| Assay ID | Title | Year | Journal | Article |
|---|
| AID208600 | In vitro binding affinity towards Human Tachykinin receptor 1 | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID25451 | Area Under the concentration-time curve from zero time to 24 hr in guinea pig when given at a dose of 10 mg/kg perorally (Microemulsion) | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID28338 | Plasma concentration in Blood of guinea pig when given at a dose of 10 mg/kg perorally | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID211893 | In vitro binding affinity towards Human Tachykinin receptor 2 | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID26486 | Bioavailability in guinea pig (dose 10 mg/kg p.o.) | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID77105 | In vivo Effective peroral dose which inhibits Beta-ala8-Neurokinin A induced bronchoconstriction (dynamic compliance) in squirrel monkey | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID290025 | Antagonist activity at NK1 receptor in guinea pig trachea as inhibition of ASM-SP-induced bronchoconstriction | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
| Design and synthesis of 3,5-disubstituted benzamide analogues of DNK333 as dual NK1/NK2 receptor probes. |
| AID211523 | In vitro relative antagonist potency towards guinea pig Tachykinin receptor 2 | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID77104 | In vivo Effective peroral dose which inhibits Beta-ala8-Neurokinin A induced bronchoconstriction (airways resistance) in squirrel monkey | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID27212 | Half life period in guinea pig when given at a dose of 10 mg/kg perorally | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID208089 | In vitro binding affinity for Tachykinin receptor 1 of bovine retinal membranes using [3H]Sar9-substance P as radioligand | 2001 | Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
| Dual neurokinin NK(1)/NK(2) antagonists: N-[(R,R)-(E)-1-arylmethyl-3-(2-oxo-azepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamides and 3-[N'-3,5-bis(trifluoromethyl)benzoyl-N-arylmethyl-N'-methylhydrazino]-N-[(R)-2-oxo-azepan-3-yl]propion |
| AID290027 | Antagonist activity at NK2 receptor in guinea pig trachea as inhibition of [beta-Ala8]NKA(4-10)-induced bronchoconstriction | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
| Design and synthesis of 3,5-disubstituted benzamide analogues of DNK333 as dual NK1/NK2 receptor probes. |
| AID25453 | Area Under the concentration-time curve from zero time to 24 hr in guinea pig when given at a dose of 3 mg/kg intravenously | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID211705 | In vitro binding affinity for Tachykinin receptor 2 of human-CHO cells using 125 I-NKA radioligand | 2001 | Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
| Dual neurokinin NK(1)/NK(2) antagonists: N-[(R,R)-(E)-1-arylmethyl-3-(2-oxo-azepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamides and 3-[N'-3,5-bis(trifluoromethyl)benzoyl-N-arylmethyl-N'-methylhydrazino]-N-[(R)-2-oxo-azepan-3-yl]propion |
| AID290026 | Antagonist activity at NK2 receptor in guinea pig trachea as inhibition of [beta-Ala8]NKA(4-10)-induced bronchoconstriction relative to control | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
| Design and synthesis of 3,5-disubstituted benzamide analogues of DNK333 as dual NK1/NK2 receptor probes. |
| AID208246 | In vitro relative antagonist potency towards guinea pig Tachykinin receptor 1 | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID27213 | Half life period in guinea pig when given at a dose of 3 mg/kg intravenously | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID25452 | Area Under the concentration-time curve from zero time to 24 hr in guinea pig when given at a dose of 10 mg/kg perorally (cremophor) | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
| Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
| AID290024 | Antagonist activity at NK1 receptor in guinea pig trachea as inhibition of ASM-SP-induced bronchoconstriction relative to control | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
| Design and synthesis of 3,5-disubstituted benzamide analogues of DNK333 as dual NK1/NK2 receptor probes. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |