Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | 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 (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | 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
| |
| 1067 | 1709 | None | 74 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -4 | 4 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | 10.1021/jm7015842 | ||
| 119 | 1709 | None | 74 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -4 | 4 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | 10.1021/jm7015842 | ||
| 1262 | 1709 | None | 74 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -4 | 4 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | 10.1021/jm7015842 | ||
| 5410 | 1709 | None | 74 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -4 | 4 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | 10.1021/jm7015842 | ||
| 6992099 | 1709 | None | 74 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -4 | 4 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | 10.1021/jm7015842 | ||
| CHEMBL96 | 1709 | None | 74 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -4 | 4 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | 10.1021/jm7015842 | ||
| DB02530 | 1709 | None | 74 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -4 | 4 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | 10.1021/jm7015842 | ||
| 11701095 | 188814 | None | 0 | Human | Functional | pEC50 | = | 4.3 | 4.3 | - | 1 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 161 | 1 | 2 | 2 | 0.9 | CP(=O)(O)C1=CCC(N)C1 | 10.1021/jm7015842 | ||
| CHEMBL504482 | 188814 | None | 0 | Human | Functional | pEC50 | = | 4.3 | 4.3 | - | 1 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 161 | 1 | 2 | 2 | 0.9 | CP(=O)(O)C1=CCC(N)C1 | 10.1021/jm7015842 | ||
| 24895101 | 172142 | None | 0 | Human | Functional | pEC50 | = | 4.3 | 4.3 | - | 1 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 161 | 1 | 2 | 2 | 0.9 | CP(=O)(O)C1=CC[C@H](N)C1 | 10.1021/jm7015842 | ||
| CHEMBL447171 | 172142 | None | 0 | Human | Functional | pEC50 | = | 4.3 | 4.3 | - | 1 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 161 | 1 | 2 | 2 | 0.9 | CP(=O)(O)C1=CC[C@H](N)C1 | 10.1021/jm7015842 | ||
| 24895106 | 170995 | None | 1 | Human | Functional | pEC50 | = | 4.1 | 4.1 | - | 1 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 161 | 1 | 2 | 2 | 0.9 | CP(=O)(O)C1=CC[C@@H](N)C1 | 10.1021/jm7015842 | ||
| CHEMBL445449 | 170995 | None | 1 | Human | Functional | pEC50 | = | 4.1 | 4.1 | - | 1 | Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method |
ChEMBL | 161 | 1 | 2 | 2 | 0.9 | CP(=O)(O)C1=CC[C@@H](N)C1 | 10.1021/jm7015842 | ||
| 16686147 | 2296 | None | 0 | Human | Functional | pEC50 | = | 8.1 | 8.1 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 141 | 3 | 2 | 2 | -0.3 | NC[C@H](CP(=O)O)F | None | ||
| 7705 | 2296 | None | 0 | Human | Functional | pEC50 | = | 8.1 | 8.1 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 141 | 3 | 2 | 2 | -0.3 | NC[C@H](CP(=O)O)F | None | ||
| CHEMBL448343 | 2296 | None | 0 | Human | Functional | pEC50 | = | 8.1 | 8.1 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 141 | 3 | 2 | 2 | -0.3 | NC[C@H](CP(=O)O)F | None | ||
| DB11920 | 2296 | None | 0 | Human | Functional | pEC50 | = | 8.1 | 8.1 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 141 | 3 | 2 | 2 | -0.3 | NC[C@H](CP(=O)O)F | None | ||
| 1067 | 1709 | None | 74 | Rat | Functional | pIC50 | = | 8.3 | 8.3 | 4 | 4 | NoneNone |
Drug Central | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | None | ||
| 119 | 1709 | None | 74 | Rat | Functional | pIC50 | = | 8.3 | 8.3 | 4 | 4 | NoneNone |
Drug Central | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | None | ||
| 1262 | 1709 | None | 74 | Rat | Functional | pIC50 | = | 8.3 | 8.3 | 4 | 4 | NoneNone |
Drug Central | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | None | ||
| 5410 | 1709 | None | 74 | Rat | Functional | pIC50 | = | 8.3 | 8.3 | 4 | 4 | NoneNone |
Drug Central | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | None | ||
| 6992099 | 1709 | None | 74 | Rat | Functional | pIC50 | = | 8.3 | 8.3 | 4 | 4 | NoneNone |
Drug Central | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | None | ||
| CHEMBL96 | 1709 | None | 74 | Rat | Functional | pIC50 | = | 8.3 | 8.3 | 4 | 4 | NoneNone |
Drug Central | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | None | ||
| DB02530 | 1709 | None | 74 | Rat | Functional | pIC50 | = | 8.3 | 8.3 | 4 | 4 | NoneNone |
Drug Central | 103 | 3 | 2 | 2 | -0.2 | NCCCC(=O)O | None | ||
| 1064 | 568 | None | 0 | Rat | Functional | pIC50 | = | 4.5 | 4.5 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 213 | 4 | 2 | 2 | 1.9 | NC[C@@H](c1ccc(cc1)Cl)CC(=O)O | 9069281 | ||
| 3428 | 568 | None | 0 | Rat | Functional | pIC50 | = | 4.5 | 4.5 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 213 | 4 | 2 | 2 | 1.9 | NC[C@@H](c1ccc(cc1)Cl)CC(=O)O | 9069281 | ||
| 44602 | 568 | None | 0 | Rat | Functional | pIC50 | = | 4.5 | 4.5 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 213 | 4 | 2 | 2 | 1.9 | NC[C@@H](c1ccc(cc1)Cl)CC(=O)O | 9069281 | ||
| 44602.0 | 568 | None | 0 | Rat | Functional | pIC50 | = | 4.5 | 4.5 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 213 | 4 | 2 | 2 | 1.9 | NC[C@@H](c1ccc(cc1)Cl)CC(=O)O | 9069281 | ||
| 6918881 | 568 | None | 0 | Rat | Functional | pIC50 | = | 4.5 | 4.5 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 213 | 4 | 2 | 2 | 1.9 | NC[C@@H](c1ccc(cc1)Cl)CC(=O)O | 9069281 | ||
| CHEMBL301742 | 568 | None | 0 | Rat | Functional | pIC50 | = | 4.5 | 4.5 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 213 | 4 | 2 | 2 | 1.9 | NC[C@@H](c1ccc(cc1)Cl)CC(=O)O | 9069281 | ||
| DB00181 | 568 | None | 0 | Rat | Functional | pIC50 | = | 4.5 | 4.5 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 213 | 4 | 2 | 2 | 1.9 | NC[C@@H](c1ccc(cc1)Cl)CC(=O)O | 9069281 | ||
| DB08891 | 568 | None | 0 | Rat | Functional | pIC50 | = | 4.5 | 4.5 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 213 | 4 | 2 | 2 | 1.9 | NC[C@@H](c1ccc(cc1)Cl)CC(=O)O | 9069281 | ||
| 1069 | 892 | None | 39 | Rat | Functional | pIC50 | = | 4.7 | 4.7 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 225 | 8 | 2 | 4 | 1.0 | NCCCP(=O)(C(OCC)OCC)O | 7650685 | ||
| 1069 | 892 | None | 39 | Rat | Functional | pIC50 | = | 4.7 | 4.7 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 225 | 8 | 2 | 4 | 1.0 | NCCCP(=O)(C(OCC)OCC)O | 9069281 | ||
| 107699 | 892 | None | 39 | Rat | Functional | pIC50 | = | 4.7 | 4.7 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 225 | 8 | 2 | 4 | 1.0 | NCCCP(=O)(C(OCC)OCC)O | 7650685 | ||
| 107699 | 892 | None | 39 | Rat | Functional | pIC50 | = | 4.7 | 4.7 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 225 | 8 | 2 | 4 | 1.0 | NCCCP(=O)(C(OCC)OCC)O | 9069281 | ||
| CHEMBL40157 | 892 | None | 39 | Rat | Functional | pIC50 | = | 4.7 | 4.7 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 225 | 8 | 2 | 4 | 1.0 | NCCCP(=O)(C(OCC)OCC)O | 7650685 | ||
| CHEMBL40157 | 892 | None | 39 | Rat | Functional | pIC50 | = | 4.7 | 4.7 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 225 | 8 | 2 | 4 | 1.0 | NCCCP(=O)(C(OCC)OCC)O | 9069281 | ||
| 1081 | 96 | None | 0 | Rat | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 122 | 3 | 2 | 2 | 0.1 | NCCC[P+](=O)O | 9069281 | ||
| 5381 | 96 | None | 0 | Rat | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 122 | 3 | 2 | 2 | 0.1 | NCCC[P+](=O)O | 9069281 | ||
| 6335948 | 96 | None | 0 | Rat | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 122 | 3 | 2 | 2 | 0.1 | NCCC[P+](=O)O | 9069281 | ||
| 1075 | 3555 | None | 0 | Rat | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 173 | 2 | 2 | 3 | 0.2 | OC(=O)C[C@@H]1OCC(NC1)(C)C | 7562513 | ||
| 5311429 | 3555 | None | 0 | Rat | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 173 | 2 | 2 | 3 | 0.2 | OC(=O)C[C@@H]1OCC(NC1)(C)C | 7562513 | ||
| 86294992 | 3555 | None | 0 | Rat | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 173 | 2 | 2 | 3 | 0.2 | OC(=O)C[C@@H]1OCC(NC1)(C)C | 7562513 | ||
| CHEMBL1895916 | 3555 | None | 0 | Rat | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 173 | 2 | 2 | 3 | 0.2 | OC(=O)C[C@@H]1OCC(NC1)(C)C | 7562513 | ||
| 1072 | 897 | None | 0 | Rat | Functional | pIC50 | = | 8.9 | 8.9 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 421 | 10 | 3 | 5 | 3.2 | COc1ccc(cc1)CP(=O)(C[C@H](CN([C@@H](c1cccc(c1)C(=O)O)C)C)O)O | 9069281 | ||
| 3429 | 897 | None | 0 | Rat | Functional | pIC50 | = | 8.9 | 8.9 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 421 | 10 | 3 | 5 | 3.2 | COc1ccc(cc1)CP(=O)(C[C@H](CN([C@@H](c1cccc(c1)C(=O)O)C)C)O)O | 9069281 | ||
| 5310936 | 897 | None | 0 | Rat | Functional | pIC50 | = | 8.9 | 8.9 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 421 | 10 | 3 | 5 | 3.2 | COc1ccc(cc1)CP(=O)(C[C@H](CN([C@@H](c1cccc(c1)C(=O)O)C)C)O)O | 9069281 | ||
| 1078 | 3458 | None | 0 | Rat | Functional | pIC50 | None | 3.5 | 3.5 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 249 | 4 | 2 | 3 | 1.3 | NCC(c1ccc(cc1)Cl)CS(=O)(=O)O | 9069281 | ||
| 122150 | 3458 | None | 0 | Rat | Functional | pIC50 | None | 3.5 | 3.5 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | 249 | 4 | 2 | 3 | 1.3 | NCC(c1ccc(cc1)Cl)CS(=O)(=O)O | 9069281 | ||
Showing 1 to 50 of 76 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | 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 (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | 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
| |
| 2284 | 206531 | None | 76 | Human | Binding | pAC50 | = | 5.6 | 5.6 | - | 0 | Binding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 213 | 4 | 2 | 2 | 1.9 | NCC(CC(=O)O)c1ccc(Cl)cc1 | 10.1038/s41467-023-40064-9 | ||
| 2284.0 | 206531 | None | 76 | Human | Binding | pAC50 | = | 5.6 | 5.6 | - | 0 | Binding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 213 | 4 | 2 | 2 | 1.9 | NCC(CC(=O)O)c1ccc(Cl)cc1 | 10.1038/s41467-023-40064-9 | ||
| CHEMBL701 | 206531 | None | 76 | Human | Binding | pAC50 | = | 5.6 | 5.6 | - | 0 | Binding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 213 | 4 | 2 | 2 | 1.9 | NCC(CC(=O)O)c1ccc(Cl)cc1 | 10.1038/s41467-023-40064-9 | ||
| DB00181 | 206531 | None | 76 | Human | Binding | pAC50 | = | 5.6 | 5.6 | - | 0 | Binding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 213 | 4 | 2 | 2 | 1.9 | NCC(CC(=O)O)c1ccc(Cl)cc1 | 10.1038/s41467-023-40064-9 | ||
| 5446 | 1868 | None | 44 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Positive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alonePositive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alone |
ChEMBL | 337 | 6 | 2 | 7 | 3.8 | CSc1nc(NC2CCCC2)c(c(n1)NC1CCCC1)[N+](=O)[O-] | 10.1016/j.bmcl.2017.03.084 | ||
| 6604928 | 1868 | None | 44 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Positive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alonePositive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alone |
ChEMBL | 337 | 6 | 2 | 7 | 3.8 | CSc1nc(NC2CCCC2)c(c(n1)NC1CCCC1)[N+](=O)[O-] | 10.1016/j.bmcl.2017.03.084 | ||
| CHEMBL392394 | 1868 | None | 44 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Positive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alonePositive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alone |
ChEMBL | 337 | 6 | 2 | 7 | 3.8 | CSc1nc(NC2CCCC2)c(c(n1)NC1CCCC1)[N+](=O)[O-] | 10.1016/j.bmcl.2017.03.084 | ||
| 9964332 | 10044 | None | 0 | Rat | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 193 | 6 | 2 | 3 | 0.6 | CC(=O)CCP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| CHEMBL115162 | 10044 | None | 0 | Rat | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 193 | 6 | 2 | 3 | 0.6 | CC(=O)CCP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| 9813169 | 9785 | None | 0 | Rat | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 213 | 5 | 2 | 2 | 1.8 | NCCCP(=O)(O)Cc1ccccc1 | 10.1021/jm00017a016 | ||
| CHEMBL113613 | 9785 | None | 0 | Rat | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 213 | 5 | 2 | 2 | 1.8 | NCCCP(=O)(O)Cc1ccccc1 | 10.1021/jm00017a016 | ||
| 28560001 | 110461 | None | 4 | Rat | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 227 | 6 | 2 | 2 | 1.8 | NCCCP(=O)(O)CCc1ccccc1 | 10.1021/jm00017a016 | ||
| 659968 | 110461 | None | 4 | Rat | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 227 | 6 | 2 | 2 | 1.8 | NCCCP(=O)(O)CCc1ccccc1 | 10.1021/jm00017a016 | ||
| CHEMBL324407 | 110461 | None | 4 | Rat | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 227 | 6 | 2 | 2 | 1.8 | NCCCP(=O)(O)CCc1ccccc1 | 10.1021/jm00017a016 | ||
| 9883500 | 142416 | None | 1 | Rat | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay. |
ChEMBL | 318 | 1 | 1 | 2 | 4.6 | CC(=O)[C@H]1CCC2C3CC[C@H]4C[C@H](O)CC[C@]4(C)C3CC[C@@]21C | nan | ||
| CHEMBL38856 | 142416 | None | 1 | Rat | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay. |
ChEMBL | 318 | 1 | 1 | 2 | 4.6 | CC(=O)[C@H]1CCC2C3CC[C@H]4C[C@H](O)CC[C@]4(C)C3CC[C@@]21C | nan | ||
| 10377028 | 108663 | None | 0 | Rat | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 241 | 8 | 3 | 5 | -0.1 | CCOC(OCC)P(=O)(O)C[C@@H](O)CN | 10.1021/jm00017a016 | ||
| CHEMBL320533 | 108663 | None | 0 | Rat | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 241 | 8 | 3 | 5 | -0.1 | CCOC(OCC)P(=O)(O)C[C@@H](O)CN | 10.1021/jm00017a016 | ||
| 58227083 | 124677 | None | 0 | Rat | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay. |
ChEMBL | 321 | 1 | 1 | 3 | 4.0 | C[C@]12CC[C@@H](O)C[C@@H]1CCC1C2CC[C@@]2(C)C1CC[C@@H]2[N+](=O)[O-] | nan | ||
| CHEMBL3640615 | 124677 | None | 0 | Rat | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay. |
ChEMBL | 321 | 1 | 1 | 3 | 4.0 | C[C@]12CC[C@@H](O)C[C@@H]1CCC1C2CC[C@@]2(C)C1CC[C@@H]2[N+](=O)[O-] | nan | ||
| 9920531 | 110377 | None | 0 | Rat | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 179 | 5 | 2 | 2 | 1.3 | CC(C)CP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| CHEMBL323887 | 110377 | None | 0 | Rat | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 179 | 5 | 2 | 2 | 1.3 | CC(C)CP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| 10352529 | 110730 | None | 0 | Rat | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 191 | 5 | 2 | 3 | 0.2 | NCC(=O)CP(=O)(O)CC1CC1 | 10.1021/jm00017a016 | ||
| CHEMBL325932 | 110730 | None | 0 | Rat | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 191 | 5 | 2 | 3 | 0.2 | NCC(=O)CP(=O)(O)CC1CC1 | 10.1021/jm00017a016 | ||
| 28559746 | 9641 | None | 35 | Rat | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 137 | 3 | 2 | 2 | 0.2 | CP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| 5230 | 9641 | None | 35 | Rat | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 137 | 3 | 2 | 2 | 0.2 | CP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| CHEMBL112710 | 9641 | None | 35 | Rat | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 137 | 3 | 2 | 2 | 0.2 | CP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| 9920471 | 9465 | None | 1 | Rat | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 165 | 5 | 2 | 2 | 1.0 | CCCP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| CHEMBL111890 | 9465 | None | 1 | Rat | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 165 | 5 | 2 | 2 | 1.0 | CCCP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| 9964768 | 110431 | None | 0 | Rat | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 241 | 8 | 3 | 5 | -0.1 | CCOC(OCC)P(=O)(O)CC(O)CN | 10.1021/jm00017a016 | ||
| CHEMBL324244 | 110431 | None | 0 | Rat | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 241 | 8 | 3 | 5 | -0.1 | CCOC(OCC)P(=O)(O)CC(O)CN | 10.1021/jm00017a016 | ||
| 58227084 | 124678 | None | 0 | Rat | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay. |
ChEMBL | 335 | 1 | 1 | 3 | 4.4 | C[C@]12CC[C@@](C)(O)C[C@@H]1CCC1C2CC[C@@]2(C)C1CC[C@@H]2[N+](=O)[O-] | nan | ||
| CHEMBL3640616 | 124678 | None | 0 | Rat | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay. |
ChEMBL | 335 | 1 | 1 | 3 | 4.4 | C[C@]12CC[C@@](C)(O)C[C@@H]1CCC1C2CC[C@@]2(C)C1CC[C@@H]2[N+](=O)[O-] | nan | ||
| 9815542 | 9574 | None | 0 | Rat | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 195 | 6 | 3 | 3 | 0.7 | CCCC(O)P(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| CHEMBL112408 | 9574 | None | 0 | Rat | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 195 | 6 | 3 | 3 | 0.7 | CCCC(O)P(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| 9878233 | 111363 | None | 0 | Rat | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 253 | 8 | 2 | 4 | 1.7 | CC(C)OC(OC(C)C)P(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| CHEMBL326622 | 111363 | None | 0 | Rat | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 253 | 8 | 2 | 4 | 1.7 | CC(C)OC(OC(C)C)P(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| 10105390 | 9579 | None | 0 | Rat | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 233 | 6 | 2 | 2 | 2.6 | NCCCP(=O)(O)CCC1CCCCC1 | 10.1021/jm00017a016 | ||
| CHEMBL112460 | 9579 | None | 0 | Rat | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 233 | 6 | 2 | 2 | 2.6 | NCCCP(=O)(O)CCC1CCCCC1 | 10.1021/jm00017a016 | ||
| 10466591 | 9623 | None | 0 | Rat | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 235 | 6 | 2 | 3 | 1.6 | NCCCP(=O)(O)CCC1CCCCO1 | 10.1021/jm00017a016 | ||
| CHEMBL112639 | 9623 | None | 0 | Rat | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 235 | 6 | 2 | 3 | 1.6 | NCCCP(=O)(O)CCC1CCCCO1 | 10.1021/jm00017a016 | ||
| 44341174 | 9772 | None | 0 | Rat | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 343 | 9 | 5 | 5 | -0.5 | NCCCP(=O)(O)CC(O)CNC(=O)c1ccccc1C(N)=O | 10.1021/jm00017a016 | ||
| CHEMBL113540 | 9772 | None | 0 | Rat | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 343 | 9 | 5 | 5 | -0.5 | NCCCP(=O)(O)CC(O)CNC(=O)c1ccccc1C(N)=O | 10.1021/jm00017a016 | ||
| 9898878 | 110728 | None | 17 | Rat | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 151 | 4 | 2 | 2 | 0.6 | CCP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| CHEMBL325921 | 110728 | None | 17 | Rat | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 151 | 4 | 2 | 2 | 0.6 | CCP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| 130023 | 9778 | None | 4 | Rat | Binding | pIC50 | = | 4.7 | 4.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 207 | 8 | 2 | 2 | 2.2 | CCCCCCP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| CHEMBL113571 | 9778 | None | 4 | Rat | Binding | pIC50 | = | 4.7 | 4.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 207 | 8 | 2 | 2 | 2.2 | CCCCCCP(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| 9878836 | 10128 | None | 0 | Rat | Binding | pIC50 | = | 4.7 | 4.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 281 | 12 | 2 | 4 | 2.5 | CCCCOC(OCCCC)P(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| CHEMBL115664 | 10128 | None | 0 | Rat | Binding | pIC50 | = | 4.7 | 4.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 281 | 12 | 2 | 4 | 2.5 | CCCCOC(OCCCC)P(=O)(O)CCCN | 10.1021/jm00017a016 | ||
| 9923821 | 9984 | None | 0 | Rat | Binding | pIC50 | = | 4.7 | 4.7 | - | 0 | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. |
ChEMBL | 335 | 9 | 2 | 4 | 3.0 | CCOC(OCC)P(=O)(O)CC(CN)c1ccc(Cl)cc1 | 10.1021/jm00017a016 | ||
Showing 1 to 50 of 122 entries