Assay ID | Title | Year | Journal | Article |
AID130271 | Ratio of IC50 of morphine (agonist) expossed to the compound for 10 min and then washed 30 times to Ratio of IC50 of morphine (agonist) prior to exposure to compound | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID270158 | Intrinsic activity at mu opioid receptor in presence of 1 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
AID232963 | Ke selectivity ratio (mu/delta) of the compound | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
AID270160 | Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
AID270161 | Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP relative to control | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
AID148775 | Reversible opioid agonist activity in the electrically stimulated mouse vas deferens(MVD) at 1 uM concentration | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID148102 | The compound was evaluated for binding affinity against the opioid receptor kappa in guinea pig brain membranes using [3H]- U-69,593 | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
| Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
AID270157 | Agonist activity at delta opioid receptor at 31.6 uM | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
AID148488 | Reversible opioid agonist activity in the electrically stimulated guinea pig ileum(GPI) at 1 uM concentration (Exp 1) | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID232962 | Ke selectivity ratio (kappa/delta) of the compound | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
AID148237 | Binding affinity towards opioid receptor delta 1 expressed in CHO cells was determined by using [3H]DPDPE as radioligand | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
| Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
AID149023 | Selectivity for mu to delta opioid receptors was determined | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
| Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
AID148815 | Ratio of IC50 of ethylketazocine (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in absence of compound for Opioid receptor kappa 1 at 1 uM in GPI assay | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID148835 | Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for Opioid receptor kappa 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID149192 | Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of opioid receptor delta | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID149907 | Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of Opioid receptor delta 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID150831 | Ability to inhibit agonist-stimulated (DAMGO) [35S]GTP-gamma-S, binding, using cloned human Opioid receptor mu 1 expressed in CHO cells | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
| Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
AID147876 | Ability to inhibit agonist-stimulated (U69,593) [35S]GTP-gamma-S, binding, using cloned human Opioid receptor kappa 1 expressed in CHO cells | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
| Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
AID148788 | Ratio of IC50 of DADLE (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in the absence of compound for Opioid receptor delta 1 at 10 uM in MVD assay | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID233951 | Ratio of IC50 against mu opioid receptor to that of delta opioid receptor | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors. |
AID1237283 | Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay relative to control | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
| Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists. |
AID232965 | Ki selectivity ratio (mu/delta) of the compound | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
AID270159 | Intrinsic activity at kappa opioid receptor in presence of 1 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
AID148254 | Evaluation for the ability of kappa opioid to protect the [3H]-DAMGO binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
| 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
AID149881 | Ratio of IC50 of morpholine (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in absence of compound for Opioid receptor mu 1 at 1 uM in GPI assay | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID150010 | Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for Opioid receptor mu 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID148930 | Compound was evaluated for antagonist potency in the mouse vas deferens preparation using [D-Ala2,D-Leu5]enkephalin (Opioid receptor delta 1) | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
AID151141 | Ratio of IC50 of morpholine (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in absence of compound for Opioid receptor mu 1 at 1 uM in MVD assay | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID130268 | Ratio of IC50 of DADLE (agonist) expossed to the compound for 10 min and then washed 30 times to Ratio of IC50 of morphine (agonist) prior to exposure to compound | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID233662 | Selectivity ratio of agonist stimulated [35S]GTP-gamma-S, binding in cloned human kappa-opioid receptor versus delta-opioid receptor | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
| Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
AID148523 | Binding affinity was measured in cloned Opioid receptor delta 1 expressed in CHO cells using [3H]- DPDPE as radioligand. | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors. |
AID149279 | Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of Opioid receptor kappa 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID149367 | Evaluation for the ability of delta opioid to protect the [3H]-DAMGO binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
| 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
AID149283 | Compound was evaluated for binding affinity of Opioid receptor kappa 1 in guinea pig brain membranes | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
AID148098 | Ability to inhibit agonist-stimulated (DPDPE) [35S]GTP-gamma-S, binding, using cloned human opioid receptor delta 1 expressed in CHO cells | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
| Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
AID147964 | Opioid receptor kappa antagonistic activity was measured by the displacement of ethylketazocine in the guinea pig ileum at a concentration of 100 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID151284 | Binding affinity was measured in cloned Opioid receptor mu 1 expressed in CHO cells using [3H]- DAMGO as radioligand. | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors. |
AID151142 | Ratio of IC50 of morpholine (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in absence of compound for Opioid receptor mu 1 at 10 uM in GPI assay | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID233663 | Selectivity ratio of agonist stimulated [35S]GTP-gamma-S, binding in cloned human mu-opioid receptor versus delta-opioid receptor | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
| Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
AID270155 | Selectivity for human cloned delta opioid receptor over mu opioid receptor | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
AID148489 | Reversible opioid agonist activity in the electrically stimulated guinea pig ileum(GPI) at 1 uM concentration (Exp 2) | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID148040 | Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of Opioid receptor mu 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID138825 | Evaluation for the ability of mu opioid to protect the [3H]DAMGO binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
| 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
AID270153 | Antagonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 10 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
AID270156 | Selectivity for human cloned delta opioid receptor over kappa opioid receptor | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
AID148998 | Opioid receptor mu antagonistic activity was measured by the displacement of morphine in the guinea pig ileum at a concentration of 100 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID149872 | Opioid receptor mu 1 antagonistic activity was measured by the displacement of morphine in the guinea pig ileum at a concentration of 100 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID149910 | Compound was evaluated for binding affinity at Opioid receptor delta 1 in guinea pig brain membranes | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
AID148961 | Compound was evaluated for antagonist potency in guinea pig ileum preparation using ethylketazocine (Opioid receptor kappa 1) | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
AID148787 | Ratio of IC50 of DADLE (agonist) after 10 min of incubation along with compound (antagonist) and IC50 of agonist in the absence of compound for Opioid receptor delta 1 at 1 uM in MVD assay | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID149011 | Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of opioid receptor mu | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID148662 | Opioid receptor delta 1 antagonistic activity was measured by the displacement of DADLE in the mouse vas deferens at a concentration of 100 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID232964 | Ki selectivity ratio (kappa/delta) of the compound | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
AID270154 | Antagonist activity at human cloned kappa opioid receptor expressed in CHO cells assessed as inhibition of U69593-stimulated [35S]GTPgammaS binding in presence of 10 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
AID270152 | Antagonist activity at human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTP-gamma-S binding in presence of 10 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
AID147978 | Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of opioid receptor kappa | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID147839 | Selectivity for kappa to delta opioid receptors was determined | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
| Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
AID150029 | Compound was evaluated for antagonist potency in guinea pig ileum preparation using morphine (Opioid receptor mu 1) | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
AID310938 | Agonist activity at rat delta opioid receptor expressed in C6 cells assessed as stimulation of [35S]GTP-gamma-S binding relative to BW373U86 | 2007 | Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
| Quantitative conformationally sampled pharmacophore for delta opioid ligands: reevaluation of hydrophobic moieties essential for biological activity. |
AID148774 | Reversible opioid agonist activity in the electrically stimulated mouse vas deferens(MVD) at 10 uM of concentration | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
| Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogues as irreversible antagonists of the delta opioid receptor. |
AID310939 | Displacement of [3H]naltrindole from rat delta opioid receptor expressed in C6 cells | 2007 | Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
| Quantitative conformationally sampled pharmacophore for delta opioid ligands: reevaluation of hydrophobic moieties essential for biological activity. |
AID233705 | Selectivity ratio was determined from Ke value of Opioid receptor kappa 1 and Opioid receptor delta 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID148693 | Opioid receptor kappa 1 antagonistic activity was measured by the displacement of ethylketazocine in the guinea pig ileum at a concentration of 100 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID148041 | Compound was evaluated for binding affinity at Opioid receptor mu 1 in guinea pig brain membranes | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
AID233878 | Selectivity ratio was determined from Ke value of Opioid receptor mu 1 and Opioid receptor delta 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID149020 | The compound was evaluated for binding affinity against opioid receptor mu in guinea pig brain membranes using [3H]- DAMGO as ligand | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
| Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
AID150043 | The compound was evaluated for binding affinity against Opioid receptor delta 1 in guinea pig brain membrane using [3H]- DPDPE as ligand | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
| Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
AID148810 | Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for opioid receptor delta 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID149206 | Opioid receptor delta antagonistic activity was measured by the displacement of DADLE in the mouse vas deferens at a concentration of 100 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
AID1237282 | Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
| Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |