Assay ID | Title | Year | Journal | Article |
AID710366 | Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 15 mins prior to CGRP challenge measured after 30 mins by HTRF assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID1180717 | Antimigraine activity in migraine patient assessed as response rate for pain freedom at 150 mg after 2 hrs | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
| Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine. |
AID710349 | Inhibition of human recombinant CYP2D6 using 3-[2-(N,N-diethyl-Nmethylamino) ethyl]-7-methoxy-4-methylcoumarin as substrate after 45 mins by fluorescence assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710344 | Inhibition of human recombinant CYP3A4 using 7-benzyloxy-4-trifluoromethylcoumarin as substrate after 20 mins by fluorescence assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710363 | Half life in human liver microsomes | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID1180754 | Antimigraine activity in migraine patient assessed as pain relief incidence at 75 mg after 2 hrs (Rvb = 51.2%) | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
| Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine. |
AID710357 | Plasma concentration in Harlan marmoset at 7 mg/kg, sc at 15 mins | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID1180751 | Antimigraine activity in migraine patient assessed as pain freedom incidence at 75 mg after 2 hrs (Rvb = 15.3%) | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
| Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine. |
AID710348 | Inhibition of human recombinant CYP2A6 after 45 mins by fluorescence assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710353 | Oral bioavailability in overnight fasted cynomolgus monkey at 10 mg/kg administered as suspension of crystalline free base | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710346 | Inhibition of human recombinant CYP2E1 after 45 mins by fluorescence assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID1180752 | Antimigraine activity in migraine patient assessed as pain freedom incidence at 300 mg after 2 hrs (Rvb = 15.3%) | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
| Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine. |
AID710361 | Permeability of the compound at 100 uM at pH 5.5 after 4 hrs by PAMPA | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710339 | Toxicity in human up to 600 mg | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710364 | Aqueous solubility of the compound in crystalline form | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710365 | Fraction unbound in human plasma | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710340 | Genotoxicity in Salmonella typhimurium by Ames test | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710360 | Permeability of the compound at 100 uM at pH 7.4 after 4 hrs by PAMPA | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710345 | Inhibition of human ERG alpha subunit expressed in HEK293 cells at 10 to 30 uM | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710367 | Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cells after 2 hrs by gamma scintillation counter analysis | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710350 | Inhibition of human recombinant CYP2C9 using 7-methoxy-4-trifluoromethylcoumarin as substrate after 45 mins by fluorescence assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710355 | Oral bioavailability in fasted Sprague-Dawley rat at 10 mg/kg administered as solution | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710356 | Plasma concentration in Harlan marmoset at 7 mg/kg, sc after 60 to 105 mins | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710341 | Inhibition of L type calcium channel expressed in HEK293 cells at 10 to 30 uM | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710359 | Antagonist activity at CGRP receptor in Harlan marmoset assessed as inhibition of alphaCGRP-induced facial blood flow at 7 mg/kg, sc administered 45 mins interval for 2 hrs post alphaCGRP challenge measured after 60 to 105 mins by laser droppler flowmetry | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710352 | Inhibition of human recombinant CYP1A2 using 3-cyano-7-ethoxycoumarine as substrate after 45 mins by fluorescence assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710343 | Inhibition of human recombinant CYP3A4 using benzoylresorufin as substrate after 45 mins by fluorescence assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710358 | Antagonist activity at CGRP receptor in Harlan marmoset assessed as inhibition of CGRP-induced facial blood flow at 7 mg/kg, sc administered 45 mins interval for 2 hrs post alphaCGRP challenge measured at 15 mins by laser droppler flowmetry relative to co | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID1180755 | Antimigraine activity in migraine patient assessed as pain relief incidence at 300 mg after 2 hrs (Rvb = 51.2%) | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
| Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine. |
AID710351 | Inhibition of human recombinant CYP2C19 using 3-cyano-7-ethoxycoumarine as substrate after 45 mins by fluorescence assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710342 | Inhibition of L type sodium channel expressed in HEK293 cells at 10 to 30 uM | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710347 | Inhibition of human recombinant CYP2B6 after 45 mins by fluorescence assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
AID710354 | Oral bioavailability in overnight fasted cynomolgus monkey at 10 mg/kg administered as solution | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c |
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. |
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. |
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. |
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. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |