Ligand source activities (1 row/activity)
| 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
| |
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
| |
| 2720 | 3854 | None | 49 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 5 | 5 | Agonist activity at human DP1 expressed in human 1321N1 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 DP1 expressed in human 1321N1 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 | = | 9.2 | 9.2 | 5 | 5 | Agonist activity at human DP1 expressed in human 1321N1 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 DP1 expressed in human 1321N1 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 | = | 9.2 | 9.2 | 5 | 5 | Agonist activity at human DP1 expressed in human 1321N1 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 DP1 expressed in human 1321N1 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 | = | 9.2 | 9.2 | 5 | 5 | Agonist activity at human DP1 expressed in human 1321N1 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 DP1 expressed in human 1321N1 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 | = | 9.2 | 9.2 | 5 | 5 | Agonist activity at human DP1 expressed in human 1321N1 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 DP1 expressed in human 1321N1 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 | = | 9.2 | 9.2 | 5 | 5 | Agonist activity at human DP1 expressed in human 1321N1 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 DP1 expressed in human 1321N1 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 | ||
| 5077 | 3578 | None | 61 | Human | Functional | pEC50 | = | 7 | 7.0 | 5 | 13 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 496 | 12 | 1 | 7 | 3.9 | O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C | 10.1021/acs.jmedchem.6b00871 | ||
| 7552 | 3578 | None | 61 | Human | Functional | pEC50 | = | 7 | 7.0 | 5 | 13 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 496 | 12 | 1 | 7 | 3.9 | O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C | 10.1021/acs.jmedchem.6b00871 | ||
| 9913767 | 3578 | None | 61 | Human | Functional | pEC50 | = | 7 | 7.0 | 5 | 13 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 496 | 12 | 1 | 7 | 3.9 | O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C | 10.1021/acs.jmedchem.6b00871 | ||
| 9913767.0 | 3578 | None | 61 | Human | Functional | pEC50 | = | 7 | 7.0 | 5 | 13 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 496 | 12 | 1 | 7 | 3.9 | O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C | 10.1021/acs.jmedchem.6b00871 | ||
| CHEMBL238804 | 3578 | None | 61 | Human | Functional | pEC50 | = | 7 | 7.0 | 5 | 13 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 496 | 12 | 1 | 7 | 3.9 | O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C | 10.1021/acs.jmedchem.6b00871 | ||
| DB11362 | 3578 | None | 61 | Human | Functional | pEC50 | = | 7 | 7.0 | 5 | 13 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 496 | 12 | 1 | 7 | 3.9 | O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C | 10.1021/acs.jmedchem.6b00871 | ||
| 44236221 | 147807 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -97 | 3 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 445 | 9 | 1 | 5 | 5.0 | COc1ccc(N(C(=O)OC[C@H]2CC[C@H](COCC(=O)O)CC2)c2cccc(F)c2)cc1 | 10.1021/acs.jmedchem.6b00871 | ||
| CHEMBL3932106 | 147807 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -97 | 3 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 445 | 9 | 1 | 5 | 5.0 | COc1ccc(N(C(=O)OC[C@H]2CC[C@H](COCC(=O)O)CC2)c2cccc(F)c2)cc1 | 10.1021/acs.jmedchem.6b00871 | ||
| 11855865 | 153366 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -478 | 3 | Agonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay |
ChEMBL | 445 | 12 | 2 | 5 | 5.2 | CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 | nan | ||
| CHEMBL3977724 | 153366 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -478 | 3 | Agonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay |
ChEMBL | 445 | 12 | 2 | 5 | 5.2 | CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 | nan | ||
| 44232564 | 145517 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -162 | 3 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 449 | 8 | 1 | 4 | 5.7 | O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccc(Cl)cc2)c2cccc(F)c2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
| CHEMBL3914174 | 145517 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -162 | 3 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 449 | 8 | 1 | 4 | 5.7 | O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccc(Cl)cc2)c2cccc(F)c2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
| 118727315 | 117494 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -4 | 3 | Agonist activity at human recombinant DP1 receptor by cAMP assayAgonist activity at human recombinant DP1 receptor by cAMP assay |
ChEMBL | 520 | 7 | 1 | 5 | 5.3 | O=C(O)COc1cccc2c1CC[C@@H](Cn1ncc(-c3cccc(F)c3F)c(-c3ccc(F)cc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398236 | 117494 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -4 | 3 | Agonist activity at human recombinant DP1 receptor by cAMP assayAgonist activity at human recombinant DP1 receptor by cAMP assay |
ChEMBL | 520 | 7 | 1 | 5 | 5.3 | O=C(O)COc1cccc2c1CC[C@@H](Cn1ncc(-c3cccc(F)c3F)c(-c3ccc(F)cc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| 138107701 | 187570 | None | 33 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -354 | 7 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 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 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -354 | 7 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 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 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -354 | 7 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 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 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -354 | 7 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 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 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -354 | 7 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 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 | ||
| 5852 | 2617 | None | 48 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -1 | 6 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 419 | 11 | 1 | 5 | 4.9 | OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C | 10.1021/acs.jmedchem.6b00871 | ||
| 9931891 | 2617 | None | 48 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -1 | 6 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 419 | 11 | 1 | 5 | 4.9 | OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C | 10.1021/acs.jmedchem.6b00871 | ||
| CHEMBL239226 | 2617 | None | 48 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -1 | 6 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 419 | 11 | 1 | 5 | 4.9 | OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C | 10.1021/acs.jmedchem.6b00871 | ||
| 56839342 | 149095 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | -1 | 7 | 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 | 646 | 13 | 2 | 7 | 6.0 | O=C(CCc1ccc(Cl)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F | nan | ||
| CHEMBL3942394 | 149095 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | -1 | 7 | 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 | 646 | 13 | 2 | 7 | 6.0 | O=C(CCc1ccc(Cl)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F | nan | ||
| 44234532 | 143756 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -85 | 3 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 397 | 8 | 1 | 4 | 4.9 | O=C(O)COC[C@H]1CC[C@@H](COC(=O)N(c2ccccc2)c2ccccc2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
| CHEMBL3900038 | 143756 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -85 | 3 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 397 | 8 | 1 | 4 | 4.9 | O=C(O)COC[C@H]1CC[C@@H](COC(=O)N(c2ccccc2)c2ccccc2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
| 44234782 | 147360 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -190 | 3 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 427 | 9 | 1 | 5 | 4.9 | COc1cccc(N(C(=O)OC[C@H]2CC[C@H](COCC(=O)O)CC2)c2ccccc2)c1 | 10.1021/acs.jmedchem.6b00871 | ||
| CHEMBL3928729 | 147360 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -190 | 3 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 427 | 9 | 1 | 5 | 4.9 | COc1cccc(N(C(=O)OC[C@H]2CC[C@H](COCC(=O)O)CC2)c2ccccc2)c1 | 10.1021/acs.jmedchem.6b00871 | ||
| 56839536 | 143256 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | 1 | 7 | 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 | 604 | 15 | 2 | 7 | 5.1 | CCCCCCCCNC(=O)c1coc([C@@H]2CCCN2Cc2cc(F)ccc2CCC(=O)NS(=O)(=O)C(F)(F)F)n1 | nan | ||
| CHEMBL3896035 | 143256 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | 1 | 7 | 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 | 604 | 15 | 2 | 7 | 5.1 | CCCCCCCCNC(=O)c1coc([C@@H]2CCCN2Cc2cc(F)ccc2CCC(=O)NS(=O)(=O)C(F)(F)F)n1 | nan | ||
| 11855324 | 142692 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -14 | 2 | Agonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay |
ChEMBL | 371 | 6 | 1 | 4 | 4.0 | CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 | nan | ||
| CHEMBL3891401 | 142692 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -14 | 2 | Agonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay |
ChEMBL | 371 | 6 | 1 | 4 | 4.0 | CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 | nan | ||
| 11855324 | 142692 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -14 | 2 | Agonist activity at recombinant human DP receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human DP receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay |
ChEMBL | 371 | 6 | 1 | 4 | 4.0 | CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 | nan | ||
| CHEMBL3891401 | 142692 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -14 | 2 | Agonist activity at recombinant human DP receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human DP receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay |
ChEMBL | 371 | 6 | 1 | 4 | 4.0 | CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 | nan | ||
| 44235521 | 147044 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -346 | 3 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 449 | 8 | 1 | 4 | 5.7 | O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(Cl)c(F)c2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
| CHEMBL3926078 | 147044 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -346 | 3 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF methodAgonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method |
ChEMBL | 449 | 8 | 1 | 4 | 5.7 | O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(Cl)c(F)c2)CC1 | 10.1021/acs.jmedchem.6b00871 | ||
| 138107701 | 187570 | None | 33 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -354 | 7 | Agonist activity at human DP1 expressed in human 1321N1 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 DP1 expressed in human 1321N1 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 | = | 5.7 | 5.7 | -354 | 7 | Agonist activity at human DP1 expressed in human 1321N1 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 DP1 expressed in human 1321N1 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 | = | 5.7 | 5.7 | -354 | 7 | Agonist activity at human DP1 expressed in human 1321N1 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 DP1 expressed in human 1321N1 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 | = | 5.7 | 5.7 | -354 | 7 | Agonist activity at human DP1 expressed in human 1321N1 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 DP1 expressed in human 1321N1 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 | = | 5.7 | 5.7 | -354 | 7 | Agonist activity at human DP1 expressed in human 1321N1 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 DP1 expressed in human 1321N1 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 | ||
| 11855325 | 144779 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -19 | 3 | Agonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay |
ChEMBL | 387 | 6 | 1 | 4 | 4.5 | CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 | nan | ||
| CHEMBL3908484 | 144779 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -19 | 3 | Agonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant DP receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay |
ChEMBL | 387 | 6 | 1 | 4 | 4.5 | CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 | nan | ||
| 11855325 | 144779 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -19 | 3 | Agonist activity at recombinant human DP receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human DP receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay |
ChEMBL | 387 | 6 | 1 | 4 | 4.5 | CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 | nan | ||
Showing 1 to 50 of 877 entries
| 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
| |
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
| |
| 118727294 | 117473 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 496 | 8 | 1 | 6 | 4.9 | COc1ccc(-c2nn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)cc2-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398215 | 117473 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 496 | 8 | 1 | 6 | 4.9 | COc1ccc(-c2nn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)cc2-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727299 | 117478 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 510 | 8 | 1 | 6 | 5.2 | COc1cccc(-c2cc(=O)n(CC3CCc4c(cccc4OCC(=O)O)C3)nc2-c2ccc(C)cc2)c1 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398220 | 117478 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 510 | 8 | 1 | 6 | 5.2 | COc1cccc(-c2cc(=O)n(CC3CCc4c(cccc4OCC(=O)O)C3)nc2-c2ccc(C)cc2)c1 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727287 | 117466 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 496 | 8 | 1 | 6 | 4.9 | COc1cccc(-c2cc(=O)n(CC3CCc4c(cccc4OCC(=O)O)C3)nc2-c2ccccc2)c1 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398208 | 117466 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 496 | 8 | 1 | 6 | 4.9 | COc1cccc(-c2cc(=O)n(CC3CCc4c(cccc4OCC(=O)O)C3)nc2-c2ccccc2)c1 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727301 | 117480 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
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 | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
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 | ||
| 118727285 | 117464 | None | 0 | Human | Binding | pEC50 | = | 7.7 | 7.7 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 466 | 7 | 1 | 5 | 4.8 | O=C(O)COc1cccc2c1CCC(Cn1nc(-c3ccccc3)c(-c3ccccc3)cc1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398206 | 117464 | None | 0 | Human | Binding | pEC50 | = | 7.7 | 7.7 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 466 | 7 | 1 | 5 | 4.8 | O=C(O)COc1cccc2c1CCC(Cn1nc(-c3ccccc3)c(-c3ccccc3)cc1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727316 | 117495 | None | 0 | Human | Binding | pEC50 | = | 7.7 | 7.7 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 427 | 9 | 1 | 4 | 5.3 | O=C(O)COc1cccc2c1CCC=C2CCON=C(c1ccccc1)c1ccccc1 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398237 | 117495 | None | 0 | Human | Binding | pEC50 | = | 7.7 | 7.7 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 427 | 9 | 1 | 4 | 5.3 | O=C(O)COc1cccc2c1CCC=C2CCON=C(c1ccccc1)c1ccccc1 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727300 | 117479 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 514 | 8 | 1 | 6 | 5.0 | COc1cccc(-c2cc(=O)n(CC3CCc4c(cccc4OCC(=O)O)C3)nc2-c2ccc(F)cc2)c1 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398221 | 117479 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 514 | 8 | 1 | 6 | 5.0 | COc1cccc(-c2cc(=O)n(CC3CCc4c(cccc4OCC(=O)O)C3)nc2-c2ccc(F)cc2)c1 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727288 | 117467 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 480 | 7 | 1 | 5 | 5.2 | Cc1cccc(-c2cc(=O)n(CC3CCc4c(cccc4OCC(=O)O)C3)nc2-c2ccccc2)c1 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398209 | 117467 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 480 | 7 | 1 | 5 | 5.2 | Cc1cccc(-c2cc(=O)n(CC3CCc4c(cccc4OCC(=O)O)C3)nc2-c2ccccc2)c1 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727298 | 117477 | None | 0 | Human | Binding | pEC50 | = | 8.5 | 8.5 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
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 | Binding | pEC50 | = | 8.5 | 8.5 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
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 | ||
| 118727297 | 117476 | None | 0 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
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 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
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 | ||
| 118727306 | 117485 | None | 0 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 484 | 7 | 1 | 5 | 5.0 | O=C(O)COc1cccc2c1CCC(Cn1ncc(-c3ccccc3F)c(-c3ccccc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398227 | 117485 | None | 0 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 484 | 7 | 1 | 5 | 5.0 | O=C(O)COc1cccc2c1CCC(Cn1ncc(-c3ccccc3F)c(-c3ccccc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727307 | 117486 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
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 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
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 | ||
| 118727308 | 117487 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
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 | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
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 | ||
| 118727314 | 117493 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 520 | 7 | 1 | 5 | 5.3 | O=C(O)COc1cccc2c1CCC(Cn1ncc(-c3cccc(F)c3F)c(-c3ccc(F)cc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398235 | 117493 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 520 | 7 | 1 | 5 | 5.3 | O=C(O)COc1cccc2c1CCC(Cn1ncc(-c3cccc(F)c3F)c(-c3ccc(F)cc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727289 | 117468 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 484 | 7 | 1 | 5 | 5.0 | O=C(O)COc1cccc2c1CCC(Cn1nc(-c3ccccc3)c(-c3cccc(F)c3)cc1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398210 | 117468 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 484 | 7 | 1 | 5 | 5.0 | O=C(O)COc1cccc2c1CCC(Cn1nc(-c3ccccc3)c(-c3cccc(F)c3)cc1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727302 | 117481 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 496 | 8 | 1 | 6 | 4.9 | COc1cccc(-c2cnn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)c2-c2ccccc2)c1 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398223 | 117481 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 496 | 8 | 1 | 6 | 4.9 | COc1cccc(-c2cnn(CC3CCc4c(cccc4OCC(=O)O)C3)c(=O)c2-c2ccccc2)c1 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727315 | 117494 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 520 | 7 | 1 | 5 | 5.3 | O=C(O)COc1cccc2c1CC[C@@H](Cn1ncc(-c3cccc(F)c3F)c(-c3ccc(F)cc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398236 | 117494 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 520 | 7 | 1 | 5 | 5.3 | O=C(O)COc1cccc2c1CC[C@@H](Cn1ncc(-c3cccc(F)c3F)c(-c3ccc(F)cc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727291 | 117470 | None | 0 | Human | Binding | pEC50 | = | 8.2 | 8.2 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 514 | 8 | 1 | 6 | 5.0 | COc1cccc(-c2cc(=O)n(CC3CCc4c(cccc4OCC(=O)O)C3)nc2-c2ccccc2)c1F | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398212 | 117470 | None | 0 | Human | Binding | pEC50 | = | 8.2 | 8.2 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 514 | 8 | 1 | 6 | 5.0 | COc1cccc(-c2cc(=O)n(CC3CCc4c(cccc4OCC(=O)O)C3)nc2-c2ccccc2)c1F | 10.1016/j.bmcl.2015.01.024 | ||
| 118727290 | 117469 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 500 | 7 | 1 | 5 | 5.5 | O=C(O)COc1cccc2c1CCC(Cn1nc(-c3ccccc3)c(-c3cccc(Cl)c3)cc1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398211 | 117469 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 500 | 7 | 1 | 5 | 5.5 | O=C(O)COc1cccc2c1CCC(Cn1nc(-c3ccccc3)c(-c3cccc(Cl)c3)cc1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| 118727303 | 117482 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 484 | 7 | 1 | 5 | 5.0 | O=C(O)COc1cccc2c1CCC(Cn1ncc(-c3cccc(F)c3)c(-c3ccccc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| CHEMBL3398224 | 117482 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 minsAgonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins |
ChEMBL | 484 | 7 | 1 | 5 | 5.0 | O=C(O)COc1cccc2c1CCC(Cn1ncc(-c3cccc(F)c3)c(-c3ccccc3)c1=O)C2 | 10.1016/j.bmcl.2015.01.024 | ||
| 10741899 | 10521 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Inhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranesInhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranes |
ChEMBL | 443 | 8 | 2 | 3 | 6.0 | CC1(C)[C@H]2C[C@H](C/C=C\CCCC(=O)O)[C@@H](NC(=O)c3csc4ccc(F)cc34)[C@@H]1C2 | 10.1021/jm970343g | ||
| CHEMBL116836 | 10521 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Inhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranesInhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranes |
ChEMBL | 443 | 8 | 2 | 3 | 6.0 | CC1(C)[C@H]2C[C@H](C/C=C\CCCC(=O)O)[C@@H](NC(=O)c3csc4ccc(F)cc34)[C@@H]1C2 | 10.1021/jm970343g | ||
| 9867949 | 10522 | None | 23 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Inhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranesInhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranes |
ChEMBL | 441 | 8 | 3 | 4 | 5.6 | CC1(C)[C@H]2C[C@H](C/C=C\CCCC(=O)O)[C@@H](NC(=O)c3csc4ccc(O)cc34)[C@@H]1C2 | 10.1021/jm970343g | ||
| CHEMBL116837 | 10522 | None | 23 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Inhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranesInhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranes |
ChEMBL | 441 | 8 | 3 | 4 | 5.6 | CC1(C)[C@H]2C[C@H](C/C=C\CCCC(=O)O)[C@@H](NC(=O)c3csc4ccc(O)cc34)[C@@H]1C2 | 10.1021/jm970343g | ||
| 44461046 | 207838 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Prostaglandin D2 receptor antagonist activity, evaluated by inhibition of [3H]PGD-2 binding to human platelet membranesProstaglandin D2 receptor antagonist activity, evaluated by inhibition of [3H]PGD-2 binding to human platelet membranes |
ChEMBL | 443 | 8 | 2 | 3 | 6.0 | CC1(C)[C@H]2C[C@H](C/C=C/CCCC(=O)O)[C@@H](NC(=O)c3csc4ccc(F)cc34)[C@@H]1C2 | 10.1021/jm0205189 | ||
| CHEMBL79943 | 207838 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Prostaglandin D2 receptor antagonist activity, evaluated by inhibition of [3H]PGD-2 binding to human platelet membranesProstaglandin D2 receptor antagonist activity, evaluated by inhibition of [3H]PGD-2 binding to human platelet membranes |
ChEMBL | 443 | 8 | 2 | 3 | 6.0 | CC1(C)[C@H]2C[C@H](C/C=C/CCCC(=O)O)[C@@H](NC(=O)c3csc4ccc(F)cc34)[C@@H]1C2 | 10.1021/jm0205189 | ||
| 10599289 | 14147 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Inhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranesInhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranes |
ChEMBL | 441 | 8 | 3 | 4 | 5.6 | CC1(C)[C@H]2C[C@H](C/C=C\CCCC(=O)O)[C@@H](NC(=O)c3csc4cc(O)ccc34)[C@@H]1C2 | 10.1021/jm970343g | ||
| CHEMBL119810 | 14147 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Inhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranesInhibition of [3H]PGD-2 specific binding to Prostaglandin D2 receptor from human platelet membranes |
ChEMBL | 441 | 8 | 3 | 4 | 5.6 | CC1(C)[C@H]2C[C@H](C/C=C\CCCC(=O)O)[C@@H](NC(=O)c3csc4cc(O)ccc34)[C@@H]1C2 | 10.1021/jm970343g | ||
| 3356 | 2280 | None | 46 | Human | Binding | pIC50 | = | 8.9 | 8.9 | 38 | 9 | Activity at sheep DP receptor by PRP assayActivity at sheep DP receptor by PRP assay |
ChEMBL | 435 | 5 | 1 | 4 | 4.4 | OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F | 10.1021/jm0603668 | ||
| 4326 | 2280 | None | 46 | Human | Binding | pIC50 | = | 8.9 | 8.9 | 38 | 9 | Activity at sheep DP receptor by PRP assayActivity at sheep DP receptor by PRP assay |
ChEMBL | 435 | 5 | 1 | 4 | 4.4 | OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F | 10.1021/jm0603668 | ||
Showing 1 to 50 of 1,596 entries