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 | |
5-oxo-ETE | 155 | None | 17 | Human | Binding | pKd | = | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | 318.2 | 14 | 1 | 2 | 5.40 | CCCCC/C=C\C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/9829988 | |
CHEMBL3115774 | 105356 | None | 5 | Human | Binding | IC50 | = | 402.00 | 6.40 | - | 1 | Antagonist activity at OXE receptor (unknown origin) expressed in neutrophils assessed as inhibition of 5-oxo-ETE-induced cell migration after 2 hrs by hematoxylin/chromotrope 2R staining-based microscopic analysis | ChEMBL | 363.2 | 9 | 1 | 3 | 5.56 | CCCCCCc1cc2ccc(Cl)cc2n1C(=O)CC(C)CC(=O)O | https://dx.doi.org/10.1021/jm401292m | |
CHEMBL3115774 | 105356 | None | 5 | Human | Binding | IC50 | = | 30.00 | 7.52 | - | 1 | Antagonist activity at OXE receptor (unknown origin) expressed in anti-CD49d-labeled eosinophils assessed as inhibition of 5-oxo-ETE-induced F-actin polymerization preincubated for 5 mins followed by 5-oxo-ETE induction measured after 20 secs by flow cytometric analysis | ChEMBL | 363.2 | 9 | 1 | 3 | 5.56 | CCCCCCc1cc2ccc(Cl)cc2n1C(=O)CC(C)CC(=O)O | https://dx.doi.org/10.1021/jm401292m | |
CHEMBL3115775 | 105357 | None | 0 | Human | Binding | IC50 | = | 454.00 | 6.34 | - | 1 | Antagonist activity at OXE receptor (unknown origin) expressed in neutrophils assessed as inhibition of 5-oxo-ETE-induced cell migration after 2 hrs by hematoxylin/chromotrope 2R staining-based microscopic analysis | ChEMBL | 377.2 | 10 | 1 | 3 | 5.64 | CCCCCCc1c(C(=O)CC(C)CC(=O)O)c2cc(Cl)ccc2n1C | https://dx.doi.org/10.1021/jm401292m | |
CHEMBL3115775 | 105357 | None | 0 | Human | Binding | IC50 | = | 33.00 | 7.48 | - | 1 | Antagonist activity at OXE receptor (unknown origin) expressed in anti-CD49d-labeled eosinophils assessed as inhibition of 5-oxo-ETE-induced F-actin polymerization preincubated for 5 mins followed by 5-oxo-ETE induction measured after 20 secs by flow cytometric analysis | ChEMBL | 377.2 | 10 | 1 | 3 | 5.64 | CCCCCCc1c(C(=O)CC(C)CC(=O)O)c2cc(Cl)ccc2n1C | https://dx.doi.org/10.1021/jm401292m | |
docosahexaenoic acid | 1455 | None | 44 | Human | Binding | pIC50 | = | 5.70 | 8.24 | - | 2 | Antagonist activity at human OXE receptor fused with G-alphai assessed as inhibition of 5-oxo-ETE-induced GTPgammaS binding after 60 mins by liquid scintillation counting analysis | Drug Central | 328.2 | 14 | 1 | 1 | 6.55 | CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)O | - | |
EPA | 1570 | None | 51 | Human | Binding | pIC50 | = | 5.70 | 8.24 | - | 2 | Antagonist activity at human OXE receptor fused with G-alphai assessed as inhibition of 5-oxo-ETE-induced GTPgammaS binding after 60 mins by liquid scintillation counting analysis | Drug Central | 302.2 | 13 | 1 | 1 | 5.99 | CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)O | - |
Showing 1 to 7 of 7 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 | |
12S-HETE | 12 | None | 27 | Human | Functional | IC50 | = | 500.00 | 6.30 | -1778 | 3 | Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition by fluorescence assay | ChEMBL | 320.2 | 14 | 2 | 2 | 5.19 | CCCCC/C=C\C[C@H](O)/C=C/C=C\C/C=C\CCCC(=O)O | https://dx.doi.org/10.1021/acs.jmedchem.8b00154 | |
5-(6-chloro-2-hexyl-1H-indol-1-yl)-5-oxo-valeric acid | 127 | None | 0 | Human | Functional | pIC50 | = | - | 6.40 | - | 1 | Unclassified | Guide to Pharmacology | 349.1 | 9 | 1 | 3 | 5.31 | CCCCCCc1cc2ccc(Cl)cc2n1C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/23581530 | |
5-oxo-12-HETE | 151 | None | 1 | Human | Functional | pIC50 | = | - | 6.30 | - | 1 | Unclassified | Guide to Pharmacology | 334.2 | 14 | 2 | 3 | 4.37 | CCCCC/C=C\C[C@H](O)/C=C/C=C\C=C\C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/9920859 | |
5-oxo-12-HETE | 151 | None | 1 | Human | Functional | IC50 | = | 500.00 | 6.30 | - | 1 | Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization by spectrofluorometric analysis | ChEMBL | 334.2 | 14 | 2 | 3 | 4.37 | CCCCC/C=C\C[C@H](O)/C=C/C=C\C=C\C(=O)CCCC(=O)O | https://dx.doi.org/10.1021/jm401292m | |
5-oxo-15-HETE | 152 | None | 5 | Human | Functional | pEC50 | = | - | 7.70 | - | 1 | Unclassified | Guide to Pharmacology | 334.2 | 14 | 2 | 3 | 4.37 | CCCCC[C@H](O)/C=C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/7803484 | |
5-oxo-15-HETE | 152 | None | 5 | Human | Functional | pEC50 | = | - | 7.70 | - | 1 | Unclassified | Guide to Pharmacology | 334.2 | 14 | 2 | 3 | 4.37 | CCCCC[C@H](O)/C=C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/8387490 | |
5-oxo-15-HETE | 152 | None | 5 | Human | Functional | pEC50 | = | - | 7.70 | - | 1 | Unclassified | Guide to Pharmacology | 334.2 | 14 | 2 | 3 | 4.37 | CCCCC[C@H](O)/C=C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/7797484 | |
5-oxo-15-HETE | 152 | None | 5 | Human | Functional | pEC50 | = | - | 7.70 | - | 1 | Unclassified | Guide to Pharmacology | 334.2 | 14 | 2 | 3 | 4.37 | CCCCC[C@H](O)/C=C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/8598482 | |
5-oxo-15-HETE | 152 | None | 5 | Human | Functional | EC50 | = | 56.00 | 7.25 | - | 1 | Agonist activity at 5-oxo-ETE receptor in human neutrophils assessed as stimulation of ca2+ mobilization | ChEMBL | 334.2 | 14 | 2 | 3 | 4.37 | CCCCC[C@H](O)/C=C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://dx.doi.org/10.1016/j.bmcl.2011.01.032 | |
5-oxo-20-HETE | 153 | None | 0 | Human | Functional | pEC50 | = | - | 6.50 | - | 1 | Unclassified | Guide to Pharmacology | 334.2 | 15 | 2 | 3 | 4.37 | O=C(O)CCCC(=O)/C=C/C=C\C/C=C\C/C=C\CCCCCO | https://pubmed.ncbi.nlm.nih.gov/8598482 | |
5-oxo-C20:3 | 154 | None | 0 | Human | Functional | pEC50 | = | - | 8.00 | - | 1 | Unclassified | Guide to Pharmacology | 320.2 | 15 | 1 | 2 | 5.62 | CCCCCCCC/C=C\C/C=C\C=C/C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/18292294 | |
5-oxo-ETE | 155 | None | 17 | Human | Functional | pEC50 | = | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | 318.2 | 14 | 1 | 2 | 5.40 | CCCCC/C=C\C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/7797484 | |
5-oxo-ETE | 155 | None | 17 | Human | Functional | pEC50 | = | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | 318.2 | 14 | 1 | 2 | 5.40 | CCCCC/C=C\C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/19450703 | |
5-oxo-ETE | 155 | None | 17 | Human | Functional | pEC50 | = | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | 318.2 | 14 | 1 | 2 | 5.40 | CCCCC/C=C\C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/18292294 | |
5-oxo-ETE | 155 | None | 17 | Human | Functional | pEC50 | = | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | 318.2 | 14 | 1 | 2 | 5.40 | CCCCC/C=C\C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/9829988 | |
5-oxo-ETE | 155 | None | 17 | Human | Functional | pEC50 | = | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | 318.2 | 14 | 1 | 2 | 5.40 | CCCCC/C=C\C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/1326548 | |
5-oxo-ETE | 155 | None | 17 | Human | Functional | EC50 | = | 7.00 | 8.15 | - | 1 | Agonist activity at 5-oxo-ETE receptor in human neutrophils assessed as stimulation of ca2+ mobilization | ChEMBL | 318.2 | 14 | 1 | 2 | 5.40 | CCCCC/C=C\C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://dx.doi.org/10.1016/j.bmcl.2011.01.032 | |
5-oxo-ETE | 155 | None | 17 | Human | Functional | EC50 | = | 220.00 | 6.66 | - | 1 | Agonist activity at human PK-tagged OXER1 expressed in CHOK1 cells assessed as EA-tagged beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation assay | ChEMBL | 318.2 | 14 | 1 | 2 | 5.40 | CCCCC/C=C\C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://dx.doi.org/10.1016/j.bmc.2018.05.036 | |
5-oxo-ETE | 155 | None | 17 | Human | Functional | EC50 | = | 67.00 | 7.17 | - | 1 | Agonist activity at OXE receptor (unknown origin) expressed in HEK293 cells co-expressing Galpha subunit G16 assessed as calcium mobilization using Oregon Green 488 BAPTA-1/AM by fluorescence assay | ChEMBL | 318.2 | 14 | 1 | 2 | 5.40 | CCCCC/C=C\C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://dx.doi.org/10.1039/C1MD00231G | |
5-oxo-ETE | 155 | None | 17 | Human | Functional | IC50 | = | 3.00 | 8.52 | - | 1 | Desensitization of 5-oxo-ETE receptor in indo-1-labeled human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization | ChEMBL | 318.2 | 14 | 1 | 2 | 5.40 | CCCCC/C=C\C/C=C\C/C=C\C=C\C(=O)CCCC(=O)O | https://dx.doi.org/10.1016/j.bmcl.2011.02.021 |
Showing 1 to 20 of 107 entries