague-Dawley rat at 10 mg/kg, ip | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318557 | Volume of distribution in rat | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312769 | Binding affinity to peripheral benzodiazepine receptor | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318440 | Inhibition of human Nav1.2 channel expressed in HEK293 cells at -120 mV by patch clamp method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312746 | Inhibition of human Nav1.7 channel at 3 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318517 | Displacement of [3H]spiperone from dopamine D2 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312689 | Inhibition of mouse recombinant Nav 1.8 channel expressed in HEK293 cells by isotopic efflux assay | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318483 | Analgesic activity in rat L5/L6 spinal nerve ligation-induced neuropathic pain model at 100 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312742 | Inhibition of human Nav1.5 channel at 10 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID312767 | Binding affinity to melatonin receptor 1 at 10 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318505 | Motor effect in rat assessed as latency to fall at 300 mg/kg, ip by edge balance test | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312724 | Inhibition of human recombinant Nav 1.8 channel expressed in HEK293 cells at 0.003 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318543 | Displacement of [3H]BRL43694 from 5HT3 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID312715 | Activity at human recombinant Nav 1.8 channel expressed in HEK293 cells in resting state with prepulse voltage of -100 mV assessed as blockade of TTx-resistant sodium current at 0.01 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318449 | Inhibition of P2X2 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID527235 | Selectivity ratio of IC50 for human NAv1.5 to IC50 for human Nav1.8 | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. |
AID318468 | Analgesic activity in ip dosed rat formalin flinching inflammatory pain model | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318489 | Analgesic activity in rat vincristine-induced mechanical allodynic neuropathic pain at 100 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID313175 | Inhibition of inactivated human Nav1.8 sodium channel | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
| Sodium channel blockers. |
AID318464 | Analgesic activity in ip dosed rat acute thermal stimulation nociception model assessed as paw withdrawal latency | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318482 | Analgesic activity in ip dosed rat L5/L6 spinal nerve ligation-induced neuropathic pain model | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318549 | Selectivity for human Nav1.8 channel over human Nav1.2 channel | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID527234 | Selectivity ratio of IC50 for human NAv1.2 to IC50 for human Nav1.8 | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. |
AID312691 | Intrinsic clearance in Sprague-Dawley rat microsomes after 1 hr | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
AID318528 | Displacement of [3H]AF-DX384 from muscarinic M2 receptor | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
AID318495 | Analgesic activity in mouse visceral pain model assessed as acetic acid induced writhing at 100 mg/kg, ip | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1346760 | Rat Nav1.8 (Voltage-gated sodium channels) | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |