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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
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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 | ||||||||||||||||||
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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 | |
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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 | |
| bergapten | 602 | None | 70 | Human | Functional | pEC50 | = | - | 5.55 | 1 | 3 | Unclassified | Guide to Pharmacology | 216.0 | 1 | 0 | 4 | 2.55 | COc1c2ccoc2cc2oc(=O)ccc12 | https://pubmed.ncbi.nlm.nih.gov/26501253 | |
| brucine | 732 | None | 34 | Human | Functional | EC50 | = | 60000.00 | 4.22 | - | 6 | Activity at human TAS2R10 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay | ChEMBL | 394.2 | 2 | 0 | 5 | 2.11 | COc1cc2c(cc1OC)[C@@]13CCN4CC5=CCO[C@H]6CC(=O)N2[C@H]1[C@H]6[C@H]5C[C@H]43 | - | |
| CHEMBL4440983 | 170016 | None | 0 | Human | Functional | EC50 | = | 21720.00 | 4.66 | -1 | 3 | Competitive-antagonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R10 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as inhibition of strychnine-induced increase in intracellular calcium level by measuring strychnine EC50 at 100 uM by FLIPR assay (Rvb = 0.39 +/- 0.09 uM) | ChEMBL | 250.2 | 0 | 1 | 3 | 2.60 | C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)[C@@H]2CC1 | - | |
| CHEMBL4440983 | 170016 | None | 0 | Human | Functional | EC50 | = | 5390.00 | 5.27 | -1 | 3 | Competitive-antagonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R10 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as inhibition of strychnine-induced increase in intracellular calcium level by measuring strychnine EC50 at 30 uM by FLIPR assay (Rvb = 0.39 +/- 0.09 uM) | ChEMBL | 250.2 | 0 | 1 | 3 | 2.60 | C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)[C@@H]2CC1 | - | |
| CHEMBL4440983 | 170016 | None | 0 | Human | Functional | EC50 | = | 2740.00 | 5.56 | -1 | 3 | Competitive-antagonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R10 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as inhibition of strychnine-induced increase in intracellular calcium level by measuring strychnine EC50 at 10 uM by FLIPR assay (Rvb = 0.39 +/- 0.09 uM) | ChEMBL | 250.2 | 0 | 1 | 3 | 2.60 | C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)[C@@H]2CC1 | - | |
| CHEMBL4440983 | 170016 | None | 0 | Human | Functional | EC50 | = | 25200.00 | 4.60 | -1 | 3 | Agonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R10 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as increase in intracellular calcium level by FLIPR assay | ChEMBL | 250.2 | 0 | 1 | 3 | 2.60 | C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)[C@@H]2CC1 | - | |
| CHEMBL4582048 | 175800 | None | 0 | Human | Functional | EC50 | = | 25200.00 | 4.60 | -3 | 3 | Agonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R10 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as effect on intracellular calcium level by FLIPR assay | ChEMBL | 250.2 | 0 | 1 | 3 | 2.60 | C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)C2CC1 | - | |
| cucurbitacin B | 1218 | None | 0 | Human | Functional | pEC50 | = | - | 5.20 | - | 1 | Unclassified | Guide to Pharmacology | 558.3 | 5 | 3 | 8 | 3.50 | CC(=O)OC(C)(C)/C=C/C(=O)[C@](C)(O)[C@H]1[C@H](O)C[C@@]2(C)[C@@H]3CC=C4[C@@H](C[C@H](O)C(=O)C4(C)C)[C@]3(C)C(=O)C[C@]12C | https://pubmed.ncbi.nlm.nih.gov/23283334 | |
| denatonium | 1365 | None | 6 | Human | Functional | pEC50 | = | - | 4.13 | -269 | 5 | Unclassified | Guide to Pharmacology | 325.2 | 7 | 1 | 1 | 4.30 | CC[N+](CC)(CC(=O)Nc1c(C)cccc1C)Cc1ccccc1 | https://pubmed.ncbi.nlm.nih.gov/23283334 | |
| denatonium | 1365 | None | 6 | Human | Functional | EC50 | = | 70000.00 | 4.16 | -269 | 5 | Activity at human TAS2R10 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay | ChEMBL | 325.2 | 7 | 1 | 1 | 4.30 | CC[N+](CC)(CC(=O)Nc1c(C)cccc1C)Cc1ccccc1 | - | |
| isoprenaline | 2091 | None | 34 | Human | Functional | pEC50 | = | 8.31 | 8.08 | -63 | 49 | Agonist activity at human TAS2R10 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | Drug Central | 211.1 | 4 | 4 | 4 | 1.13 | CC(C)NCC(O)c1ccc(O)c(O)c1 | - | |
| isoprenaline | 2091 | None | 34 | Human | Functional | EC50 | = | 4.90 | 8.31 | -63 | 49 | Agonist activity at human TAS2R10 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | ChEMBL | 211.1 | 4 | 4 | 4 | 1.13 | CC(C)NCC(O)c1ccc(O)c(O)c1 | - | |
| strychnine | 3693 | None | 28 | Human | Functional | pEC50 | = | - | 4.48 | -19 | 7 | Unclassified | Guide to Pharmacology | 334.2 | 0 | 0 | 3 | 2.09 | O=C1C[C@@H]2OCC=C3CN4CC[C@]56c7ccccc7N1[C@H]5[C@H]2[C@H]3C[C@H]46 | https://pubmed.ncbi.nlm.nih.gov/20022913 | |
| strychnine | 3693 | None | 28 | Human | Functional | EC50 | = | 40000.00 | 4.40 | -19 | 7 | Activity at human TAS2R10 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay | ChEMBL | 334.2 | 0 | 0 | 3 | 2.09 | O=C1C[C@@H]2OCC=C3CN4CC[C@]56c7ccccc7N1[C@H]5[C@H]2[C@H]3C[C@H]46 | - | |
| strychnine | 3693 | None | 28 | Human | Functional | EC50 | = | 5000.00 | 5.30 | -19 | 7 | Activity at human TAS2R10 expressed in HEK293/15 cells assessed as effect on calcium response by FLIPR assay | ChEMBL | 334.2 | 0 | 0 | 3 | 2.09 | O=C1C[C@@H]2OCC=C3CN4CC[C@]56c7ccccc7N1[C@H]5[C@H]2[C@H]3C[C@H]46 | - | |
| strychnine | 3693 | None | 28 | Human | Functional | pEC50 | = | 5.30 | 8.28 | -19 | 7 | Activity at human TAS2R10 expressed in HEK293/15 cells assessed as effect on calcium response by FLIPR assay | Drug Central | 334.2 | 0 | 0 | 3 | 2.09 | O=C1C[C@@H]2OCC=C3CN4CC[C@]56c7ccccc7N1[C@H]5[C@H]2[C@H]3C[C@H]46 | - | |
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