| Assay ID | Title | Year | Journal | Article |
|---|
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347154 | Primary screen GU AMC 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. |
| AID11812 | Maximum plasma concentration after 20 mg/kg oral administration in rat | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
| Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus. |
| AID513692 | Selectivity ratio of Ki for human oxytocin receptor Ki for human vasopressin V1a receptor | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID513683 | Displacement of [3H]-oxytocin from oxytocin receptor in rat uterus tissue | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID217518 | Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donors | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| 1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist. |
| AID8559 | Compound was tested for plasma clearance in dog | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID458560 | Displacement of [3H]AVP from human vasopressin V1a receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID458555 | Activity at human oxytocin receptor expressed in CHO cells assessed as inositol phosphate accumulation at 1 uM | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID458559 | Activity at human oxytocin receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID513689 | Inhibition of oxytocin-induced uterine contraction in intraduodenally dosed rat | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID10106 | Compound was tested for its half life in dog | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID458577 | Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID217237 | Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in rat liver | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| 1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist. |
| AID151932 | Binding affinity for rat uterine oxytocin receptor (rOTr) | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9
| Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency. |
| AID513682 | Displacement of [3H]-oxytocin from oxytocin receptor in human uterus tissue | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID151800 | Binding affinity was evaluated by measuring the displacement of [3H]OT (oxytocin) from specific binding sites in uterine tissue obtained from human | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| 1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist. |
| AID169600 | Compound tested in vivo for antagonist potency against oxytocin (OT)-induced contractions in rat uterus by iv administration | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9
| Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency. |
| AID151955 | Compound was tested for displacement of 3[H] oxytocin from rat OT receptor (in vitro) | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID151807 | Displacement of 3[H]oxytocin from human oxytocin receptor | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID458564 | Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID12271 | Compound was tested for its half life in rat | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID151803 | Binding affinity against cloned human oxytocin receptor from human embryonic kidney cells | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
| Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus. |
| AID203500 | Compound was tested for Serum albumin binding | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID217396 | Binding affinity towards human kidney Vasopressin V2 receptor by using functional assay | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9
| Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency. |
| AID13202 | Bioavailability in rat | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID458562 | Activity at human vasopressin V1a receptor expressed in CHO cells assessed as inositol phosphate accumulation at 1 uM | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID365930 | Antagonist activity at human cloned oxytocin receptor by cell based beta lactamase reporter assay | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Design and optimization of potent, selective antagonists of Oxytocin. |
| AID513686 | Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID513693 | Selectivity ratio of Ki for human oxytocin receptor Ki for human vasopressin V2 receptor | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID24181 | Compound was tested for its lipophilicity | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID513687 | Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID151794 | Tested for ratio of displacement of 3H oxytocin from human OT in presence and absence of 50 mg/mL human serum albumin | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID217089 | Binding affinity towards human Vasopressin V1a receptor by using functional assay | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9
| Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency. |
| AID151796 | Binding affinity for cloned human oxytocin receptor (OT-R) | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
| Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines. |
| AID9152 | Bioavailability in dog | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID13193 | Oral bioavailability in rat (dose 20 mg/kg) | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9
| Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency. |
| AID458567 | Activity at human vasopressin V2 receptor expressed in CHO cells assessed as inhibition of agonist-induced cAMP accumulation | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID458576 | Activity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID217690 | Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| 1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist. |
| AID10988 | Compound was tested for plasma clearance in rat | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID151799 | Binding affinity for human oxytocin receptor | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9
| Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency. |
| AID151808 | Ability to displace [3H]oxytocin from human OT receptor (hOT) | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives. |
| AID180486 | Serum concentration for 50% inhibition of uterine contractility response to oxytocin in rat | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID458556 | Activity at human oxytocin receptor expressed in CHO cells assessed as inhibition of agonist-induced inositol phosphate accumulation | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID217090 | Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in human platelets | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| 1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist. |
| AID10423 | Half life period after 3 mg/kg iv administration in the rat | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
| Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus. |
| AID513697 | Oral bioavailability in rhesus monkey | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID513684 | Displacement of [3H]vasopressin from vasopressin V1a receptor in human liver tissue | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID169603 | Compound was evaluated for its ability to antagonize rat OT-induced uterine contractile response in the vehicle treated group by 50% | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
| Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus. |
| AID12270 | Compound was evaluated in vivo in rat for the plasma half-life at a oral dose of 20 mg/kg experiment by using concentration vs time curve | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9
| Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency. |
| AID458553 | Displacement of [3H]AVP from human oxytocin receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID151933 | Binding affinity was evaluated by measuring the displacement of [3H]-OT (oxytocin) from specific binding sites in uterine tissue obtained from rats | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| 1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist. |
| AID513685 | Displacement of [3H]vasopressin from vasopressin V1a receptor in rat liver tissue | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID458566 | Activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation at 1 uM | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID513688 | Inhibition of oxytocin-induced uterine contraction in iv dosed rat | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID12976 | Oral bioavailability in rat | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
| Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus. |
| AID195731 | Binding affinity against oxytocin receptor (rOTr) in DES pretreated rat uterine | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
| Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus. |
| AID458578 | Activity at human vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced inositol phosphate accumulation at 1 uM | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. |
| AID513690 | Oral bioavailability in rat | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Oral oxytocin antagonists. |
| AID217219 | Compound was tested for its ability to displace vasopressin from human Vasopressin V1a receptor | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives. |
| AID169601 | Compound tested in vivo for antagonist potency against oxytocin (OT)-induced in rats by id administration | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9
| Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency. |
| AID1346469 | Human OT receptor (Vasopressin and oxytocin receptors) | 2005 | British journal of pharmacology, Nov, Volume: 146, Issue:5
| Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |