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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 | |
13,14-dihydro-16-m-chlorophenoxy-w-tetranor-PGF1α | 16 | None | 0 | Human | Binding | IC50 | = | 1360.00 | 5.87 | - | 5 | Affinity for Prostanoid EP1 receptor expressed in COS-7 cells. | 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 | |
17-phenyl-ω-trinor-PGE2 | 26 | None | 0 | Human | Binding | pKi | = | - | 8.10 | -2 | 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/11999132 | |
17-phenyl-ω-trinor-PGE2 | 26 | None | 0 | Mouse | Binding | pKi | None | - | 7.90 | -3 | 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 | |
17-phenyl-ω-trinor-PGE2 | 26 | None | 0 | Rat | Binding | pKi | None | - | 7.60 | -6 | 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 | |
AH-23848 | 218901 | 3H-PGE2 | 0 | Human | Binding | pKi | = | 10000.00 | 5.00 | -10 | 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 | -10 | 6 | - | PDSP KiDatabase | 477.3 | 11 | 1 | 5 | 5.08 | O=C1CCC(CCC(=CCC(C(=O)O)N2CCOCC2)OCc2ccc(-c3ccccc3)cc2)C1 | - | |
AH6809 | 320 | None | 49 | Human | Binding | pKi | None | - | 5.95 | -3 | 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 | None | 49 | Human | Binding | pKi | None | - | 5.95 | -3 | 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/11999132 | |
AH6809 | 320 | 3H-PGE2 | 49 | Human | Binding | pKi | = | 1217.00 | 5.91 | -3 | 10 | - | PDSP KiDatabase | 298.1 | 3 | 1 | 4 | 3.43 | CC(C)Oc1ccc2c(=O)c3cc(C(=O)O)ccc3oc2c1 | - | |
AH6809 | 320 | None | 49 | Rat | Binding | pKi | None | - | 5.90 | -3 | 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/9537820 | |
BUTAPROST | 97856 | 3H-PGE2 | 23 | Human | Binding | pKi | = | 10000.00 | 5.00 | -91 | 9 | - | PDSP KiDatabase | 408.3 | 13 | 2 | 5 | 4.34 | CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 | - | |
BUTAPROST | 97856 | 3H-PGE2 | 23 | Human | Binding | pKi | = | 10000.00 | 5.00 | -91 | 9 | - | PDSP KiDatabase | 408.3 | 13 | 2 | 5 | 4.34 | CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 | - | |
BW 245C | 752 | 3H-PGE2 | 0 | Human | Binding | pKi | = | 10000.00 | 5.00 | -14125 | 9 | - | PDSP KiDatabase | 368.2 | 11 | 3 | 4 | 2.66 | O=C(O)CCCCCCC1C(=O)NC(=O)N1CCC(O)C1CCCCC1 | - | |
carbacyclin | 795 | None | 0 | Human | Binding | pKi | None | - | 7.60 | -1 | 13 | Unclassified | Guide to Pharmacology | 350.2 | 10 | 3 | 3 | 4.07 | CCCCC[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C\CCCC(=O)O)C[C@H]2C[C@H]1O | https://pubmed.ncbi.nlm.nih.gov/10634944 | |
CARBACYCLIN | 218534 | 3H-PGE2 | 0 | Human | Binding | pKi | = | 23.00 | 7.64 | 1 | 14 | - | PDSP KiDatabase | 350.2 | 10 | 3 | 3 | 4.07 | CCCCCC(O)C=CC1C(O)CC2CC(=CCCCC(=O)O)CC21 | - | |
CARBACYCLIN | 218534 | None | 0 | Human | Binding | pKi | = | 4.80 | 8.32 | 1 | 14 | None | Drug Central | 350.2 | 10 | 3 | 3 | 4.07 | CCCCCC(O)C=CC1C(O)CC2CC(=CCCCC(=O)O)CC21 | - | |
CHEMBL1084009 | 6840 | None | 21 | Human | Binding | Ki | = | 20000.00 | 4.70 | -70794 | 7 | Displacement of [3H]PGE2 from human prostanoid EP1 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting | 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 | |
CHEMBL1090937 | 8048 | None | 0 | Mouse | Binding | Ki | = | 260.00 | 6.58 | -2187 | 3 | Displacement of [3H]PGE2 from mouse EP1 receptor expressed in CHO cells after 60 mins by scintillation counter | 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 | |
CHEMBL1091741 | 8136 | None | 0 | Mouse | Binding | Ki | = | 2100.00 | 5.68 | -24547 | 3 | Displacement of [3H]PGE2 from mouse EP1 receptor expressed in CHO cells after 60 mins by scintillation counter | 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 | |
CHEMBL1091743 | 8138 | None | 0 | Mouse | Binding | Ki | = | 5300.00 | 5.28 | -40738 | 3 | Displacement of [3H]PGE2 from mouse EP1 receptor expressed in CHO cells after 60 mins by scintillation counter | 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 |
Showing 1 to 20 of 983 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 | |
13,14-dihydro-16-m-chlorophenoxy-w-tetranor-PGF1α | 16 | None | 0 | Human | Functional | EC50 | = | 19000.00 | 4.72 | -2089 | 5 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=100%) | 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/10.1016/s0960-894x(00)00273-0 | |
AH6809 | 320 | None | 49 | Human | Functional | Ki | = | 1200.00 | 5.92 | - | 10 | Antagonist activity at EP1 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 | |
bupivacaine | 220185 | None | 0 | Human | Functional | pIC50 | = | 5.51 | 8.26 | - | 1 | None | Drug Central | 288.2 | 5 | 1 | 2 | 3.90 | CCCCN1CCCCC1C(=O)Nc1c(C)cccc1C | - | |
CHEMBL1186812 | 12578 | None | 0 | Human | Functional | Ki | = | 79.43 | 7.10 | - | 1 | Antagonist activity of human PGE2 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium mobilisation by FLIPR assay | ChEMBL | 530.2 | 9 | 1 | 6 | 5.56 | Cc1cc(C(=O)Nc2ccc(CN3CCOCC3)cc2)nn1Cc1cc(Cl)ccc1OCc1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2008.05.118 | |
CHEMBL1186852 | 12587 | None | 0 | Human | Functional | Ki | = | 125.89 | 6.90 | - | 1 | Antagonist activity of human PGE2 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium mobilisation by FLIPR assay | ChEMBL | 474.2 | 9 | 2 | 5 | 5.44 | CNCc1ccc(NC(=O)c2cc(C)n(Cc3cc(Cl)ccc3OCc3ccccc3)n2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2008.05.118 | |
CHEMBL1186853 | 12588 | None | 0 | Human | Functional | IC50 | = | 7000.00 | 5.16 | - | 1 | Antagonist activity at EP1 receptor (unknown origin) | ChEMBL | 488.2 | 10 | 2 | 5 | 5.83 | CCNCc1ccc(NC(=O)c2cc(C)n(Cc3cc(Cl)ccc3OCc3ccccc3)n2)cc1 | https://dx.doi.org/10.1016/j.bmc.2022.116614 | |
CHEMBL1186882 | 12595 | None | 0 | Human | Functional | Ki | = | 158.49 | 6.80 | - | 1 | Antagonist activity of human PGE2 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium mobilisation by FLIPR assay | ChEMBL | 480.2 | 9 | 1 | 5 | 5.78 | Cc1cc(NC(=O)c2ccc(CN3CCCC3)cc2)nn1Cc1cc(Cl)ccc1OCC(C)C | https://dx.doi.org/10.1016/j.bmcl.2008.05.118 | |
CHEMBL1186890 | 12597 | None | 0 | Human | Functional | Ki | = | 158.49 | 6.80 | - | 1 | Antagonist activity of human PGE2 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium mobilisation by FLIPR assay | ChEMBL | 454.2 | 10 | 2 | 5 | 5.29 | CCNCc1ccc(C(=O)Nc2cc(C)n(Cc3cc(Cl)ccc3OCC(C)C)n2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2008.05.118 | |
CHEMBL1187164 | 12645 | None | 0 | Human | Functional | Ki | = | 79.43 | 7.10 | - | 1 | Antagonist activity of human PGE2 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium mobilisation by FLIPR assay | ChEMBL | 440.2 | 9 | 2 | 5 | 4.90 | CNCc1ccc(NC(=O)c2cc(C)n(Cc3cc(Cl)ccc3OCC(C)C)n2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2008.05.118 | |
CHEMBL1187203 | 12660 | None | 0 | Human | Functional | Ki | = | 125.89 | 6.90 | - | 1 | Antagonist activity of human PGE2 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium mobilisation by FLIPR assay | ChEMBL | 452.2 | 7 | 2 | 5 | 4.83 | Cc1cc(NC(=O)c2ccc3c(c2)CCNC3)nn1Cc1cc(Cl)ccc1OCC(C)C | https://dx.doi.org/10.1016/j.bmcl.2008.05.118 | |
CHEMBL1187235 | 12666 | None | 0 | Human | Functional | Ki | = | 100.00 | 7.00 | - | 1 | Antagonist activity of human PGE2 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium mobilisation by FLIPR assay | ChEMBL | 466.2 | 8 | 2 | 5 | 5.61 | Cc1cc(NC(=O)c2ccc(C3CCCN3)cc2)nn1Cc1cc(Cl)ccc1OCC(C)C | https://dx.doi.org/10.1016/j.bmcl.2008.05.118 | |
CHEMBL1187258 | 12669 | None | 0 | Human | Functional | Ki | = | 50.12 | 7.30 | - | 1 | Antagonist activity of human PGE2 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium mobilisation by FLIPR assay | ChEMBL | 494.2 | 8 | 1 | 5 | 5.60 | CCN1CCc2ccc(C(=O)Nc3cc(C)n(Cc4cc(Cl)ccc4OCC(C)C)n3)cc2CC1 | https://dx.doi.org/10.1016/j.bmcl.2008.05.118 | |
CHEMBL1187259 | 12670 | None | 0 | Human | Functional | Ki | = | 100.00 | 7.00 | - | 1 | Antagonist activity of human PGE2 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium mobilisation by FLIPR assay | ChEMBL | 470.2 | 11 | 3 | 6 | 4.26 | Cc1cc(C(=O)Nc2ccc(CNCCO)cc2)nn1Cc1cc(Cl)ccc1OCC(C)C | https://dx.doi.org/10.1016/j.bmcl.2008.05.118 | |
CHEMBL1187781 | 12742 | None | 0 | Human | Functional | Ki | = | 39.81 | 7.40 | - | 1 | Antagonist activity of human PGE2 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium mobilisation by FLIPR assay | ChEMBL | 461.2 | 8 | 2 | 5 | 5.22 | Cc1cc(C(=O)Nc2ccc(CO)cc2)nn1Cc1cc(Cl)ccc1OCc1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2008.05.118 | |
CHEMBL1187830 | 12756 | None | 0 | Human | Functional | Ki | = | 79.43 | 7.10 | - | 1 | Antagonist activity of human PGE2 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium mobilisation by FLIPR assay | ChEMBL | 514.2 | 13 | 3 | 7 | 3.97 | Cc1cc(C(=O)Nc2ccc(CN(CCO)CCO)cc2)nn1Cc1cc(Cl)ccc1OCC(C)C | https://dx.doi.org/10.1016/j.bmcl.2008.05.118 | |
CHEMBL1206254 | 14723 | None | 0 | Human | Functional | Ki | = | 19.95 | 7.70 | - | 2 | Antagonist activity against human EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay | ChEMBL | 328.1 | 4 | 1 | 3 | 4.58 | CC(C)Cc1cn(-c2cccc(C(=O)O)n2)c2cc(Cl)ccc12 | https://dx.doi.org/10.1016/j.bmcl.2008.03.018 | |
CHEMBL1206265 | 14728 | None | 0 | Human | Functional | Ki | = | 3.98 | 8.40 | - | 3 | Antagonist activity against human EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay | ChEMBL | 362.1 | 4 | 1 | 4 | 5.42 | CC(C)(C)CCc1cn(-c2nc(C(=O)O)cs2)c2cc(Cl)ccc12 | https://dx.doi.org/10.1016/j.bmcl.2008.03.018 | |
CHEMBL1206284 | 14739 | None | 0 | Human | Functional | Ki | = | 0.20 | 9.70 | - | 3 | Antagonist activity against human EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay | ChEMBL | 378.0 | 4 | 1 | 4 | 4.75 | CC(C)Cc1cn(-c2nc(C(=O)O)cs2)c2cc(Br)ccc12 | https://dx.doi.org/10.1016/j.bmcl.2008.03.018 | |
CHEMBL1206289 | 14742 | None | 0 | Human | Functional | Ki | = | 1.58 | 8.80 | - | 1 | Antagonist activity at EP1 receptor by FLIPR assay | ChEMBL | 343.1 | 6 | 1 | 4 | 4.20 | O=C(O)c1coc(Cc2cc(Cl)ccc2OCc2ccccc2)n1 | https://dx.doi.org/10.1016/j.bmcl.2008.01.071 | |
CHEMBL1206294 | 14745 | None | 0 | Human | Functional | Ki | = | 0.50 | 9.30 | - | 3 | Antagonist activity against human EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay | ChEMBL | 334.1 | 4 | 1 | 4 | 4.64 | CC(C)Cc1cn(-c2nc(C(=O)O)cs2)c2cc(Cl)ccc12 | https://dx.doi.org/10.1016/j.bmcl.2008.03.018 |
Showing 1 to 20 of 383 entries