Assay ID | Title | Year | Journal | Article |
AID262760 | Displacement of [125I]BH-CCK-8S from human recombinant CCK2 receptor expressed in NIH3T3 cells | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors. |
AID183390 | Inhibition of pentagastrin-induced gastric acid secretion in anathesized rats at 0.1 uM/Kg upon intravenous administration | 1997 | Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
| (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist. |
AID312995 | Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Rationalizing the activities of diverse cholecystokinin 2 receptor antagonists using molecular field points. |
AID290979 | Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells | 2007 | Journal of medicinal chemistry, Jun-28, Volume: 50, Issue:13
| Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion. |
AID330893 | Binding affinity at human CCK2 receptor | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
| Achiral, selective CCK2 receptor antagonists based on a 1,3,5-benzotriazepine-2,4-dione template. |
AID290980 | Antagonist activity at CCK2 receptor in perfused rat stomach assessed as inhibition of pentagastrin-stimulated gastric acid secretion | 2007 | Journal of medicinal chemistry, Jun-28, Volume: 50, Issue:13
| Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion. |
AID290983 | Inhibition of pentagastrin-stimulated gastric acid secretion in conscious gastric fistula dog at 0.05 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jun-28, Volume: 50, Issue:13
| Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion. |
AID178226 | Inhibition of pentagastrin-induced gastric acid secretion in Dawley rats following intravenous administration | 1997 | Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
| (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist. |
AID262758 | Affinity for CCK2 receptor assessed by inhibition of pentagastrin-stimulated acid secretion in perfused rat stomach | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors. |
AID330894 | Binding affinity to human CCK1 receptor | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
| Achiral, selective CCK2 receptor antagonists based on a 1,3,5-benzotriazepine-2,4-dione template. |
AID262761 | Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors. |
AID290976 | Displacement of [3H]BH-CCK-8S from human recombinant CCK2 receptor expressed in NIH3T3 cells | 2007 | Journal of medicinal chemistry, Jun-28, Volume: 50, Issue:13
| Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion. |
AID290982 | Inhibition of pentagastrin-stimulated gastric acid secretion in conscious gastric fistula dog at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Jun-28, Volume: 50, Issue:13
| Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion. |
AID312994 | Antagonist activity at CCK2 receptor in stomach-lumen perfused immature rat | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Rationalizing the activities of diverse cholecystokinin 2 receptor antagonists using molecular field points. |
AID51448 | Inhibitory concentration against radioligand [125I]CCK-8 binding to gastrin/Cholecystokinin type B receptor from rat brain | 1997 | Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
| (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist. |
AID53046 | Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas | 1997 | Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
| (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist. |
AID59643 | Concentration required to inhibit pentagastrin-induced gastric acid secretion in heidenhain pouch dogs upon intravenous administration | 1997 | Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
| (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist. |
AID60209 | Compound at an peroral dose of 0.03 uM/Kg was tested for the inhibition of pentagastrin-induced gastric acid secretion in heidenhain pouch dogs | 1997 | Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
| (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist. |
AID60210 | Compound at an peroral dose of 0.1 uM/Kg was tested for the inhibition of pentagastrin-induced gastric acid secretion in heidenhain pouch dogs | 1997 | Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
| (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist. |
AID229347 | Ratio of inhibitory concentration; CCK-A receptor to CCK-B receptor | 1997 | Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
| (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist. |
AID59644 | Concentration required to inhibit pentagastrin-induced gastric acid secretion in heidenhain pouch dogs upon peroral administration | 1997 | Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
| (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist. |
AID1346883 | Human CCK2 receptor (Cholecystokinin receptors) | 1997 | Alimentary pharmacology & therapeutics, Feb, Volume: 11, Issue:1
| YF476 is a new potent and selective gastrin/cholecystokinin-B receptor antagonist in vitro and in vivo. |
AID1346883 | Human CCK2 receptor (Cholecystokinin receptors) | 2012 | Alimentary pharmacology & therapeutics, Jul, Volume: 36, Issue:2
| Single oral doses of netazepide (YF476), a gastrin receptor antagonist, cause dose-dependent, sustained increases in gastric pH compared with placebo and ranitidine in healthy subjects. |
AID1346809 | Rat CCK1 receptor (Cholecystokinin receptors) | 1997 | Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
| (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist. |
AID1346883 | Human CCK2 receptor (Cholecystokinin receptors) | 2002 | Regulatory peptides, Jan-15, Volume: 103, Issue:1
| Pharmacological analysis of CCK(2) receptor ligands using COS-7 and SK-N-MC cells, expressing the human CCK(2) receptor. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |