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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 | |
1-OH-PGE1 | 36 | None | 0 | Mouse | Binding | pKi | None | - | 6.70 | - | 1 | Unclassified | Guide to Pharmacology | 370.2 | 13 | 4 | 5 | 2.45 | CC(O)CCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/9313928 | |
11-deoxy-PGE1 | 7 | None | 0 | Human | Binding | pKi | None | - | 8.90 | 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/10952683 | |
11-deoxy-PGE1 | 7 | None | 0 | Mouse | Binding | pKi | None | - | 7.60 | -19 | 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 | |
11-deoxy-PGE2 | 8 | None | 0 | Rat | Binding | pKi | None | - | 9.00 | - | 1 | Unclassified | Guide to Pharmacology | 336.2 | 12 | 2 | 3 | 4.28 | CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)[C@@H]1C/C=C\CCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/9537820 | |
13,14-dihydro-PGE1 | 17 | None | 0 | Human | Binding | pKi | None | - | 8.50 | - | 1 | Unclassified | Guide to Pharmacology | 356.3 | 14 | 3 | 4 | 3.70 | CCCCC[C@H](O)CC[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/10952683 | |
16,16-dimethyl-PGE2 | 24 | None | 0 | Mouse | Binding | pKi | None | - | 7.40 | -20 | 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 | |
19(R)-OH-PGE2 | 28 | None | 0 | Rat | Binding | pKi | None | - | 7.50 | 5 | 3 | Unclassified | Guide to Pharmacology | 368.2 | 12 | 4 | 5 | 2.22 | C[C@@H](O)CCC[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/9537820 | |
2-(4'-Methylaminophenyl)Benzothiazole | 220178 | 3H-EP2 | 0 | Human | Binding | pKi | = | 12.00 | 7.92 | -6 | 7 | - | PDSP KiDatabase | 268.1 | 3 | 1 | 5 | 4.75 | CNc1ccc(N=Nc2ccc3ncsc3c2)cc1 | - | |
AH-23848 | 218901 | 3H-PGE2 | 0 | Human | Binding | pKi | = | 9287.00 | 5.03 | -9 | 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 | = | 10000.00 | 5.00 | -9 | 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 | = | 10000.00 | 5.00 | -9 | 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 | = | 10000.00 | 5.00 | -9 | 6 | - | PDSP KiDatabase | 477.3 | 11 | 1 | 5 | 5.08 | O=C1CCC(CCC(=CCC(C(=O)O)N2CCOCC2)OCc2ccc(-c3ccccc3)cc2)C1 | - | |
AH23848 | 318 | None | 0 | Human | Binding | pKi | None | - | 5.25 | -12 | 3 | Unclassified | Guide to Pharmacology | 477.3 | 11 | 1 | 5 | 4.73 | O=C(O)CC/C=C\CC[C@H]1[C@@H](OCc2ccc(-c3ccccc3)cc2)CC(=O)[C@@H]1N1CCOCC1 | https://pubmed.ncbi.nlm.nih.gov/10634944 | |
AH23848 | 318 | None | 0 | Human | Binding | pKi | None | - | 5.25 | -12 | 3 | Unclassified | Guide to Pharmacology | 477.3 | 11 | 1 | 5 | 4.73 | O=C(O)CC/C=C\CC[C@H]1[C@@H](OCc2ccc(-c3ccccc3)cc2)CC(=O)[C@@H]1N1CCOCC1 | https://pubmed.ncbi.nlm.nih.gov/10952683 | |
AH23848 | 318 | None | 0 | Human | Binding | pKi | None | - | 5.00 | -12 | 3 | Unclassified | Guide to Pharmacology | 477.3 | 11 | 1 | 5 | 4.73 | O=C(O)CC/C=C\CC[C@H]1[C@@H](OCc2ccc(-c3ccccc3)cc2)CC(=O)[C@@H]1N1CCOCC1 | https://pubmed.ncbi.nlm.nih.gov/10634944 | |
AH23848 | 318 | None | 0 | Rat | Binding | pKi | None | - | 5.10 | -12 | 3 | Unclassified | Guide to Pharmacology | 477.3 | 11 | 1 | 5 | 4.73 | O=C(O)CC/C=C\CC[C@H]1[C@@H](OCc2ccc(-c3ccccc3)cc2)CC(=O)[C@@H]1N1CCOCC1 | https://pubmed.ncbi.nlm.nih.gov/9537820 | |
AH23848 (racemic) | 319 | None | 0 | Rat | Binding | pKi | None | - | 5.00 | - | 1 | Unclassified | Guide to Pharmacology | 477.3 | 11 | 1 | 5 | 4.73 | O=C(O)CC/C=C/CCC1C(OCc2ccc(-c3ccccc3)cc2)CC(=O)C1N1CCOCC1 | https://pubmed.ncbi.nlm.nih.gov/9537820 | |
AH6809 | 320 | 3H-PGE2 | 49 | Human | Binding | pKi | = | 10000.00 | 5.00 | -10 | 10 | - | PDSP KiDatabase | 298.1 | 3 | 1 | 4 | 3.43 | CC(C)Oc1ccc2c(=O)c3cc(C(=O)O)ccc3oc2c1 | - | |
AH6809 | 320 | 3H-PGE2 | 49 | Human | Binding | pKi | = | 1150.00 | 5.94 | -10 | 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 | - |
Showing 1 to 20 of 1,261 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 | |
11-deoxy-PGE1 | 7 | None | 0 | Human | Functional | pEC50 | = | - | 9.33 | - | 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/19584306 | |
BAY1316957 | 578 | None | 26 | Human | Functional | pIC50 | = | - | 7.82 | - | 1 | Unclassified | Guide to Pharmacology | 441.2 | 6 | 1 | 5 | 5.79 | CCn1c2ccc(C)cc2c2cc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)ccc21 | https://pubmed.ncbi.nlm.nih.gov/30707023 | |
BAY1316957 | 578 | None | 26 | Human | Functional | IC50 | = | 15.30 | 7.82 | - | 1 | Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay | ChEMBL | 441.2 | 6 | 1 | 5 | 5.79 | CCn1c2ccc(C)cc2c2cc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)ccc21 | https://dx.doi.org/10.1021/acs.jmedchem.8b01862 | |
CHEMBL1083400 | 6660 | None | 0 | Human | Functional | IC50 | = | 1.12 | 8.95 | - | 2 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 500.1 | 6 | 2 | 3 | 6.55 | C[C@H](NC(=O)c1cc(Cl)cc2ccn(Cc3ccc(C(F)(F)F)cc3)c12)c1ccc(C(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.065 | |
CHEMBL1084009 | 6840 | None | 21 | Human | Functional | IC50 | = | 9.50 | 8.02 | - | 7 | Antagonist activity at prostanoid EP4 receptor in human whole blood assessed as inhibition of TNF-alpha-induced IP-10 release in presence EP4 agonist L-000902688 | ChEMBL | 478.1 | 6 | 2 | 3 | 5.83 | O=C(O)c1ccc(C2(NC(=O)c3cccc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.065 | |
CHEMBL1084009 | 6840 | None | 21 | Human | Functional | IC50 | = | 1.80 | 8.74 | - | 7 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum | ChEMBL | 478.1 | 6 | 2 | 3 | 5.83 | O=C(O)c1ccc(C2(NC(=O)c3cccc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.065 | |
CHEMBL1084009 | 6840 | None | 21 | Human | Functional | IC50 | = | 1.30 | 8.89 | - | 7 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 478.1 | 6 | 2 | 3 | 5.83 | O=C(O)c1ccc(C2(NC(=O)c3cccc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.065 | |
CHEMBL1084551 | 6959 | None | 0 | Human | Functional | IC50 | = | 11.80 | 7.93 | - | 2 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 466.1 | 6 | 2 | 3 | 5.90 | C[C@H](NC(=O)c1cccc2ccn(Cc3cccc(C(F)(F)F)c3)c12)c1ccc(C(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.065 | |
CHEMBL1084552 | 6960 | None | 0 | Human | Functional | IC50 | = | 1.40 | 8.85 | - | 2 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 516.1 | 7 | 2 | 4 | 6.43 | C[C@H](NC(=O)c1cccc2ccn(Cc3cc(Cl)cc(OC(F)(F)F)c3)c12)c1ccc(C(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.065 | |
CHEMBL1084553 | 6961 | None | 0 | Human | Functional | IC50 | = | 2.70 | 8.57 | - | 2 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 466.1 | 6 | 2 | 3 | 5.90 | C[C@H](NC(=O)c1cccc2ccn(Cc3ccc(C(F)(F)F)cc3)c12)c1ccc(C(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.065 | |
CHEMBL1085040 | 7087 | None | 0 | Human | Functional | IC50 | = | 1.50 | 8.82 | - | 2 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 466.1 | 6 | 2 | 3 | 6.19 | C[C@H](NC(=O)c1cc(Cl)cc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.065 | |
CHEMBL1085041 | 7088 | None | 0 | Human | Functional | IC50 | = | 3.30 | 8.48 | - | 2 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 450.1 | 6 | 2 | 3 | 5.67 | C[C@H](NC(=O)c1cc(F)cc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.065 | |
CHEMBL1085081 | 7091 | None | 0 | Human | Functional | IC50 | = | 5.90 | 8.23 | - | 2 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 432.1 | 6 | 2 | 3 | 5.53 | C[C@H](NC(=O)c1cccc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.065 | |
CHEMBL1085081 | 7091 | None | 0 | Human | Functional | IC50 | = | 6.00 | 8.22 | - | 2 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 432.1 | 6 | 2 | 3 | 5.53 | C[C@H](NC(=O)c1cccc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.10.106 | |
CHEMBL1086490 | 7397 | None | 0 | Human | Functional | IC50 | = | 1.26 | 8.90 | - | 2 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 512.1 | 6 | 2 | 3 | 6.48 | O=C(O)c1ccc(C2(NC(=O)c3cc(Cl)cc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.065 | |
CHEMBL14359 | 35261 | None | 0 | Human | Functional | EC50 | = | 140.00 | 6.85 | - | 3 | Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells | ChEMBL | 359.2 | 11 | 2 | 3 | 3.17 | O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)Cc1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2004.01.063 | |
CHEMBL1644003 | 56889 | None | 0 | Human | Functional | IC50 | = | 1.20 | 8.92 | - | 4 | Antagonist activity at human EP4 receptor in HEK293 cells by cell-based functional assay | ChEMBL | 549.2 | 7 | 2 | 5 | 5.43 | Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(C)cc(C)cc34)cc2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.118 | |
CHEMBL1644016 | 56903 | None | 0 | Human | Functional | IC50 | = | 2.40 | 8.62 | - | 1 | Antagonist activity at human EP4 receptor in HEK293 cells by cell-based functional assay | ChEMBL | 500.2 | 8 | 1 | 4 | 5.80 | COc1ccccc1CC(=O)NCCc1ccc(-c2c(C(=O)N(C)C)sc3c(C)cc(C)cc23)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.118 | |
CHEMBL1645133 | 57112 | None | 0 | Human | Functional | EC50 | = | 0.82 | 9.09 | - | 1 | Agonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 434.1 | 6 | 2 | 3 | 5.09 | C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(Cl)c1)CC2)c1ccc(C(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.10.106 | |
CHEMBL1645134 | 57113 | None | 0 | Human | Functional | IC50 | = | 1.10 | 8.96 | - | 1 | Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay | ChEMBL | 468.1 | 6 | 2 | 3 | 5.75 | C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(Cl)c(Cl)c1)CC2)c1ccc(C(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.10.106 |
Showing 1 to 20 of 744 entries