| Assay ID | Title | Year | Journal | Article |
|---|
| AID701485 | Antiinflammatory activity in po dosed rat assessed as inhibition of LPS-induced TNFalpha production administered 4 hrs prior to LPS-challenge measured after 1 to 1.5 hrs by ELISA relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701481 | Inhibition of human recombinant JNK2alpha2-mediated ATF-2 phosphorylation after 30 mins by immunoblotting method | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701478 | Inhibition of CYP2D6 | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701484 | Antiinflammatory activity in po dosed Lewis rat assessed as suppression of Mycobacterium tuberculosis adjuvant-induced paw edema administered QD from days 15 to 24 post adjuvant-challenge measured on day 25 relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701476 | Inhibition of CYP3A4 using midazolam as substrate | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701477 | Inhibition of CYP2C9 | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701491 | Permeability of the compound by PAMPA assay at pH 6.5 | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701492 | Total clearance in Sprague-Dawley rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701489 | Half life in Sprague-Dawley rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701488 | AUC in Sprague-Dawley rat at 1 mg/kg, po | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701474 | Solubility of the compound at pH 6.8 | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701487 | Oral bioavailability in Sprague-Dawley rat at 1 mg/kg | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701497 | Antiinflammatory activity in rat assessed as inhibition of LPS-induced TNFalpha production at 1 mg/kg, po administered 4 hrs prior to LPS-challenge measured after 1 to 1.5 hrs by ELISA relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701475 | Inhibition of human ERG by Rb ion flux assay | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701486 | Antiinflammatory activity in Lewis rat assessed as suppression of Mycobacterium tuberculosis adjuvant-induced paw edema at 1 mg/kg, po administered QD from days 15 to 24 post adjuvant-challenge measured on day 25 relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701480 | Inhibition of CYP1A2 | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701490 | Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701482 | Inhibition of human MAPK p38beta by Z'-LYTE assay | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701479 | Inhibition of CYP2C19 | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701496 | Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production after 20 hrs | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID701483 | Inhibition of human MAPK p38alpha by Z'-LYTE assay | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| 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. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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. |
| 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. |
| AID1347169 | Tertiary RLuc qRT-PCR qHTS assay 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. |
| AID1347157 | Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347161 | Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |