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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 | |
(+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid | 218819 | 3H-LY341495 | 0 | Human | Binding | pKi | = | 125.60 | 6.90 | -4 | 3 | - | PDSP KiDatabase | 185.1 | 2 | 3 | 3 | -0.49 | NC1(C(=O)O)CCC2C(C(=O)O)C21 | - | |
(+)-MCPG | 2475 | None | 35 | Human | Binding | pKi | None | - | 3.80 | -6 | 8 | Unclassified | Guide to Pharmacology | 209.1 | 3 | 3 | 3 | 0.64 | C[C@@](N)(C(=O)O)c1ccc(C(=O)O)cc1 | https://pubmed.ncbi.nlm.nih.gov/10530814 | |
(1S,3R)-ACPD | 33 | None | 30 | Human | Binding | pKi | None | - | 4.70 | -12 | 15 | Unclassified | Guide to Pharmacology | 173.1 | 2 | 3 | 3 | -0.35 | N[C@@]1(C(=O)O)CC[C@@H](C(=O)O)C1 | https://pubmed.ncbi.nlm.nih.gov/10530814 | |
(1S,3R)-ACPD | 33 | None | 30 | Rat | Binding | pKi | None | - | 4.80 | -10 | 15 | Unclassified | Guide to Pharmacology | 173.1 | 2 | 3 | 3 | -0.35 | N[C@@]1(C(=O)O)CC[C@@H](C(=O)O)C1 | https://pubmed.ncbi.nlm.nih.gov/10884552 | |
(1S,3R)-ACPD | 33 | None | 30 | Rat | Binding | EC50 | = | 8000.00 | 5.10 | -10 | 15 | Concentration for half maximal activation of metabotropic glutamate mGluR3 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 | |
(2R,3R)-APDC | 73 | None | 32 | Human | Binding | pKi | None | - | 5.30 | 1 | 5 | Unclassified | Guide to Pharmacology | 174.1 | 2 | 4 | 4 | -1.78 | N[C@@]1(C(=O)O)CN[C@@H](C(=O)O)C1 | https://pubmed.ncbi.nlm.nih.gov/10530814 | |
1S, 3R-ACPD | 218660 | Functional | 0 | Human | Binding | pKi | = | 8000.00 | 5.10 | -1 | 7 | - | PDSP KiDatabase | 173.1 | 2 | 3 | 3 | -0.35 | NC1(C(=O)O)CCC(C(=O)O)C1 | - | |
CHEMBL108735 | 7529 | None | 0 | Rat | Binding | IC50 | = | 1300.00 | 5.89 | - | 2 | Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant Metabotropic glutamate receptor 3 expressed in HEK293 cells | ChEMBL | 353.1 | 5 | 3 | 4 | 2.67 | NC(C(=O)O)[C@@H]1[C@@H](C(=O)O)[C@@H]1CC1c2ccccc2Oc2ccccc21 | https://dx.doi.org/10.1016/s0960-894x(01)00656-4 | |
CHEMBL140197 | 31349 | None | 0 | Human | Binding | Ki | = | 3.00 | 8.52 | 7 | 7 | Binding affinity towards metabotropic glutamate receptor 3 was determined | ChEMBL | 175.0 | 3 | 4 | 4 | -1.91 | N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O | https://dx.doi.org/10.1021/jm030967o | |
CHEMBL144151 | 35826 | None | 1 | Rat | Binding | Ki | = | 4.11 | 8.39 | -1 | 4 | Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand | ChEMBL | 353.1 | 5 | 3 | 4 | 2.82 | N[C@@](CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1C[C@@H]1C(=O)O | https://dx.doi.org/10.1021/jm000346k | |
CHEMBL183956 | 66135 | None | 0 | Rat | Binding | Ki | = | 88.10 | 7.05 | -2 | 2 | Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | ChEMBL | 233.1 | 3 | 3 | 4 | -0.77 | CO[C@@H]1C[C@@H]2[C@H]([C@]1(N)C(=O)O)[C@@]2(F)C(=O)O | https://dx.doi.org/10.1021/jm0400294 | |
CHEMBL185210 | 66478 | None | 0 | Rat | Binding | Ki | = | 5.43 | 8.27 | -2 | 2 | Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | ChEMBL | 359.1 | 5 | 3 | 4 | 1.95 | N[C@@]1(C(=O)O)[C@H](OCc2ccc3ccccc3c2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O | https://dx.doi.org/10.1021/jm0400294 | |
CHEMBL185822 | 66774 | None | 0 | Rat | Binding | Ki | = | 67.10 | 7.17 | -2 | 2 | Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | ChEMBL | 219.1 | 2 | 4 | 4 | -1.43 | N[C@@]1(C(=O)O)[C@H](O)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O | https://dx.doi.org/10.1021/jm0400294 | |
CHEMBL186214 | 66873 | None | 0 | Rat | Binding | Ki | = | 15.90 | 7.80 | -2 | 2 | Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | ChEMBL | 309.1 | 5 | 3 | 4 | 0.80 | N[C@@]1(C(=O)O)[C@H](OCc2ccccc2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O | https://dx.doi.org/10.1021/jm0400294 | |
CHEMBL186630 | 66958 | None | 0 | Rat | Binding | Ki | = | 3.00 | 8.52 | -1 | 2 | Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | ChEMBL | 345.1 | 5 | 3 | 4 | 1.07 | N[C@@]1(C(=O)O)[C@H](OCc2ccc(F)c(F)c2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O | https://dx.doi.org/10.1021/jm0400294 | |
CHEMBL189814 | 67581 | None | 0 | Rat | Binding | Ki | = | 4.77 | 8.32 | -1 | 2 | Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | ChEMBL | 343.1 | 5 | 3 | 4 | 1.45 | N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)cc2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O | https://dx.doi.org/10.1021/jm0400294 | |
CHEMBL192977 | 69397 | None | 1 | Human | Binding | Ki | = | 146.00 | 6.84 | 6 | 2 | Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3 | ChEMBL | 199.1 | 2 | 3 | 3 | -0.24 | C[C@@H]1C[C@H]2[C@H](C(=O)O)[C@H]2[C@]1(N)C(=O)O | https://dx.doi.org/10.1021/jm040222y | |
CHEMBL218710 | 83279 | None | 1 | Human | Binding | Ki | = | 0.17 | 9.77 | 5 | 3 | Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells | ChEMBL | 219.0 | 2 | 3 | 4 | -1.77 | N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 | https://dx.doi.org/10.1021/jm060917u | |
CHEMBL218710 | 83279 | None | 1 | Human | Binding | Ki | = | 447.00 | 6.35 | 5 | 3 | Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells | ChEMBL | 219.0 | 2 | 3 | 4 | -1.77 | N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 | https://dx.doi.org/10.1021/jm060917u | |
CHEMBL2204437 | 83633 | None | 0 | Human | Binding | IC50 | = | 3801.89 | 5.42 | - | 1 | Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay | ChEMBL | 335.2 | 2 | 1 | 3 | 2.69 | COc1ccc(C#Cc2ccc(C(=O)N3CCC(O)CC3)cc2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2012.04.112 |
Showing 1 to 20 of 245 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 | EC50 | = | 30000.00 | 4.52 | -8 | 15 | Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor | 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(99)00266-8 | |
(2R,3R)-APDC | 73 | None | 32 | Human | Functional | Ki | = | 410.00 | 6.39 | -9 | 5 | Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). | ChEMBL | 174.1 | 2 | 4 | 4 | -1.78 | N[C@@]1(C(=O)O)CN[C@@H](C(=O)O)C1 | https://dx.doi.org/10.1021/jm000007r | |
(2R,3R)-APDC | 73 | None | 32 | Human | Functional | EC50 | = | 3000.00 | 5.52 | -9 | 5 | Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor | ChEMBL | 174.1 | 2 | 4 | 4 | -1.78 | N[C@@]1(C(=O)O)CN[C@@H](C(=O)O)C1 | https://dx.doi.org/10.1016/s0960-894x(99)00266-8 | |
(2R,3R)-APDC | 73 | None | 32 | Rat | Functional | EC50 | = | 1700.00 | 5.77 | -5 | 5 | Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3 | ChEMBL | 174.1 | 2 | 4 | 4 | -1.78 | N[C@@]1(C(=O)O)CN[C@@H](C(=O)O)C1 | https://dx.doi.org/10.1016/s0960-894x(01)00329-8 | |
CHEMBL1189303 | 12956 | None | 0 | Rat | Functional | IC50 | = | 21000.00 | 4.68 | 1 | 3 | Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3 | ChEMBL | 308.1 | 5 | 4 | 5 | -0.25 | N[C@]1(C(=O)O)C[C@H](C(=O)O)N(C(C(=O)O)c2ccccc2)C1 | https://dx.doi.org/10.1016/s0960-894x(01)00329-8 | |
CHEMBL1189797 | 13018 | None | 0 | Rat | Functional | IC50 | = | 23000.00 | 4.64 | 1 | 2 | Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3 | ChEMBL | 364.1 | 4 | 3 | 4 | 1.53 | N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2C#Cc2ccccc2)C1 | https://dx.doi.org/10.1016/s0960-894x(01)00329-8 | |
CHEMBL1189910 | 13037 | None | 0 | Rat | Functional | IC50 | = | 93000.00 | 4.03 | -2 | 3 | Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3 | ChEMBL | 309.1 | 5 | 3 | 6 | 0.04 | N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 | https://dx.doi.org/10.1016/s0960-894x(01)00329-8 | |
CHEMBL1192345 | 13360 | None | 0 | Rat | Functional | EC50 | = | 7500.00 | 5.12 | 3 | 3 | Effective concentration required for partial agonistic activity at Metabotropic glutamate receptor 3; Partial agonist | ChEMBL | 280.1 | 4 | 4 | 5 | -0.17 | N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(O)cc2)C1 | https://dx.doi.org/10.1016/s0960-894x(01)00329-8 | |
CHEMBL1192558 | 13383 | None | 0 | Rat | Functional | EC50 | = | 37000.00 | 4.43 | 1 | 2 | Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3 | ChEMBL | 265.1 | 4 | 3 | 5 | -0.48 | N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccn2)C1 | https://dx.doi.org/10.1016/s0960-894x(01)00329-8 | |
CHEMBL1193146 | 13464 | None | 0 | Rat | Functional | EC50 | = | 6800.00 | 5.17 | -1 | 2 | Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3 | ChEMBL | 309.1 | 5 | 3 | 6 | 0.04 | N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2[N+](=O)[O-])C1 | https://dx.doi.org/10.1016/s0960-894x(01)00329-8 | |
CHEMBL1194613 | 13664 | None | 0 | Rat | Functional | IC50 | = | 77000.00 | 4.11 | 1 | 2 | Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3 | ChEMBL | 342.0 | 4 | 3 | 4 | 0.89 | N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2Br)C1 | https://dx.doi.org/10.1016/s0960-894x(01)00329-8 | |
CHEMBL1198741 | 14191 | None | 0 | Rat | Functional | IC50 | = | 27000.00 | 4.57 | -4 | 3 | Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3 | ChEMBL | 280.1 | 4 | 4 | 5 | -0.17 | N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2O)C1 | https://dx.doi.org/10.1016/s0960-894x(01)00329-8 | |
CHEMBL123842 | 16571 | None | 0 | Human | Functional | IC50 | = | 200.00 | 6.70 | 15 | 2 | Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3 | ChEMBL | 278.1 | 6 | 4 | 4 | 0.70 | Nc1cccc(CC[C@](N)(C(=O)O)C2C[C@@H]2C(=O)O)c1 | https://dx.doi.org/10.1021/jm970498o | |
CHEMBL123847 | 16573 | None | 0 | Human | Functional | IC50 | = | 420.00 | 6.38 | -1 | 2 | Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3 | ChEMBL | 331.1 | 6 | 3 | 3 | 2.14 | N[C@@](CCc1cccc(C(F)(F)F)c1)(C(=O)O)C1C[C@@H]1C(=O)O | https://dx.doi.org/10.1021/jm970498o | |
CHEMBL124078 | 16611 | None | 0 | Human | Functional | IC50 | = | 170.00 | 6.77 | 1 | 2 | Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3 | ChEMBL | 339.1 | 7 | 3 | 3 | 2.71 | N[C@](CC(c1ccccc1)c1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O | https://dx.doi.org/10.1021/jm970498o | |
CHEMBL124483 | 16788 | None | 0 | Human | Functional | IC50 | = | 260.00 | 6.58 | 3 | 2 | Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3 | ChEMBL | 279.1 | 6 | 4 | 4 | 0.83 | N[C@@](CCc1cccc(O)c1)(C(=O)O)C1C[C@@H]1C(=O)O | https://dx.doi.org/10.1021/jm970498o | |
CHEMBL124501 | 16792 | None | 0 | Human | Functional | IC50 | = | 80.00 | 7.10 | 2 | 2 | Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3 | ChEMBL | 277.1 | 6 | 3 | 3 | 1.43 | Cc1cccc(CC[C@](N)(C(=O)O)[C@H]2C[C@@H]2C(=O)O)c1 | https://dx.doi.org/10.1021/jm970498o | |
CHEMBL134749 | 25142 | None | 12 | Human | Functional | EC50 | = | 39000.00 | 4.41 | - | 1 | Agonist potency against cloned Metabotropic glutamate receptor 3 | ChEMBL | 354.1 | 12 | 5 | 5 | 0.39 | O=C(O)CCC(CP(=O)(O)CC(CCC(=O)O)C(=O)O)C(=O)O | https://dx.doi.org/10.1021/jm9905559 | |
CHEMBL134749 | 25142 | None | 12 | Human | Functional | EC50 | = | 45000.00 | 4.35 | - | 1 | Agonist potency against cloned Metabotropic glutamate receptor 3 | ChEMBL | 354.1 | 12 | 5 | 5 | 0.39 | O=C(O)CCC(CP(=O)(O)CC(CCC(=O)O)C(=O)O)C(=O)O | https://dx.doi.org/10.1021/jm9905559 | |
CHEMBL134749 | 25142 | None | 12 | Human | Functional | EC50 | = | 51000.00 | 4.29 | - | 1 | Agonist potency against cloned Metabotropic glutamate receptor 3 | ChEMBL | 354.1 | 12 | 5 | 5 | 0.39 | O=C(O)CCC(CP(=O)(O)CC(CCC(=O)O)C(=O)O)C(=O)O | https://dx.doi.org/10.1021/jm9905559 |
Showing 1 to 20 of 473 entries