| Assay ID | Title | Year | Journal | Article |
|---|
| AID361798 | Displacement of [I125]CGRP from marmoset CGRP receptor | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361849 | Inhibition of human ERG at 30 uM | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361834 | Total AUC in New Zealand white rabbit at 0.1 mg/kg, intranasally | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361843 | Bioavailability in sc dosed Sprague-Dawley rat in presence of PBS vehicle | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361820 | Inhibition of human alpha CGRP-induced increase in facial blood flow in marmoset at 0.01 mg/kg, sc after 15 mins by laser Doppler flowmetry | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361815 | Ex vivo reversal of human alpha CGRP-induced artery dilation in human intracranial artery | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361823 | Oral bioavailability in cynomolgus monkey | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361831 | Half life in New Zealand white rabbit at 0.5 mg/kg, iv | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361818 | Inhibition of human alpha CGRP-induced increase in facial blood flow in marmoset at 0.03 mg/kg, sc after 15, 60 and 105 mins by laser Doppler flowmetry | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID754778 | Toxicity in Sprague-Dawley rat assessed as nasal irritation at 175 mg/mL administered intranasally for 7 days | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migr |
| AID361801 | Inhibition of human recombinant CYP2C19 expressed in insect microsomes | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361802 | Inhibition of human recombinant CYP2C9 expressed in insect microsomes | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID1281303 | Permeability of compound by PAMPA | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
| Synthesis and SAR of calcitonin gene-related peptide (CGRP) antagonists containing substituted aryl-piperazines and piperidines. |
| AID361836 | Cmax in New Zealand white rabbit at 0.3 mg/kg, intranasally | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361840 | Drug level in New Zealand white rabbit after 24 hrs | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID375828 | Oxidative stability assessed as compound remaining in water at 0.15 mg/mL at pH 4 after 48 hrs in presence of free radical generator AAPH | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability. |
| AID361811 | Selectivity for human CGRP receptor over adrenomedullin 2 receptor | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID1281304 | Permeability of compound across apical to basolateral side in human Caco2 cells | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
| Synthesis and SAR of calcitonin gene-related peptide (CGRP) antagonists containing substituted aryl-piperazines and piperidines. |
| AID362055 | Antagonist activity at human CGRP receptor in SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361800 | Inhibition of human recombinant CYP1A2 expressed in insect microsomes | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361838 | Total AUC in New Zealand white rabbit at 0.3 mg/kg, intranasally | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361830 | Volume of distribution at steady state in New Zealand white rabbit at 0.5 mg/kg, iv | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361824 | Intrinsic permeability across human Caco-2 cells | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361812 | Selectivity for human CGRP receptor over human calcitonin receptor | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361805 | Displacement of [I125]AM from adrenomedullin 1 receptor expressed in CHO cells | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361847 | Inhibition of CYP2D6-mediated metabolism of dextromethorphan in human liver microsomes | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361794 | Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361837 | Tmax in New Zealand white rabbit at 0.3 mg/kg, intranasally | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361829 | Clearance in New Zealand white rabbit at 0.5 mg/kg, iv | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID375822 | Hydrolytic stability assessed as formation of (R)-2-(4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)piperidine-1-carboxamido)-3-(7-methyl-1H-indazol-5-yl)propanoic acid in 0.05 M buffer at pH 5 after 12 weeks | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability. |
| AID772961 | Permeability of the compound by PAMPA method at pH 7.4 | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists. |
| AID375827 | Hydrolytic stability assessed as compound remaining in water at 0.15 mg/mL at pH 4 after 4 weeks | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability. |
| AID361807 | Displacement of [125I]calcitonin from calcitonin receptor in human T47D cells | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361844 | Bioavailability in sc dosed cynomolgus monkey | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361814 | Selectivity for human CGRP receptor over amylin 3 receptor | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361842 | Bioavailability in sc dosed Sprague-Dawley rat in presence of PG:D5W vehicle | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361821 | Inhibition of human alpha CGRP-induced increase in facial blood flow in marmoset at 0.003 mg/kg, sc by laser Doppler flowmetry | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID736591 | Inhibition of CYP3A4 (unknown origin) using 7-benzyloxy-4-trifluoromethylcoumarin as substrate | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
| The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2. |
| AID361828 | Total AUC in New Zealand white rabbit at 0.5 mg/kg, iv | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361806 | Displacement of [I125]AM from adrenomedullin 2 receptor expressed in CHO cells | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID736592 | Inhibition of CYP3A4 (unknown origin) using 7-benzyloxy-resorufin as substrate | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
| The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2. |
| AID361833 | Tmax in New Zealand white rabbit at 0.1 mg/kg, intranasally | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID772965 | Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists. |
| AID361835 | Bioavailability in New Zealand white rabbit at 0.1 mg/kg, intranasally | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID375824 | Hydrolytic stability assessed as formation of 8-fluoro-3-(piperidin-4-yl)-3,4-dihydroquinazolin-2(1H)-one in 0.05 M buffer at pH 5 after 12 weeks | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability. |
| AID361808 | Displacement of [I125]AMY from amylin 1 receptor expressed in CHO cells | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361817 | Ex vivo effect on basal artery tension in human coronary artery assessed as contractility | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361827 | Tmax in New Zealand white rabbit at 0.5 mg/kg, iv | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361822 | Oral bioavailability in Sprague-Dawley rat | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID658193 | Displacement of [I125]CGRP from CGRP receptor in human SK-N-MC cell membrane after 2 hrs by gamma or scintillation counting | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group. |
| AID754777 | Toxicity in Sprague-Dawley rat assessed as nasal irritation at 75 mg/mL administered intranasally for 7 days | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migr |
| AID361816 | Ex vivo inhibition of human alpha CGRP-induced artery dilation in human intracranial artery preincubated for 30 mins | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361841 | Bioavailability in intratracheally dosed Sprague-Dawley rat | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361813 | Selectivity for human CGRP receptor over amylin 1 receptor | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361846 | Inhibition of human recombinant CYP2D6 expressed in insect microsomes by AMMC assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361839 | Bioavailability in New Zealand white rabbit at 0.3 mg/kg, intranasally | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361845 | Fraction unbound in human serum at 10 uM | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361848 | Inhibition of human recombinant CYP3A4 expressed in insect microsomes assessed as metabolism of testosterone | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361826 | Cmax in New Zealand white rabbit at 0.5 mg/kg, iv | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361796 | Inhibition of recombinant CYP3A4 expressed in insect microsomes after 20 mins in presence of BFC substrate | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361825 | Aqueous solubility of compound at pH 1 to 6.8 | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361819 | Inhibition of human alpha CGRP-induced increase in facial blood flow in marmoset at 0.01 mg/kg, sc after 60 and 105 mins by laser Doppler flowmetry | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID754796 | Antagonist activity at human CGRP receptor | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migr |
| AID361795 | Inhibition of recombinant CYP3A4 expressed in insect microsomes after 45 mins in presence of BZR substrate | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361809 | Displacement of [I125]AMY from amylin 3 receptor expressed in CHO cells | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361810 | Selectivity for human CGRP receptor over adrenomedullin 1 receptor | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID375823 | Oxidative stability assessed as formation of N-((R)-1-(1,4'-bipiperidin-1'-yl)-3-(7-methyl-1H-indazol-5-yl)-1-oxopropan-2-yl)-4-(8-fluoro-4-hydroxy-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)piperidine-1-carboxamide in 0.05 M buffer at pH 5 after 12 weeks | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability. |
| AID736593 | Binding affinity to CGRP receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
| The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2. |
| AID361799 | Displacement of [I125]CGRP from rat CGRP receptor | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| AID361832 | Cmax in New Zealand white rabbit at 0.1 mg/kg, intranasally | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptid |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |