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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 | |
11-deoxy-PGE1 | 7 | None | 0 | Rat | Binding | pKi | None | - | 8.50 | -2 | 6 | Unclassified | Guide to Pharmacology | 338.2 | 13 | 2 | 3 | 4.50 | CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/9537820 | |
11-deoxy-PGE1 | 7 | None | 0 | Mouse | Binding | pKi | = | - | 8.82 | -1 | 6 | Unclassified | Guide to Pharmacology | 338.2 | 13 | 2 | 3 | 4.50 | CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/9313928 | |
13,14-dihydro-16-m-chlorophenoxy-w-tetranor-PGF1α | 16 | None | 0 | Human | Binding | IC50 | = | 3100.00 | 5.51 | - | 5 | Affinity for Prostanoid EP3 receptor expressed in CHO cell line | ChEMBL | 428.2 | 13 | 4 | 5 | 3.64 | O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)COc1cccc(Cl)c1 | https://dx.doi.org/10.1021/jm990542v | |
16,16-dimethyl-PGE2 | 24 | None | 0 | Mouse | Binding | pKi | = | - | 8.72 | 8 | 3 | Unclassified | Guide to Pharmacology | 380.3 | 12 | 3 | 4 | 3.89 | CCCCC(C)(C)[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/9313928 | |
17-phenyl-ω-trinor-PGE2 | 26 | None | 0 | Rat | Binding | pKi | = | - | 8.37 | -1 | 7 | Unclassified | Guide to Pharmacology | 386.2 | 11 | 3 | 4 | 3.30 | O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCc1ccccc1 | https://pubmed.ncbi.nlm.nih.gov/9537820 | |
17-phenyl-ω-trinor-PGE2 | 26 | None | 0 | Mouse | Binding | pKi | = | - | 8.43 | 1 | 7 | Unclassified | Guide to Pharmacology | 386.2 | 11 | 3 | 4 | 3.30 | O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCc1ccccc1 | https://pubmed.ncbi.nlm.nih.gov/9313928 | |
2-(4'-Methylaminophenyl)Benzothiazole | 220178 | 3H-EP2 | 0 | Human | Binding | pKi | = | 2.00 | 8.70 | 1 | 7 | - | PDSP KiDatabase | 268.1 | 3 | 1 | 5 | 4.75 | CNc1ccc(N=Nc2ccc3ncsc3c2)cc1 | - | |
AH-23848 | 218901 | 3H-PGE2 | 0 | Human | Binding | pKi | = | 4419.00 | 5.35 | -4 | 6 | - | PDSP KiDatabase | 477.3 | 11 | 1 | 5 | 5.08 | O=C1CCC(CCC(=CCC(C(=O)O)N2CCOCC2)OCc2ccc(-c3ccccc3)cc2)C1 | - | |
AH-23848 | 218901 | 3H-PGE2 | 0 | Human | Binding | pKi | = | 4090.00 | 5.39 | -4 | 6 | - | PDSP KiDatabase | 477.3 | 11 | 1 | 5 | 5.08 | O=C1CCC(CCC(=CCC(C(=O)O)N2CCOCC2)OCc2ccc(-c3ccccc3)cc2)C1 | - | |
AH13205 | 317 | 3H-PGE2 | 0 | Mouse | Binding | pKi | = | 82.00 | 7.09 | 3 | 3 | - | PDSP KiDatabase | 388.3 | 13 | 2 | 3 | 5.79 | CCCCCC(O)c1ccc(C2CCC(=O)C2CCCCCCC(=O)O)cc1 | - | |
AH13205 | 317 | 3H-PGE2 | 0 | Mouse | Binding | pKi | = | 82.00 | 7.09 | 3 | 3 | - | PDSP KiDatabase | 388.3 | 13 | 2 | 3 | 5.79 | CCCCCC(O)c1ccc(C2CCC(=O)C2CCCCCCC(=O)O)cc1 | - | |
AH6809 | 320 | None | 49 | Human | Binding | pKi | = | - | 5.80 | -4 | 10 | Unclassified | Guide to Pharmacology | 298.1 | 3 | 1 | 4 | 3.43 | CC(C)Oc1ccc2c(=O)c3cc(C(=O)O)ccc3oc2c1 | https://pubmed.ncbi.nlm.nih.gov/10634944 | |
AH6809 | 320 | 3H-PGE2 | 49 | Human | Binding | pKi | = | 1597.00 | 5.80 | -4 | 10 | - | PDSP KiDatabase | 298.1 | 3 | 1 | 4 | 3.43 | CC(C)Oc1ccc2c(=O)c3cc(C(=O)O)ccc3oc2c1 | - | |
amisulpride | 400 | 3H-PGE2 | 72 | Human | Binding | pKi | = | 10000.00 | 5.00 | -4365 | 53 | - | PDSP KiDatabase | 369.2 | 7 | 2 | 6 | 1.28 | CCN1CCCC1CNC(=O)c1cc(S(=O)(=O)CC)c(N)cc1OC | - | |
ANANDAMIDE | 218558 | 3H-PGE2 | 0 | Bovine | Binding | pKi | = | 10000.00 | 5.00 | -147 | 6 | - | PDSP KiDatabase | 347.3 | 16 | 2 | 2 | 5.24 | CCCCCC=CCC=CCC=CCC=CCCCC(=O)NCCO | - | |
aripiprazole | 470 | 3H-PGE2 | 70 | Human | Binding | pKi | = | 10000.00 | 5.00 | -7244 | 60 | - | PDSP KiDatabase | 447.1 | 7 | 1 | 4 | 4.86 | O=C1CCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 | - | |
aripiprazole | 470 | 3H-PGE2 | 70 | Human | Binding | pKi | = | 10000.00 | 5.00 | -7244 | 60 | - | PDSP KiDatabase | 447.1 | 7 | 1 | 4 | 4.86 | O=C1CCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 | - | |
ASENAPINE | 107587 | 3H-PGE2 | 16 | Human | Binding | pKi | = | 10000.00 | 5.00 | -58884 | 54 | - | PDSP KiDatabase | 285.1 | 0 | 0 | 2 | 4.26 | CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 | - | |
beraprost | 601 | None | 0 | Human | Binding | pKi | = | - | 6.17 | -42 | 5 | Unclassified | Guide to Pharmacology | 398.2 | 8 | 3 | 4 | 3.29 | CC#CCC(C)C(O)/C=C/C1C(O)CC2Oc3c(CCCC(=O)O)cccc3C21 | https://pubmed.ncbi.nlm.nih.gov/17545310 | |
beraprost | 220183 | None | 0 | Human | Binding | pKi | = | 6.17 | 8.21 | -1 | 5 | None | Drug Central | 398.2 | 8 | 3 | 4 | 3.29 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2c3cccc(CCCC(=O)O)c3O[C@H]2C[C@H]1O | - |
Showing 1 to 20 of 1,344 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 | |
AH6809 | 320 | None | 49 | Human | Functional | Ki | = | 1600.00 | 5.80 | - | 10 | Antagonist activity at EP3 receptor (unknown origin) by functional cAMP assay | ChEMBL | 298.1 | 3 | 1 | 4 | 3.43 | CC(C)Oc1ccc2c(=O)c3cc(C(=O)O)ccc3oc2c1 | https://dx.doi.org/10.1021/jm401431x | |
bimatoprost (free acid form) | 659 | None | 34 | Human | Functional | EC50 | = | 8600.00 | 5.07 | -1737 | 2 | Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay | ChEMBL | 388.2 | 11 | 4 | 4 | 3.10 | O=C(O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCc1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.6b00415 | |
CHEMBL1090937 | 8048 | None | 0 | Mouse | Functional | IC50 | = | 3.80 | 8.42 | - | 3 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 554.2 | 12 | 1 | 7 | 4.16 | CN(CCOc1cc(Cn2cccn2)ccc1CCC(=O)NS(=O)(=O)c1ccc(F)c(F)c1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1090938 | 8049 | None | 0 | Mouse | Functional | IC50 | = | 24.00 | 7.62 | - | 1 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 552.2 | 11 | 1 | 5 | 5.24 | CN(C)Cc1ccc(CCC(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c(OCCc2ccc3ccccc3c2)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1091738 | 8133 | None | 0 | Mouse | Functional | IC50 | = | 10.00 | 8.00 | - | 1 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 587.2 | 11 | 1 | 6 | 6.11 | Cc1ccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)cc1Cl | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1091739 | 8134 | None | 0 | Mouse | Functional | IC50 | = | 7.80 | 8.11 | - | 1 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 607.1 | 11 | 1 | 6 | 6.45 | O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1091740 | 8135 | None | 0 | Mouse | Functional | IC50 | = | 5.50 | 8.26 | - | 1 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 591.1 | 11 | 1 | 6 | 5.94 | O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(Cl)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1091741 | 8136 | None | 0 | Mouse | Functional | IC50 | = | 1.20 | 8.92 | - | 3 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 575.2 | 11 | 1 | 6 | 5.42 | O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1091742 | 8137 | None | 0 | Mouse | Functional | IC50 | = | 18.00 | 7.75 | - | 1 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 564.2 | 11 | 1 | 7 | 5.01 | N#Cc1cccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1091743 | 8138 | None | 0 | Mouse | Functional | IC50 | = | 1.40 | 8.85 | - | 3 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 576.2 | 11 | 2 | 7 | 4.88 | O=C(CCc1ccc(Cn2cccn2)cc1ONCc1cccc2ccccc12)NS(=O)(=O)c1ccc(F)c(F)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1091744 | 8139 | None | 0 | Mouse | Functional | IC50 | = | 6.40 | 8.19 | - | 3 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 610.2 | 12 | 1 | 8 | 4.11 | O=C(CCc1ccc(Cn2cccn2)cc1OCCc1cccc(N2CCOCC2)c1)NS(=O)(=O)c1ccc(F)c(F)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1092097 | 8197 | None | 0 | Mouse | Functional | IC50 | = | 47.00 | 7.33 | - | 2 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 594.2 | 11 | 1 | 6 | 5.01 | O=C(CCc1ccc(CN2CCOCC2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1092266 | 8227 | None | 0 | Mouse | Functional | IC50 | = | 140.00 | 6.85 | - | 1 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 539.2 | 11 | 1 | 6 | 5.14 | O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1092267 | 8228 | None | 0 | Mouse | Functional | IC50 | = | 820.00 | 6.09 | - | 1 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 540.2 | 10 | 2 | 6 | 4.89 | O=C(NCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1092431 | 8259 | None | 0 | Mouse | Functional | IC50 | = | 24.00 | 7.62 | - | 2 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 626.2 | 12 | 1 | 6 | 6.63 | N#Cc1cccc(OCc2ccc(CCC(=O)NS(=O)(=O)c3ccc(F)c(F)c3)c(OCCc3ccc4ccccc4c3)c2)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1092432 | 8260 | None | 0 | Mouse | Functional | IC50 | = | 0.40 | 9.40 | - | 3 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 602.2 | 12 | 1 | 6 | 6.15 | O=C(CCc1ccc(COc2cccnc2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1092976 | 8352 | None | 0 | Mouse | Functional | IC50 | = | 51.00 | 7.29 | - | 2 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 541.1 | 12 | 1 | 7 | 4.11 | O=C(CCc1ccc(Cn2cccn2)cc1OCCOc1ccccc1)NS(=O)(=O)c1ccc(F)c(F)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1093537 | 8428 | None | 0 | Mouse | Functional | IC50 | = | 190.00 | 6.72 | - | 1 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 540.2 | 11 | 1 | 7 | 4.54 | O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccn1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1093819 | 8464 | None | 0 | Mouse | Functional | IC50 | = | 110.00 | 6.96 | - | 1 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 560.2 | 11 | 1 | 8 | 4.91 | Cc1csc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)n1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 | |
CHEMBL1093820 | 8465 | None | 0 | Mouse | Functional | IC50 | = | 59.00 | 7.23 | - | 3 | Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin | ChEMBL | 525.2 | 11 | 1 | 6 | 4.27 | O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccccc1)NS(=O)(=O)c1ccc(F)c(F)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.034 |
Showing 1 to 20 of 498 entries