ID Source | ID |
---|---|
PubMed CID | 9826034 |
CHEMBL ID | 485832 |
SCHEMBL ID | 17736072 |
MeSH ID | M0367041 |
Synonym |
---|
gtpl1669 |
2-[(1s,2s,13r,21r)-22-(cyclopropylmethyl)-2,16-dihydroxy-14-oxa-11,22-diazaheptacyclo[13.9.1.0^{1,13}.0^{2,21}.0^{4,12}.0^{5,10}.0^{19,25}]pentacosa-4(12),5,7,9,15(25),16,18-heptaen-7-yl]guanidine |
LOPAC0_000559 |
NCGC00162187-01 |
gnti |
NCGC00162187-02 |
5'-guanidinylnaltrindole |
5'-guanidinonaltrindole |
c5'-guanidinyl naltrindole |
CHEMBL485832 , |
5''''-guanidinonaltrindole |
bdbm50027039 |
guanidinonaltrindole |
5`-guanidinonaltrindole |
c5''''-guanidinyl naltrindole |
5''''-guanidinylnaltrindole |
CCG-204649 |
bdbm50346950 |
5'-guanidinonaltrindole di(trifluoroacetate) salt hydrate |
SCHEMBL17736072 |
219655-56-8 |
2-[(1s,2s,13r,21r)-22-(cyclopropylmethyl)-2,16-dihydroxy-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5(10),6,8,15,17,19(25)-heptaen-7-yl]guanidine |
DTXSID101018243 |
SDCCGSBI-0050542.P002 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Delta-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0240 | AID149085; AID149086; AID149248 |
Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0355 | AID149248; AID149675 |
Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0258 | AID151614; AID151766; AID152373; AID152386; AID152388; AID152389 |
Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0022 | AID148568; AID148575; AID148584; AID148585; AID148586; AID148588; AID148589; AID148590; AID148598; AID148599 |
Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.0001 | AID152386 |
Delta-type opioid receptor | Homo sapiens (human) | Ki | 0.0001 | AID152386 |
Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0002 | AID149260 |
Kappa-type opioid receptor | Homo sapiens (human) | Ki | 0.0001 | AID152386; AID603174; AID603175 |
Serine/threonine-protein kinase mTOR | Homo sapiens (human) | Ki | 0.0001 | AID603174 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Delta-type opioid receptor | Mus musculus (house mouse) | Kd | 0.0155 | AID148383 |
Mu-type opioid receptor | Homo sapiens (human) | Kd | 0.0032 | AID151116 |
Delta-type opioid receptor | Homo sapiens (human) | Kd | 0.0155 | AID148383 |
Kappa-type opioid receptor | Homo sapiens (human) | Kd | 0.0000 | AID148169 |
Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.0000 | AID148169 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Delta-type opioid receptor | Mus musculus (house mouse) | Ke | 0.1150 | AID148938; AID148939 |
Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ke | 0.0002 | AID148975 |
Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ke | 0.0300 | AID147889 |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID227092 | Ratio of the IC50 of Kappa receptor agonist, ethylketazocine in the presence of compound in GPI divided by the control IC50. | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID148972 | Opioid antagonist potencies against Opioid receptor kappa 1 from guinea pig ileum employing ethylketazocine (EKC) as agonist. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 ISSN: 0022-2623 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
AID148589 | Effect on binding to kappa(Glu297Ala) opioid receptor, using [3H]diprenorphine in transiently expressed rat HEK293 cells | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 ISSN: 0022-2623 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
AID148575 | Binding affinity towards rat opioid receptor kappa 1 was determined using [3H]diprenorphine radioligand | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 ISSN: 0022-2623 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
AID152389 | Displacement of [3H]- diprenorphine from mu-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 ISSN: 0022-2623 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
AID381429 | Increase of JNK phosphorylation in U50488 treated untransfected HEK293 cells at 10 uM after 1 hr | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41 ISSN: 0021-9258 | Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase. |
AID149783 | Inhibition of [3H]-DADLE binding to Opioid receptor delta 1 of rat brain tissue | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 ISSN: 0022-2623 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
AID148704 | Opioid antagonist potency, determined in the guinea pig ileum (GPI) preparation, by employing EK (kappa-opioid) as agonist, expressed as IC50 ratio (tested at 20 nM) | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 ISSN: 0022-2623 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
AID148588 | Effect on binding affinity of mutational exchange of Glu297 in the Opioid receptor kappa 1 in transiently expressed rat cos-7 cells activity expressed as binding affinity. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 ISSN: 0022-2623 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
AID149260 | Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of guinea pig brain | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 ISSN: 0022-2623 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
AID603175 | Displacement of [125I]-IBNalA from KOR-1 expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13 ISSN: 1464-3405 | Generation of novel radiolabeled opiates through site-selective iodination. |
AID148975 | Opioid receptor kappa 1 Antagonism (100 nM) is expressed as (Ke = [antagonist] / (IC50 ratio -1) | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID152386 | Displacement of [3H]- diprenorphine from mu-K303E-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 ISSN: 0022-2623 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
AID229883 | Selectivity ratio, ratio of binding affinity of mu to kappa opioid receptor | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID227093 | Ratio of the IC50 of delta receptor agonist, [D-Ala-2, D-Leu5]-enkephalin in the presence of compound in MVD divided by the control IC50. | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID756068 | Selectivity ratio of Ki for delta opioid receptor (unknown origin) to Ki for kappa opioid receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13 ISSN: 1464-3405 | Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives. |
AID756071 | Selectivity ratio of Ki for mu opioid receptor (unknown origin) to Ki for kappa opioid receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13 ISSN: 1464-3405 | Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives. |
AID148447 | Mutant factor against mutant receptor with Opioid receptor kappa 1 | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 ISSN: 0022-2623 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
AID149675 | Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor delta 1 | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID147887 | Opioid antagonist potencies against Opioid receptor mu 1 from guinea pig ileum employing morphine(M) as agonist. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 ISSN: 0022-2623 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
AID147889 | Opioid receptor mu 1 Antagonism (100 nM) is expressed as (Ke = [antagonist] / (IC50 ratio -1) | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID152388 | Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 ISSN: 0022-2623 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
AID148973 | Opioid antagonist potency towards opioid receptor kappa 1 determined in guinea pig ileum preparation | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 ISSN: 0022-2623 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
AID151766 | Effect on binding affinity of mutational exchange of Lys303 in the Opioid receptor mu 1 in transiently expressed rat cos-7 cells activity expressed as binding affinity. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 ISSN: 0022-2623 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
AID149086 | Displacement of [3H]- diprenorphine from delta-W284E-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 ISSN: 0022-2623 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
AID148446 | Effect on binding affinity of mutational exchange of Glu297 in the Opioid receptor kappa 1 in transiently expressed rat cos-7 cells activity expressed as binding ratio with nor-BNI. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 ISSN: 0022-2623 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
AID152373 | Binding affinity towards rat mu-opioid receptor was determined using [3H]diprenorphine as radioligand | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 ISSN: 0022-2623 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
AID233597 | Ratio of Ke value to kappa receptor to that of mu receptor | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 ISSN: 0022-2623 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
AID148598 | Mutant factor of the compound against kappa[E297K] with Opioid receptor kappa 1 for binding affinity. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 ISSN: 0022-2623 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
AID148786 | Opioid antagonist potency, determined in mouse vas deferens (MVD) preparation, using DADLE (delta-opioid) as agonist, expressed as IC50 ratio | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 ISSN: 0022-2623 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
AID229881 | Selectivity ratio, ratio of Ke value of mu to kappa opioid receptor | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID229882 | Selectivity ratio, ratio of binding affinity of delta to kappa opioid receptor | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID151620 | Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain tissue | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 ISSN: 0022-2623 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
AID148590 | Effect on binding to wild-type opioid receptor kappa 1 using [3H]diprenorphine in transiently expressed rat HEK293 cells | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 ISSN: 0022-2623 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
AID229876 | Selectivity ratio, ratio of Ke value of Kappa to Delta opioid receptor (extrapolated value) | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID152219 | Opioid antagonist potency, determined in guinea pig ileum (GPI) preparation, using morphine (mu-opioid) as agonist, expressed as IC50 ratio | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 ISSN: 0022-2623 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
AID233596 | Ratio of Ke value to kappa receptor to that of delta receptor | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 ISSN: 0022-2623 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
AID415716 | Selectivity ratio of Ki for delta opioid receptor to Ki for kappa opioid receptor | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 ISSN: 1464-3405 | 14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies. |
AID148169 | Antagonistic activity against human cloned kOpioid receptor kappa 1 using U69,593 in [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 ISSN: 0022-2623 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
AID603174 | Displacement of [125I]-IBNtxA from KOR-1 expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13 ISSN: 1464-3405 | Generation of novel radiolabeled opiates through site-selective iodination. |
AID148585 | Displacement of [3H]diprenorphine from k-Y312A-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 ISSN: 0022-2623 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
AID149248 | Binding affinity towards mouse delta-opioid receptor was determined using [3H]diprenorphine as radioligand | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 ISSN: 0022-2623 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
AID148939 | Opioid antagonist potency, determined in mouse vas deferens (MVD) preparation, using DADLE (delta-opioid) as agonist (Ke=antagonist/IC50 ratio -1) | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 ISSN: 0022-2623 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
AID233363 | Selectivity ratio of mu and kappa opioid receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 ISSN: 0022-2623 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
AID152223 | Opioid antagonist potency, determined in guinea pig ileum (GPI) preparation, using morphine (mu-opioid) as agonist (Ke=antagonist/IC50 ratio -1) | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 ISSN: 0022-2623 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
AID779513 | Selectivity ratio of Ki for DOR (unknown origin) to Ki for KOR (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 ISSN: 1464-3391 | Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of mu opio |
AID148383 | Antagonistic activity against human cloned Opioid receptor delta 1 using DPDPE in [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 ISSN: 0022-2623 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
AID149085 | Displacement of [3H]- diprenorphine from delta receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 ISSN: 0022-2623 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
AID148568 | Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor kappa 1 | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID151116 | Antagonistic activity against human cloned Opioid receptor mu 1 using DPDPE in [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 ISSN: 0022-2623 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
AID381420 | Inhibition of U50488-induced analgesic activity against C57BL/6 mouse assessed as tail withdrawal latency at 10 mg/kg, ip upto 21 days | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41 ISSN: 0021-9258 | Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase. |
AID148584 | Displacement of [3H]diprenorphine from k-E297A-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 ISSN: 0022-2623 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
AID148938 | Opioid antagonist potencies against Opioid receptor delta 1 from mouse vas-deferens preparation employing [D-Ala2,D-Leu5]enkephalin (DADLE) as agonist. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 ISSN: 0022-2623 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
AID415715 | Selectivity ratio of Ki for mu opioid receptor to Ki for kappa opioid receptor | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 ISSN: 1464-3405 | 14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies. |
AID148599 | Mutant factor of the compound against mu-[K303E] with Opioid receptor kappa 1 for binding affinity | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 ISSN: 0022-2623 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
AID148586 | Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 ISSN: 0022-2623 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
AID227211 | Ratio of the IC50 of mu receptor agonist, Morphine in the presence of compound in GPI divided by the control IC50. | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID779514 | Selectivity ratio of Ki for MOR (unknown origin) to Ki for KOR (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 ISSN: 1464-3391 | Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of mu opio |
AID233141 | Selectivity ratio of delta and kappa opioid receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 ISSN: 0022-2623 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
AID151614 | Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor mu 1 | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID148942 | Opioid receptor delta 1 Antagonism (100 nM) is expressed as (Ke = [antagonist] / (IC50 ratio -1) | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 ISSN: 1552-454X | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173ISSN: 1872-9096 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173ISSN: 1872-9096 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
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 ISSN: 2211-1247 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 ISSN: 1932-6203 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 ISSN: 0021-9258 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 ISSN: 1945-7170 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 ISSN: 1554-8937 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173ISSN: 1872-9096 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 ISSN: 1946-6242 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 ISSN: 1945-7170 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 ISSN: 1932-6203 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | 2022 | The Journal of biological chemistry, 08, Volume: 298, Issue:8 ISSN: 1083-351X | |
AID1347151 | Optimization of GU AMC 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID588378 | qHTS for Inhibitors of ATXN expression: Validation | 2022 | The Journal of biological chemistry, 08, Volume: 298, Issue:8 ISSN: 1083-351X | |
AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 ISSN: 1946-6242 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 ISSN: 1932-6203 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 ISSN: 1946-6242 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60ISSN: 1873-3913 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
AID1346329 | Human kappa receptor (Opioid receptors) | 2000 | European journal of pharmacology, May-12, Volume: 396, Issue:1 ISSN: 0014-2999 | 5'-Guanidinonaltrindole, a highly selective and potent kappa-opioid receptor antagonist. |
AID1346329 | Human kappa receptor (Opioid receptors) | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 ISSN: 0022-2623 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 1 (4.55) | 18.2507 |
2000's | 8 (36.36) | 29.6817 |
2010's | 8 (36.36) | 24.3611 |
2020's | 5 (22.73) | 2.80 |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 22 (100.00%) | 84.16% |
Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
---|---|---|---|---|---|---|---|---|---|---|---|---|
Anemia, Fanconi | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Contact Dermatitis | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Dermatitis, Contact | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Disease Models, Animal | 0 | 2019 | 2020 | 4.5 | medium | 0 | 0 | 0 | 0 | 2 | 0 | |
Fanconi Anemia | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Itching | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Muscle Contraction | 0 | 2001 | 2001 | 23.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Pruritus | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |