| Assay ID | Title | Year | Journal | Article |
|---|
| AID608510 | Antiarthritic activity in rat assessed as inhibition of Freund-s adjuvant-induced paw swelling at 10 mg/kg, po bid administered 11 day after adjuvant challenge for 20 days | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors. |
| AID758207 | Selectivity ratio of IC50 for p38beta (unknown origin) to IC50 for p38alpha (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
| The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode. |
| AID1251183 | Bioavailability in Sprague-Dawley rat at 10 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID1251184 | Bioavailability in Sprague-Dawley rat at 100 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID515679 | AUC (0 to 24 hrs) in Sprague-Dawley rat at 2.5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID1251176 | AUC in Sprague-Dawley rat at 1 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID1251219 | Stability in pH 6.5 solution | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID758206 | Inhibition of p38beta (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
| The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode. |
| AID515673 | Cmax in Sprague-Dawley rat at 2.5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515658 | Mutagenic activity in Salmonella Typhimurium TA98 by Ames test in presence of S9 fraction | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515687 | Selectivity ratio of p38alpha over p38beta | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515639 | Selectivity ratio of p38alpha over p38delta | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID1251220 | Drug level in basal side of human Caco2 cells assessed as BMS-582949 level incubated at 37 degC for 2 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID748818 | AUC (0 to 24 hrs) in rat at 10 mg/kg, po administered with 1:1 PEG 300/water as vehicle | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38α inhibitor. |
| AID515657 | Mutagenic activity in Salmonella Typhimurium TA100 by Ames test in presence of S9 fraction | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515654 | Selectivity ratio of p38alpha over serine kinase | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515670 | Volume of distribution at steady state in BALB/c mouse at 5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515663 | Antiinflammatory effect in Freund's complete adjuvant-induced Lewis rat arthritis model assessed as reduction of paw swelling at 10 mg/kg, po qd administered on day 11 post adjuvant challenge measured repeated 3 times per week by volume displacement pleth | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515647 | Inhibition of CYP2C9 | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID1251193 | Bioavailability in cynomolgus monkey at 10 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID515686 | Selectivity ratio of p38alpha over Raf | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515666 | Tmax in BALB/c mouse at 5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515649 | Metabolic stability in human hepatocytes assessed as metabolic rate per million cells | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID1251218 | Stability in pH 1.2 solution | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID1251158 | Cmax in Sprague-Dawley rat at 10 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID1251177 | AUC in Sprague-Dawley rat at 10 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID515665 | Antiinflammatory effect in Freund's complete adjuvant-induced Lewis rat arthritis model assessed as reduction of paw swelling at 0.3 mg/kg, po bid administered on day 11 post adjuvant challenge measured repeated 3 times per week by volume displacement ple | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515671 | AUC (0 to 8 hrs) in BALB/c mouse at 5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515644 | Inhibition of CYP3A4 | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515682 | Metabolic stability in human liver microsomes assessed as metabolic rate | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID1251199 | Inhibition of paw swelling in Lewis rat adjuvant arthritis model assessed as reduction in hind paw volume at 3 mg/kg, po bid beginning on day 11 post adjuvant challenge by volume displacement plethysmometry method relative to control | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID515652 | Selectivity ratio of p38alpha over nonreceptor tyrosine kinase | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515661 | Antiinflammatory activity in BALB/c mouse serum assessed as inhibition of LPS-induced TNFalpha production at 5 mg/kg, po administered 2 hrs before LPS challenge measured after 90 mins by ELISA | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515650 | Inhibition of CYP1A2 | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID1251202 | AUC (0 to 24 hrs) in Lewis rat adjuvant arthritis model at 1 mg/kg, po bid beginning on day 11 post adjuvant challenge | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID1251194 | Inhibition of LPS-induced TNFalpha level in Lewis rat at 0.03 to 10 mg/kg, po dosed 1 hr before LPS challenge and measured 90 mins post LPS challenge by ELISA method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID1251187 | Cmax in cynomolgus monkey at 10 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID748820 | Tmax in rat at 10 mg/kg, po administered with 1:1 PEG 300/water as vehicle | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38α inhibitor. |
| AID515642 | Selectivity ratio of p38alpha over receptor tyrosine kinase | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515645 | Permeability of the compound in human Caco-2 cells | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID1251182 | Bioavailability in Sprague-Dawley rat at 1 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID1251190 | AUC in cynomolgus monkey at 10 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID515678 | Volume of distribution at steady state in Sprague-Dawley rat at 2.5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515655 | Inhibition of Cytochrome P450 in human liver | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515664 | Antiinflammatory effect in Freund's complete adjuvant-induced Lewis rat arthritis model assessed as reduction of paw swelling at 1 to 5 mg/kg, po bid administered on day 11 post adjuvant challenge measured repeated 3 times per week by volume displacement | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515672 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID748814 | Tmax in rat at 100 mg/kg, po administered in 0.75% methocel vehicle as suspension | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38α inhibitor. |
| AID515677 | Clearance in Sprague-Dawley rat at 2.5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515653 | Inhibition of human ERG at 30 uM | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515676 | Mean residence time in Sprague-Dawley rat at 2.5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515641 | Protein binding in human serum | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515635 | Oral bioavailability in BALB/c mouse at 10 mg/kg | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515675 | Half life in Sprague-Dawley rat at 2.5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID1251159 | Cmax in Sprague-Dawley rat at 1 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID515681 | Metabolic stability in rat liver microsomes assessed as metabolic rate | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID1251178 | AUC in Sprague-Dawley rat at 100 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID1251172 | Cmax in Sprague-Dawley rat at 100 mg/kg, po after 24 hrs by LC/MS/MS method | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID515659 | Inhibition of bacterially expressed p38alpha pretreated for 10 mins measured after 45 mins | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515648 | Inhibition of CYP2C19 | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID748817 | Cmax in rat at 10 mg/kg, po administered with 1:1 PEG 300/water as vehicle | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38α inhibitor. |
| AID1251216 | Drug level in apical side of human Caco2 cells assessed as BMS-582949 level incubated at 37 degC for 2 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID515684 | Metabolic stability in rat hepatocytes assessed as metabolic rate per million cells | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515668 | Mean residence time in BALB/c mouse at 5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515680 | Metabolic stability in mouse liver microsomes assessed as metabolic rate | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID608410 | Antiinflammatory activity in BALB/c mouse assessed as inhibition of LPS-induced TNFalpha production at 5 mg/kg, po administered 2 hrs before LPS challenge measured after 90 mins by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors. |
| AID515669 | Clearance in BALB/c mouse at 5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID1251203 | AUC (0 to 24 hrs) in Lewis rat adjuvant arthritis model at 3 mg/kg, po bid beginning on day 11 post adjuvant challenge | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID1540358 | Inhibition of P38alpha MAPK (unknown origin) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of potent p38α MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation. |
| AID515656 | Genotoxicity in Escherichia coli by SOS-ChromoTest | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515637 | Antiinflammatory effect in Freund's complete adjuvant-induced Lewis rat arthritis model assessed as reduction of paw swelling at 100 mg/kg, po qd administered on day 11 post adjuvant challenge measured repeated 3 times per week by volume displacement plet | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515662 | Antiinflammatory activity in BALB/c mouse serum assessed as inhibition of LPS-induced TNFalpha production at 5 mg/kg, po administered 6 hrs before LPS challenge measured after 90 mins by ELISA | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID748811 | AUC (0 to 24 hrs) in rat at 100 mg/kg, po administered in 0.75% methocel vehicle as suspension | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38α inhibitor. |
| AID515640 | Protein binding in rat serum | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515643 | Protein binding in mouse serum | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515674 | Tmax in Sprague-Dawley rat at 2.5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515646 | Inhibition of CYP2D6 | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515636 | Cmax in BALB/c mouse at 5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515660 | Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production treated 30 mins before LPS challenge measured after 6 hrs by ELISA | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515651 | Selectivity ratio of p38alpha over p38-gamma | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515683 | Metabolic stability in mouse hepatocytes assessed as metabolic rate per million cells | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID748812 | Cmax in rat at 100 mg/kg, po administered in 0.75% methocel vehicle as suspension | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38α inhibitor. |
| AID515638 | Antiinflammatory effect in Freund's complete adjuvant-induced Lewis rat arthritis model assessed as reduction of paw swelling administered as po qd on day 11 post adjuvant challenge measured repeated 3 times per week by volume displacement plethysmometry | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID515667 | Half life in BALB/c mouse at 5 mg/kg, iv and 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID1251198 | Inhibition of paw swelling in Lewis rat adjuvant arthritis model assessed as reduction in hind paw volume at 1 mg/kg, po bid beginning on day 11 post adjuvant challenge by volume displacement plethysmometry method relative to control | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor. |
| AID515685 | Selectivity ratio of p38alpha over Jnk2 | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| 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. |
| AID1345304 | Human mitogen-activated protein kinase 14 (p38 subfamily) | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |