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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 | - | |
(S)-3,4-DCPG | 2079 | None | 36 | Human | Binding | EC50 | = | 31.00 | 7.51 | - | 8 | Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 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/acs.jmedchem.8b01120 | |
ADX88178 | 300 | None | 40 | Human | Binding | EC50 | = | 1200.00 | 5.92 | - | 4 | Positive allosteric modulation of mGluR8 (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 | |
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 | - | |
CHEMBL180822 | 64133 | None | 0 | Human | Binding | Kd | = | 6.30 | 8.20 | - | 1 | Dissociation constant of radiolabeled compound against recombinant human Metabotropic glutamate receptor 8 | ChEMBL | 189.1 | 4 | 4 | 4 | -1.66 | N[C@H](C(=O)O)[C@@H]1C(C(=O)O)[C@@H]1CO | https://dx.doi.org/10.1016/j.bmcl.2004.10.093 | |
CHEMBL197976 | 72197 | None | 1 | Rat | Binding | Ki | = | 63000.00 | 4.20 | -8 | 3 | Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cells | ChEMBL | 195.0 | 3 | 4 | 3 | -1.04 | N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O | https://dx.doi.org/10.1016/j.bmcl.2005.09.014 | |
CHEMBL199626 | 72701 | None | 1 | Rat | Binding | Ki | = | 54000.00 | 4.27 | -1 | 3 | Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cells | ChEMBL | 195.0 | 3 | 4 | 3 | -1.04 | N[C@H](C(=O)O)[C@@H]1C[C@H]1P(=O)(O)O | https://dx.doi.org/10.1016/j.bmcl.2005.09.014 | |
CHEMBL2381640 | 90084 | None | 2 | Human | Binding | EC50 | = | 6530.00 | 5.18 | - | 4 | Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay | ChEMBL | 199.0 | 2 | 3 | 4 | -1.31 | N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O | https://dx.doi.org/10.1021/jm4000165 | |
CHEMBL2381641 | 90085 | None | 1 | Human | Binding | EC50 | = | 1590.00 | 5.80 | - | 4 | Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay | ChEMBL | 197.1 | 2 | 3 | 3 | -0.33 | C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 | https://dx.doi.org/10.1021/jm4000165 | |
CHEMBL2381644 | 90088 | None | 0 | Human | Binding | EC50 | = | 12400.00 | 4.91 | - | 4 | Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay | ChEMBL | 226.1 | 3 | 3 | 4 | -0.20 | [N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 | https://dx.doi.org/10.1021/jm4000165 | |
CHEMBL2381645 | 90089 | None | 0 | Human | Binding | EC50 | = | 12000.00 | 4.92 | - | 4 | Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay | ChEMBL | 226.1 | 3 | 3 | 4 | -0.20 | [N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 | https://dx.doi.org/10.1021/jm4000165 | |
CHEMBL2381649 | 90093 | None | 0 | Human | Binding | EC50 | = | 4300.00 | 5.37 | - | 4 | Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay | ChEMBL | 242.1 | 3 | 4 | 4 | -1.38 | CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 | https://dx.doi.org/10.1021/jm4000165 | |
CHEMBL2381652 | 90096 | None | 0 | Human | Binding | EC50 | = | 11500.00 | 4.94 | - | 4 | Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay | ChEMBL | 203.1 | 2 | 3 | 3 | -0.54 | N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 | https://dx.doi.org/10.1021/jm4000165 | |
CHEMBL285843 | 99919 | None | 47 | Human | Binding | IC50 | = | 5.10 | 8.29 | 1 | 8 | Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8 | ChEMBL | 183.0 | 4 | 4 | 3 | -1.03 | NC(CCP(=O)(O)O)C(=O)O | https://dx.doi.org/10.1016/j.bmcl.2004.10.093 | |
CHEMBL285843 | 99919 | Functional | 47 | Human | Binding | pKi | = | 400.00 | 6.40 | 1 | 8 | - | PDSP KiDatabase | 183.0 | 4 | 4 | 3 | -1.03 | NC(CCP(=O)(O)O)C(=O)O | - | |
CHEMBL285843 | 99919 | Functional | 47 | Rat | Binding | pKi | = | 1258.93 | 5.90 | -4 | 8 | - | PDSP KiDatabase | 183.0 | 4 | 4 | 3 | -1.03 | NC(CCP(=O)(O)O)C(=O)O | - | |
CHEMBL285843 | 99919 | 3H-CPPG | 47 | Rat | Binding | pKi | = | 2700.00 | 5.57 | -4 | 8 | - | PDSP KiDatabase | 183.0 | 4 | 4 | 3 | -1.03 | NC(CCP(=O)(O)O)C(=O)O | - | |
CHEMBL3955188 | 150689 | None | 0 | Human | Binding | IC50 | = | 26670.00 | 4.57 | - | 4 | Binding affinity to mGluR8 (unknown origin) by FLIPR assay | ChEMBL | 416.2 | 6 | 1 | 5 | 4.03 | COc1ccc(-c2cc(C(N)=O)nc3cc(CCc4cnc(C)nc4)ccc23)c(F)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00175 | |
CHEMBL404886 | 155755 | None | 0 | Rat | Binding | IC50 | = | 5000.00 | 5.30 | - | 2 | Displacement of [3H]-L-AP4 from rat mGluR8 | ChEMBL | 437.1 | 2 | 2 | 6 | 3.98 | O=C1CC(c2cccc(-n3ccnn3)c2)=Nc2cc(O)c(C#Cc3ccc(F)cc3)cc2N1 | https://dx.doi.org/10.1016/j.bmcl.2007.12.005 | |
CHEMBL4160748 | 162172 | None | 38 | Human | Binding | EC50 | = | 2600.00 | 5.58 | - | 5 | Agonist activity at mGlu8 (unknown origin) | ChEMBL | 357.1 | 2 | 0 | 4 | 4.32 | COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F | https://dx.doi.org/10.1039/C8MD00524A |
Showing 1 to 20 of 64 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 | |
α-methylserine-O-phosphate | 365 | None | 0 | Rat | Functional | pIC50 | None | - | 5.30 | 15 | 4 | Unclassified | Guide to Pharmacology | 199.0 | 4 | 4 | 4 | -1.10 | CC(N)(COP(=O)(O)O)C(=O)O | https://pubmed.ncbi.nlm.nih.gov/12769621 | |
(1S,3R)-ACPD | 33 | None | 30 | Human | Functional | pEC50 | None | - | 4.40 | -11 | 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/9473604 | |
(1S,3R)-ACPD | 33 | None | 30 | Human | Functional | Ki | = | 45000.00 | 4.35 | -11 | 15 | Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8). | 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 | |
(1S,3R)-ACPD | 33 | None | 30 | Rat | Functional | pEC50 | None | - | 4.30 | -14 | 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/9016353 | |
(R,S)-4-PPG | 2073 | None | 26 | Human | Functional | Ki | = | 210.00 | 6.68 | 1 | 7 | Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8). | 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 | Human | Functional | pEC50 | None | - | 6.70 | 1 | 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 | - | 6.70 | 1 | 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 | pEC50 | None | - | 6.70 | 1 | 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/11166323 | |
(R,S)-4-PPG | 2073 | None | 26 | Rat | Functional | EC50 | = | 210.00 | 6.68 | -1 | 7 | Metabotropic glutamate receptor 8 agonist activity against 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 | EC50 | = | 44.00 | 7.36 | -1 | 8 | Agonist activity at mGlu8 (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 | Human | Functional | EC50 | = | 23.00 | 7.64 | -1 | 8 | Agonist activity at mGlu8 (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 | pEC50 | = | - | 7.50 | -1 | 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 | Rat | Functional | EC50 | = | 31.00 | 7.51 | 1 | 8 | Metabotropic glutamate receptor 8 agonist activity against 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 | |
ACPT-I | 265 | None | 24 | Human | Functional | EC50 | = | 5100.00 | 5.29 | -1 | 7 | Agonist activity at mGlu8 (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 | 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/10771029 | |
ACPT-I | 265 | None | 24 | Rat | Functional | EC50 | = | 5100.00 | 5.29 | -1 | 7 | Agonist activity at rat mGlu8 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 | = | 10100.00 | 5.00 | -1 | 7 | Activity at rat mGluR8 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 | Rat | Functional | EC50 | = | 1200.00 | 5.92 | -138 | 4 | Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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 | |
AZ12216052 | 535 | None | 0 | Human | Functional | pEC50 | = | - | 6.00 | 2 | 2 | Unclassified | Guide to Pharmacology | 391.1 | 7 | 1 | 2 | 5.83 | CCC(C)c1ccc(NC(=O)CSCc2ccc(Br)cc2)cc1 | https://pubmed.ncbi.nlm.nih.gov/20385173 | |
AZ12216052 | 535 | None | 0 | Human | Functional | pKB | = | - | 5.43 | 2 | 2 | Unclassified | Guide to Pharmacology | 391.1 | 7 | 1 | 2 | 5.83 | CCC(C)c1ccc(NC(=O)CSCc2ccc(Br)cc2)cc1 | https://pubmed.ncbi.nlm.nih.gov/29514854 |
Showing 1 to 20 of 236 entries