Assay ID | Title | Year | Journal | Article |
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. |
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. |
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. |
AID149927 | Inhibition of [3H]-DADLE binding to Opioid receptor delta 1 of rat brain membranes | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
| Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists. |
AID150044 | The compound was tested for antagonist activity by selective inhibition of [35S]GTP-gamma-S, binding in Guinea pig caudate stimulated by SMC-80 (Opioid receptor delta 1) | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
| Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists. |
AID218773 | Tested for affinity against dopamine autoreceptor using [3H]apomorphine in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID256843 | Inhibition of DAMGO stimulated [35S]GTP-gamma-S binding to cloned human mu opioid receptor | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
| N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists. |
AID1188325 | Antagonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTPgammaS binding | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profil |
AID256845 | Inhibition of U69,593 stimulated [35S]GTP-gamma-S binding to cloned human kappa opioid receptor | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
| N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists. |
AID218772 | Tested for affinity against dopamine D1 receptor using [3H]SCH-23,390 in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID147884 | Inhibition of [35S]GTP-gamma-S, binding in guines pig caudate stimulated by DAMGO for Opioid receptor mu 1 | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
| 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
AID256844 | Inhibition of DPDPE stimulated [35S]GTP-gamma-S binding to cloned human delta opioid receptor | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
| N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists. |
AID303905 | Displacement of [3H]diprenorphine from cloned human mu opioid receptor expressed in CHO cells | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2. |
AID223599 | Antagonist activity towards U50 488 induced kappa opioid receptor by mouse writhing assay at 2.5 mg/kg subcutaneously | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID224587 | Binding affinity towards mu-opioid receptor by the displacement of [3H]Nal in rat brain homogenates | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID303906 | Displacement of [3H]diprenorphine from cloned human kappa opioid receptor expressed in CHO cells | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2. |
AID301032 | Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2007 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
| Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1. |
AID149435 | Inhibition of binding of [3H]U69, 593 to Opioid receptor kappa 1 in guinea pig membranes | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
| 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
AID223601 | Antagonism of bremazocine induced kappa receptor diuresis in rats at a concentration of 0.08 mg/kg subcutaneously | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID149431 | Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of guinea pig membranes | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
| Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists. |
AID223596 | Binding affinity towards kappa opioid receptor by displacement of [3H]EKC in guinea pig cortical tissue | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID301033 | Antagonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2007 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
| Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1. |
AID303908 | Antagonist activity at cloned human mu opioid receptor expressed in CHO cells assessed as inhibition of agonist-stimulated GTPgammaS binding | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2. |
AID151889 | Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
| Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists. |
AID218539 | Tested for affinity against beta-adrenergic using [3H]dihydroalprenolol in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID220523 | Tested for the opioid antagonist effect at delta-opioid receptor in isolated mouse vas deferens at 2 nM | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID1188323 | Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profil |
AID301034 | Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO cells in presence of high sodium by SPA | 2007 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
| Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1. |
AID301031 | Antagonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2007 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
| Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1. |
AID150034 | Inhibition of binding of [3H]DADLE to Opioid receptor delta 1 in guinea pig membranes | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
| 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
AID219804 | Tested for affinity against alpha-2-adrenergic using [3H]clonidine in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID148966 | Inhibition of [35S]GTP-gamma-S, binding in guines pig caudate stimulated by U69, 593 of Opioid receptor kappa 1 | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
| 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
AID225080 | Tested for affinity against phencyclidine using [3H]phencyclidine in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID1188324 | Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-stimulated [35S]GTPgammaS binding | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profil |
AID148057 | Inhibition of binding of [3H]DAMGO to Opioid receptor mu 1 in guinea pig membranes | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
| 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
AID229003 | Tested for affinity against serotonin 5-HT1 receptor using [3H]5-HT in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID1188320 | Binding affinity to human mu opioid receptor expressed in CHO cells | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profil |
AID1188321 | Binding affinity to human kappa opioid receptor expressed in CHO cells | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profil |
AID225381 | Tested for affinity against muscarinic acetylcholine using [3H]quinuclidinyl benzylate in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID224568 | Tested for the opioid antagonist effect at mu-opioid receptor in isolated guinea pig ileum at 2 nM | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID148182 | The compound was tested for antagonist activity by selective inhibition of [35S]GTP-gamma-S, binding to Opioid receptor mu 1 in Guinea pig caudate stimulated by DAMGO[mu] | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
| Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists. |
AID303909 | Antagonist activity at cloned human kappa opioid receptor expressed in CHO cells assessed as inhibition of agonist-stimulated GTPgammaS binding | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2. |
AID224576 | Antagonistic activity towards morphine induced mu-opioid receptor by mouse writhing assay at 1.25 mg/kg subcutaneously | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID64605 | Tested for affinity against dopamine D2 receptor using [3H]SCH-23390 in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID223594 | Tested for the opioid antagonist effect at kappa-opioid receptor in isolated guinea pig ileum at 2 nM | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID1188322 | Binding affinity to human delta opioid receptor expressed in CHO cells | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profil |
AID301036 | Displacement of [3H]bremazocine from human delta opioid receptor expressed in CHO cells in presence of high sodium by SPA | 2007 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
| Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1. |
AID303910 | Antagonist activity at cloned human delta opioid receptor expressed in CHO cells assessed as inhibition of agonist-stimulated GTPgammaS binding | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2. |
AID149552 | The compound was tested for antagonist activity by selective inhibition of [35S]GTP-gamma-S, binding in Guinea pig caudate stimulated by U69,593 to Opioid receptor kappa 1 | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
| Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists. |
AID220524 | Binding affinity towards delta-opioid receptor by displacement of [3H]DADL in rat brain homogenates | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID301035 | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells in presence of high sodium by SPA | 2007 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
| Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1. |
AID229004 | Tested for affinity against serotonin 5-HT2 receptor using [3H]SCH-23,390 (frontal cortex) in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID149761 | Inhibition of [35S]GTP-gamma-S, binding in guines pig caudate stimulated by SNC-80 to Opioid receptor delta 1 | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
| 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
AID303907 | Displacement of [3H]bremazocine from cloned human delta opioid receptor expressed in CHO cells | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
| Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2. |
AID176827 | Tested for concentration required to reduce the food consumption by 20 % subcutaneously | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID218970 | Tested for affinity against alpha-adrenergic using [3H]WB-4101 in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |