| Assay ID | Title | Year | Journal | Article |
|---|
| AID1677356 | MRT in C57BL/6 mouse at 1 mg/kg, iv | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1677336 | Terminal half life in C57BL/6 mouse at 3 mg/kg, po | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1648719 | Inhibition of NLRP3 inflammasome activation in LPS-primed human THP1 cells assessed as reduction in IL-1beta level preincubated for 1 hr followed by addition of ATP and nigericin further incubated for 1 hrs and measured post ATP addition 1 hr by ELISA met | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4
| Discovery of |
| AID1677353 | AUC (0 to t) in C57BL/6 mouse at 1 mg/kg, iv | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1527546 | Half life in C57BL/6 mouse plasma at 3 mg/kg, iv or 20 mg/kg, po | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Development of small molecule inhibitors targeting NLRP3 inflammasome pathway for inflammatory diseases. |
| AID1875552 | Inhibition of NLRP3 inflammasome activation in LPS/nigericin-treated mouse J774A.1 cells assessed as decrease in LDH release pretreated for 0.5 hrs followed by stimulation with nigericin for 1 hr by LDH release assay | | | |
| AID1617059 | Inhibition of NLRP3 in mouse peritoneal macrophages assessed as inhibition of LPS and ATP-induced IL-1beta production pre-stimulated with LPS for 4.5 hrs before compound addition with ATP for 30 mins by ELISA | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Discovery of Second-Generation NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization. |
| AID1744045 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced lymphocyte level in BALF at 10 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744074 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced IL-1beta mRNA expression in lungs at 10 to 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by qRT-PCR analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744087 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced caspase-1 expression in lungs at 10 to 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by Western blot analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1867339 | Cytotoxicity against human THP-1 assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Synthesis and pharmacological validation of fluorescent diarylsulfonylurea analogues as NLRP3 inhibitors and imaging probes. |
| AID1907683 | Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability at 0.01 to 3 uM measured after 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| AID1286179 | Inhibition of NLRP3 in mouse BMDM cells preincubated for 30 mins followed by ATP addition by ELISA analysis | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Inhibiting the Inflammasome: A Chemical Perspective. |
| AID1324648 | Drug metabolism in Escherichia coli membranes expressing recombinant CYP2C18 (unknown origin) co-expressed with human NADPH-CPR/bacterial GroEL/GroES assessed as CYP2C18-mediated R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hy | | | |
| AID1324650 | Drug metabolism in Escherichia coli membranes expressing recombinant CYP2J2 (unknown origin) co-expressed with human NADPH-CPR/bacterial GroEL/GroES assessed as CYP2J2-mediated R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydr | | | |
| AID1607606 | Oral bioavailability in human | 2019 | Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
| Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs). |
| AID1677357 | Oral bioavailability in C57BL/6 mouse at 3 mg/kg | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1743883 | Inhibition of NLRP3 in PMA-stimulated human THP-1 cells assessed as reduction in IL-1beta release at 500 nM pre-treated for 24 hrs followed by stimulation with LPS for 3 hrs and ATP for 1 hr by ELISA analysis | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Development of Novel Tetrahydroquinoline Inhibitors of NLRP3 Inflammasome for Potential Treatment of DSS-Induced Mouse Colitis. |
| AID1607605 | Half life in human | 2019 | Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
| Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs). |
| AID1324652 | Cytotoxicity against human HEK293 cells assessed as decrease in cell viability after 20 hrs by resazurin based fluorescence assay | | | |
| AID1744041 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophils in BALF at 10 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1324651 | Drug metabolism in Escherichia coli membranes expressing recombinant CYP3A4 (unknown origin) co-expressed with human NADPH-CPR/bacterial GroEL/GroES assessed as CYP3A4-mediated R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydr | | | |
| AID1867338 | Inhibition of NLRP3 inflammasome activation in PMA differentiated LPS-primed human THP-1 cells assessed as reduction in nigericin-induced IL-1beta level pretreated for 2 hrs followed by nigericin addition and measured after 30 mins by ELISA | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Synthesis and pharmacological validation of fluorescent diarylsulfonylurea analogues as NLRP3 inhibitors and imaging probes. |
| AID1743880 | Inhibition of NLRP3 in human monocyte-derived macrophages | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Development of Novel Tetrahydroquinoline Inhibitors of NLRP3 Inflammasome for Potential Treatment of DSS-Induced Mouse Colitis. |
| AID1324649 | Drug metabolism in Escherichia coli membranes expressing recombinant CYP2C19 (unknown origin) co-expressed with human NADPH-CPR/bacterial GroEL/GroES assessed as CYP2C19-mediated R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hy | | | |
| AID1677354 | Volume of distribution at steady state in C57BL/6 mouse at 1 mg/kg, iv | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1907681 | Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability at 10 uM measured after 24 hrs by MTT assay relative to control | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| AID1744046 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced lymphocyte level in BALF at 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1677339 | Tmax in C57BL/6 mouse at 3 mg/kg, po | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1882499 | Inhibition of NLRP3 inflammasome activation in LPS/nigericin-stimulated PMA-differentiated human THP-1 macrophages assessed as reduction in pyroptosis pretreated with LPS followed by compound treatment for 30 mins then stimulation with nigericin and measu | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Discovery of a novel and potent inhibitor with differential species-specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis. |
| AID1744082 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced IL-1beta expression in lungs at 10 to 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by Western blot analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744054 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced lymphocyte level in BALF at 10 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1324644 | Drug metabolism in Escherichia coli membranes expressing recombinant CYP1A2 (unknown origin) co-expressed with human NADPH-CPR/bacterial GroEL/GroES assessed as CYP1A2-mediated R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydr | | | |
| AID1744076 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced TGF-beta1 mRNA expression in lungs at 10 to 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by qRT-PCR analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1324646 | Drug metabolism in Escherichia coli membranes expressing recombinant CYP2B6 (unknown origin) co-expressed with human NADPH-CPR/bacterial GroEL/GroES assessed as CYP2B6-mediated R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydr | | | |
| AID1324653 | Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 20 hrs by resazurin based fluorescence assay | | | |
| AID1816013 | Antiinflammatory activity in human THP-1 cells assessed as inhibition of LPS-induced IL-1beta secretion in LPS stimulation for 3 hrs followed by pretreatment at 2uM for 40 min before induced with nigericin for 40 min measured by ELISA | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| New Highly Potent NLRP3 Inhibitors: Furanochalcone Velutone F Analogues. |
| AID1677337 | Cmax in C57BL/6 mouse at 3 mg/kg, po | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1867343 | Inhibition of NLRP3 inflammasome activation in PMA differentiated LPS-primed human THP-1 cells assessed as inhibition of nigericin-induced pro caspase-1 secretion at 0.01 to 1 uM pretreated for 30 mins followed by nigericin addition and measured after 2 h | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Synthesis and pharmacological validation of fluorescent diarylsulfonylurea analogues as NLRP3 inhibitors and imaging probes. |
| AID1907682 | Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability at 30 uM measured after 24 hrs by MTT assay relative to control | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| AID1744077 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced MMP-1 mRNA expression in lungs at 10 to 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by qRT-PCR analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1373377 | Inhibition of NLRP3 in human monocyte derived macrophages assessed as reduction in LPS-induced IL-1beta production incubated for 30 mins followed by nigericin sodium salt stimulation for 2 hrs post LPS challenge for 3 hrs by ELISA | 2018 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
| Synthesis of deuterium-labelled analogues of NLRP3 inflammasome inhibitor MCC950. |
| AID1907684 | Inhibition of NLRP3 inflammasome activation in LPS-primed mouse BMDM cells assessed as reduction in ATP induced IL-1beta release pretreated for 15 mins followed by ATP stimulation for 30 mins by ELISA | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| AID1744098 | Inhibition of NLRP3 inflammasome activation in LPS-primed mouse bone marrow derived macrophages assessed as reduction in IL-1beta level preincubated for 30 mins followed by ATP addition and measured after 4 hrs by ELISA method | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1324641 | Drug metabolism in human liver microsomes assessed as N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide formation at 5 uM preincubated for 20 mins followed by NADPH addition measured after 120 mins b | | | |
| AID1677338 | AUC (0 to t) in C57BL/6 mouse at 3 mg/kg, po | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1907680 | Cytotoxicity against mouse AML12 cells assessed as reduction in cell viability at 0.01 to 30 uM measured after 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| AID1744075 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced IL-8 mRNA expression in lungs at 10 to 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by qRT-PCR analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1867342 | Inhibition of NLRP3 inflammasome activation in PMA differentiated LPS-primed human THP-1 cells assessed as inhibition of nigericin-induced pro IL-1beta secretion at 0.01 to 1 uM pretreated for 30 mins followed by nigericin addition and measured after 2 hr | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Synthesis and pharmacological validation of fluorescent diarylsulfonylurea analogues as NLRP3 inhibitors and imaging probes. |
| AID1744067 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced MMP-1 mRNA expression in lungs at 10 to 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by qRT-PCR analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1875553 | Inhibition of NLRP3 inflammasome activation in LPS/nigericin-treated mouse J774A.1 cells assessed as decrease in IL-1beta level pretreated for 0.5 hrs followed by stimulation with nigericin for 1 hr by ELISA | | | |
| AID1677333 | Clearance in C57BL/6 mouse at 1 mg/kg, iv | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1744065 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced IL-1beta mRNA expression in lungs at 10 to 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by qRT-PCR analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1759589 | Inhibition of NLRP3 inflammasome activation in LPS/nigericin-treated mouse BMDM cells assessed as inhibition of LPS and nigericin-induced IL-1beta production pre-treated for 1 hr measured after 1 hr of stimulation by ELISA | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of chalcone analogues as novel NLRP3 inflammasome inhibitors with potent anti-inflammation activities. |
| AID1324654 | Inhibition of NLRP3 inflammasome activation in LPS-stimulated mouse BMDM assessed as reduction in NLRP3 inflammasome-induced IL-1beta production preincubated for 30 mins followed by NLRP3 stimulation with ATP by ELISA | | | |
| AID1744069 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced TGF-beta1 mRNA expression in lungs at 10 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by qRT-PCR analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1727549 | Protection against nigericin-induced pyroptosis in human THP-1 cells assessed as cell viability at 10 uM | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Structure-activity relationship studies of phenothiazine derivatives as a new class of ferroptosis inhibitors together with the therapeutic effect in an ischemic stroke model. |
| AID1907678 | Inhibition of NLRP3 inflammasome activation in LPS-primed mouse BMDM cells assessed as reduction in IL-1beta level at 3 uM pre-treated for 15 mins followed by ATP stimulation for 30 mins by ELISA relative to control | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| AID1907691 | Antiinflammatory activity in MSU-induced acute gout arthritis in wild type male C57BL/6J mouse model assessed as decrease in paw inflammation at 3 mg/kg, ip measured after 24 hrs | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| AID1864382 | Inhibition of NLRP3 inflammasome activation in LPS-primed mouse J774.A1 cells assessed as reduction in IL-1beta secretion preincubated for 1 hr followed by nigericin stimulation and measured after 1 hr by ELISA | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity. |
| AID1744060 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophil infiltration in lungs at 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by H and E staining based imaging analysis relative to contr | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744062 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophil infiltration in lungs at 10 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by H and E staining based imaging analysis relative to contro | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744083 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced caspase-1 expression in lungs at 10 to 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by Western blot analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1743885 | Cytotoxicity in human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Development of Novel Tetrahydroquinoline Inhibitors of NLRP3 Inflammasome for Potential Treatment of DSS-Induced Mouse Colitis. |
| AID1907679 | Inhibition of NLRP3 inflammasome activation in LPS-primed mouse BMDM cells assessed as reduction in IL-1beta level at 10 uM pre-treated for 15 mins followed by ATP stimulation for 30 mins by ELISA relative to control | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| AID1324647 | Drug metabolism in Escherichia coli membranes expressing recombinant CYP2C9 (unknown origin) co-expressed with human NADPH-CPR/bacterial GroEL/GroES assessed as CYP2C9-mediated R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydr | | | |
| AID1660159 | Inhibition of NLRP3 inflammasome activation in LPS-stimulated human THP1 cells assessed as IL-1beta secretion at 10 uM incubated for 1 hr followed by nigericin addition and measured after 1 hr by ELISA relative to control | 2020 | Journal of natural products, 06-26, Volume: 83, Issue:6
| Inhibitory Effect of Cannabidiol on the Activation of NLRP3 Inflammasome Is Associated with Its Modulation of the P2X7 Receptor in Human Monocytes. |
| AID1744053 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced macrophage level in BALF at 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1907701 | Inhibition of NLRP3 inflammasome activation in LPS-primed mouse BMDM cells assessed as reduction in ATP induced IL-1beta release at 1 uM pretreated for 15 mins followed by ATP addition for 30 mins by ELISA | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| AID1677335 | MRT in C57BL/6 mouse at 3 mg/kg, po | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1373378 | Inhibition of NLRP3 in human monocyte derived macrophages assessed as reduction in LPS-induced IL-1beta production by ELISA | 2018 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
| Synthesis of deuterium-labelled analogues of NLRP3 inflammasome inhibitor MCC950. |
| AID1527545 | Oral bioavailability in C57BL/6 mouse at 20 mg/kg | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Development of small molecule inhibitors targeting NLRP3 inflammasome pathway for inflammatory diseases. |
| AID1677334 | Initial plasma concentration in C57BL/6 mouse at 1 mg/kg, iv | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1660160 | Inhibition of TNF-alpha secretion in LPS-stimulated human THP1 cells assessed as TNF-alpha level at 10 uM incubated for 1 hr followed by nigericin addition and measured after 1 hr by ELISA (Rvb = 957.6 pg/mL) | 2020 | Journal of natural products, 06-26, Volume: 83, Issue:6
| Inhibitory Effect of Cannabidiol on the Activation of NLRP3 Inflammasome Is Associated with Its Modulation of the P2X7 Receptor in Human Monocytes. |
| AID1918284 | Inhibition of NLRP3 inflammasome activation in LPS and nigericin-stimulated human PBMC cells assessed as reduction in IL-1beta release preincubated with LPS for 3 hrs followed by compound addition for 30 mins and further stimulated with nigericin for 1.5 | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
| Overcoming Preclinical Safety Obstacles to Discover ( |
| AID1744055 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced lymphocyte level in BALF at 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1907685 | Inhibition of NLRP3 inflammasome activation in LPS-primed mouse BMDM cells assessed as reduction in MSU induced IL-1beta release at 1 uM pretreated for 15 mins followed by MSU addition for 30 mins by ELISA | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| AID1286181 | Oral bioavailability in single dosed C57BL/6 mouse at 20 mg/kg | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Inhibiting the Inflammasome: A Chemical Perspective. |
| AID1744059 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophil infiltration in lungs at 10 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by H and E staining based imaging analysis relative to contr | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744094 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced IL-1beta expression in serum at 10 to 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by ELISA | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744066 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced IL-8 mRNA expression in lungs at 10 to 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by qRT-PCR analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744044 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced macrophages level in BALF at 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744090 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced IL-1beta expression in serum at 10 to 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by ELISA | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744095 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced IL-18 expression in serum at 10 to 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by ELISA | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744086 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced IL-1beta expression in lungs at 10 to 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by Western blot analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1907677 | Inhibition of NLRP3 inflammasome activation in LPS-primed mouse BMDM cells assessed as reduction in IL-1beta level at 1 uM pre-treated for 15 mins followed by ATP stimulation for 30 mins by ELISA relative to control | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| AID1527543 | Inhibition of NLRP3 in LPS/ATP-treated mouse bone marrow derived macrophages assessed as reduction in NLRP3 inflammasome activation by measuring reduction in IL-1beta level by ELISA method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Development of small molecule inhibitors targeting NLRP3 inflammasome pathway for inflammatory diseases. |
| AID1324645 | Drug metabolism in Escherichia coli membranes expressing recombinant CYP2A6 (unknown origin) co-expressed with human NADPH-CPR/bacterial GroEL/GroES assessed as CYP2A6-mediated R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydr | | | |
| AID1677355 | Terminal half life in C57BL/6 mouse at 1 mg/kg, iv | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1744091 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced IL-18 expression in serum at 10 to 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by ELISA | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1607604 | Inhibition of human ERG by high throughput automated patch clamp method | 2019 | Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
| Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs). |
| AID1324643 | Drug metabolism in human liver microsomes assessed as R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide formation at 5 uM preincubated for 20 mins followed by NADPH addition measured after 120 | | | |
| AID1744052 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced macrophage level in BALF at 10 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1674260 | Inhibition of NLRP3 in mouse J774A.1 cells assessed as inhibition of LPS and nigericin-induced cleaved IL-1beta production at 300 nM pre-stimulated with LPS for 5 hrs before compound addition with ATP for 45 mins by Western blot analysis | 2020 | Journal of natural products, 07-24, Volume: 83, Issue:7
| Dehydrohispanolone Derivatives Attenuate the Inflammatory Response through the Modulation of Inflammasome Activation. |
| AID1743884 | Inhibition of NLRP3 in PMA-stimulated human THP-1 cells assessed as reduction in IL-1beta release at 2 uM pre-treated for 24 hrs followed by stimulation with LPS for 3 hrs and ATP for 1 hr by ELISA analysis | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Development of Novel Tetrahydroquinoline Inhibitors of NLRP3 Inflammasome for Potential Treatment of DSS-Induced Mouse Colitis. |
| AID1324639 | Drug metabolism in human liver microsomes assessed as R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide formation at 5 uM preincubated for 20 mins followed by NADPH addition measured after 120 | | | |
| AID1744042 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophils in BALF at 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744099 | Inhibition of NLRP3 inflammasome activation in LPS-primed human monocyte derived macrophages assessed as reduction in IL-1beta level preincubated for 30 mins followed by Pam3CSK4 addition and measured after 4 hrs by ELISA method | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744068 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced TGF-beta1 mRNA expression in lungs at 50 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by qRT-PCR analysis | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1527544 | Inhibition of NLRP3 in LPS/ATP-treated human monocyte derived macrophages assessed as reduction in NLRP3 inflammasome activation by measuring reduction in IL-1beta level by ELISA method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Development of small molecule inhibitors targeting NLRP3 inflammasome pathway for inflammatory diseases. |
| AID1743879 | Inhibition of NLRP3 in mouse BMDMs | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Development of Novel Tetrahydroquinoline Inhibitors of NLRP3 Inflammasome for Potential Treatment of DSS-Induced Mouse Colitis. |
| AID1677351 | Inhibition of NLRP3 in human THP1 cells assessed as inhibition of IL-1beta production | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor. |
| AID1744043 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced macrophages level in BALF at 10 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1286180 | Half life in C57BL/6 mouse at 3 mg/kg, iv administered as single dose | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Inhibiting the Inflammasome: A Chemical Perspective. |
| AID1744050 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophils in BALF at 10 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744051 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophils in BALF at 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1744063 | Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophil infiltration in lungs at 50 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by H and E staining based imaging analysis relative to contro | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice. |
| AID1866994 | Inhibition of NLRP3 inflammasome activation in LPS-primed mouse BMDM cells assessed as reduction in LPS/ATP induced cleaved IL-1beta release in supernatant at 10 uM preincubated for 30 mins followed by LPS addition for 3 hrs prior to ATP addition for 30 m | 2022 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 65 | Design and synthesis of an N-benzyl 5-(4-sulfamoylbenzylidene-2-thioxothiazolidin-4-one scaffold as a novel NLRP3 inflammasome inhibitor. |
| AID1617056 | Inhibition of LPS-induced serum IL-1beta production in C57BL/6 mouse at 10 mg/kg, ip pretreated before LPS challenge and measured after 2.5 hrs post LPS challenge by ELISA | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Discovery of Second-Generation NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization. |
| AID1907696 | Antiinflammatory activity in MSU-induced acute gout arthritis in NLRP3 knock out C57BL/6J mouse model assessed as reduction in paw swelling at 3 mg/kg, ip measured after 24 hrs relative to control | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| Synthesis and Pharmacological Evaluation of New |
| 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. |
| AID1345556 | Human NLRP3 (NOD-like receptor family) | 2015 | Nature medicine, Mar, Volume: 21, Issue:3
| A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |