Ligand source activities (1 row/activity)
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
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Sel. page | 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 (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | 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
| |
138107701 | 187570 | None | 33 | Human | Functional | pEC50 | = | 9.4 | 9.4 | -4 | 7 | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.ejmech.2022.114154 | ||
5311181 | 187570 | None | 33 | Human | Functional | pEC50 | = | 9.4 | 9.4 | -4 | 7 | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.ejmech.2022.114154 | ||
5311181.0 | 187570 | None | 33 | Human | Functional | pEC50 | = | 9.4 | 9.4 | -4 | 7 | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.ejmech.2022.114154 | ||
CHEMBL494 | 187570 | None | 33 | Human | Functional | pEC50 | = | 9.4 | 9.4 | -4 | 7 | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.ejmech.2022.114154 | ||
DB01088 | 187570 | None | 33 | Human | Functional | pEC50 | = | 9.4 | 9.4 | -4 | 7 | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.ejmech.2022.114154 | ||
138107701 | 187570 | None | 33 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 7 | Agonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1021/acs.jmedchem.6b00871 | ||
5311181 | 187570 | None | 33 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 7 | Agonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1021/acs.jmedchem.6b00871 | ||
5311181.0 | 187570 | None | 33 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 7 | Agonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1021/acs.jmedchem.6b00871 | ||
CHEMBL494 | 187570 | None | 33 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 7 | Agonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1021/acs.jmedchem.6b00871 | ||
DB01088 | 187570 | None | 33 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 7 | Agonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1021/acs.jmedchem.6b00871 | ||
138 | 3081 | None | 57 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -16 | 10 | Effective concentration which increases intracellular c-AMP production in human Prostanoid IP receptorEffective concentration which increases intracellular c-AMP production in human Prostanoid IP receptor |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(01)00359-6 | ||
149351 | 3081 | None | 57 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -16 | 10 | Effective concentration which increases intracellular c-AMP production in human Prostanoid IP receptorEffective concentration which increases intracellular c-AMP production in human Prostanoid IP receptor |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(01)00359-6 | ||
149351.0 | 3081 | None | 57 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -16 | 10 | Effective concentration which increases intracellular c-AMP production in human Prostanoid IP receptorEffective concentration which increases intracellular c-AMP production in human Prostanoid IP receptor |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(01)00359-6 | ||
1882 | 3081 | None | 57 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -16 | 10 | Effective concentration which increases intracellular c-AMP production in human Prostanoid IP receptorEffective concentration which increases intracellular c-AMP production in human Prostanoid IP receptor |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(01)00359-6 | ||
5280723 | 3081 | None | 57 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -16 | 10 | Effective concentration which increases intracellular c-AMP production in human Prostanoid IP receptorEffective concentration which increases intracellular c-AMP production in human Prostanoid IP receptor |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(01)00359-6 | ||
5280723.0 | 3081 | None | 57 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -16 | 10 | Effective concentration which increases intracellular c-AMP production in human Prostanoid IP receptorEffective concentration which increases intracellular c-AMP production in human Prostanoid IP receptor |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(01)00359-6 | ||
CHEMBL495 | 3081 | None | 57 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -16 | 10 | Effective concentration which increases intracellular c-AMP production in human Prostanoid IP receptorEffective concentration which increases intracellular c-AMP production in human Prostanoid IP receptor |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(01)00359-6 | ||
DB00770 | 3081 | None | 57 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -16 | 10 | Effective concentration which increases intracellular c-AMP production in human Prostanoid IP receptorEffective concentration which increases intracellular c-AMP production in human Prostanoid IP receptor |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(01)00359-6 | ||
2720 | 3854 | None | 49 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -5 | 5 | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis |
ChEMBL | 390 | 10 | 3 | 4 | 3.6 | CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O | 10.1016/j.ejmech.2022.114154 | ||
5820 | 3854 | None | 49 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -5 | 5 | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis |
ChEMBL | 390 | 10 | 3 | 4 | 3.6 | CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O | 10.1016/j.ejmech.2022.114154 | ||
6918140 | 3854 | None | 49 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -5 | 5 | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis |
ChEMBL | 390 | 10 | 3 | 4 | 3.6 | CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O | 10.1016/j.ejmech.2022.114154 | ||
6918140.0 | 3854 | None | 49 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -5 | 5 | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis |
ChEMBL | 390 | 10 | 3 | 4 | 3.6 | CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O | 10.1016/j.ejmech.2022.114154 | ||
CHEMBL1237119 | 3854 | None | 49 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -5 | 5 | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis |
ChEMBL | 390 | 10 | 3 | 4 | 3.6 | CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O | 10.1016/j.ejmech.2022.114154 | ||
DB00374 | 3854 | None | 49 | Human | Functional | pEC50 | = | 8.7 | 8.7 | -5 | 5 | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis |
ChEMBL | 390 | 10 | 3 | 4 | 3.6 | CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O | 10.1016/j.ejmech.2022.114154 | ||
118727298 | 117477 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | -3 | 3 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 514 | 8 | 1 | 6 | 5.0 | COc1ccc(-c2nn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)cc2-c2ccccc2)cc1F | 10.1016/j.bmcl.2015.01.024 | ||
CHEMBL3398219 | 117477 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | -3 | 3 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 514 | 8 | 1 | 6 | 5.0 | COc1ccc(-c2nn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)cc2-c2ccccc2)cc1F | 10.1016/j.bmcl.2015.01.024 | ||
118727308 | 117487 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | 1 | 3 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 514 | 8 | 1 | 6 | 5.0 | COc1cccc(-c2cnn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)c2-c2ccccc2)c1F | 10.1016/j.bmcl.2015.01.024 | ||
CHEMBL3398229 | 117487 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | 1 | 3 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 514 | 8 | 1 | 6 | 5.0 | COc1cccc(-c2cnn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)c2-c2ccccc2)c1F | 10.1016/j.bmcl.2015.01.024 | ||
44235755 | 153797 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | 81 | 3 | Agonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 433 | 8 | 1 | 4 | 5.1 | O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(F)c(F)c2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
CHEMBL3981509 | 153797 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | 81 | 3 | Agonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 433 | 8 | 1 | 4 | 5.1 | O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(F)c(F)c2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
118727301 | 117480 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | -1 | 3 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 466 | 7 | 1 | 5 | 4.8 | O=C(O)COc1cccc2c1CCC(Cn1ncc(-c3ccccc3)c(-c3ccccc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
CHEMBL3398222 | 117480 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | -1 | 3 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 466 | 7 | 1 | 5 | 4.8 | O=C(O)COc1cccc2c1CCC(Cn1ncc(-c3ccccc3)c(-c3ccccc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
56839344 | 152140 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | -3311 | 8 | Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA. |
ChEMBL | 656 | 13 | 2 | 9 | 5.1 | O=C(CCc1cc2c(cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC3CCCCC3)co1)OCO2)NS(=O)(=O)C(F)(F)F | nan | ||
CHEMBL3967284 | 152140 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | -3311 | 8 | Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA. |
ChEMBL | 656 | 13 | 2 | 9 | 5.1 | O=C(CCc1cc2c(cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC3CCCCC3)co1)OCO2)NS(=O)(=O)C(F)(F)F | nan | ||
137636847 | 156083 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 554 | 11 | 3 | 7 | 4.1 | O=C(COC[C@H]1CC[C@H](COC(=O)N(c2ccc(O)cc2)c2ccc(Cl)cc2)CC1)NCCS(=O)(=O)O | 10.1021/acs.jmedchem.6b00871 | ||
CHEMBL4061744 | 156083 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 554 | 11 | 3 | 7 | 4.1 | O=C(COC[C@H]1CC[C@H](COC(=O)N(c2ccc(O)cc2)c2ccc(Cl)cc2)CC1)NCCS(=O)(=O)O | 10.1021/acs.jmedchem.6b00871 | ||
118727293 | 117472 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 2 | 2 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 484 | 7 | 1 | 5 | 5.0 | O=C(O)COc1cccc2c1CCC(Cn1nc(-c3cccc(F)c3)c(-c3ccccc3)cc1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
CHEMBL3398214 | 117472 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 2 | 2 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 484 | 7 | 1 | 5 | 5.0 | O=C(O)COc1cccc2c1CCC(Cn1nc(-c3cccc(F)c3)c(-c3ccccc3)cc1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
118727305 | 117484 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 496 | 8 | 1 | 6 | 4.9 | COc1ccc(-c2cnn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)c2-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.01.024 | ||
CHEMBL3398226 | 117484 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 496 | 8 | 1 | 6 | 4.9 | COc1ccc(-c2cnn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)c2-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.01.024 | ||
127052613 | 140293 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | -13 | 6 | Agonist activity at human IP receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human IP receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method |
ChEMBL | 431 | 7 | 3 | 7 | 3.1 | O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/[C@@H](O)COc3ccccc3)O2)n1 | 10.1021/acsmedchemlett.5b00455 | ||
CHEMBL3804978 | 140293 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | -13 | 6 | Agonist activity at human IP receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human IP receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method |
ChEMBL | 431 | 7 | 3 | 7 | 3.1 | O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/[C@@H](O)COc3ccccc3)O2)n1 | 10.1021/acsmedchemlett.5b00455 | ||
118727312 | 117491 | None | 0 | Rat | Functional | pEC50 | = | 8.0 | 8.0 | 3 | 2 | Agonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 496 | 8 | 1 | 6 | 4.9 | COc1ccc(-c2c(-c3ccccc3)cnn(CC3CCc4c(cccc4OCC(=O)O)C3)c2=O)cc1 | 10.1016/j.bmcl.2015.01.024 | ||
CHEMBL3398233 | 117491 | None | 0 | Rat | Functional | pEC50 | = | 8.0 | 8.0 | 3 | 2 | Agonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 496 | 8 | 1 | 6 | 4.9 | COc1ccc(-c2c(-c3ccccc3)cnn(CC3CCc4c(cccc4OCC(=O)O)C3)c2=O)cc1 | 10.1016/j.bmcl.2015.01.024 | ||
118727307 | 117486 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -1 | 3 | Agonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 502 | 7 | 1 | 5 | 5.1 | O=C(O)COc1cccc2c1CCC(Cn1ncc(-c3cccc(F)c3F)c(-c3ccccc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
CHEMBL3398228 | 117486 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -1 | 3 | Agonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 502 | 7 | 1 | 5 | 5.1 | O=C(O)COc1cccc2c1CCC(Cn1ncc(-c3cccc(F)c3F)c(-c3ccccc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
118727297 | 117476 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -5 | 3 | Agonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 514 | 8 | 1 | 6 | 5.0 | COc1ccc(-c2nn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)cc2-c2ccccc2)c(F)c1 | 10.1016/j.bmcl.2015.01.024 | ||
CHEMBL3398218 | 117476 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -5 | 3 | Agonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at rat recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 514 | 8 | 1 | 6 | 5.0 | COc1ccc(-c2nn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)cc2-c2ccccc2)c(F)c1 | 10.1016/j.bmcl.2015.01.024 | ||
118727296 | 117475 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 13 | 2 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 484 | 7 | 1 | 5 | 5.0 | O=C(O)COc1cccc2c1CCC(Cn1nc(-c3ccc(F)cc3)c(-c3ccccc3)cc1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
CHEMBL3398217 | 117475 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 13 | 2 | Agonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assayAgonist activity at human recombinant IP receptor expressed in CHO-K1 cells incubated for 1 hr by HTRF cAMP assay |
ChEMBL | 484 | 7 | 1 | 5 | 5.0 | O=C(O)COc1cccc2c1CCC(Cn1nc(-c3ccc(F)cc3)c(-c3ccccc3)cc1=O)C2 | 10.1016/j.bmcl.2015.01.024 |
Showing 1 to 50 of 658 entries
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
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Sel. page | 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
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Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | 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
| |
9955130 | 9507 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Compound was tested for prostacyclin (PGI-2) binding by displacement of [3H]iloprost from human platelets using conventional ligand binding assayCompound was tested for prostacyclin (PGI-2) binding by displacement of [3H]iloprost from human platelets using conventional ligand binding assay |
ChEMBL | 444 | 9 | 2 | 4 | 5.2 | O=C(O)COc1cccc2c1CCCC2CCC(=O)NN(c1ccccc1)c1ccccc1 | 10.1016/0960-894X(95)00169-T | ||
CHEMBL11211 | 9507 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Compound was tested for prostacyclin (PGI-2) binding by displacement of [3H]iloprost from human platelets using conventional ligand binding assayCompound was tested for prostacyclin (PGI-2) binding by displacement of [3H]iloprost from human platelets using conventional ligand binding assay |
ChEMBL | 444 | 9 | 2 | 4 | 5.2 | O=C(O)COc1cccc2c1CCCC2CCC(=O)NN(c1ccccc1)c1ccccc1 | 10.1016/0960-894X(95)00169-T | ||
138107701 | 187570 | None | 33 | Human | Binding | pIC50 | = | 8 | 8.0 | -5 | 15 | Displacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2016.11.014 | ||
5311181 | 187570 | None | 33 | Human | Binding | pIC50 | = | 8 | 8.0 | -5 | 15 | Displacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2016.11.014 | ||
5311181.0 | 187570 | None | 33 | Human | Binding | pIC50 | = | 8 | 8.0 | -5 | 15 | Displacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2016.11.014 | ||
CHEMBL494 | 187570 | None | 33 | Human | Binding | pIC50 | = | 8 | 8.0 | -5 | 15 | Displacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2016.11.014 | ||
DB01088 | 187570 | None | 33 | Human | Binding | pIC50 | = | 8 | 8.0 | -5 | 15 | Displacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2016.11.014 | ||
138107701 | 187570 | None | 33 | Human | Binding | pIC50 | = | 8 | 8.0 | -5 | 15 | Displacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cellsDisplacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cells |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2016.03.006 | ||
5311181 | 187570 | None | 33 | Human | Binding | pIC50 | = | 8 | 8.0 | -5 | 15 | Displacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cellsDisplacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cells |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2016.03.006 | ||
5311181.0 | 187570 | None | 33 | Human | Binding | pIC50 | = | 8 | 8.0 | -5 | 15 | Displacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cellsDisplacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cells |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2016.03.006 | ||
CHEMBL494 | 187570 | None | 33 | Human | Binding | pIC50 | = | 8 | 8.0 | -5 | 15 | Displacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cellsDisplacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cells |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2016.03.006 | ||
DB01088 | 187570 | None | 33 | Human | Binding | pIC50 | = | 8 | 8.0 | -5 | 15 | Displacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cellsDisplacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cells |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2016.03.006 | ||
127029421 | 139407 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Agonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometryAgonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometry |
ChEMBL | 424 | 10 | 1 | 4 | 3.9 | CCCc1ccc(N(CCN2CCC(OCC(=O)O)CC2)C(=O)c2ccccc2)cc1 | 10.1016/j.bmcl.2016.03.009 | ||
CHEMBL3792615 | 139407 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Agonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometryAgonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometry |
ChEMBL | 424 | 10 | 1 | 4 | 3.9 | CCCc1ccc(N(CCN2CCC(OCC(=O)O)CC2)C(=O)c2ccccc2)cc1 | 10.1016/j.bmcl.2016.03.009 | ||
86277844 | 111989 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of prostanoid IP receptor (unknown origin)Inhibition of prostanoid IP receptor (unknown origin) |
ChEMBL | 512 | 6 | 2 | 3 | 7.5 | CCc1ccccc1NC(=O)N1C[C@@H](C)Oc2cc(-c3ccc([C@H]4CC[C@H](CC(=O)O)CC4)cc3)ccc21 | 10.1021/ml400527n | ||
CHEMBL3287898 | 111989 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of prostanoid IP receptor (unknown origin)Inhibition of prostanoid IP receptor (unknown origin) |
ChEMBL | 512 | 6 | 2 | 3 | 7.5 | CCc1ccccc1NC(=O)N1C[C@@H](C)Oc2cc(-c3ccc([C@H]4CC[C@H](CC(=O)O)CC4)cc3)ccc21 | 10.1021/ml400527n | ||
44235520 | 153047 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Agonist activity at IP receptor in human primary platelets assessed as inhibition of ADP-induced platelet aggregationAgonist activity at IP receptor in human primary platelets assessed as inhibition of ADP-induced platelet aggregation |
ChEMBL | 415 | 8 | 1 | 4 | 5.0 | O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(F)cc2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
CHEMBL3975122 | 153047 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Agonist activity at IP receptor in human primary platelets assessed as inhibition of ADP-induced platelet aggregationAgonist activity at IP receptor in human primary platelets assessed as inhibition of ADP-induced platelet aggregation |
ChEMBL | 415 | 8 | 1 | 4 | 5.0 | O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(F)cc2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
24901449 | 153687 | None | 0 | Human | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Displacement of [3H]iloprost from IP receptor in human platelet membraneDisplacement of [3H]iloprost from IP receptor in human platelet membrane |
ChEMBL | 349 | 5 | 2 | 4 | 3.3 | CNC(=O)c1ncoc1Cc1ccc(-c2cccc(NC(C)=O)c2)cc1 | 10.1016/j.bmcl.2006.12.025 | ||
CHEMBL398063 | 153687 | None | 0 | Human | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Displacement of [3H]iloprost from IP receptor in human platelet membraneDisplacement of [3H]iloprost from IP receptor in human platelet membrane |
ChEMBL | 349 | 5 | 2 | 4 | 3.3 | CNC(=O)c1ncoc1Cc1ccc(-c2cccc(NC(C)=O)c2)cc1 | 10.1016/j.bmcl.2006.12.025 | ||
24901439 | 86820 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Displacement of [3H]iloprost from IP receptor in human platelet membraneDisplacement of [3H]iloprost from IP receptor in human platelet membrane |
ChEMBL | 439 | 7 | 2 | 4 | 5.4 | CC(=O)Nc1cccc(-c2ccc(Cc3ocnc3C(=O)NC(C)c3ccccc3)cc2)c1 | 10.1016/j.bmcl.2006.12.025 | ||
CHEMBL232156 | 86820 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Displacement of [3H]iloprost from IP receptor in human platelet membraneDisplacement of [3H]iloprost from IP receptor in human platelet membrane |
ChEMBL | 439 | 7 | 2 | 4 | 5.4 | CC(=O)Nc1cccc(-c2ccc(Cc3ocnc3C(=O)NC(C)c3ccccc3)cc2)c1 | 10.1016/j.bmcl.2006.12.025 | ||
44432434 | 86720 | None | 0 | Human | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Displacement of [3H]iloprost from IP receptor in human platelet membraneDisplacement of [3H]iloprost from IP receptor in human platelet membrane |
ChEMBL | 363 | 5 | 1 | 4 | 3.6 | CC(=O)Nc1cccc(-c2ccc(Cc3ocnc3C(=O)N(C)C)cc2)c1 | 10.1016/j.bmcl.2006.12.025 | ||
CHEMBL231709 | 86720 | None | 0 | Human | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Displacement of [3H]iloprost from IP receptor in human platelet membraneDisplacement of [3H]iloprost from IP receptor in human platelet membrane |
ChEMBL | 363 | 5 | 1 | 4 | 3.6 | CC(=O)Nc1cccc(-c2ccc(Cc3ocnc3C(=O)N(C)C)cc2)c1 | 10.1016/j.bmcl.2006.12.025 | ||
155544367 | 173478 | None | 0 | Human | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Antagonist activity at human Gs-coupled PTGIR assessed as inhibition in beraprost-induced beta-arrestin 2 recruitment incubated for 30 mins followed by beraprost- addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human Gs-coupled PTGIR assessed as inhibition in beraprost-induced beta-arrestin 2 recruitment incubated for 30 mins followed by beraprost- addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay |
ChEMBL | 508 | 3 | 0 | 4 | 6.0 | CC[C@]12CCCN(C(=O)c3cccc(Br)c3)CCc3c(n(c4ccccc34)C(=O)C1)[C@@H]2OC | 10.1021/acs.jmedchem.9b01924 | ||
CHEMBL4527708 | 173478 | None | 0 | Human | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | Antagonist activity at human Gs-coupled PTGIR assessed as inhibition in beraprost-induced beta-arrestin 2 recruitment incubated for 30 mins followed by beraprost- addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human Gs-coupled PTGIR assessed as inhibition in beraprost-induced beta-arrestin 2 recruitment incubated for 30 mins followed by beraprost- addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay |
ChEMBL | 508 | 3 | 0 | 4 | 6.0 | CC[C@]12CCCN(C(=O)c3cccc(Br)c3)CCc3c(n(c4ccccc34)C(=O)C1)[C@@H]2OC | 10.1021/acs.jmedchem.9b01924 | ||
58602756 | 139518 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Agonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometryAgonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometry |
ChEMBL | 466 | 8 | 1 | 5 | 4.3 | O=C(O)COc1cccc2c1OCCN2CCN(C(=O)c1ccccc1)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2016.03.009 | ||
CHEMBL3793903 | 139518 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Agonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometryAgonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometry |
ChEMBL | 466 | 8 | 1 | 5 | 4.3 | O=C(O)COc1cccc2c1OCCN2CCN(C(=O)c1ccccc1)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2016.03.009 | ||
138107701 | 187570 | None | 33 | Human | Binding | pIC50 | = | 7.9 | 7.9 | -5 | 15 | Binding affinity to PGI2 receptor (unknown origin) by radioligand displacement assayBinding affinity to PGI2 receptor (unknown origin) by radioligand displacement assay |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2013.03.016 | ||
5311181 | 187570 | None | 33 | Human | Binding | pIC50 | = | 7.9 | 7.9 | -5 | 15 | Binding affinity to PGI2 receptor (unknown origin) by radioligand displacement assayBinding affinity to PGI2 receptor (unknown origin) by radioligand displacement assay |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2013.03.016 | ||
5311181.0 | 187570 | None | 33 | Human | Binding | pIC50 | = | 7.9 | 7.9 | -5 | 15 | Binding affinity to PGI2 receptor (unknown origin) by radioligand displacement assayBinding affinity to PGI2 receptor (unknown origin) by radioligand displacement assay |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2013.03.016 | ||
CHEMBL494 | 187570 | None | 33 | Human | Binding | pIC50 | = | 7.9 | 7.9 | -5 | 15 | Binding affinity to PGI2 receptor (unknown origin) by radioligand displacement assayBinding affinity to PGI2 receptor (unknown origin) by radioligand displacement assay |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2013.03.016 | ||
DB01088 | 187570 | None | 33 | Human | Binding | pIC50 | = | 7.9 | 7.9 | -5 | 15 | Binding affinity to PGI2 receptor (unknown origin) by radioligand displacement assayBinding affinity to PGI2 receptor (unknown origin) by radioligand displacement assay |
ChEMBL | 360 | 8 | 3 | 3 | 3.5 | CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O | 10.1016/j.bmc.2013.03.016 | ||
127029417 | 139522 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometryAgonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometry |
ChEMBL | 396 | 8 | 1 | 4 | 3.2 | Cc1ccc(N(CCN2CCC(OCC(=O)O)CC2)C(=O)c2ccccc2)cc1 | 10.1016/j.bmcl.2016.03.009 | ||
CHEMBL3793911 | 139522 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometryAgonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometry |
ChEMBL | 396 | 8 | 1 | 4 | 3.2 | Cc1ccc(N(CCN2CCC(OCC(=O)O)CC2)C(=O)c2ccccc2)cc1 | 10.1016/j.bmcl.2016.03.009 | ||
138 | 3081 | None | 57 | Human | Binding | pIC50 | = | 5.9 | 5.9 | -165 | 18 | Displacement of [3H]iloprost from Prostaglandin I2 receptor of human plateletsDisplacement of [3H]iloprost from Prostaglandin I2 receptor of human platelets |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/0960-894X(95)00168-S | ||
149351 | 3081 | None | 57 | Human | Binding | pIC50 | = | 5.9 | 5.9 | -165 | 18 | Displacement of [3H]iloprost from Prostaglandin I2 receptor of human plateletsDisplacement of [3H]iloprost from Prostaglandin I2 receptor of human platelets |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/0960-894X(95)00168-S | ||
149351.0 | 3081 | None | 57 | Human | Binding | pIC50 | = | 5.9 | 5.9 | -165 | 18 | Displacement of [3H]iloprost from Prostaglandin I2 receptor of human plateletsDisplacement of [3H]iloprost from Prostaglandin I2 receptor of human platelets |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/0960-894X(95)00168-S | ||
1882 | 3081 | None | 57 | Human | Binding | pIC50 | = | 5.9 | 5.9 | -165 | 18 | Displacement of [3H]iloprost from Prostaglandin I2 receptor of human plateletsDisplacement of [3H]iloprost from Prostaglandin I2 receptor of human platelets |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/0960-894X(95)00168-S | ||
5280723 | 3081 | None | 57 | Human | Binding | pIC50 | = | 5.9 | 5.9 | -165 | 18 | Displacement of [3H]iloprost from Prostaglandin I2 receptor of human plateletsDisplacement of [3H]iloprost from Prostaglandin I2 receptor of human platelets |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/0960-894X(95)00168-S | ||
5280723.0 | 3081 | None | 57 | Human | Binding | pIC50 | = | 5.9 | 5.9 | -165 | 18 | Displacement of [3H]iloprost from Prostaglandin I2 receptor of human plateletsDisplacement of [3H]iloprost from Prostaglandin I2 receptor of human platelets |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/0960-894X(95)00168-S | ||
CHEMBL495 | 3081 | None | 57 | Human | Binding | pIC50 | = | 5.9 | 5.9 | -165 | 18 | Displacement of [3H]iloprost from Prostaglandin I2 receptor of human plateletsDisplacement of [3H]iloprost from Prostaglandin I2 receptor of human platelets |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/0960-894X(95)00168-S | ||
DB00770 | 3081 | None | 57 | Human | Binding | pIC50 | = | 5.9 | 5.9 | -165 | 18 | Displacement of [3H]iloprost from Prostaglandin I2 receptor of human plateletsDisplacement of [3H]iloprost from Prostaglandin I2 receptor of human platelets |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O | 10.1016/0960-894X(95)00168-S | ||
44235522 | 142607 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Agonist activity at IP receptor in human primary platelets assessed as inhibition of ADP-induced platelet aggregationAgonist activity at IP receptor in human primary platelets assessed as inhibition of ADP-induced platelet aggregation |
ChEMBL | 449 | 8 | 1 | 4 | 5.7 | O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(F)c(Cl)c2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
CHEMBL3890685 | 142607 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Agonist activity at IP receptor in human primary platelets assessed as inhibition of ADP-induced platelet aggregationAgonist activity at IP receptor in human primary platelets assessed as inhibition of ADP-induced platelet aggregation |
ChEMBL | 449 | 8 | 1 | 4 | 5.7 | O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(F)c(Cl)c2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
11296282 | 1409 | None | 31 | Human | Binding | pIC50 | = | 4.8 | 4.8 | - | 1 | Displacement of [3H]iloprost from human IP receptor after 1 hr by liquid scintillation countingDisplacement of [3H]iloprost from human IP receptor after 1 hr by liquid scintillation counting |
ChEMBL | 590 | 6 | 1 | 5 | 7.3 | Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C | 10.1021/jm9005912 | ||
5822 | 1409 | None | 31 | Human | Binding | pIC50 | = | 4.8 | 4.8 | - | 1 | Displacement of [3H]iloprost from human IP receptor after 1 hr by liquid scintillation countingDisplacement of [3H]iloprost from human IP receptor after 1 hr by liquid scintillation counting |
ChEMBL | 590 | 6 | 1 | 5 | 7.3 | Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C | 10.1021/jm9005912 | ||
CHEMBL565591 | 1409 | None | 31 | Human | Binding | pIC50 | = | 4.8 | 4.8 | - | 1 | Displacement of [3H]iloprost from human IP receptor after 1 hr by liquid scintillation countingDisplacement of [3H]iloprost from human IP receptor after 1 hr by liquid scintillation counting |
ChEMBL | 590 | 6 | 1 | 5 | 7.3 | Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C | 10.1021/jm9005912 | ||
9847589 | 97263 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | Displacement of [3H]iloprost from Prostaglandin I2 receptor of human plateletsDisplacement of [3H]iloprost from Prostaglandin I2 receptor of human platelets |
ChEMBL | 471 | 11 | 1 | 4 | 6.6 | CCC/C(CC1CCc2c(cccc2OCC(=O)O)C1)=N\OC(c1ccccc1)c1ccccc1 | 10.1016/0960-894X(95)00168-S | ||
CHEMBL268477 | 97263 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | Displacement of [3H]iloprost from Prostaglandin I2 receptor of human plateletsDisplacement of [3H]iloprost from Prostaglandin I2 receptor of human platelets |
ChEMBL | 471 | 11 | 1 | 4 | 6.6 | CCC/C(CC1CCc2c(cccc2OCC(=O)O)C1)=N\OC(c1ccccc1)c1ccccc1 | 10.1016/0960-894X(95)00168-S |
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