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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
(1R,2S)-PHENYLPROPANOLAMINE | 27120 | Functional | 13 | Rat | Binding | pKi | = | 10000.00 | 5.00 | -38 | 42 | - | PDSP KiDatabase | 151.1 | 2 | 2 | 2 | 1.07 | C[C@H](N)[C@H](O)c1ccccc1 | - | |
(1S,3R)-ACPD | 33 | None | 30 | Human | Binding | EC50 | = | 39000.00 | 4.41 | -61 | 15 | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay | ChEMBL | 173.1 | 2 | 3 | 3 | -0.35 | N[C@@]1(C(=O)O)CC[C@@H](C(=O)O)C1 | https://dx.doi.org/10.1016/s0960-894x(00)00247-x | |
(1S,3R)-ACPD | 33 | None | 30 | Rat | Binding | EC50 | = | 39000.00 | 4.41 | - | 15 | Concentration for half maximal activation of metabotropic glutamate mGluR4a in rat | ChEMBL | 173.1 | 2 | 3 | 3 | -0.35 | N[C@@]1(C(=O)O)CC[C@@H](C(=O)O)C1 | https://dx.doi.org/10.1021/jm00009a001 | |
(R,S)-4-PPG | 2073 | None | 26 | Human | Binding | EC50 | = | 4700.00 | 5.33 | -25 | 7 | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay | ChEMBL | 231.0 | 3 | 4 | 3 | -0.43 | NC(C(=O)O)c1ccc(P(=O)(O)O)cc1 | https://dx.doi.org/10.1016/s0960-894x(00)00247-x | |
1S, 3R-ACPD | 218660 | Functional | 0 | Rat | Binding | pKi | = | 10000.00 | 5.00 | -2 | 7 | - | PDSP KiDatabase | 173.1 | 2 | 3 | 3 | -0.35 | NC1(C(=O)O)CCC(C(=O)O)C1 | - | |
1S, 3R-ACPD | 218660 | Functional | 0 | Rat | Binding | pKi | = | 10000.00 | 5.00 | -2 | 7 | - | PDSP KiDatabase | 173.1 | 2 | 3 | 3 | -0.35 | NC1(C(=O)O)CCC(C(=O)O)C1 | - | |
1S, 3R-ACPD | 218660 | Functional | 0 | Rat | Binding | pKi | = | 10000.00 | 5.00 | -2 | 7 | - | PDSP KiDatabase | 173.1 | 2 | 3 | 3 | -0.35 | NC1(C(=O)O)CCC(C(=O)O)C1 | - | |
ACPT-I | 265 | None | 24 | Human | Binding | EC50 | = | 7000.00 | 5.16 | - | 7 | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay | ChEMBL | 217.1 | 3 | 4 | 4 | -1.04 | N[C@@]1(C(=O)O)C[C@H](C(=O)O)[C@H](C(=O)O)C1 | https://dx.doi.org/10.1016/s0960-894x(00)00247-x | |
ADX88178 | 300 | None | 40 | Human | Binding | pKi | = | - | 7.40 | - | 4 | Unclassified | Guide to Pharmacology | 272.1 | 3 | 2 | 6 | 2.68 | Cc1ccnc(Nc2nc(-c3cn[nH]c3)c(C)s2)n1 | https://pubmed.ncbi.nlm.nih.gov/22787118 | |
ADX88178 | 300 | None | 40 | Human | Binding | EC50 | = | 52.00 | 7.28 | - | 4 | Positive allosteric modulation of mGluR4 (unknown origin) | ChEMBL | 272.1 | 3 | 2 | 6 | 2.68 | Cc1ccnc(Nc2nc(-c3cn[nH]c3)c(C)s2)n1 | https://dx.doi.org/10.1016/j.bmcl.2022.129106 | |
ADX88178 | 300 | None | 40 | Human | Binding | EC50 | = | 4.00 | 8.40 | - | 4 | Positive allosteric modulator activity at human mGlu4 receptor | ChEMBL | 272.1 | 3 | 2 | 6 | 2.68 | Cc1ccnc(Nc2nc(-c3cn[nH]c3)c(C)s2)n1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.031 | |
ADX88178 | 300 | None | 40 | Rat | Binding | EC50 | = | 9.00 | 8.05 | - | 4 | Positive allosteric modulator activity at rat mGlu4 receptor | ChEMBL | 272.1 | 3 | 2 | 6 | 2.68 | Cc1ccnc(Nc2nc(-c3cn[nH]c3)c(C)s2)n1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.031 | |
Cathinone, (-) | 218812 | Functional | 0 | Rat | Binding | pKi | = | 10000.00 | 5.00 | -13 | 40 | - | PDSP KiDatabase | 149.1 | 2 | 1 | 2 | 1.22 | CC(N)C(=O)c1ccccc1 | - | |
CHEMBL1223083 | 15872 | None | 0 | Human | Binding | EC50 | = | 162.00 | 6.79 | - | 1 | Positive allosteric modulation of human mGlu4 receptor | ChEMBL | 387.0 | 5 | 2 | 4 | 3.79 | O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1ccccn1 | https://dx.doi.org/10.1016/j.bmcl.2016.05.029 | |
CHEMBL1223381 | 15977 | None | 52 | Human | Binding | EC50 | = | 20.00 | 7.70 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor | ChEMBL | 421.0 | 5 | 2 | 4 | 4.44 | O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)c(Cl)c1)c1ccccn1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.031 | |
CHEMBL1223381 | 15977 | None | 52 | Human | Binding | EC50 | = | 19.80 | 7.70 | - | 1 | Positive allosteric modulation of human mGlu4 receptor | ChEMBL | 421.0 | 5 | 2 | 4 | 4.44 | O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)c(Cl)c1)c1ccccn1 | https://dx.doi.org/10.1016/j.bmcl.2016.05.029 | |
CHEMBL1223384 | 15979 | None | 0 | Human | Binding | EC50 | = | 237.00 | 6.62 | - | 1 | Positive allosteric modulation of human mGlu4 receptor | ChEMBL | 386.0 | 5 | 1 | 4 | 3.96 | O=C(Nc1ccc(S(=O)(=O)Cc2ccccc2Cl)cc1)c1ccccn1 | https://dx.doi.org/10.1016/j.bmcl.2016.05.029 | |
CHEMBL1300476 | 19647 | None | 3 | Human | Binding | IC50 | = | 4.90 | 8.31 | - | 1 | Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method | ChEMBL | 244.1 | 3 | 1 | 3 | 3.06 | CSc1cccc(NC(=O)c2ccccn2)c1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.031 | |
CHEMBL1300476 | 19647 | None | 3 | Human | Binding | IC50 | = | 4.90 | 8.31 | - | 1 | Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method | ChEMBL | 244.1 | 3 | 1 | 3 | 3.06 | CSc1cccc(NC(=O)c2ccccn2)c1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.031 | |
CHEMBL1346011 | 24959 | None | 16 | Rat | Binding | EC50 | = | 1100.00 | 5.96 | - | 2 | Positive allosteric modulation of rat mGlu4 receptor expressed in human HEK293 cells co-expressing GIRK potassium channels assessed as potentiation of carbachol-induced thallium flux measured between 10 to 20 secs | ChEMBL | 322.0 | 4 | 2 | 4 | 3.12 | O=C(COc1ccccc1Br)c1ccc(O)cc1O | https://dx.doi.org/10.1016/j.bmcl.2011.09.131 |
Showing 1 to 20 of 256 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
(1S,3R)-ACPD | 33 | None | 30 | Human | Functional | Ki | = | 98000.00 | 4.01 | -10 | 15 | Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). | ChEMBL | 173.1 | 2 | 3 | 3 | -0.35 | N[C@@]1(C(=O)O)CC[C@@H](C(=O)O)C1 | https://dx.doi.org/10.1021/jm000007r | |
(R,S)-4-PPG | 2073 | None | 26 | Human | Functional | pEC50 | None | - | 5.30 | -22 | 7 | Unclassified | Guide to Pharmacology | 231.0 | 3 | 4 | 3 | -0.43 | NC(C(=O)O)c1ccc(P(=O)(O)O)cc1 | https://pubmed.ncbi.nlm.nih.gov/10336568 | |
(R,S)-4-PPG | 2073 | None | 26 | Human | Functional | pEC50 | None | - | 5.30 | -22 | 7 | Unclassified | Guide to Pharmacology | 231.0 | 3 | 4 | 3 | -0.43 | NC(C(=O)O)c1ccc(P(=O)(O)O)cc1 | https://pubmed.ncbi.nlm.nih.gov/10866390 | |
(R,S)-4-PPG | 2073 | None | 26 | Human | Functional | EC50 | = | 5200.00 | 5.28 | -22 | 7 | Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a | ChEMBL | 231.0 | 3 | 4 | 3 | -0.43 | NC(C(=O)O)c1ccc(P(=O)(O)O)cc1 | https://dx.doi.org/10.1016/s0960-894x(00)00197-9 | |
(R,S)-4-PPG | 2073 | None | 26 | Human | Functional | EC50 | = | 3200.00 | 5.50 | -22 | 7 | Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a | ChEMBL | 231.0 | 3 | 4 | 3 | -0.43 | NC(C(=O)O)c1ccc(P(=O)(O)O)cc1 | https://dx.doi.org/10.1016/s0960-894x(00)00197-9 | |
(R,S)-4-PPG | 2073 | None | 26 | Human | Functional | Ki | = | 5200.00 | 5.28 | -22 | 7 | Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4) | ChEMBL | 231.0 | 3 | 4 | 3 | -0.43 | NC(C(=O)O)c1ccc(P(=O)(O)O)cc1 | https://dx.doi.org/10.1021/jm000007r | |
(R,S)-4-PPG | 2073 | None | 26 | Rat | Functional | EC50 | = | 5200.00 | 5.28 | -26 | 7 | Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | ChEMBL | 231.0 | 3 | 4 | 3 | -0.43 | NC(C(=O)O)c1ccc(P(=O)(O)O)cc1 | https://dx.doi.org/10.1021/jm030967o | |
(S)-3,4-DCPG | 2079 | None | 36 | Human | Functional | pEC50 | None | - | 5.10 | -117 | 8 | Unclassified | Guide to Pharmacology | 239.0 | 4 | 4 | 4 | 0.17 | N[C@H](C(=O)O)c1ccc(C(=O)O)c(C(=O)O)c1 | https://pubmed.ncbi.nlm.nih.gov/11166323 | |
(S)-3,4-DCPG | 2079 | None | 36 | Human | Functional | EC50 | = | 1960.00 | 5.71 | -117 | 8 | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method | ChEMBL | 239.0 | 4 | 4 | 4 | 0.17 | N[C@H](C(=O)O)c1ccc(C(=O)O)c(C(=O)O)c1 | https://dx.doi.org/10.1021/acs.jmedchem.7b01438 | |
(S)-3,4-DCPG | 2079 | None | 36 | Human | Functional | EC50 | = | 3200.00 | 5.50 | -117 | 8 | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay | ChEMBL | 239.0 | 4 | 4 | 4 | 0.17 | N[C@H](C(=O)O)c1ccc(C(=O)O)c(C(=O)O)c1 | https://dx.doi.org/10.1021/acs.jmedchem.7b01438 | |
(S)-3,4-DCPG | 2079 | None | 36 | Rat | Functional | EC50 | = | 8800.00 | 5.06 | -281 | 8 | Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | ChEMBL | 239.0 | 4 | 4 | 4 | 0.17 | N[C@H](C(=O)O)c1ccc(C(=O)O)c(C(=O)O)c1 | https://dx.doi.org/10.1021/jm030967o | |
(S)-3,4-DCPG | 2079 | None | 36 | Rat | Functional | EC50 | = | 8800.00 | 5.06 | -281 | 8 | Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells | ChEMBL | 239.0 | 4 | 4 | 4 | 0.17 | N[C@H](C(=O)O)c1ccc(C(=O)O)c(C(=O)O)c1 | https://dx.doi.org/10.1021/jm049092j | |
ACPT-I | 265 | None | 24 | Human | Functional | EC50 | = | 1700.00 | 5.77 | 1 | 7 | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method | ChEMBL | 217.1 | 3 | 4 | 4 | -1.04 | N[C@@]1(C(=O)O)C[C@H](C(=O)O)[C@H](C(=O)O)C1 | https://dx.doi.org/10.1021/acs.jmedchem.7b01438 | |
ACPT-I | 265 | None | 24 | Human | Functional | EC50 | = | 7200.00 | 5.14 | 1 | 7 | Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation | ChEMBL | 217.1 | 3 | 4 | 4 | -1.04 | N[C@@]1(C(=O)O)C[C@H](C(=O)O)[C@H](C(=O)O)C1 | https://dx.doi.org/10.1021/jm970207b | |
ACPT-I | 265 | None | 24 | Rat | Functional | pEC50 | None | - | 5.10 | -1 | 7 | Unclassified | Guide to Pharmacology | 217.1 | 3 | 4 | 4 | -1.04 | N[C@@]1(C(=O)O)C[C@H](C(=O)O)[C@H](C(=O)O)C1 | https://pubmed.ncbi.nlm.nih.gov/9301676 | |
ACPT-I | 265 | None | 24 | Rat | Functional | EC50 | = | 1740.00 | 5.76 | -1 | 7 | Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting | ChEMBL | 217.1 | 3 | 4 | 4 | -1.04 | N[C@@]1(C(=O)O)C[C@H](C(=O)O)[C@H](C(=O)O)C1 | https://dx.doi.org/10.1021/jm901523t | |
ACPT-I | 265 | None | 24 | Rat | Functional | EC50 | = | 7200.00 | 5.14 | -1 | 7 | Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells | ChEMBL | 217.1 | 3 | 4 | 4 | -1.04 | N[C@@]1(C(=O)O)C[C@H](C(=O)O)[C@H](C(=O)O)C1 | https://dx.doi.org/10.1016/j.bmcl.2006.06.062 | |
ADX88178 | 300 | None | 40 | Human | Functional | pEC50 | = | - | 8.50 | 1 | 4 | Unclassified | Guide to Pharmacology | 272.1 | 3 | 2 | 6 | 2.68 | Cc1ccnc(Nc2nc(-c3cn[nH]c3)c(C)s2)n1 | https://pubmed.ncbi.nlm.nih.gov/22787118 | |
ADX88178 | 300 | None | 40 | Human | Functional | EC50 | = | 52.00 | 7.28 | 1 | 4 | Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay | ChEMBL | 272.1 | 3 | 2 | 6 | 2.68 | Cc1ccnc(Nc2nc(-c3cn[nH]c3)c(C)s2)n1 | https://dx.doi.org/10.1021/acsmedchemlett.7b00317 | |
ADX88178 | 300 | None | 40 | Rat | Functional | pEC50 | = | - | 8.04 | -1 | 4 | Unclassified | Guide to Pharmacology | 272.1 | 3 | 2 | 6 | 2.68 | Cc1ccnc(Nc2nc(-c3cn[nH]c3)c(C)s2)n1 | https://pubmed.ncbi.nlm.nih.gov/22787118 |
Showing 1 to 20 of 1,094 entries