Assay ID | Title | Year | Journal | Article |
AID1200060 | Solubility of the compound in phosphate buffer at pH 6.5 incubated for 1 hr with stirring followed by 2 hrs of shaking by Lysa assay | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
| Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. |
AID1721645 | Displacement of [3H]AVP from human V1a receptor expressed in 1132N1 cells assessed as dissociation constant by radioligand binding assay | 2020 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18
| New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives. |
AID1820294 | Displacement of [3H]-labelled arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes at 1 uM incubated for 60 mins by radioligand binding assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Synthesis and Characterization of New V |
AID1200054 | Antagonist activity at human vasopressin 1a receptor expressed in CHO cells assessed as inhibition of vasopressin-induced calcium flux preincubated for 20 mins followed by vasopressin induction measured for 5 mins by FLIPR assay | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
| Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. |
AID1721653 | Efflux ratio of Apparent permeability across apical to basolateral side in human Caco-2 cells at 10 uM by HPLC-UV or UHPLC-MS/MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18
| New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives. |
AID1820285 | Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Synthesis and Characterization of New V |
AID1200063 | Volume of distribution at steady state in mouse at 2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
| Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. |
AID1200058 | Selectivity ratio of Ki for human vasopressin V2 receptor to Ki for human vasopressin 1a receptor | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
| Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. |
AID1721646 | Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay | 2020 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18
| New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives. |
AID1200064 | Clearance in mouse at 2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
| Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. |
AID1820284 | Displacement of [3H]-arginine-vasopressin from human V1A receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Synthesis and Characterization of New V |
AID1200055 | Displacement of [3H]-vasopressin from mouse vasopressin 1a receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
| Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. |
AID1721647 | Metabolic stability in human liver microsomes assessed as intrinsic clearance at 1 uM in presence of NADPH by HPLC-UV analysis | 2020 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18
| New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives. |
AID1200052 | Displacement of [3H]-vasopressin from human vasopressin 1a receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
| Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. |
AID1560508 | Half life in iv dosed human | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
| Discovery of Balovaptan, a Vasopressin 1a Receptor Antagonist for the Treatment of Autism Spectrum Disorder. |
AID1200061 | Activity at human P-gp assessed as drug transport | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
| Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. |
AID1200062 | Ratio of drug level in brain to plasma in mouse at 10 mg/kg, po | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
| Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. |
AID1721651 | Apparent permeability across apical to basolateral side in human Caco-2 cells at 10 uM by HPLC-UV or UHPLC-MS/MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18
| New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives. |
AID1721648 | Metabolic stability in Wistar rat liver microsomes assessed as intrinsic clearance at 1 uM in presence of NADPH by HPLC-UV analysis | 2020 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18
| New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives. |
AID1721649 | Metabolic stability in NMRI mouse liver microsomes assessed as intrinsic clearance at 1 uM in presence of NADPH by HPLC-UV analysis | 2020 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18
| New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives. |
AID1200059 | Selectivity ratio of Ki for human oxytocin receptor to Ki for human vasopressin 1a receptor | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
| Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. |
AID1426367 | Antagonist activity at human vasopressin 1a receptor | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
| Recent Advances in Scaffold Hopping. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |