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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 | |
[D-Lys1,des-Arg10]kallidin | 3627 | None | 0 | Human | Binding | pKi | None | - | 7.50 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9111052 | |
[des-Arg10]icatibant | 1377 | None | 0 | Human | Binding | pKi | None | - | 7.50 | -1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10422787 | |
[des-Arg10]icatibant | 1377 | None | 0 | Human | Binding | pKi | None | - | 7.50 | -1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9313952 | |
[des-Arg10]icatibant | 1377 | None | 0 | Mouse | Binding | pKi | None | - | 7.60 | 1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8856107 | |
[des-Arg10]icatibant | 1377 | None | 0 | Rat | Binding | pKi | None | - | 7.50 | -1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10422787 | |
[des-Arg10]kallidin | 1378 | None | 24 | Human | Binding | pKi | = | - | 9.80 | 6 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9111052 | |
[des-Arg10]kallidin | 1378 | None | 24 | Human | Binding | pKi | = | - | 9.80 | 6 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10422787 | |
[des-Arg10]kallidin | 1378 | None | 24 | Human | Binding | pKi | = | - | 9.80 | 6 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9313952 | |
[des-Arg10]kallidin | 1378 | None | 24 | Human | Binding | pKi | = | - | 9.80 | 6 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8735629 | |
[des-Arg10]kallidin | 1378 | None | 24 | Human | Binding | pKd | None | - | 9.40 | 6 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | - | |
[des-Arg10]kallidin | 1378 | None | 24 | Human | Binding | IC50 | = | 0.87 | 9.06 | 6 | 4 | Displacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 mins | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1016/j.bmcl.2013.01.025 | |
[des-Arg10]kallidin | 1378 | None | 24 | Human | Binding | Ki | = | 0.22 | 9.66 | 6 | 4 | Displacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 mins | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1016/j.bmcl.2013.01.025 | |
[des-Arg10]kallidin | 1378 | None | 24 | Mouse | Binding | pKi | = | - | 8.80 | -6 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8856107 | |
[des-Arg10]kallidin | 1378 | None | 24 | Rat | Binding | pKi | = | - | 8.80 | -6 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10422787 | |
[des-Arg11]T-kinin | 1379 | None | 0 | Human | Binding | pKi | None | - | 5.80 | -35 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10422787 | |
[des-Arg11]T-kinin | 1379 | None | 0 | Rat | Binding | pKi | None | - | 7.35 | 35 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10422787 | |
[des-Arg9]bradykinin | 1380 | None | 0 | Human | Binding | pKi | None | - | 5.75 | -2818 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10422787 | |
[des-Arg9]bradykinin | 1380 | None | 0 | Human | Binding | pKi | None | - | 5.75 | -2818 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9313952 | |
[des-Arg9]bradykinin | 1380 | None | 0 | Mouse | Binding | pKi | None | - | 9.20 | 2818 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8856107 | |
[des-Phe9,des-Arg10]kallidin | 1392 | None | 0 | Human | Binding | pKi | None | - | 6.15 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9111052 |
Showing 1 to 20 of 761 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 | |
[des-Arg10]icatibant | 1377 | None | 0 | Mouse | Functional | pA2 | = | - | 7.20 | - | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9650825 | |
[des-Arg10]kallidin | 1378 | None | 24 | Rat | Functional | EC50 | = | 85.00 | 7.07 | -97 | 4 | Compound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscle | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1016/S0960-894X(97)10042-7 | |
[Leu8,des-Arg9]bradykinin | 2306 | None | 11 | Mouse | Functional | pA2 | = | - | 6.90 | - | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8834490 | |
[Leu8,des-Arg9]bradykinin | 2306 | None | 11 | Mouse | Functional | pEC50 | None | - | 7.30 | - | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9276157 | |
[Leu9,des-Arg10]kallidin | 2308 | None | 19 | Human | Functional | IC50 | = | 990.00 | 6.00 | 2 | 2 | Antagonist activity against bradykinin B1 receptor in human HeLa cells assessed as inhibition of Des-Arg9-BK-induced increase in intracellular Ca2+ level by Fluro-4 direct calcium dye based fluorescence assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/acs.jmedchem.6b01011 | |
[Leu9,des-Arg10]kallidin | 2308 | None | 19 | Human | Functional | pIC50 | = | - | 8.90 | 2 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8063797 | |
[Leu9,des-Arg10]kallidin | 2308 | None | 19 | Mouse | Functional | pA2 | = | - | 7.00 | -2 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8834490 | |
B-9430 | 565 | None | 0 | Human | Functional | pA2 | = | - | 7.70 | -5 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9650825 | |
B-9430 | 565 | None | 0 | Mouse | Functional | pA2 | = | - | 6.10 | -199 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9650825 | |
B-9858 | 566 | None | 0 | Human | Functional | pA2 | = | - | 9.20 | - | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9650825 | |
CHEMBL1210741 | 15225 | None | 0 | Human | Functional | IC50 | = | 316.00 | 6.50 | - | 1 | Antagonist activity at human bradykinin B1 receptor assessed as inhibition of Lys-desArg9-BK-induced calcium flux | ChEMBL | 627.3 | 10 | 2 | 4 | 6.90 | CC(CN1CCCCC1)c1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H](NS(=O)(=O)c1cccc(C(F)(F)F)c1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.010 | |
CHEMBL1210742 | 15226 | None | 0 | Human | Functional | IC50 | = | 88.00 | 7.06 | - | 1 | Antagonist activity at human bradykinin B1 receptor assessed as inhibition of Lys-desArg9-BK-induced calcium flux | ChEMBL | 639.3 | 10 | 2 | 4 | 6.83 | O=C(C[C@@H](NS(=O)(=O)c1cccc(C(F)(F)F)c1)c1ccccc1)N[C@@H]1CCCc2cc(C3(CN4CCCCC4)CC3)ccc21 | https://dx.doi.org/10.1016/j.bmcl.2010.06.010 | |
CHEMBL1210743 | 15227 | None | 0 | Human | Functional | IC50 | = | 41.00 | 7.39 | - | 1 | Antagonist activity at human bradykinin B1 receptor assessed as inhibition of Lys-desArg9-BK-induced calcium flux | ChEMBL | 625.3 | 10 | 2 | 4 | 6.81 | C=C(CN1CCCCC1)c1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H](NS(=O)(=O)c1cccc(C(F)(F)F)c1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.010 | |
CHEMBL1210744 | 15228 | None | 0 | Human | Functional | IC50 | = | 9.70 | 8.01 | - | 1 | Antagonist activity at human bradykinin B1 receptor assessed as inhibition of Lys-desArg9-BK-induced calcium flux | ChEMBL | 611.2 | 10 | 2 | 4 | 6.42 | C=C(CN1CCCC1)c1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H](NS(=O)(=O)c1cccc(C(F)(F)F)c1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.010 | |
CHEMBL1210745 | 15229 | None | 0 | Human | Functional | IC50 | = | 3.90 | 8.41 | - | 1 | Antagonist activity at human bradykinin B1 receptor assessed as inhibition of Lys-desArg9-BK-induced calcium flux | ChEMBL | 627.2 | 10 | 3 | 5 | 5.39 | C=C(CN1CC[C@H](O)C1)c1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H](NS(=O)(=O)c1cccc(C(F)(F)F)c1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.010 | |
CHEMBL1210746 | 15230 | None | 0 | Human | Functional | IC50 | = | 15.00 | 7.82 | - | 1 | Antagonist activity at human bradykinin B1 receptor assessed as inhibition of Lys-desArg9-BK-induced calcium flux | ChEMBL | 627.2 | 10 | 3 | 5 | 5.39 | C=C(CN1CC[C@@H](O)C1)c1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H](NS(=O)(=O)c1cccc(C(F)(F)F)c1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.010 | |
CHEMBL1210747 | 15231 | None | 0 | Human | Functional | IC50 | = | 206.00 | 6.69 | - | 1 | Antagonist activity at human bradykinin B1 receptor assessed as inhibition of Lys-desArg9-BK-induced calcium flux | ChEMBL | 597.2 | 10 | 2 | 4 | 6.03 | C=C(CN1CCC1)c1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H](NS(=O)(=O)c1cccc(C(F)(F)F)c1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.010 | |
CHEMBL1210748 | 15232 | None | 0 | Human | Functional | IC50 | = | 154.00 | 6.81 | - | 1 | Antagonist activity at human bradykinin B1 receptor assessed as inhibition of Lys-desArg9-BK-induced calcium flux | ChEMBL | 585.2 | 10 | 2 | 4 | 5.88 | C=C(CN(C)C)c1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H](NS(=O)(=O)c1cccc(C(F)(F)F)c1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.010 | |
CHEMBL1210749 | 15233 | None | 0 | Human | Functional | IC50 | = | 32.00 | 7.50 | - | 1 | Antagonist activity at human bradykinin B1 receptor assessed as inhibition of Lys-desArg9-BK-induced calcium flux | ChEMBL | 601.2 | 12 | 4 | 5 | 4.90 | C=C(CNCCO)c1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H](NS(=O)(=O)c1cccc(C(F)(F)F)c1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.010 | |
CHEMBL1210750 | 15234 | None | 0 | Human | Functional | IC50 | = | 23.00 | 7.64 | - | 1 | Antagonist activity at human bradykinin B1 receptor assessed as inhibition of Lys-desArg9-BK-induced calcium flux | ChEMBL | 615.2 | 13 | 3 | 5 | 5.56 | C=C(CNCCOC)c1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H](NS(=O)(=O)c1cccc(C(F)(F)F)c1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.010 |
Showing 1 to 20 of 625 entries