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 | = | 9.5 | 9.5 | 1 | 7 | Agonist activity at human EP1 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 EP1 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 | = | 9.5 | 9.5 | 1 | 7 | Agonist activity at human EP1 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 EP1 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 | = | 9.5 | 9.5 | 1 | 7 | Agonist activity at human EP1 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 EP1 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 | = | 9.5 | 9.5 | 1 | 7 | Agonist activity at human EP1 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 EP1 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 | = | 9.5 | 9.5 | 1 | 7 | Agonist activity at human EP1 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 EP1 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 | ||
127052613 | 140293 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | -1 | 6 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
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 | = | 8.9 | 8.9 | -1 | 6 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
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 | ||
127052614 | 140313 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -40 | 6 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
ChEMBL | 415 | 7 | 2 | 6 | 4.1 | O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCOc3ccccc3)O2)n1 | 10.1021/acsmedchemlett.5b00455 | ||
CHEMBL3805176 | 140313 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -40 | 6 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
ChEMBL | 415 | 7 | 2 | 6 | 4.1 | O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCOc3ccccc3)O2)n1 | 10.1021/acsmedchemlett.5b00455 | ||
58681361 | 144769 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -19 | 3 | Agonist activity at human recombinant EP1 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP1 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay |
ChEMBL | 318 | 8 | 2 | 3 | 3.5 | Cc1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 | nan | ||
CHEMBL3908432 | 144769 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -19 | 3 | Agonist activity at human recombinant EP1 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP1 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay |
ChEMBL | 318 | 8 | 2 | 3 | 3.5 | Cc1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 | nan | ||
1955 | 16 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | -2089 | 5 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=100%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=100%) |
ChEMBL | 428 | 13 | 4 | 5 | 3.6 | O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(00)00273-0 | ||
5311240 | 16 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | -2089 | 5 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=100%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=100%) |
ChEMBL | 428 | 13 | 4 | 5 | 3.6 | O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(00)00273-0 | ||
CHEMBL36041 | 16 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | -2089 | 5 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=100%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=100%) |
ChEMBL | 428 | 13 | 4 | 5 | 3.6 | O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(00)00273-0 | ||
56839536 | 143256 | None | 0 | Human | Functional | pEC50 | = | 7.7 | 7.7 | -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 | = | 7.7 | 7.7 | -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 | ||
56839342 | 149095 | None | 0 | Human | Functional | pEC50 | = | 7.7 | 7.7 | -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 | = | 7.7 | 7.7 | -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 | ||
145977227 | 164102 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -1995 | 4 | Agonist activity at recombinant human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level measured at 3 secs time interval by fura-2-AM dye based fluorescence assayAgonist activity at recombinant human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level measured at 3 secs time interval by fura-2-AM dye based fluorescence assay |
ChEMBL | 437 | 10 | 2 | 6 | 5.2 | C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CC1CCCC1 | 10.1016/j.bmc.2017.11.035 | ||
CHEMBL4208379 | 164102 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -1995 | 4 | Agonist activity at recombinant human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level measured at 3 secs time interval by fura-2-AM dye based fluorescence assayAgonist activity at recombinant human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level measured at 3 secs time interval by fura-2-AM dye based fluorescence assay |
ChEMBL | 437 | 10 | 2 | 6 | 5.2 | C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CC1CCCC1 | 10.1016/j.bmc.2017.11.035 | ||
11955358 | 153171 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -1 | 3 | Agonist activity at human recombinant EP1 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP1 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay |
ChEMBL | 364 | 8 | 2 | 2 | 4.7 | O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl | nan | ||
CHEMBL3976116 | 153171 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -1 | 3 | Agonist activity at human recombinant EP1 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP1 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay |
ChEMBL | 364 | 8 | 2 | 2 | 4.7 | O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl | nan | ||
156022045 | 178305 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -4 | 3 | Agonist activity at human EP1 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP1 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay |
ChEMBL | 351 | 14 | 2 | 4 | 3.8 | CCCCCC(O)CCc1cccc(=O)n1CCCCCCC(=O)O | 10.1016/j.bmcl.2020.127104 | ||
CHEMBL4649582 | 178305 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -4 | 3 | Agonist activity at human EP1 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP1 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay |
ChEMBL | 351 | 14 | 2 | 4 | 3.8 | CCCCCC(O)CCc1cccc(=O)n1CCCCCCC(=O)O | 10.1016/j.bmcl.2020.127104 | ||
2720 | 3854 | None | 49 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -478 | 5 | Agonist activity at human EP1 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 EP1 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 | = | 6.5 | 6.5 | -478 | 5 | Agonist activity at human EP1 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 EP1 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 | = | 6.5 | 6.5 | -478 | 5 | Agonist activity at human EP1 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 EP1 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 | = | 6.5 | 6.5 | -478 | 5 | Agonist activity at human EP1 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 EP1 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 | = | 6.5 | 6.5 | -478 | 5 | Agonist activity at human EP1 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 EP1 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 | = | 6.5 | 6.5 | -478 | 5 | Agonist activity at human EP1 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 EP1 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 | ||
1883 | 3082 | None | 47 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -1 | 12 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/acsmedchemlett.5b00455 | ||
1916 | 3082 | None | 47 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -1 | 12 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/acsmedchemlett.5b00455 | ||
5280360 | 3082 | None | 47 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -1 | 12 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/acsmedchemlett.5b00455 | ||
5280360.0 | 3082 | None | 47 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -1 | 12 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/acsmedchemlett.5b00455 | ||
913 | 3082 | None | 47 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -1 | 12 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/acsmedchemlett.5b00455 | ||
CHEMBL548 | 3082 | None | 47 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -1 | 12 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/acsmedchemlett.5b00455 | ||
DB00917 | 3082 | None | 47 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -1 | 12 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/acsmedchemlett.5b00455 | ||
6441607 | 155169 | None | 22 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -12 | 4 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%) |
ChEMBL | 382 | 12 | 4 | 4 | 3.7 | CCCCC(C)(C)[C@H](O)/C=C/[C@H]1[C@H](O)C[C@H](O)[C@@H]1C/C=C\CCCC(=O)O | 10.1016/s0960-894x(00)00273-0 | ||
CHEMBL40183 | 155169 | None | 22 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -12 | 4 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%) |
ChEMBL | 382 | 12 | 4 | 4 | 3.7 | CCCCC(C)(C)[C@H](O)/C=C/[C@H]1[C@H](O)C[C@H](O)[C@@H]1C/C=C\CCCC(=O)O | 10.1016/s0960-894x(00)00273-0 | ||
10389527 | 153434 | None | 17 | Human | Functional | pEC50 | = | 4.5 | 4.5 | -1122 | 2 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=100%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=100%) |
ChEMBL | 460 | 13 | 4 | 4 | 4.6 | O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCc1cccc(C(F)(F)F)c1 | 10.1016/s0960-894x(00)00273-0 | ||
CHEMBL39784 | 153434 | None | 17 | Human | Functional | pEC50 | = | 4.5 | 4.5 | -1122 | 2 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=100%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=100%) |
ChEMBL | 460 | 13 | 4 | 4 | 4.6 | O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCc1cccc(C(F)(F)F)c1 | 10.1016/s0960-894x(00)00273-0 | ||
126495398 | 140298 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -416 | 3 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
ChEMBL | 403 | 7 | 2 | 6 | 3.9 | O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCCOc3ccccc3)O2)n1 | 10.1021/acsmedchemlett.5b00455 | ||
CHEMBL3805044 | 140298 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -416 | 3 | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis |
ChEMBL | 403 | 7 | 2 | 6 | 3.9 | O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCCOc3ccccc3)O2)n1 | 10.1021/acsmedchemlett.5b00455 | ||
56649302 | 152755 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | -1 | 6 | 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 | 630 | 13 | 2 | 7 | 5.5 | O=C(CCc1ccc(F)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F | nan | ||
CHEMBL3972583 | 152755 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | -1 | 6 | 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 | 630 | 13 | 2 | 7 | 5.5 | O=C(CCc1ccc(F)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F | nan | ||
1884 | 3083 | None | 40 | Human | Functional | pEC50 | = | 6.2 | 6.2 | -22 | 9 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%) |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/s0960-894x(00)00273-0 | ||
5280363 | 3083 | None | 40 | Human | Functional | pEC50 | = | 6.2 | 6.2 | -22 | 9 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%) |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/s0960-894x(00)00273-0 | ||
912 | 3083 | None | 40 | Human | Functional | pEC50 | = | 6.2 | 6.2 | -22 | 9 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%) |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/s0960-894x(00)00273-0 | ||
CHEMBL815 | 3083 | None | 40 | Human | Functional | pEC50 | = | 6.2 | 6.2 | -22 | 9 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%) |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/s0960-894x(00)00273-0 | ||
DB12789 | 3083 | None | 40 | Human | Functional | pEC50 | = | 6.2 | 6.2 | -22 | 9 | Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%) |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/s0960-894x(00)00273-0 |
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| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
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Ligands (move mouse cursor over ligand name to see structure)
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| 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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10409554 | 149609 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell. |
ChEMBL | 414 | 11 | 3 | 4 | 3.9 | CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O | nan | ||
CHEMBL3946494 | 149609 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell. |
ChEMBL | 414 | 11 | 3 | 4 | 3.9 | CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O | nan | ||
10409554 | 149609 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell. |
ChEMBL | 414 | 11 | 3 | 4 | 3.9 | CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O | nan | ||
CHEMBL3946494 | 149609 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell. |
ChEMBL | 414 | 11 | 3 | 4 | 3.9 | CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O | nan | ||
11340370 | 80613 | None | 15 | Human | Binding | pIC50 | = | 9.9 | 9.9 | - | 1 | Displacement of [3H]PGE2 from human EP1 receptor expressed in CHO cellsDisplacement of [3H]PGE2 from human EP1 receptor expressed in CHO cells |
ChEMBL | 468 | 6 | 1 | 4 | 5.6 | Cc1cc(C(=O)O)nn1Cc1cc(Br)ccc1OCc1ccc(Cl)cc1Cl | 10.1016/j.bmcl.2009.02.112 | ||
CHEMBL2110364 | 80613 | None | 15 | Human | Binding | pIC50 | = | 9.9 | 9.9 | - | 1 | Displacement of [3H]PGE2 from human EP1 receptor expressed in CHO cellsDisplacement of [3H]PGE2 from human EP1 receptor expressed in CHO cells |
ChEMBL | 468 | 6 | 1 | 4 | 5.6 | Cc1cc(C(=O)O)nn1Cc1cc(Br)ccc1OCc1ccc(Cl)cc1Cl | 10.1016/j.bmcl.2009.02.112 | ||
CHEMBL214971 | 80613 | None | 15 | Human | Binding | pIC50 | = | 9.9 | 9.9 | - | 1 | Displacement of [3H]PGE2 from human EP1 receptor expressed in CHO cellsDisplacement of [3H]PGE2 from human EP1 receptor expressed in CHO cells |
ChEMBL | 468 | 6 | 1 | 4 | 5.6 | Cc1cc(C(=O)O)nn1Cc1cc(Br)ccc1OCc1ccc(Cl)cc1Cl | 10.1016/j.bmcl.2009.02.112 | ||
11340370 | 80613 | None | 15 | Human | Binding | pIC50 | = | 9.9 | 9.9 | - | 1 | Displacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cellsDisplacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cells |
ChEMBL | 468 | 6 | 1 | 4 | 5.6 | Cc1cc(C(=O)O)nn1Cc1cc(Br)ccc1OCc1ccc(Cl)cc1Cl | 10.1016/j.bmcl.2006.06.086 | ||
CHEMBL2110364 | 80613 | None | 15 | Human | Binding | pIC50 | = | 9.9 | 9.9 | - | 1 | Displacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cellsDisplacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cells |
ChEMBL | 468 | 6 | 1 | 4 | 5.6 | Cc1cc(C(=O)O)nn1Cc1cc(Br)ccc1OCc1ccc(Cl)cc1Cl | 10.1016/j.bmcl.2006.06.086 | ||
CHEMBL214971 | 80613 | None | 15 | Human | Binding | pIC50 | = | 9.9 | 9.9 | - | 1 | Displacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cellsDisplacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cells |
ChEMBL | 468 | 6 | 1 | 4 | 5.6 | Cc1cc(C(=O)O)nn1Cc1cc(Br)ccc1OCc1ccc(Cl)cc1Cl | 10.1016/j.bmcl.2006.06.086 | ||
10007859 | 166584 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | 5011 | 2 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 554 | 7 | 2 | 4 | 6.7 | CC(=O)Nc1cc(C(=O)O)cc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2F)c1 | 10.1016/j.bmcl.2006.10.078 | ||
CHEMBL427844 | 166584 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | 5011 | 2 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 554 | 7 | 2 | 4 | 6.7 | CC(=O)Nc1cc(C(=O)O)cc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2F)c1 | 10.1016/j.bmcl.2006.10.078 | ||
10459580 | 85707 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membraneDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane |
ChEMBL | 527 | 7 | 1 | 4 | 6.8 | COc1ccc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2F)cc1C(=O)O | 10.1016/j.bmcl.2006.11.059 | ||
CHEMBL228586 | 85707 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membraneDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane |
ChEMBL | 527 | 7 | 1 | 4 | 6.8 | COc1ccc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2F)cc1C(=O)O | 10.1016/j.bmcl.2006.11.059 | ||
44426669 | 142157 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membraneDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane |
ChEMBL | 554 | 7 | 2 | 4 | 6.7 | CC(=O)Nc1ccc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2F)cc1C(=O)O | 10.1016/j.bmcl.2006.11.059 | ||
CHEMBL387969 | 142157 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membraneDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane |
ChEMBL | 554 | 7 | 2 | 4 | 6.7 | CC(=O)Nc1ccc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2F)cc1C(=O)O | 10.1016/j.bmcl.2006.11.059 | ||
44430700 | 143982 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 512 | 6 | 2 | 4 | 6.4 | Cc1ccc(-c2cc(Br)ccc2OCc2ccc(F)cc2F)n1-c1cc(N)cc(C(=O)O)c1 | 10.1016/j.bmcl.2006.10.078 | ||
CHEMBL390189 | 143982 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 512 | 6 | 2 | 4 | 6.4 | Cc1ccc(-c2cc(Br)ccc2OCc2ccc(F)cc2F)n1-c1cc(N)cc(C(=O)O)c1 | 10.1016/j.bmcl.2006.10.078 | ||
11189804 | 80611 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 1 | Displacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cellsDisplacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cells |
ChEMBL | 436 | 6 | 1 | 4 | 4.6 | Cc1cc(C(=O)O)nn1Cc1cc(Br)ccc1OCc1ccc(F)cc1F | 10.1016/j.bmcl.2006.06.086 | ||
CHEMBL214967 | 80611 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 1 | Displacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cellsDisplacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cells |
ChEMBL | 436 | 6 | 1 | 4 | 4.6 | Cc1cc(C(=O)O)nn1Cc1cc(Br)ccc1OCc1ccc(F)cc1F | 10.1016/j.bmcl.2006.06.086 | ||
59179887 | 105891 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assayAntagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assay |
ChEMBL | 389 | 3 | 1 | 5 | 4.9 | O=C(O)c1csc(-n2nc(-c3ccccc3)c3ccc(C(F)(F)F)cc32)n1 | 10.1016/j.bmcl.2014.01.052 | ||
CHEMBL3127163 | 105891 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assayAntagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assay |
ChEMBL | 389 | 3 | 1 | 5 | 4.9 | O=C(O)c1csc(-n2nc(-c3ccccc3)c3ccc(C(F)(F)F)cc32)n1 | 10.1016/j.bmcl.2014.01.052 | ||
10099424 | 142147 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membraneDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane |
ChEMBL | 563 | 8 | 1 | 4 | 7.4 | Cc1ccc(-c2cc(Br)ccc2OCc2ccc(F)cc2F)n1-c1ccc(OC(F)F)c(C(=O)O)c1 | 10.1016/j.bmcl.2006.11.059 | ||
CHEMBL387878 | 142147 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membraneDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane |
ChEMBL | 563 | 8 | 1 | 4 | 7.4 | Cc1ccc(-c2cc(Br)ccc2OCc2ccc(F)cc2F)n1-c1ccc(OC(F)F)c(C(=O)O)c1 | 10.1016/j.bmcl.2006.11.059 | ||
44430704 | 167867 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 536 | 7 | 2 | 4 | 6.6 | CC(=O)Nc1cc(C(=O)O)cc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2)c1 | 10.1016/j.bmcl.2006.10.078 | ||
CHEMBL430360 | 167867 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 536 | 7 | 2 | 4 | 6.6 | CC(=O)Nc1cc(C(=O)O)cc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2)c1 | 10.1016/j.bmcl.2006.10.078 | ||
10324022 | 85709 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membraneDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane |
ChEMBL | 508 | 6 | 2 | 4 | 6.5 | Cc1c(N)cc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2)cc1C(=O)O | 10.1016/j.bmcl.2006.11.059 | ||
CHEMBL228593 | 85709 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membraneDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane |
ChEMBL | 508 | 6 | 2 | 4 | 6.5 | Cc1c(N)cc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2)cc1C(=O)O | 10.1016/j.bmcl.2006.11.059 | ||
59179305 | 103940 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Antagonist activity human EP1 receptor assessed as inhibition of PGE2-induced effect by reporter gene assayAntagonist activity human EP1 receptor assessed as inhibition of PGE2-induced effect by reporter gene assay |
ChEMBL | 359 | 3 | 1 | 5 | 4.3 | O=C(O)c1csc(-n2nc(-c3ccccc3)c3c2-c2ccccc2C3)n1 | 10.1016/j.bmcl.2013.10.065 | ||
CHEMBL3092131 | 103940 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Antagonist activity human EP1 receptor assessed as inhibition of PGE2-induced effect by reporter gene assayAntagonist activity human EP1 receptor assessed as inhibition of PGE2-induced effect by reporter gene assay |
ChEMBL | 359 | 3 | 1 | 5 | 4.3 | O=C(O)c1csc(-n2nc(-c3ccccc3)c3c2-c2ccccc2C3)n1 | 10.1016/j.bmcl.2013.10.065 | ||
68258993 | 105885 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Antagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assayAntagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assay |
ChEMBL | 335 | 3 | 1 | 5 | 4.2 | Cc1ccc2c(-c3ccccc3)nn(-c3nc(C(=O)O)cs3)c2c1 | 10.1016/j.bmcl.2014.01.052 | ||
CHEMBL3127157 | 105885 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Antagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assayAntagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assay |
ChEMBL | 335 | 3 | 1 | 5 | 4.2 | Cc1ccc2c(-c3ccccc3)nn(-c3nc(C(=O)O)cs3)c2c1 | 10.1016/j.bmcl.2014.01.052 | ||
10051605 | 79712 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Inhibition of [3H]PGE2 binding to EP1 receptor expressed in CHO cellsInhibition of [3H]PGE2 binding to EP1 receptor expressed in CHO cells |
ChEMBL | 497 | 6 | 1 | 3 | 6.8 | Cc1ccc(-c2cc(Br)ccc2OCc2c(F)cccc2F)n1-c1cccc(C(=O)O)c1 | 10.1016/j.bmcl.2006.04.073 | ||
CHEMBL211534 | 79712 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Inhibition of [3H]PGE2 binding to EP1 receptor expressed in CHO cellsInhibition of [3H]PGE2 binding to EP1 receptor expressed in CHO cells |
ChEMBL | 497 | 6 | 1 | 3 | 6.8 | Cc1ccc(-c2cc(Br)ccc2OCc2c(F)cccc2F)n1-c1cccc(C(=O)O)c1 | 10.1016/j.bmcl.2006.04.073 | ||
59179936 | 105887 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | Antagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assayAntagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assay |
ChEMBL | 351 | 4 | 1 | 6 | 3.9 | COc1ccc2c(-c3ccccc3)nn(-c3nc(C(=O)O)cs3)c2c1 | 10.1016/j.bmcl.2014.01.052 | ||
CHEMBL3127159 | 105887 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | Antagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assayAntagonist activity at human EP1 receptor assessed as inhibition of PGE-induced effect by reporter gene assay |
ChEMBL | 351 | 4 | 1 | 6 | 3.9 | COc1ccc2c(-c3ccccc3)nn(-c3nc(C(=O)O)cs3)c2c1 | 10.1016/j.bmcl.2014.01.052 | ||
1883 | 3082 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | -12 | 24 | Binding affinity to EP1 receptorBinding affinity to EP1 receptor |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/jm9018756 | ||
1916 | 3082 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | -12 | 24 | Binding affinity to EP1 receptorBinding affinity to EP1 receptor |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/jm9018756 | ||
5280360 | 3082 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | -12 | 24 | Binding affinity to EP1 receptorBinding affinity to EP1 receptor |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/jm9018756 | ||
5280360.0 | 3082 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | -12 | 24 | Binding affinity to EP1 receptorBinding affinity to EP1 receptor |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/jm9018756 | ||
913 | 3082 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | -12 | 24 | Binding affinity to EP1 receptorBinding affinity to EP1 receptor |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/jm9018756 | ||
CHEMBL548 | 3082 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | -12 | 24 | Binding affinity to EP1 receptorBinding affinity to EP1 receptor |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/jm9018756 | ||
DB00917 | 3082 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | -12 | 24 | Binding affinity to EP1 receptorBinding affinity to EP1 receptor |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/jm9018756 | ||
44430703 | 88082 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 518 | 7 | 2 | 4 | 6.5 | CC(=O)Nc1cc(C(=O)O)cc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccccc2)c1 | 10.1016/j.bmcl.2006.10.078 | ||
CHEMBL234519 | 88082 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 518 | 7 | 2 | 4 | 6.5 | CC(=O)Nc1cc(C(=O)O)cc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccccc2)c1 | 10.1016/j.bmcl.2006.10.078 | ||
44430706 | 88201 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 508 | 7 | 2 | 4 | 6.7 | CC(=O)Nc1cc(C(=O)O)cc(-n2c(C)ccc2-c2cc(C(F)(F)F)ccc2OCc2ccccc2)c1 | 10.1016/j.bmcl.2006.10.078 | ||
CHEMBL234727 | 88201 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 508 | 7 | 2 | 4 | 6.7 | CC(=O)Nc1cc(C(=O)O)cc(-n2c(C)ccc2-c2cc(C(F)(F)F)ccc2OCc2ccccc2)c1 | 10.1016/j.bmcl.2006.10.078 | ||
44430708 | 144033 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 568 | 7 | 1 | 4 | 6.8 | CC(=O)N(C)c1cc(C(=O)O)cc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2F)c1 | 10.1016/j.bmcl.2006.10.078 | ||
CHEMBL390238 | 144033 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 568 | 7 | 1 | 4 | 6.8 | CC(=O)N(C)c1cc(C(=O)O)cc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2F)c1 | 10.1016/j.bmcl.2006.10.078 | ||
44430710 | 166856 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranesDisplacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHO cell membranes |
ChEMBL | 594 | 7 | 1 | 4 | 7.3 | Cc1ccc(-c2cc(Br)ccc2OCc2ccc(F)cc2F)n1-c1cc(C(=O)O)cc(N2CCCCC2=O)c1 | 10.1016/j.bmcl.2006.10.078 |
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