Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
14429703 149150 0 None 5248 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 467 12 4 7 1.5 CS(=O)(=O)NC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)COc1ccccc1 10.1021/acsmedchemlett.6b00415
CHEMBL3889508 149150 0 None 5248 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 467 12 4 7 1.5 CS(=O)(=O)NC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)COc1ccccc1 10.1021/acsmedchemlett.6b00415
11294085 144030 0 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human EP3 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 EP3 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 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmc.2017.11.035
CHEMBL3751951 144030 0 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human EP3 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 EP3 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 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmc.2017.11.035
127052613 146984 0 None 1 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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 146984 0 None 1 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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
145971909 171479 0 None -11 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human EP3 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 EP3 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 411 11 2 6 4.8 CCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4217198 171479 0 None -11 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human EP3 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 EP3 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 411 11 2 6 4.8 CCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
13174090 158909 9 None 17 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 388 11 3 5 2.8 O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)COc1ccccc1 10.1021/acsmedchemlett.6b00415
CHEMBL3967903 158909 9 None 17 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 388 11 3 5 2.8 O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)COc1ccccc1 10.1021/acsmedchemlett.6b00415
66978356 170487 0 None -10 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP3 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 EP3 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 425 12 2 6 5.2 CCCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4204996 170487 0 None -10 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP3 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 EP3 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 425 12 2 6 5.2 CCCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
145977227 170786 0 None 1 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human EP3 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 EP3 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 170786 0 None 1 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human EP3 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 EP3 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
56839343 151057 0 None -2 6 Human 7.0 pEC50 = 7 Functional
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 642 14 2 8 5.4 COc1ccc(CCC(=O)NS(=O)(=O)C(F)(F)F)c(CN2CCC[C@H]2c2nc(C(=O)NCCCCC3CCCCC3)co2)c1 nan
CHEMBL3904989 151057 0 None -2 6 Human 7.0 pEC50 = 7 Functional
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 642 14 2 8 5.4 COc1ccc(CCC(=O)NS(=O)(=O)C(F)(F)F)c(CN2CCC[C@H]2c2nc(C(=O)NCCCCC3CCCCC3)co2)c1 nan
17757350 159533 0 None -870 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
CHEMBL3973347 159533 0 None -870 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
56839536 149947 0 None -6 7 Human 7.0 pEC50 = 7.0 Functional
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 149947 0 None -6 7 Human 7.0 pEC50 = 7.0 Functional
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
11855868 159323 0 None -24 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 159323 0 None -24 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855868 159323 0 None -24 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 159323 0 None -24 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
68751402 151015 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 416 10 3 5 3.3 O=C(O)CCCCC1=CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
CHEMBL3904644 151015 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 416 10 3 5 3.3 O=C(O)CCCCC1=CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
134151657 159893 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 418 10 3 5 3.4 O=C(O)CCCC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
CHEMBL3976382 159893 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 418 10 3 5 3.4 O=C(O)CCCC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
126495463 147085 0 None -1000 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis
ChEMBL 389 6 2 6 3.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3806130 147085 0 None -1000 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis
ChEMBL 389 6 2 6 3.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
24760052 157964 0 None -24 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3959769 157964 0 None -24 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
70667255 158253 0 None -24 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3962183 158253 0 None -24 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
56839344 158830 0 None -501 8 Human 6.8 pEC50 = 6.8 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 656 13 2 9 5.1 O=C(CCc1cc2c(cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC3CCCCC3)co1)OCO2)NS(=O)(=O)C(F)(F)F nan
CHEMBL3967284 158830 0 None -501 8 Human 6.8 pEC50 = 6.8 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 656 13 2 9 5.1 O=C(CCc1cc2c(cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC3CCCCC3)co1)OCO2)NS(=O)(=O)C(F)(F)F nan
59465574 152723 0 None -1 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 400 12 1 4 5.7 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)OC)cc1 nan
CHEMBL3918084 152723 0 None -1 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 400 12 1 4 5.7 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)OC)cc1 nan
118517490 159934 0 None -602 4 Human 5.8 pEC50 = 5.8 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
CHEMBL3976710 159934 0 None -602 4 Human 5.8 pEC50 = 5.8 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
11502897 149571 0 None -43 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 149571 0 None -43 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11502897 149571 0 None -43 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 149571 0 None -43 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
67082722 171407 0 None -2 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP3 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 EP3 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 425 12 2 6 5.2 CCCCC[C@@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4216182 171407 0 None -2 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP3 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 EP3 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 425 12 2 6 5.2 CCCCC[C@@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
11955156 155233 1 None 2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 3 4 4.9 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
CHEMBL3937945 155233 1 None 2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 3 4 4.9 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
118517359 151174 0 None -363 4 Human 6.8 pEC50 = 6.8 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 151174 0 None -363 4 Human 6.8 pEC50 = 6.8 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
68749474 153011 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 8 3 5 2.8 O=C(O)CC[C@H]1CCC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.6b00415
CHEMBL3920347 153011 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 8 3 5 2.8 O=C(O)CC[C@H]1CCC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.6b00415
118517359 151174 0 None -363 4 Human 6.8 pEC50 = 6.8 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 151174 0 None -363 4 Human 6.8 pEC50 = 6.8 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
11855325 151469 0 None -154 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A 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 151469 0 None -154 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A 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 151469 0 None -154 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 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
CHEMBL3908484 151469 0 None -154 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 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
57529188 153973 0 None -19 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 153973 0 None -19 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
57529188 153973 0 None -19 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 153973 0 None -19 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
11855588 154135 0 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3929446 154135 0 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
11855588 154135 0 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3929446 154135 0 None -12 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
134147356 156391 0 None 123 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 404 9 3 5 3.0 O=C(O)CCC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
CHEMBL3947086 156391 0 None 123 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 404 9 3 5 3.0 O=C(O)CCC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
1883 9856 75 None 1 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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 9856 75 None 1 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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 9856 75 None 1 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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 9856 75 None 1 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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 9856 75 None 1 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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 9856 75 None 1 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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
15979081 170619 0 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP3 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 EP3 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 425 12 2 6 5.2 CCCCCC(C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4206444 170619 0 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP3 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 EP3 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 425 12 2 6 5.2 CCCCCC(C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
6441607 161858 28 None -83 4 Human 5.7 pEC50 = 5.7 Functional
Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=130%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=130%)
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 161858 28 None -83 4 Human 5.7 pEC50 = 5.7 Functional
Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=130%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=130%)
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
11955193 150362 0 None -17 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 378 7 2 2 5.3 CC(C)(C)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3899346 150362 0 None -17 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 378 7 2 2 5.3 CC(C)(C)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
1884 9857 52 None -26 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=50%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=50%)
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 9857 52 None -26 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=50%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=50%)
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 9857 52 None -26 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=50%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=50%)
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 9857 52 None -26 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=50%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=50%)
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 9857 52 None -26 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=50%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=50%)
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
11855870 153058 0 None -467 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 153058 0 None -467 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855870 153058 0 None -467 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 153058 0 None -467 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
17751059 155047 0 None -3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3936540 155047 0 None -3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
44564804 183479 0 None 100 5 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human EP3-2 receptor expressed in CHOK1 cellsAntagonist activity at human EP3-2 receptor expressed in CHOK1 cells
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL459885 183479 0 None 100 5 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human EP3-2 receptor expressed in CHOK1 cellsAntagonist activity at human EP3-2 receptor expressed in CHOK1 cells
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
127052614 147004 0 None -67 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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 147004 0 None -67 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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
68785185 157595 0 None -7 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 8 3 5 2.8 O=C(O)CC[C@@H]1CCC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.6b00415
CHEMBL3956817 157595 0 None -7 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 8 3 5 2.8 O=C(O)CC[C@@H]1CCC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.6b00415
68747456 152544 0 None -5 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 388 8 3 5 2.6 O=C(O)CCC1=CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
CHEMBL3916674 152544 0 None -5 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 388 8 3 5 2.6 O=C(O)CCC1=CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
156022045 184979 0 None -4 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human EP3 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP3 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 184979 0 None -4 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human EP3 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP3 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
58708282 159903 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 412 11 2 3 6.0 CCCC1([C@@H](O)c2cccc([C@H]3CCC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
CHEMBL3976452 159903 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 412 11 2 3 6.0 CCCC1([C@@H](O)c2cccc([C@H]3CCC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
145978309 170531 0 None -27 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP3 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 EP3 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 429 12 2 6 4.8 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCCCF 10.1016/j.bmc.2017.11.035
CHEMBL4205480 170531 0 None -27 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP3 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 EP3 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 429 12 2 6 4.8 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCCCF 10.1016/j.bmc.2017.11.035
66857988 170901 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP3 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 EP3 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 428 12 2 7 4.0 CCCCCC(C)(O)C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4209929 170901 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP3 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 EP3 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 428 12 2 7 4.0 CCCCCC(C)(O)C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
145965248 171009 0 None 9 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP3 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 EP3 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 439 10 2 6 5.4 CC(C)(C)CC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4211120 171009 0 None 9 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP3 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 EP3 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 439 10 2 6 5.4 CC(C)(C)CC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
67082748 171142 0 None -9 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP3 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 EP3 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 451 10 2 6 5.0 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCC(F)(F)F 10.1016/j.bmc.2017.11.035
CHEMBL4212770 171142 0 None -9 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP3 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 EP3 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 451 10 2 6 5.0 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCC(F)(F)F 10.1016/j.bmc.2017.11.035
69753740 147000 0 None 1 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 9 3 5 2.8 O=C(O)CCC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.6b00415
CHEMBL3805134 147000 0 None 1 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 9 3 5 2.8 O=C(O)CCC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.6b00415
57395059 76249 0 None -6025 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL1933725 76249 0 None -6025 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1021/acsmedchemlett.5b00455
54013831 153238 0 None -1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3922151 153238 0 None -1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
11955179 153260 0 None -5 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 450 12 3 3 6.2 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
CHEMBL3922332 153260 0 None -5 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 450 12 3 3 6.2 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
145966519 171178 0 None -15 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP3 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 EP3 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
CHEMBL4213312 171178 0 None -15 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP3 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 EP3 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
11955384 154316 0 None -33 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 360 8 2 3 4.4 CC(C)(C)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3930718 154316 0 None -33 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 360 8 2 3 4.4 CC(C)(C)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
1940 8444 41 None -933 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O 10.1021/acsmedchemlett.6b00415
3417 8444 41 None -933 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O 10.1021/acsmedchemlett.6b00415
5311100 8444 41 None -933 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O 10.1021/acsmedchemlett.6b00415
CHEMBL1201379 8444 41 None -933 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O 10.1021/acsmedchemlett.6b00415
DB11519 8444 41 None -933 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O 10.1021/acsmedchemlett.6b00415
66858036 170670 0 None 93 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP3 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 EP3 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 468 10 2 7 4.8 C[C@@H]1OC(=O)N(CCSc2nc(C(=O)O)cs2)[C@H]1/C=C/CC(C)(O)CC1CCCCC1 10.1016/j.bmc.2017.11.035
CHEMBL4207054 170670 0 None 93 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP3 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 EP3 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 468 10 2 7 4.8 C[C@@H]1OC(=O)N(CCSc2nc(C(=O)O)cs2)[C@H]1/C=C/CC(C)(O)CC1CCCCC1 10.1016/j.bmc.2017.11.035
126495491 147003 0 None -28 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis
ChEMBL 429 8 2 6 4.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805169 147003 0 None -28 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis
ChEMBL 429 8 2 6 4.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
92135977 159675 0 None -18620 4 Human 5.4 pEC50 = 5.4 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
CHEMBL3974652 159675 0 None -18620 4 Human 5.4 pEC50 = 5.4 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
59465599 153339 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 414 12 2 3 6.2 CCCC1(C(O)c2cccc([C@H]3CCC(=O)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
CHEMBL3922856 153339 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 414 12 2 3 6.2 CCCC1(C(O)c2cccc([C@H]3CCC(=O)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
68747479 158900 0 None 7 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 404 9 3 5 3.0 O=C(O)CCC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
CHEMBL3967855 158900 0 None 7 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 404 9 3 5 3.0 O=C(O)CCC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
6443852 160627 5 None 1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 9 3 5 2.8 O=C(O)CCC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.6b00415
CHEMBL3982726 160627 5 None 1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 9 3 5 2.8 O=C(O)CCC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.6b00415
57564500 157989 0 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959926 157989 0 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
11955178 160566 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 448 11 3 3 6.0 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
CHEMBL3982222 160566 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 448 11 3 3 6.0 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
118517483 151049 0 None -4265 3 Human 5.3 pEC50 = 5.3 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
CHEMBL3904946 151049 0 None -4265 3 Human 5.3 pEC50 = 5.3 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
11855865 160056 0 None -35 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A 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 160056 0 None -35 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A 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
56839342 155786 0 None -4 7 Human 7.3 pEC50 = 7.3 Functional
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 155786 0 None -4 7 Human 7.3 pEC50 = 7.3 Functional
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
68747472 154562 0 None -7 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 402 9 3 5 3.0 O=C(O)CCCC1=CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
CHEMBL3932636 154562 0 None -7 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 402 9 3 5 3.0 O=C(O)CCCC1=CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
134149776 155282 0 None -43 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 8 3 5 2.6 O=C(O)CC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
CHEMBL3938300 155282 0 None -43 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 8 3 5 2.6 O=C(O)CC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
1894 7744 41 None -331 5 Human 5.3 pEC50 = 5.3 Functional
Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3(% of control ligand, sulprostone=75%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3(% of control ligand, sulprostone=75%)
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1016/s0960-894x(00)00273-0
5311053 7744 41 None -331 5 Human 5.3 pEC50 = 5.3 Functional
Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3(% of control ligand, sulprostone=75%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3(% of control ligand, sulprostone=75%)
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1016/s0960-894x(00)00273-0
CHEMBL37853 7744 41 None -331 5 Human 5.3 pEC50 = 5.3 Functional
Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3(% of control ligand, sulprostone=75%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3(% of control ligand, sulprostone=75%)
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1016/s0960-894x(00)00273-0
DB11507 7744 41 None -331 5 Human 5.3 pEC50 = 5.3 Functional
Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3(% of control ligand, sulprostone=75%)Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3(% of control ligand, sulprostone=75%)
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1016/s0960-894x(00)00273-0
134138103 154658 0 None -12 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 418 10 3 5 3.4 O=C(O)CCCC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
CHEMBL3933326 154658 0 None -12 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 418 10 3 5 3.4 O=C(O)CCCC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
59465581 150890 0 None -22 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3903611 150890 0 None -22 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
59465571 153063 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3920796 153063 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
126495398 146989 0 None -575 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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 146989 0 None -575 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 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
118517489 150469 0 None -3162 3 Human 5.2 pEC50 = 5.2 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
CHEMBL3900245 150469 0 None -3162 3 Human 5.2 pEC50 = 5.2 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
134144861 157460 0 None -7 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 430 11 3 5 3.7 O=C(O)CCCCCC1=CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
CHEMBL3955821 157460 0 None -7 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 430 11 3 5 3.7 O=C(O)CCCCCC1=CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
118517453 158674 0 None -134 2 Human 7.2 pEC50 = 7.2 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 434 8 2 4 5.3 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc3ccsc3c2)cc1 nan
CHEMBL3965850 158674 0 None -134 2 Human 7.2 pEC50 = 7.2 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 434 8 2 4 5.3 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc3ccsc3c2)cc1 nan
16725337 156380 0 None -4 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 156380 0 None -4 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
16725337 156380 0 None -4 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 156380 0 None -4 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855865 160056 0 None -35 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM 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 160056 0 None -35 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP3A receptor expressed in HEK293-EBNA cells co-expressing Gqi5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM 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
127052615 147048 0 None -1995 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis
ChEMBL 401 6 2 6 3.7 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805693 147048 0 None -1995 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysisAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis
ChEMBL 401 6 2 6 3.7 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
66857975 171267 0 None 10 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human EP3 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 EP3 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 454 10 2 7 4.4 CC(O)(C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1)CC1CCCCC1 10.1016/j.bmc.2017.11.035
CHEMBL4214346 171267 0 None 10 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human EP3 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 EP3 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 454 10 2 7 4.4 CC(O)(C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1)CC1CCCCC1 10.1016/j.bmc.2017.11.035
56649302 159445 0 None -2 6 Human 7.1 pEC50 = 7.1 Functional
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 159445 0 None -2 6 Human 7.1 pEC50 = 7.1 Functional
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
1959 7446 41 None -1737 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 388 11 4 4 3.1 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 10.1021/acsmedchemlett.6b00415
5283081 7446 41 None -1737 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 388 11 4 4 3.1 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 10.1021/acsmedchemlett.6b00415
CHEMBL3914661 7446 41 None -1737 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 388 11 4 4 3.1 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 10.1021/acsmedchemlett.6b00415
134157766 160829 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 8 3 5 2.6 O=C(O)CC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
CHEMBL3984438 160829 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay
ChEMBL 390 8 3 5 2.6 O=C(O)CC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 10.1021/acsmedchemlett.6b00415
132836 66469 23 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL1722929 66469 23 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP3A receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
118517485 149528 0 None -346 4 Human 6.0 pEC50 = 6.0 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
CHEMBL3892492 149528 0 None -346 4 Human 6.0 pEC50 = 6.0 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
118517488 160490 0 None -4073 3 Human 5.0 pEC50 = 5 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
CHEMBL3981554 160490 0 None -4073 3 Human 5.0 pEC50 = 5 Functional
FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.FLIPR Assay: Calciium Signal Studies of the Flipr. Cells were seeded at a density of 5×104 cells per well in Biocoati® Poly-D-lysine-coated black-wall, clear-bottom 96-well plates (Becton-Dickinson) and allowed to attach overnight in an incubator at 37° C. Cells were then washed two times with HBSS-HEPES buffer (Hanks Balanced Salt Solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using a Denley Cellwash plate washer (Labsystems). After 45 minutes of dye-loading in the dark, using the calcium-sensitive dye Fluo-4 AM at a final concentration of 2 μM, plates were washed four times with HBSS-HEPES buffer to remove excess dye leaving 100 μl in each well. Plates were re-equilibrated to 37° C. for a few minutes. Cells were excited with an Argon laser at 488 nm, and emission was measured through a 510-570 nm bandwidth emission filter (FLIPR, Molecular Devices, Sunnyvale, Calif.). Drug solution was added in a 50 μl volume to each well to give the desired final concentration.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
25181432 198425 0 None 20 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human EP3 receptor assessed as cAMP production by cell-based assayAntagonist activity at human EP3 receptor assessed as cAMP production by cell-based assay
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL519598 198425 0 None 20 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human EP3 receptor assessed as cAMP production by cell-based assayAntagonist activity at human EP3 receptor assessed as cAMP production by cell-based assay
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
23017414 15030 0 None - 1 Mouse 9.4 pIC50 = 9.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 602 12 1 6 6.2 O=C(CCc1ccc(COc2cccnc2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1092432 15030 0 None - 1 Mouse 9.4 pIC50 = 9.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 602 12 1 6 6.2 O=C(CCc1ccc(COc2cccnc2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
25181438 190634 0 None -1 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human EP3 receptor assessed as cAMP production by cell-based assayAntagonist activity at human EP3 receptor assessed as cAMP production by cell-based assay
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480809 190634 0 None -1 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human EP3 receptor assessed as cAMP production by cell-based assayAntagonist activity at human EP3 receptor assessed as cAMP production by cell-based assay
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL5078847 221369 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
23017788 14906 0 None - 1 Mouse 8.9 pIC50 = 8.9 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 575 11 1 6 5.4 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091741 14906 0 None - 1 Mouse 8.9 pIC50 = 8.9 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 575 11 1 6 5.4 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
46886451 14908 0 None - 1 Mouse 8.9 pIC50 = 8.9 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 576 11 2 7 4.9 O=C(CCc1ccc(Cn2cccn2)cc1ONCc1cccc2ccccc12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091743 14908 0 None - 1 Mouse 8.9 pIC50 = 8.9 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 576 11 2 7 4.9 O=C(CCc1ccc(Cn2cccn2)cc1ONCc1cccc2ccccc12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
137478210 192843 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 380 5 2 2 4.6 CC(C)NC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
CHEMBL4871125 192843 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 380 5 2 2 4.6 CC(C)NC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
11620429 15289 0 None - 1 Mouse 8.8 pIC50 = 8.8 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094161 15289 0 None - 1 Mouse 8.8 pIC50 = 8.8 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
44571243 196635 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 592 6 1 5 6.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL516765 196635 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 592 6 1 5 6.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
11562422 15367 0 None - 1 Mouse 8.8 pIC50 = 8.8 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 501 11 2 3 7.0 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cc(C)ccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094813 15367 0 None - 1 Mouse 8.8 pIC50 = 8.8 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 501 11 2 3 7.0 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cc(C)ccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
137487344 192019 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 392 5 2 2 4.6 CC(C)[C@H](C[C@H]1CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4858203 192019 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 392 5 2 2 4.6 CC(C)[C@H](C[C@H]1CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
46887058 15286 0 None - 1 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(Cl)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094156 15286 0 None - 1 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(Cl)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
46887059 15287 2 None - 1 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 487 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094157 15287 2 None - 1 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 487 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
137487348 189119 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 406 4 2 4 4.2 CC(C)[C@H](/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4784483 189119 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 406 4 2 4 4.2 CC(C)[C@H](/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137477995 192468 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 393 5 2 4 5.6 CC(C)C(Nc1nccs1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4865321 192468 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 393 5 2 4 5.6 CC(C)C(Nc1nccs1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23016900 14903 0 None - 1 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 587 11 1 6 6.1 Cc1ccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)cc1Cl 10.1016/j.bmcl.2010.02.034
CHEMBL1091738 14903 0 None - 1 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 587 11 1 6 6.1 Cc1ccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)cc1Cl 10.1016/j.bmcl.2010.02.034
23017556 207466 0 None - 1 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599836 207466 0 None - 1 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
137477872 186978 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 419 4 2 3 4.1 CC(C)C(/C=C1/C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4749557 186978 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 419 4 2 3 4.1 CC(C)C(/C=C1/C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137477920 192643 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 406 5 1 2 5.1 CC(C)C(CN1CCCCC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4867987 192643 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 406 5 1 2 5.1 CC(C)C(CN1CCCCC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL5086191 221792 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
23017690 207263 0 None - 1 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 489 12 2 4 6.1 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1C 10.1016/j.bmc.2009.12.068
CHEMBL598613 207263 0 None - 1 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 489 12 2 4 6.1 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1C 10.1016/j.bmc.2009.12.068
10368531 15403 0 None - 1 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 495 10 2 3 6.9 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095117 15403 0 None - 1 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 495 10 2 3 6.9 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
137477697 187264 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 410 4 2 4 4.4 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1SC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4753054 187264 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 410 4 2 4 4.4 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1SC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
23017402 15234 0 None - 1 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 560 11 1 8 4.9 Cc1csc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)n1 10.1016/j.bmcl.2010.02.034
CHEMBL1093819 15234 0 None - 1 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 560 11 1 8 4.9 Cc1csc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)n1 10.1016/j.bmcl.2010.02.034
23017322 207012 0 None - 1 Mouse 6.0 pIC50 = 6.0 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 459 12 2 3 5.7 CC(C)CC(Cc1ccccc1)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.11.023
CHEMBL596902 207012 0 None - 1 Mouse 6.0 pIC50 = 6.0 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 459 12 2 3 5.7 CC(C)CC(Cc1ccccc1)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.11.023
CHEMBL5081848 221551 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None COc1ccccc1S(=O)(=O)NC(=O)NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21 10.1021/acsmedchemlett.1c00594
44626788 203688 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP level after 10 mins by EIAAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP level after 10 mins by EIA
ChEMBL 422 6 1 5 4.3 O=C(/C=C/c1cccc2ccn(Cc3ccccc3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL566211 203688 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP level after 10 mins by EIAAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP level after 10 mins by EIA
ChEMBL 422 6 1 5 4.3 O=C(/C=C/c1cccc2ccn(Cc3ccccc3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
137478225 192631 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 484 13 2 5 3.9 COCCOCCOCCNC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
CHEMBL4867692 192631 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 484 13 2 5 3.9 COCCOCCOCCNC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
CHEMBL5074870 221116 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1ccc(Cl)cc1 10.1021/acsmedchemlett.1c00594
137477756 191417 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 408 6 1 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nncn4C)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL4849526 191417 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 408 6 1 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nncn4C)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
137477893 192435 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 471 6 1 4 3.7 CC(C)C(CN1CCN(S(C)(=O)=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4864757 192435 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 471 6 1 4 3.7 CC(C)C(CN1CCN(S(C)(=O)=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017180 207889 0 None - 1 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSA
ChEMBL 413 8 2 4 4.0 O=C(O)CCc1ccc(Cn2cccn2)cc1C(=O)NCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
CHEMBL603059 207889 0 None - 1 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSA
ChEMBL 413 8 2 4 4.0 O=C(O)CCc1ccc(Cn2cccn2)cc1C(=O)NCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
44520992 206759 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 396 6 1 4 4.1 O=C(O)C#Cc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595159 206759 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 396 6 1 4 4.1 O=C(O)C#Cc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
137487367 192078 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 428 4 1 3 4.5 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCCCS1(=O)=O 10.1016/j.bmcl.2021.128172
CHEMBL4859300 192078 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 428 4 1 3 4.5 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCCCS1(=O)=O 10.1016/j.bmcl.2021.128172
CHEMBL5077079 221255 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00594
23017429 208038 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL603881 208038 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017660 207842 0 None - 1 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1F 10.1016/j.bmc.2009.12.068
CHEMBL602688 207842 0 None - 1 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1F 10.1016/j.bmc.2009.12.068
137477597 189501 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 392 3 2 4 4.0 CC(C)/C(=C1/OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4789676 189501 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 392 3 2 4 4.0 CC(C)/C(=C1/OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137477657 191265 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 377 5 2 4 3.8 CC(C)C(Cc1nnn[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4847115 191265 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 377 5 2 4 3.8 CC(C)C(Cc1nnn[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137477638 192590 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 394 5 1 3 4.4 CC(C)C(CN1CCOCC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4867086 192590 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 394 5 1 3 4.4 CC(C)C(CN1CCOCC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017347 14997 0 None - 1 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 539 11 1 6 5.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.02.034
CHEMBL1092266 14997 0 None - 1 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 539 11 1 6 5.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.02.034
10273914 206451 0 None - 1 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(COc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL593041 206451 0 None - 1 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(COc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
23017739 206316 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 465 10 2 3 5.8 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL592213 206316 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 465 10 2 3 5.8 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.11.023
137487263 187225 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 408 5 2 4 4.1 CC(C)[C@H](C[C@H]1OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4752588 187225 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 408 5 2 4 4.1 CC(C)[C@H](C[C@H]1OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137478217 192668 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 394 6 2 2 5.0 CC(C)NC(=O)CC(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
CHEMBL4868434 192668 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 394 6 2 2 5.0 CC(C)NC(=O)CC(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
23016850 207047 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597146 207047 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017669 207142 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 531 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.12.068
CHEMBL597785 207142 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 531 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.12.068
23017606 15237 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 540 11 1 7 4.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1cccnc1 10.1016/j.bmcl.2010.02.034
CHEMBL1093841 15237 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 540 11 1 7 4.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1cccnc1 10.1016/j.bmcl.2010.02.034
23017746 206628 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 414 8 1 3 6.2 O=C(O)/C=C/c1ccc(Cc2cccs2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL594365 206628 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 414 8 1 3 6.2 O=C(O)/C=C/c1ccc(Cc2cccs2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
23016719 207999 0 None - 1 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(OCc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL603625 207999 0 None - 1 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(OCc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
164616453 192084 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 337 4 3 3 3.1 CC(C)C(O)(C(=O)O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4859363 192084 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 337 4 3 3 3.1 CC(C)C(O)(C(=O)O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL5087384 221871 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00594
23017438 206992 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(C#N)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL596738 206992 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(C#N)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017153 207233 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 473 11 2 3 6.4 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1C 10.1016/j.bmc.2009.12.068
CHEMBL598410 207233 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 473 11 2 3 6.4 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1C 10.1016/j.bmc.2009.12.068
23017221 207372 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 487 11 2 3 6.7 Cc1ccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)cc1 10.1016/j.bmc.2009.12.068
CHEMBL599204 207372 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 487 11 2 3 6.7 Cc1ccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)cc1 10.1016/j.bmc.2009.12.068
CHEMBL5083509 221647 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None COc1ccc(Cl)cc1S(=O)(=O)NC(=O)NC/C(F)=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21 10.1021/acsmedchemlett.1c00594
127047602 146483 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 299 3 1 6 2.6 Cn1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3798145 146483 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 299 3 1 6 2.6 Cn1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
137487338 189985 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 424 5 2 4 4.8 CC(C)[C@@H](C[C@H]1SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4795879 189985 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 424 5 2 4 4.8 CC(C)[C@@H](C[C@H]1SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137487318 191352 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 376 5 2 3 4.4 CC(C)C(Cc1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4848523 191352 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 376 5 2 3 4.4 CC(C)C(Cc1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017080 207021 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 473 11 2 3 6.4 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL596956 207021 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 473 11 2 3 6.4 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL5083128 221622 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None COc1ccc(S(=O)(=O)NC(=O)NC/C(F)=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)cc1Cl 10.1021/acsmedchemlett.1c00594
23016838 14907 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 564 11 1 7 5.0 N#Cc1cccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091742 14907 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 564 11 1 7 5.0 N#Cc1cccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2010.02.034
23017295 208193 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 477 11 2 3 6.2 Cc1cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)ccc1F 10.1016/j.bmc.2009.12.068
CHEMBL604708 208193 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 477 11 2 3 6.2 Cc1cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)ccc1F 10.1016/j.bmc.2009.12.068
127047729 146434 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 347 4 1 6 3.7 CCn1ncc2c(Cl)cc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3797824 146434 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 347 4 1 6 3.7 CCn1ncc2c(Cl)cc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
162651616 187065 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 434 6 2 6 3.9 CCn1nc(C)c2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
CHEMBL4750762 187065 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 434 6 2 6 3.9 CCn1nc(C)c2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
137477572 192838 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 377 5 3 4 4.3 CC(C)C(Nc1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4871021 192838 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 377 5 3 4 4.3 CC(C)C(Nc1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
5311234 121917 25 None -93 4 Human 6.7 pIC50 = 6.7 Functional
Functional activity in RAT-1 cells, transiently transfected with human prostaglandin EP3 receptorFunctional activity in RAT-1 cells, transiently transfected with human prostaglandin EP3 receptor
ChEMBL 390 11 4 5 2.5 O=C(O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)COc1ccccc1 10.1021/jm010264b
CHEMBL334398 121917 25 None -93 4 Human 6.7 pIC50 = 6.7 Functional
Functional activity in RAT-1 cells, transiently transfected with human prostaglandin EP3 receptorFunctional activity in RAT-1 cells, transiently transfected with human prostaglandin EP3 receptor
ChEMBL 390 11 4 5 2.5 O=C(O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)COc1ccccc1 10.1021/jm010264b
23017223 207300 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 481 11 2 3 6.1 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cc(F)cc(F)c1 10.1016/j.bmc.2009.12.068
CHEMBL598813 207300 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 481 11 2 3 6.1 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cc(F)cc(F)c1 10.1016/j.bmc.2009.12.068
23017116 208053 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 503 11 2 5 5.6 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc2c(c1)OCCO2 10.1016/j.bmc.2009.12.068
CHEMBL603969 208053 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 503 11 2 5 5.6 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc2c(c1)OCCO2 10.1016/j.bmc.2009.12.068
46887126 15473 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@H](CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095768 15473 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@H](CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
137487355 189712 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 440 4 2 4 4.6 O=C1NC(=O)/C(=C/C(c2ccccc2)c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4792611 189712 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 440 4 2 4 4.6 O=C1NC(=O)/C(=C/C(c2ccccc2)c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)O1 10.1021/acsmedchemlett.0c00667
23017463 15198 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 540 11 1 7 4.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccn1 10.1016/j.bmcl.2010.02.034
CHEMBL1093537 15198 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 540 11 1 7 4.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccn1 10.1016/j.bmcl.2010.02.034
23016807 207517 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 475 12 2 4 5.8 COc1ccccc1C(CC(C)C)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.12.068
CHEMBL600209 207517 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 475 12 2 4 5.8 COc1ccccc1C(CC(C)C)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.12.068
137478241 192900 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 320 4 2 2 3.4 CC(C)C(C(N)=O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4871834 192900 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 320 4 2 2 3.4 CC(C)C(C(N)=O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
9982348 15368 0 None - 1 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 474 11 2 4 5.8 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccnc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094814 15368 0 None - 1 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 474 11 2 4 5.8 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccnc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
10413147 15852 0 None - 1 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 486 10 3 3 7.2 Cc1cc(C)cc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1099047 15852 0 None - 1 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 486 10 3 3 7.2 Cc1cc(C)cc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
23017224 207013 0 None - 1 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 495 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL596903 207013 0 None - 1 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 495 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
137487375 192549 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 499 6 2 4 3.6 CC(C)C(C(=O)NC1CCN(S(C)(=O)=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4866485 192549 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 499 6 2 4 3.6 CC(C)C(C(=O)NC1CCN(S(C)(=O)=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
46887091 15472 0 None - 1 Mouse 8.6 pIC50 = 8.6 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095767 15472 0 None - 1 Mouse 8.6 pIC50 = 8.6 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23017462 208485 0 None - 1 Mouse 8.6 pIC50 = 8.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 502 11 2 4 6.1 Cc1cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)ccc1F 10.1016/j.bmc.2009.12.068
CHEMBL606393 208485 0 None - 1 Mouse 8.6 pIC50 = 8.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 502 11 2 4 6.1 Cc1cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)ccc1F 10.1016/j.bmc.2009.12.068
46887057 15321 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3Cl)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094464 15321 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3Cl)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
10028427 15398 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 487 10 2 3 7.2 Cc1cc(C)cc(Oc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095064 15398 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 487 10 2 3 7.2 Cc1cc(C)cc(Oc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL5072303 221057 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(-c3ccc(C(F)(F)F)cc3)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
23016797 207616 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)cc1 10.1016/j.bmc.2009.12.068
CHEMBL601029 207616 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)cc1 10.1016/j.bmc.2009.12.068
162656122 187692 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 454 5 2 4 4.8 O=C1NC(=O)/C(=C/C(Cc2ccccc2)c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4757838 187692 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 454 5 2 4 4.8 O=C1NC(=O)/C(=C/C(Cc2ccccc2)c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)O1 10.1021/acsmedchemlett.0c00667
137477592 191482 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 411 6 2 5 3.6 CCN1CCOc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL4850242 191482 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 411 6 2 5 3.6 CCN1CCOc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
137477812 189611 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 406 4 2 4 4.2 CC(C)C(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4791261 189611 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 406 4 2 4 4.2 CC(C)C(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137477709 193012 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 362 4 2 3 4.2 CC(C)C(c1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4873446 193012 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 362 4 2 3 4.2 CC(C)C(c1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017359 207974 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 475 12 2 4 5.8 COc1cccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL603497 207974 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 475 12 2 4 5.8 COc1cccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
10157813 208395 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSA
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
CHEMBL605833 208395 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSA
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
10157813 208395 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL605833 208395 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
162657359 187756 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 437 6 2 6 3.5 CCN1CCOc2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
CHEMBL4758607 187756 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 437 6 2 6 3.5 CCN1CCOc2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
23016909 206301 0 None - 1 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 403 9 2 3 4.8 CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL592061 206301 0 None - 1 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 403 9 2 3 4.8 CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
141730897 182895 0 None -72 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP3 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assayAntagonist activity at human EP3 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
ChEMBL 456 6 2 5 3.9 CC#Cc1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4591792 182895 0 None -72 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP3 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assayAntagonist activity at human EP3 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
ChEMBL 456 6 2 5 3.9 CC#Cc1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
137477918 188295 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 434 6 2 4 5.0 CCC(CC)C(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4765017 188295 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 434 6 2 4 5.0 CCC(CC)C(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137477849 193065 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 382 6 3 3 3.2 CC(C)C(C(=O)NCCO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4874159 193065 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 382 6 3 3 3.2 CC(C)C(C(=O)NCCO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017343 207296 0 None - 1 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 459 11 2 3 6.1 Cc1ccccc1C(CC(C)C)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.12.068
CHEMBL598795 207296 0 None - 1 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 459 11 2 3 6.1 Cc1ccccc1C(CC(C)C)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.12.068
137477997 192627 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 415 5 2 3 5.1 CC(C)C(C(=O)Nc1ccncc1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4867652 192627 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 415 5 2 3 5.1 CC(C)C(C(=O)Nc1ccncc1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017168 14819 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 552 11 1 5 5.2 CN(C)Cc1ccc(CCC(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c(OCCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1090938 14819 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 552 11 1 5 5.2 CN(C)Cc1ccc(CCC(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c(OCCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2010.02.034
23017332 15029 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 626 12 1 6 6.6 N#Cc1cccc(OCc2ccc(CCC(=O)NS(=O)(=O)c3ccc(F)c(F)c3)c(OCCc3ccc4ccccc4c3)c2)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1092431 15029 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 626 12 1 6 6.6 N#Cc1cccc(OCc2ccc(CCC(=O)NS(=O)(=O)c3ccc(F)c(F)c3)c(OCCc3ccc4ccccc4c3)c2)c1 10.1016/j.bmcl.2010.02.034
23016858 207054 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 505 13 2 5 5.8 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1OC 10.1016/j.bmc.2009.12.068
CHEMBL597160 207054 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 505 13 2 5 5.8 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1OC 10.1016/j.bmc.2009.12.068
23017035 206213 0 None - 1 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 431 11 2 3 5.6 CCCC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL591299 206213 0 None - 1 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 431 11 2 3 5.6 CCCC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
23017331 207143 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 497 11 2 3 6.6 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2009.12.068
CHEMBL597786 207143 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 497 11 2 3 6.6 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2009.12.068
23017142 208572 0 None - 1 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 443 11 2 3 5.6 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NC(CC1CC1)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL606857 208572 0 None - 1 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 443 11 2 3 5.6 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NC(CC1CC1)c1ccccc1 10.1016/j.bmc.2009.11.023
10272453 208000 0 None - 1 Mouse 5.6 pIC50 = 5.6 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 402 9 1 5 4.2 O=C(O)COc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL603633 208000 0 None - 1 Mouse 5.6 pIC50 = 5.6 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 402 9 1 5 4.2 O=C(O)COc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
137487264 186235 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 408 5 2 4 4.1 CC(C)[C@H](C[C@@H]1OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4740657 186235 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 408 5 2 4 4.1 CC(C)[C@H](C[C@@H]1OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137477983 189722 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 422 4 2 4 4.9 CC(C)C(/C=C1\SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4792728 189722 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 422 4 2 4 4.9 CC(C)C(/C=C1\SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL5091517 222091 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None COc1ccc(-n2ncc3c2/C(=C/CNC(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)CCC3)cn1 10.1021/acsmedchemlett.1c00594
23017687 206315 0 None - 1 Mouse 5.6 pIC50 = 5.6 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 461 11 3 4 4.9 CC(C)(O)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL592212 206315 0 None - 1 Mouse 5.6 pIC50 = 5.6 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 461 11 3 4 4.9 CC(C)(O)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
137477851 193104 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 379 4 2 2 4.1 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCNC1=O 10.1016/j.bmcl.2021.128172
CHEMBL4874814 193104 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 379 4 2 2 4.1 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCNC1=O 10.1016/j.bmcl.2021.128172
CHEMBL5087700 221891 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cccs1 10.1021/acsmedchemlett.1c00594
127047605 146627 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 327 4 1 6 3.6 CC(C)n1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3799153 146627 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 327 4 1 6 3.6 CC(C)n1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
137477590 191555 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 394 6 2 5 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL4851298 191555 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 394 6 2 5 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL5092711 222162 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None COc1ccc(S(=O)(=O)NC(=O)NC/C=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)cc1 10.1021/acsmedchemlett.1c00594
44250281 203286 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 434 4 1 6 5.0 CCN1CCOc2ccc(C(=O)Nc3nnc(-c4c(Cl)cccc4Cl)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL563480 203286 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 434 4 1 6 5.0 CCN1CCOc2ccc(C(=O)Nc3nnc(-c4c(Cl)cccc4Cl)s3)cc21 10.1016/j.bmcl.2016.04.009
137477985 191211 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 422 5 2 3 4.4 CC(C)C(C(=O)NC1CCOCC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4846309 191211 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 422 5 2 3 4.4 CC(C)C(C(=O)NC1CCOCC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
44570829 190736 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)cc(Cl)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL481614 190736 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)cc(Cl)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
23017339 207167 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 500 12 2 5 5.7 COc1cccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597974 207167 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 500 12 2 5 5.7 COc1cccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017699 207406 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 503 12 2 4 6.4 COc1cccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2009.12.068
CHEMBL599405 207406 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 503 12 2 4 6.4 COc1cccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2009.12.068
46887092 15288 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094160 15288 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
25195248 189714 0 None 741 4 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 540 6 1 4 4.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479263 189714 0 None 741 4 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 540 6 1 4 4.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44571355 198096 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL519137 198096 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
23016978 207374 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(F)c3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599213 207374 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(F)c3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017423 207080 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 530 13 2 6 5.7 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)cc1OC 10.1016/j.bmc.2009.12.068
CHEMBL597367 207080 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 530 13 2 6 5.7 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)cc1OC 10.1016/j.bmc.2009.12.068
23017255 14818 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 554 12 1 7 4.2 CN(CCOc1cc(Cn2cccn2)ccc1CCC(=O)NS(=O)(=O)c1ccc(F)c(F)c1)c1ccccc1 10.1016/j.bmcl.2010.02.034
CHEMBL1090937 14818 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 554 12 1 7 4.2 CN(CCOc1cc(Cn2cccn2)ccc1CCC(=O)NS(=O)(=O)c1ccc(F)c(F)c1)c1ccccc1 10.1016/j.bmcl.2010.02.034
23017484 207456 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(Cl)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599810 207456 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(Cl)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
10368064 15399 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 484 10 2 4 6.5 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095065 15399 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 484 10 2 4 6.5 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23016737 206993 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 487 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL596745 206993 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 487 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017557 207458 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599812 207458 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL5080528 221469 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CS(=O)(=O)c1ccc(-n2ncc3c2/C(=C/CNC(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)CCC3)cc1 10.1021/acsmedchemlett.1c00594
23016744 207116 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(Cl)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597552 207116 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(Cl)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017180 207889 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSA
ChEMBL 413 8 2 4 4.0 O=C(O)CCc1ccc(Cn2cccn2)cc1C(=O)NCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
CHEMBL603059 207889 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSA
ChEMBL 413 8 2 4 4.0 O=C(O)CCc1ccc(Cn2cccn2)cc1C(=O)NCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
10199656 206944 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 378 10 1 5 3.9 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCCOc1ccccc1 10.1016/j.bmc.2009.08.007
CHEMBL596499 206944 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 378 10 1 5 3.9 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCCOc1ccccc1 10.1016/j.bmc.2009.08.007
137477780 190064 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 407 5 3 3 3.7 CC(C)C(CC1NC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4796825 190064 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 407 5 3 3 3.7 CC(C)C(CC1NC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
44520990 206632 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 410 6 2 4 5.3 Cc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
CHEMBL594423 206632 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 410 6 2 4 5.3 Cc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
23017621 207232 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 513 11 2 3 6.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.12.068
CHEMBL598409 207232 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 513 11 2 3 6.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.12.068
137477755 187515 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 407 4 2 3 3.6 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1C(=O)NC(=O)N1C 10.1021/acsmedchemlett.0c00667
CHEMBL4755933 187515 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 407 4 2 3 3.6 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1C(=O)NC(=O)N1C 10.1021/acsmedchemlett.0c00667
137478002 190243 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 393 4 3 3 3.3 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1NC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4799069 190243 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 393 4 3 3 3.3 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1NC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
23017216 205938 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSA
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL589411 205938 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSA
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
137477703 187073 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 404 4 2 4 4.0 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4750905 187073 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 404 4 2 4 4.0 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CC2)O1 10.1021/acsmedchemlett.0c00667
137477676 188682 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 438 6 2 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
CHEMBL4779295 188682 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 438 6 2 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
137477566 192451 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 361 4 2 2 4.8 CC(C)C(c1ncc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4864985 192451 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 361 4 2 2 4.8 CC(C)C(c1ncc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
10200281 206605 1 None - 1 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 388 8 1 5 4.4 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCc1cc2ccccc2o1 10.1016/j.bmc.2009.08.007
CHEMBL594210 206605 1 None - 1 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 388 8 1 5 4.4 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCc1cc2ccccc2o1 10.1016/j.bmc.2009.08.007
CHEMBL5089190 221976 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cccc(Cl)c1 10.1021/acsmedchemlett.1c00594
137477794 191248 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 393 5 3 3 3.2 CC(C)C(C(=O)NC1CNC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4846915 191248 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 393 5 3 3 3.2 CC(C)C(C(=O)NC1CNC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017771 208429 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 479 11 2 3 6.5 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(Cl)c1 10.1016/j.bmc.2009.12.068
CHEMBL605991 208429 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 479 11 2 3 6.5 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(Cl)c1 10.1016/j.bmc.2009.12.068
162647817 186612 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 405 3 2 3 3.9 CC(C)/C(=C1\C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4745085 186612 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 405 3 2 3 3.9 CC(C)/C(=C1\C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137478291 191198 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 394 5 2 3 4.7 CCC(CC)(c1nnc[nH]1)c1ccc(-c2ccc3cc(F)cc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4846132 191198 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 394 5 2 3 4.7 CCC(CC)(c1nnc[nH]1)c1ccc(-c2ccc3cc(F)cc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
10271818 207926 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 392 11 1 5 4.3 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCCCOc1ccccc1 10.1016/j.bmc.2009.08.007
CHEMBL603227 207926 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 392 11 1 5 4.3 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCCCOc1ccccc1 10.1016/j.bmc.2009.08.007
164619977 192321 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 376 5 2 3 4.6 CCC(CC)(c1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4863000 192321 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 376 5 2 3 4.6 CCC(CC)(c1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137477766 192980 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 375 4 2 2 5.2 Cc1c[nH]c(C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C(C)C)n1 10.1016/j.bmcl.2021.128172
CHEMBL4872962 192980 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 375 4 2 2 5.2 Cc1c[nH]c(C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C(C)C)n1 10.1016/j.bmcl.2021.128172
137478179 188246 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 440 4 2 4 4.9 CC(C)C(/C=C1\OC(=O)NC1=O)c1cc(Cl)c(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4764526 188246 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 440 4 2 4 4.9 CC(C)C(/C=C1\OC(=O)NC1=O)c1cc(Cl)c(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
10157813 208395 0 None - 1 Mouse 5.4 pIC50 = 5.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSA
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
CHEMBL605833 208395 0 None - 1 Mouse 5.4 pIC50 = 5.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 2% BSA
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
127047604 146361 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 313 4 1 6 3.0 CCn1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3797362 146361 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 313 4 1 6 3.0 CCn1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
23017043 207297 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 459 11 2 3 6.1 Cc1cccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL598796 207297 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 459 11 2 3 6.1 Cc1cccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
137477714 192028 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 403 4 2 3 3.8 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCN/C1=N\C#N 10.1016/j.bmcl.2021.128172
CHEMBL4858376 192028 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 403 4 2 3 3.8 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCN/C1=N\C#N 10.1016/j.bmcl.2021.128172
137478196 187760 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 420 4 2 4 4.6 C/C(=C1/OC(=O)NC1=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1021/acsmedchemlett.0c00667
CHEMBL4758663 187760 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 420 4 2 4 4.6 C/C(=C1/OC(=O)NC1=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1021/acsmedchemlett.0c00667
137478269 192295 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 393 4 2 4 5.2 CC(C)C(c1cnc(N)s1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4862628 192295 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 393 4 2 4 5.2 CC(C)C(c1cnc(N)s1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017610 208453 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 513 11 2 3 6.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(C(F)(F)F)c1 10.1016/j.bmc.2009.12.068
CHEMBL606181 208453 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 513 11 2 3 6.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(C(F)(F)F)c1 10.1016/j.bmc.2009.12.068
46887177 15362 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 459 10 2 3 6.6 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094790 15362 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 459 10 2 3 6.6 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
46201043 207361 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 453 9 2 3 5.9 C[C@@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL599154 207361 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 453 9 2 3 5.9 C[C@@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL5080602 221474 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None Cc1nc(C)c(S(=O)(=O)NC(=O)NC/C=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)s1 10.1021/acsmedchemlett.1c00594
CHEMBL5092858 222171 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(-c3ccc(C(F)(F)F)cc3)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
23017762 207371 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 487 11 2 3 6.7 Cc1cccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2009.12.068
CHEMBL599203 207371 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 487 11 2 3 6.7 Cc1cccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2009.12.068
10345923 15474 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 501 11 2 3 7.0 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(C)cc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095769 15474 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 501 11 2 3 7.0 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(C)cc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
10480657 15578 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 488 11 2 4 6.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccnc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1096750 15578 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 488 11 2 4 6.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccnc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
44570668 190796 0 None 1698 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 572 6 1 4 5.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL482018 190796 0 None 1698 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 572 6 1 4 5.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
10413031 15722 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 483 10 3 4 6.5 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Nc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1098047 15722 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 483 10 3 4 6.5 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Nc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
137477747 191449 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 392 4 1 2 5.0 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCCCC1=O 10.1016/j.bmcl.2021.128172
CHEMBL4849811 191449 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 392 4 1 2 5.0 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCCCC1=O 10.1016/j.bmcl.2021.128172
23016874 207595 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(F)c1 10.1016/j.bmc.2009.12.068
CHEMBL600831 207595 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(F)c1 10.1016/j.bmc.2009.12.068
10136146 208003 0 None - 1 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 408 8 1 2 6.2 O=C(O)/C=C/c1ccc(Cc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL603653 208003 0 None - 1 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 408 8 1 2 6.2 O=C(O)/C=C/c1ccc(Cc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
137477876 191332 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 412 7 4 4 2.5 CC(C)C(C(=O)NC(CO)CO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4848264 191332 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 412 7 4 4 2.5 CC(C)C(C(=O)NC(CO)CO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137478100 192429 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 379 4 2 4 3.8 CC(C)C(c1noc(=O)[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4864589 192429 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 379 4 2 4 3.8 CC(C)C(c1noc(=O)[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017033 208455 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 493 12 2 4 5.9 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1F 10.1016/j.bmc.2009.12.068
CHEMBL606195 208455 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 493 12 2 4 5.9 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1F 10.1016/j.bmc.2009.12.068
137477568 191814 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 356 4 2 2 3.6 CC(C)C(F)(C(N)=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4855134 191814 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 356 4 2 2 3.6 CC(C)C(F)(C(N)=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137478289 192217 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 409 7 2 3 3.8 CC(C)C(C(=O)NCCN(C)C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4861530 192217 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 409 7 2 3 3.8 CC(C)C(C(=O)NCCN(C)C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
162662909 188740 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 438 5 2 4 4.7 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cc(F)cc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4780007 188740 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 438 5 2 4 4.7 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cc(F)cc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
44626787 203832 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP level after 10 mins by EIAAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP level after 10 mins by EIA
ChEMBL 472 6 1 5 5.4 O=C(/C=C/c1cccc2ccn(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL567274 203832 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP level after 10 mins by EIAAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP level after 10 mins by EIA
ChEMBL 472 6 1 5 5.4 O=C(/C=C/c1cccc2ccn(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
23017362 206757 0 None - 1 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 414 10 1 4 5.1 O=C(O)CCCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595157 206757 0 None - 1 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 414 10 1 4 5.1 O=C(O)CCCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
23016804 14967 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 594 11 1 6 5.0 O=C(CCc1ccc(CN2CCOCC2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1092097 14967 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 594 11 1 6 5.0 O=C(CCc1ccc(CN2CCOCC2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
23017440 207408 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 481 11 2 3 6.1 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)c(F)c1 10.1016/j.bmc.2009.12.068
CHEMBL599419 207408 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 481 11 2 3 6.1 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)c(F)c1 10.1016/j.bmc.2009.12.068
44520989 206543 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 396 6 2 4 5.0 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1ccccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
CHEMBL593764 206543 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 396 6 2 4 5.0 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1ccccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
CHEMBL5094127 222253 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NS(=O)(=O)c1cc(Cl)c(Cl)s1)OC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21 10.1021/acsmedchemlett.1c00594
44571289 190020 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 560 6 1 5 5.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479632 190020 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 560 6 1 5 5.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
23017697 207048 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597147 207048 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
10051189 15361 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 488 11 2 4 6.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(C)nc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094789 15361 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 488 11 2 4 6.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(C)nc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23017311 14905 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 591 11 1 6 5.9 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091740 14905 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 591 11 1 6 5.9 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2010.02.034
46887719 15316 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 473 11 2 3 6.4 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094419 15316 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 473 11 2 3 6.4 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
46887240 15526 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 472 10 3 3 6.9 Cc1cccc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1096382 15526 0 None - 1 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 472 10 3 3 6.9 Cc1cccc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
23016869 207465 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)c(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599835 207465 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)c(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
44571291 196935 0 None 1000 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 554 7 1 6 5.3 COc1cccc(CN2C(=O)CC3(C)CCCC(/C=C/C(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)=C23)c1 10.1016/j.bmcl.2008.12.027
CHEMBL517377 196935 0 None 1000 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP productionAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reversal of inhibition of forskolin-induced cAMP production
ChEMBL 554 7 1 6 5.3 COc1cccc(CN2C(=O)CC3(C)CCCC(/C=C/C(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)=C23)c1 10.1016/j.bmcl.2008.12.027
137477950 193153 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 470 5 2 4 3.8 CC(C)C(C(=O)NC1CCS(=O)(=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4875575 193153 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 470 5 2 4 3.8 CC(C)C(C(=O)NC1CCS(=O)(=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137477779 191951 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 389 4 2 2 5.5 Cc1nc(C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C(C)C)[nH]c1C 10.1016/j.bmcl.2021.128172
CHEMBL4857240 191951 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 389 4 2 2 5.5 Cc1nc(C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C(C)C)[nH]c1C 10.1016/j.bmcl.2021.128172
10294289 206950 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL596515 206950 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
137478051 192682 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 336 4 3 3 2.5 CC(C)C(O)(C(N)=O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4868701 192682 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 336 4 3 3 2.5 CC(C)C(O)(C(N)=O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23016842 15122 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 541 12 1 7 4.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCOc1ccccc1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1092976 15122 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 541 12 1 7 4.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCOc1ccccc1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
23017126 207327 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 459 11 2 3 6.1 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1 10.1016/j.bmc.2009.12.068
CHEMBL598995 207327 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 459 11 2 3 6.1 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1 10.1016/j.bmc.2009.12.068
23017561 207519 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 479 11 2 3 6.5 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(Cl)cc1 10.1016/j.bmc.2009.12.068
CHEMBL600219 207519 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 479 11 2 3 6.5 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(Cl)cc1 10.1016/j.bmc.2009.12.068
CHEMBL5086151 221791 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(Cc3ccc(C(F)(F)F)cc3)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
23016747 206212 0 None - 1 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 417 10 2 3 5.2 CCC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL591298 206212 0 None - 1 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 417 10 2 3 5.2 CCC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
23017180 207889 0 None - 1 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 413 8 2 4 4.0 O=C(O)CCc1ccc(Cn2cccn2)cc1C(=O)NCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
CHEMBL603059 207889 0 None - 1 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 413 8 2 4 4.0 O=C(O)CCc1ccc(Cn2cccn2)cc1C(=O)NCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
137478254 192976 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 352 5 2 2 3.9 CC(C)C(CC(N)=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4872930 192976 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 352 5 2 2 3.9 CC(C)C(CC(N)=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017081 207410 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 531 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(C(F)(F)F)c(F)c1 10.1016/j.bmc.2009.12.068
CHEMBL599420 207410 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 531 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(C(F)(F)F)c(F)c1 10.1016/j.bmc.2009.12.068
23017109 206853 0 None - 1 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 416 10 1 5 4.3 O=C(O)COCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595830 206853 0 None - 1 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 416 10 1 5 4.3 O=C(O)COCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
162654507 187443 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 390 3 2 4 3.5 O=C1NC(=O)/C(=C/C2(c3ccc(-c4ccc5cccc(F)c5c4)[nH]c3=O)CC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4755147 187443 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 390 3 2 4 3.5 O=C1NC(=O)/C(=C/C2(c3ccc(-c4ccc5cccc(F)c5c4)[nH]c3=O)CC2)O1 10.1021/acsmedchemlett.0c00667
137477903 189809 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 392 3 2 4 3.8 CC(C)(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4793929 189809 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 392 3 2 4 3.8 CC(C)(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
10157813 208395 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmcl.2010.02.034
CHEMBL605833 208395 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmcl.2010.02.034
10157813 208395 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
CHEMBL605833 208395 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.11.023
10295336 208225 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 415 8 1 3 4.7 O=C(O)/C=C/c1ccc(CN2CCCC2=O)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL604897 208225 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 415 8 1 3 4.7 O=C(O)/C=C/c1ccc(CN2CCCC2=O)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
23017297 15235 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 525 11 1 6 4.3 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccccc1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1093820 15235 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 525 11 1 6 4.3 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccccc1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
23017728 207841 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 475 12 2 4 5.8 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1 10.1016/j.bmc.2009.12.068
CHEMBL602687 207841 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 475 12 2 4 5.8 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1 10.1016/j.bmc.2009.12.068
23017225 208456 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3c(F)cccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL606197 208456 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3c(F)cccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL5084190 221679 3 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None Cc1cc(S(=O)(=O)NC(=O)NC/C(F)=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)sc1Cl 10.1021/acsmedchemlett.1c00594
CHEMBL5093140 222190 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(C3CCN(c4ccc(F)cc4)CC3)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
23017299 208426 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL605974 208426 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
137477971 191298 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 468 5 2 4 5.6 CC(C)C(C(=O)Nc1ccc2c(c1)ncn2C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4847629 191298 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 468 5 2 4 5.6 CC(C)C(C(=O)Nc1ccc2c(c1)ncn2C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017529 14909 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 610 12 1 8 4.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1cccc(N2CCOCC2)c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091744 14909 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 610 12 1 8 4.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1cccc(N2CCOCC2)c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
23017600 207298 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 484 11 2 4 6.0 Cc1cccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL598802 207298 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 484 11 2 4 6.0 Cc1cccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
46887056 15285 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094155 15285 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
46887210 15400 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 494 10 3 3 6.9 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Nc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095066 15400 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 494 10 3 3 6.9 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Nc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23016963 206514 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 476 8 2 6 5.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1cc(Cn3ccnc3)ccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
CHEMBL593526 206514 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 476 8 2 6 5.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1cc(Cn3ccnc3)ccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
162661390 188298 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 420 5 2 4 4.5 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4765027 188298 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 420 5 2 4 4.5 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
127048124 146367 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 331 4 1 6 3.2 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3797387 146367 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 331 4 1 6 3.2 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
137487291 187909 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 394 4 2 4 3.7 CC(C)[C@@H](c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)[C@@H]1OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4760599 187909 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 394 4 2 4 3.7 CC(C)[C@@H](c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)[C@@H]1OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
137487342 188220 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 408 3 2 4 4.7 CC(C)/C(=C1/SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4764161 188220 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 408 3 2 4 4.7 CC(C)/C(=C1/SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
164615533 191419 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 362 4 1 3 5.1 CC(C)C(c1ncco1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4849556 191419 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 362 4 1 3 5.1 CC(C)C(c1ncco1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137478093 186974 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 421 5 2 3 4.0 CC(C)C(CC1C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4749494 186974 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 421 5 2 3 4.0 CC(C)C(CC1C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
162674113 189939 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 418 3 2 4 4.3 O=C1NC(=O)/C(=C/C2(c3ccc(-c4ccc5cccc(F)c5c4)[nH]c3=O)CCCC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4795369 189939 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 418 3 2 4 4.3 O=C1NC(=O)/C(=C/C2(c3ccc(-c4ccc5cccc(F)c5c4)[nH]c3=O)CCCC2)O1 10.1021/acsmedchemlett.0c00667
137477803 191693 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 421 5 2 4 5.2 CC(C)C(C(=O)Nc1nccs1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4853296 191693 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 421 5 2 4 5.2 CC(C)C(C(=O)Nc1nccs1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017321 208113 2 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 477 11 2 3 6.2 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1F 10.1016/j.bmc.2009.12.068
CHEMBL604297 208113 2 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 477 11 2 3 6.2 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1F 10.1016/j.bmc.2009.12.068
49850345 68194 6 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
CHEMBL1770317 68194 6 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
137477601 191559 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 442 5 1 4 3.8 CC(C)C(CN1CCS(=O)(=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4851344 191559 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 442 5 1 4 3.8 CC(C)C(CN1CCS(=O)(=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017731 207807 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 445 11 2 3 5.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.12.068
CHEMBL602337 207807 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 445 11 2 3 5.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.12.068
23017216 205938 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSA
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL589411 205938 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 0.1% BSA
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
23017731 207807 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 445 11 2 3 5.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL602337 207807 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 445 11 2 3 5.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
162668445 189458 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 392 3 2 4 4.0 CC(C)/C(=C1\NC(=O)OC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4789221 189458 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 392 3 2 4 4.0 CC(C)/C(=C1\NC(=O)OC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL5075763 221177 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1ccc(Cl)cc1 10.1021/acsmedchemlett.1c00594
137478131 189878 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 432 4 2 4 4.8 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CCCC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4794537 189878 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 432 4 2 4 4.8 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CCCC2)O1 10.1021/acsmedchemlett.0c00667
11752564 207082 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597375 207082 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017457 207201 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 488 11 2 4 5.8 CC(C)CC(NC(=O)c1cc(COc2cccc(C#N)c2)ccc1CCC(=O)O)c1ccc(F)cc1 10.1016/j.bmc.2009.12.068
CHEMBL598174 207201 0 None - 1 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 488 11 2 4 5.8 CC(C)CC(NC(=O)c1cc(COc2cccc(C#N)c2)ccc1CCC(=O)O)c1ccc(F)cc1 10.1016/j.bmc.2009.12.068
46887090 15325 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 503 12 2 4 6.4 COc1ccccc1OCc1ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c2cc(C)cc(C)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094470 15325 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albuminAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
ChEMBL 503 12 2 4 6.4 COc1ccccc1OCc1ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c2cc(C)cc(C)c2)c1 10.1016/j.bmc.2010.03.028
23017638 14904 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 607 11 1 6 6.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091739 14904 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 607 11 1 6 6.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.034
137477942 193183 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 393 5 2 4 4.0 CC(C)C(Cc1noc(=O)[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4875937 193183 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 393 5 2 4 4.0 CC(C)C(Cc1noc(=O)[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
10294290 206832 0 None - 1 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595632 206832 0 None - 1 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentrationAntagonist activity at mouse EP3alpha receptor expressed in CHo cells assessed as inhibition of PGE2-stimulated intracellular calcium concentration
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
127047601 146552 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 330 4 1 6 2.9 CCN1CCOc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3798598 146552 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assayAntagonist activity at human recombinant EP3 receptor expressed in CHOK1 cells assessed as inhibition of sulprostone-induced decrease in cAMP level preincubated with compound followed by sulprostone addition by HTRF assay
ChEMBL 330 4 1 6 2.9 CCN1CCOc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
137477890 191337 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 375 5 2 2 5.0 CC(C)C(Cc1ncc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4848372 191337 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 375 5 2 2 5.0 CC(C)C(Cc1ncc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017216 205938 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL589411 205938 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
137477635 187630 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 446 4 2 4 5.1 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CCCCC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4757179 187630 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 446 4 2 4 5.1 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CCCCC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL5076035 221189 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None COc1ccc(Cl)cc1S(=O)(=O)NC(=O)NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21 10.1021/acsmedchemlett.1c00594
CHEMBL5085586 221753 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None Cn1cc(S(=O)(=O)NC(=O)NC/C=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)cn1 10.1021/acsmedchemlett.1c00594
137478205 191794 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 390 4 2 2 4.5 CC(C)C(/C=C1/CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4854881 191794 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 390 4 2 2 4.5 CC(C)C(/C=C1/CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017083 207075 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3Cl)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597348 207075 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3Cl)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
137477910 191415 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 390 4 2 2 4.5 CC(C)C(/C=C1\CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4849504 191415 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 390 4 2 2 4.5 CC(C)C(/C=C1\CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
46886376 14998 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 540 10 2 6 4.9 O=C(NCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.02.034
CHEMBL1092267 14998 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 540 10 2 6 4.9 O=C(NCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.02.034
162673365 189789 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 405 4 3 3 3.8 CC(C)C(/C=C1\NC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4793698 189789 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 405 4 3 3 3.8 CC(C)C(/C=C1\NC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
23017539 15238 0 None - 1 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 543 11 1 7 5.0 Cc1ccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)o1 10.1016/j.bmcl.2010.02.034
CHEMBL1093842 15238 0 None - 1 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albuminAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
ChEMBL 543 11 1 7 5.0 Cc1ccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)o1 10.1016/j.bmcl.2010.02.034
137490797 188141 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 424 5 2 4 4.8 CC(C)[C@H](C[C@H]1SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4763179 188141 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 424 5 2 4 4.8 CC(C)[C@H](C[C@H]1SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137487349 188195 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 406 4 2 4 4.2 CC(C)[C@@H](/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4763806 188195 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 406 4 2 4 4.2 CC(C)[C@@H](/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL5077024 221254 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None Cc1ncc(S(=O)(=O)NC(=O)NC/C=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)s1 10.1021/acsmedchemlett.1c00594
23016733 207457 0 None - 1 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3C#N)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599811 207457 0 None - 1 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetryAntagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase intracellular calcium level in presence of 1% BSA by fluorimetry
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3C#N)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
137477644 191874 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 368 5 2 3 3.8 CONC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
CHEMBL4856048 191874 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 368 5 2 3 3.8 CONC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
137477673 192583 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 408 6 2 5 4.1 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc(C)[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL4866965 192583 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 408 6 2 5 4.1 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc(C)[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
137487333 189238 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 430 6 2 4 5.0 CCc1cccc2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc12 10.1021/acsmedchemlett.0c00667
CHEMBL4786317 189238 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 430 6 2 4 5.0 CCc1cccc2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc12 10.1021/acsmedchemlett.0c00667
137477752 187018 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 420 4 2 4 4.5 Cc1cc(C(/C=C2\OC(=O)NC2=O)C(C)C)c(=O)[nH]c1-c1ccc2cccc(F)c2c1 10.1021/acsmedchemlett.0c00667
CHEMBL4750135 187018 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 420 4 2 4 4.5 Cc1cc(C(/C=C2\OC(=O)NC2=O)C(C)C)c(=O)[nH]c1-c1ccc2cccc(F)c2c1 10.1021/acsmedchemlett.0c00667
137487290 188477 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 394 4 2 4 3.7 CC(C)[C@@H](c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)[C@H]1OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4776714 188477 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assayAntagonist activity at human EP3 expressed in CHO cells assessed as suppression of sulprostone-induced inhibition of forskolin induced cAMP production measured after 30 mins by HTR-FRET assay
ChEMBL 394 4 2 4 3.7 CC(C)[C@@H](c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)[C@H]1OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
CHEMBL5082682 221598 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assayAntagonist activity at human EP3 receptor expressed in CHO-K1 cells assessed as reduction in sulprostone induced inhibition of forskolin stimulated cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None O=C(NS(=O)(=O)c1ccc(Cl)cc1)OC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21 10.1021/acsmedchemlett.1c00594
46230201 207395 0 None - 1 Mouse 5.0 pIC50 = 5.0 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 453 9 2 3 5.9 C[C@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL599355 207395 0 None - 1 Mouse 5.0 pIC50 = 5.0 Functional
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSAAntagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level by fluorescence assay in presence of 1% BSA
ChEMBL 453 9 2 3 5.9 C[C@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
137477947 192464 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 408 6 1 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4ncn(C)n4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL4865168 192464 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 408 6 1 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4ncn(C)n4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
137478136 192926 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 442 8 5 5 1.9 CC(C)C(C(=O)NC(CO)(CO)CO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4872246 192926 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assayAntagonist activity at human EP3 receptor expressed in CHO cells by cell based cAMP functional assay
ChEMBL 442 8 5 5 1.9 CC(C)C(C(=O)NC(CO)(CO)CO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
45272639 202637 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 420 3 1 6 4.6 CN1CCOc2ccc(C(=O)Nc3nnc(-c4c(Cl)cccc4Cl)s3)cc21 10.1016/j.bmcl.2009.05.074
CHEMBL558644 202637 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 420 3 1 6 4.6 CN1CCOc2ccc(C(=O)Nc3nnc(-c4c(Cl)cccc4Cl)s3)cc21 10.1016/j.bmcl.2009.05.074
44250281 203286 0 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 434 4 1 6 5.0 CCN1CCOc2ccc(C(=O)Nc3nnc(-c4c(Cl)cccc4Cl)s3)cc21 10.1016/j.bmcl.2009.05.074
CHEMBL563480 203286 0 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 434 4 1 6 5.0 CCN1CCOc2ccc(C(=O)Nc3nnc(-c4c(Cl)cccc4Cl)s3)cc21 10.1016/j.bmcl.2009.05.074
49850345 68194 6 None - 1 Human 8.0 pKi = 8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770317 68194 6 None - 1 Human 8.0 pKi = 8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
49850345 68194 6 None - 1 Human 8.0 pKi = 8 Functional
Antagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assayAntagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
CHEMBL1770317 68194 6 None - 1 Human 8.0 pKi = 8 Functional
Antagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assayAntagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
49850345 68194 6 None - 1 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assayAntagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
CHEMBL1770317 68194 6 None - 1 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assayAntagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
45268367 203418 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 353 3 1 6 3.8 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)OCO3)s1 10.1016/j.bmcl.2009.05.074
CHEMBL564317 203418 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 353 3 1 6 3.8 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)OCO3)s1 10.1016/j.bmcl.2009.05.074
52944290 25237 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 365 5 2 3 4.2 CCc1cccc(NC(=O)Nc2cccn(Cc3ccccc3F)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1272086 25237 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 365 5 2 3 4.2 CCc1cccc(NC(=O)Nc2cccn(Cc3ccccc3F)c2=O)c1 10.1016/j.bmcl.2010.08.137
1450040 25182 6 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 349 5 2 4 3.5 COc1cccc(NC(=O)Nc2cccn(Cc3ccccc3)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271635 25182 6 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 349 5 2 4 3.5 COc1cccc(NC(=O)Nc2cccn(Cc3ccccc3)c2=O)c1 10.1016/j.bmcl.2010.08.137
52948962 25195 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 5 2 4 3.7 COc1cccc(NC(=O)Nc2cccn(Cc3cccc(F)c3)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271743 25195 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 5 2 4 3.7 COc1cccc(NC(=O)Nc2cccn(Cc3cccc(F)c3)c2=O)c1 10.1016/j.bmcl.2010.08.137
1450104 25212 5 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 2 4 4.2 COc1cccc(NC(=O)Nc2cccn(Cc3ccc(Cl)cc3)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271915 25212 5 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 2 4 4.2 COc1cccc(NC(=O)Nc2cccn(Cc3ccc(Cl)cc3)c2=O)c1 10.1016/j.bmcl.2010.08.137
52947148 25255 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 387 4 2 3 4.8 O=C(Nc1cccc(Cl)c1)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
CHEMBL1272240 25255 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 387 4 2 3 4.8 O=C(Nc1cccc(Cl)c1)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
52941063 25256 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 431 4 2 3 5.0 O=C(Nc1cccc(Br)c1)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
CHEMBL1272241 25256 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 431 4 2 3 5.0 O=C(Nc1cccc(Br)c1)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
24784836 74933 0 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHO-K1 cells assessed as inhibition of PGE2-mediated intracellular calcium mobilization by FLIPR methodAntagonist activity at human recombinant EP3 receptor expressed in CHO-K1 cells assessed as inhibition of PGE2-mediated intracellular calcium mobilization by FLIPR method
ChEMBL 332 4 1 4 4.5 Cc1cc(C(=O)O)nn1Cc1cc(Cl)cc2cc(C(C)C)oc12 10.1016/j.bmcl.2011.05.047
CHEMBL1915012 74933 0 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity at human recombinant EP3 receptor expressed in CHO-K1 cells assessed as inhibition of PGE2-mediated intracellular calcium mobilization by FLIPR methodAntagonist activity at human recombinant EP3 receptor expressed in CHO-K1 cells assessed as inhibition of PGE2-mediated intracellular calcium mobilization by FLIPR method
ChEMBL 332 4 1 4 4.5 Cc1cc(C(=O)O)nn1Cc1cc(Cl)cc2cc(C(C)C)oc12 10.1016/j.bmcl.2011.05.047
44377464 126863 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity at Prostanoid EP3 receptor in human was determinedAntagonistic activity at Prostanoid EP3 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)cc1Cl 10.1016/s0960-894x(01)00056-7
CHEMBL350832 126863 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity at Prostanoid EP3 receptor in human was determinedAntagonistic activity at Prostanoid EP3 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)cc1Cl 10.1016/s0960-894x(01)00056-7
45270915 201820 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 367 3 1 6 3.8 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)OCCO3)s1 10.1016/j.bmcl.2009.05.074
CHEMBL549437 201820 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 367 3 1 6 3.8 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)OCCO3)s1 10.1016/j.bmcl.2009.05.074
45270922 202316 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 437 4 1 7 4.5 COc1cc(Cl)c(-c2nnc(NC(=O)c3ccc4c(c3)OCCO4)s2)c(Cl)c1 10.1016/j.bmcl.2009.05.074
CHEMBL554297 202316 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 437 4 1 7 4.5 COc1cc(Cl)c(-c2nnc(NC(=O)c3ccc4c(c3)OCCO4)s2)c(Cl)c1 10.1016/j.bmcl.2009.05.074
49850348 81835 0 None - 0 Rat 7.9 pKi = 7.9 Functional
Antagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assayAntagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assay
ChEMBL 340 3 2 4 2.8 Cc1ccc(-c2ccc(C3(C(C)C)OC(=O)NC3=O)c(=O)[nH]2)cc1C 10.1021/ml100077x
CHEMBL2035509 81835 0 None - 0 Rat 7.9 pKi = 7.9 Functional
Antagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assayAntagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assay
ChEMBL 340 3 2 4 2.8 Cc1ccc(-c2ccc(C3(C(C)C)OC(=O)NC3=O)c(=O)[nH]2)cc1C 10.1021/ml100077x
54586642 68200 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 388 2 2 4 3.2 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)(C(F)(F)F)O1 10.1016/j.bmcl.2011.03.107
CHEMBL1770323 68200 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 388 2 2 4 3.2 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)(C(F)(F)F)O1 10.1016/j.bmcl.2011.03.107
52943117 25229 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 395 5 2 3 5.1 CCc1cccc(NC(=O)Nc2ccc(C)n(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1272030 25229 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 395 5 2 3 5.1 CCc1cccc(NC(=O)Nc2ccc(C)n(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
52946739 25234 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 387 4 2 3 4.8 O=C(Nc1ccccc1Cl)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
CHEMBL1272083 25234 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 387 4 2 3 4.8 O=C(Nc1ccccc1Cl)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
52946740 25236 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 399 5 2 3 4.9 CCc1cccc(NC(=O)Nc2cccn(Cc3ccc(F)cc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1272085 25236 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 399 5 2 3 4.9 CCc1cccc(NC(=O)Nc2cccn(Cc3ccc(F)cc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
54583738 68209 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 333 2 2 4 3.7 CC1(c2ccc(-c3ccc4ccccc4c3)cc2O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770331 68209 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 333 2 2 4 3.7 CC1(c2ccc(-c3ccc4ccccc4c3)cc2O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
45272630 202566 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 381 3 1 6 4.2 Cc1cc(C)c(-c2nnc(NC(=O)c3cccc4c3OCCO4)s2)c(C)c1 10.1016/j.bmcl.2009.05.074
CHEMBL557857 202566 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 381 3 1 6 4.2 Cc1cc(C)c(-c2nnc(NC(=O)c3cccc4c3OCCO4)s2)c(C)c1 10.1016/j.bmcl.2009.05.074
52940662 25200 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 363 5 2 4 3.9 COc1cccc(NC(=O)Nc2cccn(Cc3cccc(C)c3)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271803 25200 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 363 5 2 4 3.9 COc1cccc(NC(=O)Nc2cccn(Cc3cccc(C)c3)c2=O)c1 10.1016/j.bmcl.2010.08.137
52940700 25205 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 5 2 4 3.7 COc1cccc(NC(=O)Nc2cccn(Cc3ccc(F)cc3)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271859 25205 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 5 2 4 3.7 COc1cccc(NC(=O)Nc2cccn(Cc3ccc(F)cc3)c2=O)c1 10.1016/j.bmcl.2010.08.137
52941891 25214 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 397 5 2 4 4.5 COc1cccc(NC(=O)Nc2cc(C)cn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271917 25214 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 397 5 2 4 4.5 COc1cccc(NC(=O)Nc2cc(C)cn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
52941863 25223 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 397 5 2 4 4.5 COc1cccc(NC(=O)Nc2ccc(C)n(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271974 25223 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 397 5 2 4 4.5 COc1cccc(NC(=O)Nc2ccc(C)n(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
54582745 68199 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 410 4 2 4 3.9 O=C1NC(=O)C(Cc2ccccc2)(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)O1 10.1016/j.bmcl.2011.03.107
CHEMBL1770322 68199 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 410 4 2 4 3.9 O=C1NC(=O)C(Cc2ccccc2)(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)O1 10.1016/j.bmcl.2011.03.107
45268369 203106 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 380 3 1 6 3.9 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)OCCN3C)s1 10.1016/j.bmcl.2009.05.074
CHEMBL562329 203106 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 380 3 1 6 3.9 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)OCCN3C)s1 10.1016/j.bmcl.2009.05.074
45269218 203417 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 319 2 1 6 2.9 CC(C)(C)c1nnc(NC(=O)c2ccc3c(c2)OCCO3)s1 10.1016/j.bmcl.2009.05.074
CHEMBL564305 203417 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 319 2 1 6 2.9 CC(C)(C)c1nnc(NC(=O)c2ccc3c(c2)OCCO3)s1 10.1016/j.bmcl.2009.05.074
1450080 25181 6 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 2 4 4.2 COc1cccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271634 25181 6 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 2 4 4.2 COc1cccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
52944309 25228 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 371 4 2 3 4.3 O=C(Nc1ccccc1F)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
CHEMBL1272029 25228 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 371 4 2 3 4.3 O=C(Nc1ccccc1F)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
54583736 68203 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 376 3 1 4 3.8 CC(C)N1C(=O)OC(C)(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)C1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770326 68203 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 376 3 1 4 3.8 CC(C)N1C(=O)OC(C)(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)C1=O 10.1016/j.bmcl.2011.03.107
52950153 25250 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 371 4 2 3 4.3 O=C(Nc1cccc(F)c1)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
CHEMBL1272186 25250 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 371 4 2 3 4.3 O=C(Nc1cccc(F)c1)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
119461 7108 72 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at EP3 receptor (unknown origin) by functional cAMP assayAntagonist activity at EP3 receptor (unknown origin) by functional cAMP assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
1896 7108 72 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at EP3 receptor (unknown origin) by functional cAMP assayAntagonist activity at EP3 receptor (unknown origin) by functional cAMP assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
CHEMBL1317823 7108 72 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at EP3 receptor (unknown origin) by functional cAMP assayAntagonist activity at EP3 receptor (unknown origin) by functional cAMP assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
54587664 68193 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 334 2 2 4 2.7 CC1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770316 68193 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 334 2 2 4 2.7 CC1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
54581786 68217 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)[C@]1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770340 68217 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)[C@]1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
45269223 203398 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 381 3 1 6 4.2 Cc1cc(C)c(-c2nnc(NC(=O)c3ccc4c(c3)OCCO4)s2)c(C)c1 10.1016/j.bmcl.2009.05.074
CHEMBL564190 203398 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 381 3 1 6 4.2 Cc1cc(C)c(-c2nnc(NC(=O)c3ccc4c(c3)OCCO4)s2)c(C)c1 10.1016/j.bmcl.2009.05.074
49850348 81835 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assayAntagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assay
ChEMBL 340 3 2 4 2.8 Cc1ccc(-c2ccc(C3(C(C)C)OC(=O)NC3=O)c(=O)[nH]2)cc1C 10.1021/ml100077x
CHEMBL2035509 81835 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assayAntagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assay
ChEMBL 340 3 2 4 2.8 Cc1ccc(-c2ccc(C3(C(C)C)OC(=O)NC3=O)c(=O)[nH]2)cc1C 10.1021/ml100077x
54582746 68201 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 404 3 2 5 3.1 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)(C2CCOCC2)O1 10.1016/j.bmcl.2011.03.107
CHEMBL1770324 68201 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 404 3 2 5 3.1 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)(C2CCOCC2)O1 10.1016/j.bmcl.2011.03.107
45268368 203073 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 381 3 1 6 4.2 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)OCCCO3)s1 10.1016/j.bmcl.2009.05.074
CHEMBL562132 203073 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 381 3 1 6 4.2 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)OCCCO3)s1 10.1016/j.bmcl.2009.05.074
45267483 203128 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 331 3 1 6 3.2 O=C(Nc1nnc(C2CCCC2)s1)c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2009.05.074
CHEMBL562465 203128 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 331 3 1 6 3.2 O=C(Nc1nnc(C2CCCC2)s1)c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2009.05.074
45267497 203169 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 365 3 1 5 4.3 Cc1cc(C)c(-c2nnc(NC(=O)c3ccc4c(c3)CCO4)s2)c(C)c1 10.1016/j.bmcl.2009.05.074
CHEMBL562692 203169 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 365 3 1 5 4.3 Cc1cc(C)c(-c2nnc(NC(=O)c3ccc4c(c3)CCO4)s2)c(C)c1 10.1016/j.bmcl.2009.05.074
52946754 25215 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 395 5 2 3 5.1 CCc1cccc(NC(=O)Nc2cc(C)cn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271918 25215 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 395 5 2 3 5.1 CCc1cccc(NC(=O)Nc2cc(C)cn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
52943118 25230 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 415 5 2 3 5.1 CCc1cccc(NC(=O)Nc2cccn(Cc3cccc(C(F)(F)F)c3)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1272031 25230 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 415 5 2 3 5.1 CCc1cccc(NC(=O)Nc2cccn(Cc3cccc(C(F)(F)F)c3)c2=O)c1 10.1016/j.bmcl.2010.08.137
70681702 81833 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assayAntagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assay
ChEMBL 320 2 2 4 2.5 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)O1 10.1021/ml100077x
CHEMBL2035507 81833 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assayAntagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assay
ChEMBL 320 2 2 4 2.5 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)O1 10.1021/ml100077x
45269240 202832 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 394 3 1 6 3.4 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)N(C)C(=O)CO3)s1 10.1016/j.bmcl.2009.05.074
CHEMBL560388 202832 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 394 3 1 6 3.4 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)N(C)C(=O)CO3)s1 10.1016/j.bmcl.2009.05.074
52941886 25204 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 379 6 2 5 3.6 COc1cccc(Cn2cccc(NC(=O)Nc3cccc(OC)c3)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271858 25204 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 379 6 2 5 3.6 COc1cccc(Cn2cccc(NC(=O)Nc3cccc(OC)c3)c2=O)c1 10.1016/j.bmcl.2010.08.137
9817405 172182 5 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonistic activity at Prostanoid EP3 receptor in human was determinedAntagonistic activity at Prostanoid EP3 receptor in human was determined
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/s0960-894x(01)00056-7
CHEMBL423815 172182 5 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonistic activity at Prostanoid EP3 receptor in human was determinedAntagonistic activity at Prostanoid EP3 receptor in human was determined
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/s0960-894x(01)00056-7
45269232 203213 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 363 3 1 4 5.0 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)CCCC3)s1 10.1016/j.bmcl.2009.05.074
CHEMBL562994 203213 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 363 3 1 4 5.0 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)CCCC3)s1 10.1016/j.bmcl.2009.05.074
52949188 25243 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 401 5 2 4 4.3 COc1cccc(NC(=O)Nc2cccn(Cc3c(F)cccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1272135 25243 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 401 5 2 4 4.3 COc1cccc(NC(=O)Nc2cccn(Cc3c(F)cccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
52946882 25169 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 4 2 3 4.5 Cc1cccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271475 25169 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 4 2 3 4.5 Cc1cccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
54587665 68214 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 438 4 2 4 5.0 CC(C)C1(c2cc(-c3ccccc3)c(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770338 68214 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 438 4 2 4 5.0 CC(C)C1(c2cc(-c3ccccc3)c(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
52940697 25194 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 363 5 2 4 3.9 COc1cccc(NC(=O)Nc2cccn(Cc3ccccc3C)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271742 25194 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 363 5 2 4 3.9 COc1cccc(NC(=O)Nc2cccn(Cc3ccccc3C)c2=O)c1 10.1016/j.bmcl.2010.08.137
45270083 202044 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 407 3 1 6 4.5 O=C(Nc1nnc(-c2c(Cl)cccc2Cl)s1)c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2009.05.074
CHEMBL551202 202044 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 407 3 1 6 4.5 O=C(Nc1nnc(-c2c(Cl)cccc2Cl)s1)c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2009.05.074
49850346 81836 9 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assayAntagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assay
ChEMBL 380 3 2 4 3.5 CC(C)C1(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
CHEMBL2035510 81836 9 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assayAntagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assay
ChEMBL 380 3 2 4 3.5 CC(C)C1(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
49850346 81836 9 None - 0 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assayAntagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assay
ChEMBL 380 3 2 4 3.5 CC(C)C1(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
CHEMBL2035510 81836 9 None - 0 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assayAntagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assay
ChEMBL 380 3 2 4 3.5 CC(C)C1(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
54583735 68198 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 396 3 2 4 3.7 O=C1NC(=O)C(c2ccccc2)(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)O1 10.1016/j.bmcl.2011.03.107
CHEMBL1770321 68198 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 396 3 2 4 3.7 O=C1NC(=O)C(c2ccccc2)(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)O1 10.1016/j.bmcl.2011.03.107
24760470 21511 0 None - 1 Human 6.5 pKi = 6.5 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 334 4 1 4 4.6 CC(C)Cc1cn(-c2nc(C(=O)O)cs2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL1206294 21511 0 None - 1 Human 6.5 pKi = 6.5 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 334 4 1 4 4.6 CC(C)Cc1cn(-c2nc(C(=O)O)cs2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL257997 21511 0 None - 1 Human 6.5 pKi = 6.5 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 334 4 1 4 4.6 CC(C)Cc1cn(-c2nc(C(=O)O)cs2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
54580770 68204 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 333 2 3 3 2.3 CC1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)NC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770327 68204 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 333 2 3 3 2.3 CC1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)NC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
1450111 25188 6 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 427 5 2 4 4.3 COc1cccc(NC(=O)Nc2cccn(Cc3ccccc3Br)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271687 25188 6 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 427 5 2 4 4.3 COc1cccc(NC(=O)Nc2cccn(Cc3ccccc3Br)c2=O)c1 10.1016/j.bmcl.2010.08.137
70681702 81833 0 None - 0 Rat 6.5 pKi = 6.5 Functional
Antagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assayAntagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assay
ChEMBL 320 2 2 4 2.5 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)O1 10.1021/ml100077x
CHEMBL2035507 81833 0 None - 0 Rat 6.5 pKi = 6.5 Functional
Antagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assayAntagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assay
ChEMBL 320 2 2 4 2.5 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)O1 10.1021/ml100077x
54580771 68208 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 347 3 1 4 4.0 COc1cc(-c2ccc3ccccc3c2)ccc1C1(C)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770330 68208 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 347 3 1 4 4.0 COc1cc(-c2ccc3ccccc3c2)ccc1C1(C)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
52947935 25189 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 4 2 3 4.5 Cc1ccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)cc1 10.1016/j.bmcl.2010.08.137
CHEMBL1271688 25189 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 4 2 3 4.5 Cc1ccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)cc1 10.1016/j.bmcl.2010.08.137
1450090 25213 6 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 363 5 2 4 3.9 COc1cccc(NC(=O)Nc2cccn(Cc3ccc(C)cc3)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271916 25213 6 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 363 5 2 4 3.9 COc1cccc(NC(=O)Nc2cccn(Cc3ccc(C)cc3)c2=O)c1 10.1016/j.bmcl.2010.08.137
10402929 64317 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonistic activity at Prostanoid EP3 receptor in human was determinedAntagonistic activity at Prostanoid EP3 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(01)00056-7
CHEMBL166351 64317 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonistic activity at Prostanoid EP3 receptor in human was determinedAntagonistic activity at Prostanoid EP3 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(01)00056-7
54583737 68205 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 319 2 3 2 2.7 CC1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)CNC(=O)N1 10.1016/j.bmcl.2011.03.107
CHEMBL1770328 68205 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 319 2 3 2 2.7 CC1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)CNC(=O)N1 10.1016/j.bmcl.2011.03.107
54581785 68212 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 440 3 2 4 4.1 CC(C)C1(c2cc(Br)c(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770336 68212 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 440 3 2 4 4.1 CC(C)C1(c2cc(Br)c(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
24760322 21494 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 362 4 1 4 5.4 CC(C)(C)CCc1cn(-c2nc(C(=O)O)cs2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL1206265 21494 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 362 4 1 4 5.4 CC(C)(C)CCc1cn(-c2nc(C(=O)O)cs2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL255675 21494 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 362 4 1 4 5.4 CC(C)(C)CCc1cn(-c2nc(C(=O)O)cs2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
24760390 21505 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 378 4 1 4 4.7 CC(C)Cc1cn(-c2nc(C(=O)O)cs2)c2cc(Br)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL1206284 21505 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 378 4 1 4 4.7 CC(C)Cc1cn(-c2nc(C(=O)O)cs2)c2cc(Br)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL257134 21505 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 378 4 1 4 4.7 CC(C)Cc1cn(-c2nc(C(=O)O)cs2)c2cc(Br)ccc12 10.1016/j.bmcl.2008.03.018
45271759 201884 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 395 3 1 6 4.5 Cc1cc(C)c(C)c(-c2nnc(NC(=O)c3ccc4c(c3)OCCO4)s2)c1C 10.1016/j.bmcl.2009.05.074
CHEMBL549909 201884 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 395 3 1 6 4.5 Cc1cc(C)c(C)c(-c2nnc(NC(=O)c3ccc4c(c3)OCCO4)s2)c1C 10.1016/j.bmcl.2009.05.074
52949166 25199 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 2 4 4.2 COc1cccc(NC(=O)Nc2cccn(Cc3cccc(Cl)c3)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271802 25199 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 2 4 4.2 COc1cccc(NC(=O)Nc2cccn(Cc3cccc(Cl)c3)c2=O)c1 10.1016/j.bmcl.2010.08.137
52945504 25221 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 401 5 2 4 4.3 COc1cccc(NC(=O)Nc2cccn(Cc3ccc(F)cc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271972 25221 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 401 5 2 4 4.3 COc1cccc(NC(=O)Nc2cccn(Cc3ccc(F)cc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
52944708 25259 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 479 4 2 3 4.8 O=C(Nc1cccc(I)c1)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
CHEMBL1272295 25259 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 479 4 2 3 4.8 O=C(Nc1cccc(I)c1)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
52948954 25242 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 381 5 2 3 4.8 CCc1ccccc1NC(=O)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
CHEMBL1272134 25242 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 381 5 2 3 4.8 CCc1ccccc1NC(=O)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
45271767 201937 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 380 3 1 6 3.9 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)N(C)CCO3)s1 10.1016/j.bmcl.2009.05.074
CHEMBL550316 201937 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 380 3 1 6 3.9 Cc1cccc(C)c1-c1nnc(NC(=O)c2ccc3c(c2)N(C)CCO3)s1 10.1016/j.bmcl.2009.05.074
54581783 68195 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 360 3 2 4 3.1 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)(C2CC2)O1 10.1016/j.bmcl.2011.03.107
CHEMBL1770318 68195 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 360 3 2 4 3.1 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)(C2CC2)O1 10.1016/j.bmcl.2011.03.107
54582748 68211 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 396 3 2 4 4.0 CC(C)C1(c2cc(Cl)c(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770335 68211 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 396 3 2 4 4.0 CC(C)C1(c2cc(Cl)c(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
52946883 25170 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 381 5 2 3 4.8 CCc1cccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271476 25170 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 381 5 2 3 4.8 CCc1cccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
24760466 21610 0 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 368 4 1 4 5.0 CC(C)Cc1cn(-c2nc(C(=O)O)cs2)c2cc(C(F)(F)F)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL1207394 21610 0 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 368 4 1 4 5.0 CC(C)Cc1cn(-c2nc(C(=O)O)cs2)c2cc(C(F)(F)F)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL402392 21610 0 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 368 4 1 4 5.0 CC(C)Cc1cn(-c2nc(C(=O)O)cs2)c2cc(C(F)(F)F)ccc12 10.1016/j.bmcl.2008.03.018
24760471 21616 0 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 317 4 1 3 4.8 CC(C)Cc1cn(-c2ccc(C(=O)O)o2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL1207406 21616 0 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 317 4 1 3 4.8 CC(C)Cc1cn(-c2ccc(C(=O)O)o2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL403407 21616 0 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 317 4 1 3 4.8 CC(C)Cc1cn(-c2ccc(C(=O)O)o2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
54584714 68202 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 348 2 1 4 3.0 CN1C(=O)OC(C)(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)C1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770325 68202 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 348 2 1 4 3.0 CN1C(=O)OC(C)(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)C1=O 10.1016/j.bmcl.2011.03.107
45273534 202520 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 353 3 1 6 3.5 Cc1ccccc1-c1nnc(NC(=O)c2ccc3c(c2)OCCO3)s1 10.1016/j.bmcl.2009.05.074
CHEMBL557312 202520 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 353 3 1 6 3.5 Cc1ccccc1-c1nnc(NC(=O)c2ccc3c(c2)OCCO3)s1 10.1016/j.bmcl.2009.05.074
52946711 25187 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 5 2 4 3.7 COc1cccc(NC(=O)Nc2cccn(Cc3ccccc3F)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271686 25187 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 5 2 4 3.7 COc1cccc(NC(=O)Nc2cccn(Cc3ccccc3F)c2=O)c1 10.1016/j.bmcl.2010.08.137
52945505 25222 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 415 5 2 3 5.4 CCc1cccc(NC(=O)Nc2cc(Cl)cn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271973 25222 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 415 5 2 3 5.4 CCc1cccc(NC(=O)Nc2cc(Cl)cn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
10007859 173268 0 None - 3 Human 6.3 pKi = 6.3 Functional
Inhibition of EP3 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assayInhibition of EP3 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assay
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 173268 0 None - 3 Human 6.3 pKi = 6.3 Functional
Inhibition of EP3 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assayInhibition of EP3 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assay
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
10095268 92931 0 None - 3 Human 6.3 pKi = 6.3 Functional
Inhibition of human recombinant EP3 receptor expressed in CHO cells by calcium mobilisation assayInhibition of human recombinant EP3 receptor expressed in CHO cells by calcium mobilisation assay
ChEMBL 449 6 1 3 6.8 Cc1ccc(-n2c(C)ccc2-c2cc(Cl)ccc2OCc2ccc(F)cc2)cc1C(=O)O 10.1016/j.bmcl.2006.11.059
CHEMBL231184 92931 0 None - 3 Human 6.3 pKi = 6.3 Functional
Inhibition of human recombinant EP3 receptor expressed in CHO cells by calcium mobilisation assayInhibition of human recombinant EP3 receptor expressed in CHO cells by calcium mobilisation assay
ChEMBL 449 6 1 3 6.8 Cc1ccc(-n2c(C)ccc2-c2cc(Cl)ccc2OCc2ccc(F)cc2)cc1C(=O)O 10.1016/j.bmcl.2006.11.059
52943098 25235 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 479 4 2 3 4.8 O=C(Nc1ccccc1I)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
CHEMBL1272084 25235 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 479 4 2 3 4.8 O=C(Nc1ccccc1I)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
53234014 68213 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 376 3 2 4 3.6 Cc1cc(C2(C(C)C)OC(=O)NC2=O)c(=O)[nH]c1-c1ccc2ccccc2c1 10.1016/j.bmcl.2011.03.107
CHEMBL1770337 68213 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 376 3 2 4 3.6 Cc1cc(C2(C(C)C)OC(=O)NC2=O)c(=O)[nH]c1-c1ccc2ccccc2c1 10.1016/j.bmcl.2011.03.107
50899741 25244 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 399 5 2 3 4.9 CCc1cccc(NC(=O)Nc2cccn(Cc3c(F)cccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1272136 25244 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 399 5 2 3 4.9 CCc1cccc(NC(=O)Nc2cccn(Cc3c(F)cccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
49850347 81834 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assayAntagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assay
ChEMBL 365 3 2 5 2.7 CC(C)C1(c2ccc(-c3ccc4c(ccn4C)c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
CHEMBL2035508 81834 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assayAntagonist activity at human EP3c receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced calcium mobilization after 24 hrs by FLIPR assay
ChEMBL 365 3 2 5 2.7 CC(C)C1(c2ccc(-c3ccc4c(ccn4C)c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
52947722 25175 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 395 5 2 3 5.3 CC(C)c1cccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271527 25175 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 395 5 2 3 5.3 CC(C)c1cccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
54587666 68215 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 430 3 2 4 4.3 CC(C)C1(c2cc(C(F)(F)F)c(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770339 68215 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 430 3 2 4 4.3 CC(C)C1(c2cc(C(F)(F)F)c(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
45270084 202045 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 383 5 1 6 4.4 COc1ccc(C(=O)Nc2nnc(-c3c(C)cc(C)cc3C)s2)cc1OC 10.1016/j.bmcl.2009.05.074
CHEMBL551203 202045 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 383 5 1 6 4.4 COc1ccc(C(=O)Nc2nnc(-c3c(C)cc(C)cc3C)s2)cc1OC 10.1016/j.bmcl.2009.05.074
1450082 25249 5 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 2 4 4.2 COc1ccccc1NC(=O)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
CHEMBL1272185 25249 5 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 383 5 2 4 4.2 COc1ccccc1NC(=O)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
54584713 68196 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 388 3 2 4 3.8 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)(C2CCCC2)O1 10.1016/j.bmcl.2011.03.107
CHEMBL1770319 68196 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 388 3 2 4 3.8 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)(C2CCCC2)O1 10.1016/j.bmcl.2011.03.107
54581784 68197 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 402 3 2 4 4.2 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)(C2CCCCC2)O1 10.1016/j.bmcl.2011.03.107
CHEMBL1770320 68197 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 402 3 2 4 4.2 O=C1NC(=O)C(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)(C2CCCCC2)O1 10.1016/j.bmcl.2011.03.107
54586644 68218 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)[C@@]1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770341 68218 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)[C@@]1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
44250282 201902 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 406 3 2 6 4.6 O=C(Nc1nnc(-c2c(Cl)cccc2Cl)s1)c1ccc2c(c1)NCCO2 10.1016/j.bmcl.2009.05.074
CHEMBL550055 201902 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 406 3 2 6 4.6 O=C(Nc1nnc(-c2c(Cl)cccc2Cl)s1)c1ccc2c(c1)NCCO2 10.1016/j.bmcl.2009.05.074
49850347 81834 0 None - 0 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assayAntagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assay
ChEMBL 365 3 2 5 2.7 CC(C)C1(c2ccc(-c3ccc4c(ccn4C)c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
CHEMBL2035508 81834 0 None - 0 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assayAntagonist activity at rat EP3 receptor expressed in human U2OS cells co-expressing Gqi5 assessed as inhibition of PGE2-induced response after 24 hrs by FLIPR assay
ChEMBL 365 3 2 5 2.7 CC(C)C1(c2ccc(-c3ccc4c(ccn4C)c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
54586643 68206 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 320 2 2 3 3.2 CC1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)CNC(=O)O1 10.1016/j.bmcl.2011.03.107
CHEMBL1770329 68206 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 320 2 2 3 3.2 CC1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)CNC(=O)O1 10.1016/j.bmcl.2011.03.107
2114670 202501 5 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 333 5 1 6 3.5 CCC(CC)c1nnc(NC(=O)c2ccc3c(c2)OCCO3)s1 10.1016/j.bmcl.2009.05.074
CHEMBL557109 202501 5 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 333 5 1 6 3.5 CCC(CC)c1nnc(NC(=O)c2ccc3c(c2)OCCO3)s1 10.1016/j.bmcl.2009.05.074
24760472 21489 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 328 4 1 3 4.6 CC(C)Cc1cn(-c2cccc(C(=O)O)n2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL1206254 21489 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 328 4 1 3 4.6 CC(C)Cc1cn(-c2cccc(C(=O)O)n2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
CHEMBL254763 21489 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity against EP3 receptor by FLIPR assayAntagonist activity against EP3 receptor by FLIPR assay
ChEMBL 328 4 1 3 4.6 CC(C)Cc1cn(-c2cccc(C(=O)O)n2)c2cc(Cl)ccc12 10.1016/j.bmcl.2008.03.018
1283333 98310 7 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 expressed in CHOK1 cells receptor assessed as inhibition intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 expressed in CHOK1 cells receptor assessed as inhibition intracellular calcium mobilization by FLIPR assay
ChEMBL 456 8 1 3 4.7 CCc1ccccc1N(CC(=O)NCc1ccc(Cl)cc1)S(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2006.12.060
CHEMBL240436 98310 7 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 expressed in CHOK1 cells receptor assessed as inhibition intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 expressed in CHOK1 cells receptor assessed as inhibition intracellular calcium mobilization by FLIPR assay
ChEMBL 456 8 1 3 4.7 CCc1ccccc1N(CC(=O)NCc1ccc(Cl)cc1)S(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2006.12.060
54583739 68210 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2c[nH]c(-c3ccc4ccccc4c3)cc2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
CHEMBL1770333 68210 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assayAntagonist activity at human EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium concentration after 1 hr by FLIPR assay
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2c[nH]c(-c3ccc4ccccc4c3)cc2=O)OC(=O)NC1=O 10.1016/j.bmcl.2011.03.107
45267514 202876 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 408 3 1 6 3.8 CC(=O)N1CCOc2ccc(C(=O)Nc3nnc(-c4c(C)cccc4C)s3)cc21 10.1016/j.bmcl.2009.05.074
CHEMBL560868 202876 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assayAntagonist activity at human EP3 receptor expressed in cells assessed as mobilization of intracellular calcium by FLIPR assay
ChEMBL 408 3 1 6 3.8 CC(=O)N1CCOc2ccc(C(=O)Nc3nnc(-c4c(C)cccc4C)s3)cc21 10.1016/j.bmcl.2009.05.074
3231721 25220 5 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 379 6 2 5 3.6 COc1ccc(Cn2cccc(NC(=O)Nc3cccc(OC)c3)c2=O)cc1 10.1016/j.bmcl.2010.08.137
CHEMBL1271971 25220 5 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 379 6 2 5 3.6 COc1ccc(Cn2cccc(NC(=O)Nc3cccc(OC)c3)c2=O)cc1 10.1016/j.bmcl.2010.08.137
52946459 25227 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 401 5 2 4 4.3 COc1cccc(NC(=O)Nc2cccn(Cc3cc(F)ccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1272028 25227 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 401 5 2 4 4.3 COc1cccc(NC(=O)Nc2cccn(Cc3cc(F)ccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
52941873 25241 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 4 2 3 4.5 Cc1ccccc1NC(=O)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
CHEMBL1272133 25241 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human EP3 receptor expressed in human U2OS cells assessed as inhibition of PGE2-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 367 4 2 3 4.5 Cc1ccccc1NC(=O)Nc1cccn(Cc2ccccc2Cl)c1=O 10.1016/j.bmcl.2010.08.137
9817292 64001 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonistic activity at Prostanoid EP3 receptor in human was determinedAntagonistic activity at Prostanoid EP3 receptor in human was determined
ChEMBL 284 5 1 2 4.1 CSc1ccc(Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/s0960-894x(01)00056-7
CHEMBL165010 64001 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonistic activity at Prostanoid EP3 receptor in human was determinedAntagonistic activity at Prostanoid EP3 receptor in human was determined
ChEMBL 284 5 1 2 4.1 CSc1ccc(Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/s0960-894x(01)00056-7
138107701 194243 46 None -4 7 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 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 None
5311181 194243 46 None -4 7 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 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 None
CHEMBL494 194243 46 None -4 7 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 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 None
DB01088 194243 46 None -4 7 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 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 None
91798918 222842 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 400 10 2 6 2.6 COC(=O)CCC=C=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
1884 9857 52 None 2 9 Rat 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 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 None
5280363 9857 52 None 2 9 Rat 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 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 None
912 9857 52 None 2 9 Rat 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 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 None
CHEMBL815 9857 52 None 2 9 Rat 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 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 None
DB12789 9857 52 None 2 9 Rat 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 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 None
138 9855 88 None -5 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
149351 9855 88 None -5 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 9855 88 None -5 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 9855 88 None -5 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 9855 88 None -5 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 9855 88 None -5 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
138107701 194243 46 None -5 7 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 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 None
5311181 194243 46 None -5 7 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 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 None
CHEMBL494 194243 46 None -5 7 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 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 None
DB01088 194243 46 None -5 7 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 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 None
138 9855 88 None -1 10 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
149351 9855 88 None -1 10 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 9855 88 None -1 10 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 9855 88 None -1 10 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 9855 88 None -1 10 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 9855 88 None -1 10 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
134689669 222829 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 465 12 3 7 1.7 CS(=O)(=O)NC(=O)CCCC=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
1883 9856 75 None -1 12 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 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 None
1916 9856 75 None -1 12 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 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 None
5280360 9856 75 None -1 12 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 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 None
913 9856 75 None -1 12 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 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 None
CHEMBL548 9856 75 None -1 12 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 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 None
DB00917 9856 75 None -1 12 Rat 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 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 None
1931 9720 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 21323896
1931 9720 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 22342278
5311229 9720 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 21323896
5311229 9720 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 22342278
1894 7744 41 None -331 5 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 9694973
5311053 7744 41 None -331 5 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 9694973
CHEMBL37853 7744 41 None -331 5 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 9694973
DB11507 7744 41 None -331 5 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 9694973
1888 10672 29 None - 1 Rat 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
1974 10672 29 None - 1 Rat 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
5311493 10672 29 None - 1 Rat 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
CHEMBL521784 10672 29 None - 1 Rat 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
1881 9853 0 None -7 3 Rat 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
1891 9853 0 None -7 3 Rat 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
448457 9853 0 None -7 3 Rat 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
CHEMBL1235252 9853 0 None -7 3 Rat 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
DB02056 9853 0 None -7 3 Rat 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
1884 9857 52 None 2 9 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
5280363 9857 52 None 2 9 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
912 9857 52 None 2 9 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
CHEMBL815 9857 52 None 2 9 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
DB12789 9857 52 None 2 9 Rat 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
1918 8348 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 400 10 2 6 2.6 COC(=O)CCC=C=CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9694973
5311225 8348 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 400 10 2 6 2.6 COC(=O)CCC=C=CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9694973
CHEMBL2104194 8348 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 400 10 2 6 2.6 COC(=O)CCC=C=CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9694973
3331 10312 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 11 2 5 4.2 COC(=O)CC/C=C\CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/C[C@](/C=C/C1=CCCC1)(O)C)O 16737803
5311427 10312 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 11 2 5 4.2 COC(=O)CC/C=C\CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/C[C@](/C=C/C1=CCCC1)(O)C)O 16737803
CHEMBL49922 10312 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 11 2 5 4.2 COC(=O)CC/C=C\CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/C[C@](/C=C/C1=CCCC1)(O)C)O 16737803
1919 10476 0 None -3 2 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9694973
2538 10476 0 None -3 2 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9694973
5312153 10476 0 None -3 2 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9694973
CHEMBL1472830 10476 0 None -3 2 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9694973
DB12708 10476 0 None -3 2 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9694973
1895 8788 0 None 630 2 Rat 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
6435378 8788 0 None 630 2 Rat 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
CHEMBL236025 8788 0 None 630 2 Rat 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
DB01088 8788 0 None 630 2 Rat 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
1913 9242 0 None 32 2 Rat 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 9537820
5311223 9242 0 None 32 2 Rat 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 9537820
138 9855 88 None -1 10 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
149351 9855 88 None -1 10 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
1882 9855 88 None -1 10 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
5280723 9855 88 None -1 10 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
CHEMBL495 9855 88 None -1 10 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
DB00770 9855 88 None -1 10 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
1919 10476 0 None 3 2 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
2538 10476 0 None 3 2 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
5312153 10476 0 None 3 2 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
CHEMBL1472830 10476 0 None 3 2 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
DB12708 10476 0 None 3 2 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
1883 9856 75 None -1 12 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
1916 9856 75 None -1 12 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
5280360 9856 75 None -1 12 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
913 9856 75 None -1 12 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
CHEMBL548 9856 75 None -1 12 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
DB00917 9856 75 None -1 12 Rat 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
5311232 9719 13 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 2 2 5.9 O=C(C(c1cccc2c1cccc2)C)Nc1ccccc1Cc1ccccc1C(=O)O 11782353
5824 9719 13 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 2 2 5.9 O=C(C(c1cccc2c1cccc2)C)Nc1ccccc1Cc1ccccc1C(=O)O 11782353
CHEMBL3260772 9719 13 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 2 2 5.9 O=C(C(c1cccc2c1cccc2)C)Nc1ccccc1Cc1ccccc1C(=O)O 11782353
15984632 9723 0 None - 1 Mouse 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 531 10 2 4 7.1 CC(CC(c1cccc2c1cccc2)C(=O)Nc1cc(ccc1Cc1ccccc1C(=O)O)Cn1cccn1)C 12538661
1943 9723 0 None - 1 Mouse 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 531 10 2 4 7.1 CC(CC(c1cccc2c1cccc2)C(=O)Nc1cc(ccc1Cc1ccccc1C(=O)O)Cn1cccn1)C 12538661
5823 9724 0 None - 1 Mouse 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 12 2 3 7.6 CC(C[C@H](c1cc(C)cc(c1)C)NC(=C)c1cc(ccc1CCC(=O)O)COc1ccccc1C)C 17512019
73755159 9724 0 None - 1 Mouse 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 12 2 3 7.6 CC(C[C@H](c1cc(C)cc(c1)C)NC(=C)c1cc(ccc1CCC(=O)O)COc1ccccc1C)C 17512019
5844 9041 0 None - 1 Human 8.4 pKB = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 569 7 1 4 6.4 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1cc(Cl)ccc1Cc1ccc2c(c1)cccc2)Br 18287210
9808643 9041 0 None - 1 Human 8.4 pKB = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 569 7 1 4 6.4 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1cc(Cl)ccc1Cc1ccc2c(c1)cccc2)Br 18287210




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
50902259 9713 1 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at EP3 (unknown origin)Agonist activity at EP3 (unknown origin)
ChEMBL 482 10 2 6 4.2 CC(OC(=O)CCC[C@H]1CC[C@H]2[C@@H](OC1)C[C@H]([C@@H]2/C=C/[C@H](COc1cc(F)ccc1F)O)O)C 10.1016/j.ejmech.2021.113842
9875 9713 1 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at EP3 (unknown origin)Agonist activity at EP3 (unknown origin)
ChEMBL 482 10 2 6 4.2 CC(OC(=O)CCC[C@H]1CC[C@H]2[C@@H](OC1)C[C@H]([C@@H]2/C=C/[C@H](COc1cc(F)ccc1F)O)O)C 10.1016/j.ejmech.2021.113842
CHEMBL4297633 9713 1 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at EP3 (unknown origin)Agonist activity at EP3 (unknown origin)
ChEMBL 482 10 2 6 4.2 CC(OC(=O)CCC[C@H]1CC[C@H]2[C@@H](OC1)C[C@H]([C@@H]2/C=C/[C@H](COc1cc(F)ccc1F)O)O)C 10.1016/j.ejmech.2021.113842
DB12043 9713 1 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at EP3 (unknown origin)Agonist activity at EP3 (unknown origin)
ChEMBL 482 10 2 6 4.2 CC(OC(=O)CCC[C@H]1CC[C@H]2[C@@H](OC1)C[C@H]([C@@H]2/C=C/[C@H](COc1cc(F)ccc1F)O)O)C 10.1016/j.ejmech.2021.113842
11294085 144030 0 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmcl.2015.12.039
CHEMBL3751951 144030 0 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmcl.2015.12.039
10045223 158746 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
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 378 10 3 4 3.3 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1CC#CCCCC(=O)O nan
CHEMBL3966610 158746 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
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 378 10 3 4 3.3 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1CC#CCCCC(=O)O nan
66857670 144179 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 436 9 2 7 3.3 CC#CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753268 144179 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 436 9 2 7 3.3 CC#CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
10409554 156300 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 156300 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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
11328569 144246 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 456 12 2 8 3.3 COCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753788 144246 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 456 12 2 8 3.3 COCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
127026652 144260 0 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 456 12 2 8 3.3 CCOCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753898 144260 0 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 456 12 2 8 3.3 CCOCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
66858111 144229 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 488 11 2 7 4.5 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCc3ccccc3)CCC2)n1 10.1016/j.bmcl.2015.12.039
CHEMBL3753622 144229 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 488 11 2 7 4.5 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCc3ccccc3)CCC2)n1 10.1016/j.bmcl.2015.12.039
68749980 195840 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP3 (unknown origin)Agonist activity at EP3 (unknown origin)
ChEMBL 440 9 3 5 3.3 O=C(O)CCC[C@H]1CC[C@@H]2[C@@H](/C=C/[C@@H](O)COc3cc(F)ccc3F)[C@H](O)C[C@@H]2OC1 10.1016/j.ejmech.2021.113842
CHEMBL5095395 195840 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP3 (unknown origin)Agonist activity at EP3 (unknown origin)
ChEMBL 440 9 3 5 3.3 O=C(O)CCC[C@H]1CC[C@@H]2[C@@H](/C=C/[C@@H](O)COc3cc(F)ccc3F)[C@H](O)C[C@@H]2OC1 10.1016/j.ejmech.2021.113842
59554822 144172 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 440 11 2 7 4.0 CCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753221 144172 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 440 11 2 7 4.0 CCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
127037150 144338 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 426 12 2 6 4.1 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3754586 144338 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 426 12 2 6 4.1 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
10339756 149863 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
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 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
CHEMBL3895324 149863 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
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 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
11362836 144074 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 446 12 2 7 3.8 CC(C)(CCCCF)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3752406 144074 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 446 12 2 7 3.8 CC(C)(CCCCF)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
59554824 144253 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 428 11 2 7 3.9 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3753853 144253 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 428 11 2 7 3.9 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
10023570 160115 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
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 394 12 2 5 4.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)OC nan
CHEMBL3978305 160115 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
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 394 12 2 5 4.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)OC nan
10000608 149193 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
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 392 10 2 5 3.4 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1CC#CCCCC(=O)OC nan
CHEMBL3889855 149193 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
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 392 10 2 5 3.4 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1CC#CCCCC(=O)OC nan
10046549 158514 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 400 10 3 4 3.6 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)Cc2ccccc2)[C@@H]1O nan
CHEMBL3964563 158514 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 400 10 3 4 3.6 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)Cc2ccccc2)[C@@H]1O nan
66857738 144078 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 468 10 2 7 4.7 CC(C)(C)CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3752435 144078 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 468 10 2 7 4.7 CC(C)(C)CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
10409554 156300 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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 156300 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
11156167 144298 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 494 11 2 7 5.2 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCC3CCCCC3)CCC2)n1 10.1016/j.bmcl.2015.12.039
CHEMBL3754197 144298 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 494 11 2 7 5.2 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCC3CCCCC3)CCC2)n1 10.1016/j.bmcl.2015.12.039
59554827 144071 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 426 11 2 6 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3752377 144071 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP3 receptorAgonist activity at human EP3 receptor
ChEMBL 426 11 2 6 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
46885984 15249 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 552 6 1 4 5.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1093897 15249 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 552 6 1 4 5.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
46885837 14468 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 572 6 1 4 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088780 14468 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 572 6 1 4 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
46885838 14524 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 604 6 1 4 6.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1089094 14524 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 604 6 1 4 6.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
46885839 14525 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 570 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1089095 14525 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 570 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
46885384 14669 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 554 6 1 4 5.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1090112 14669 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 554 6 1 4 5.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
46885786 14737 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 590 6 1 4 5.6 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1090501 14737 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 590 6 1 4 5.6 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
46885881 15159 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 554 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1093239 15159 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 554 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
46885946 15239 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 554 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1093843 15239 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 554 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
44570279 185119 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL465122 185119 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
46885432 14472 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1088815 14472 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
46885947 14688 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 586 6 1 4 6.3 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1090222 14688 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 586 6 1 4 6.3 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
46885688 14725 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090460 14725 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
46885503 15107 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1092871 15107 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
46885945 15199 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 572 6 1 4 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1093559 15199 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 572 6 1 4 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
44570190 184330 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 562 7 2 6 6.7 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL464032 184330 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 562 7 2 6 6.7 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
46885433 14475 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 518 6 1 4 4.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088822 14475 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 518 6 1 4 4.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
46885504 14482 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 502 6 1 4 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088848 14482 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 502 6 1 4 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
46885732 14573 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 530 6 1 4 5.7 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089454 14573 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 530 6 1 4 5.7 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
46885539 14840 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 542 6 1 5 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1091146 14840 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 542 6 1 5 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
46885604 14846 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1091164 14846 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2010.02.028
44570401 189853 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 542 8 2 7 5.6 COc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
CHEMBL479434 189853 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 542 8 2 7 5.6 COc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
46885434 14476 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 550 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088823 14476 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 550 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
46885650 14537 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 548 6 1 4 5.8 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089161 14537 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 548 6 1 4 5.8 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
46885651 14585 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 568 6 1 4 5.6 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089491 14585 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 568 6 1 4 5.6 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
46885343 14986 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 534 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1092230 14986 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 534 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
46885501 14480 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 516 6 1 4 5.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088846 14480 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 516 6 1 4 5.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
46885733 14574 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 564 6 1 4 6.3 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089455 14574 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 564 6 1 4 6.3 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
46885687 14724 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 532 6 1 4 5.3 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090459 14724 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 532 6 1 4 5.3 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2010.02.028
46885735 15140 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 552 6 2 5 4.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1093125 15140 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 552 6 2 5 4.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
46885689 15227 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 550 6 1 5 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1093790 15227 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 550 6 1 5 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
44570230 185199 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 518 8 2 6 5.4 COc1ccc(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(Sc4ccc5ccccc5c4)c23)cc1 10.1016/j.bmcl.2008.11.007
CHEMBL465947 185199 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 518 8 2 6 5.4 COc1ccc(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(Sc4ccc5ccccc5c4)c23)cc1 10.1016/j.bmcl.2008.11.007
46885385 14670 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1090113 14670 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
46885538 14839 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 522 6 1 4 4.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1091145 14839 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 522 6 1 4 4.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
44570036 185228 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 524 7 2 5 5.6 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2008.11.007
CHEMBL466184 185228 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 524 7 2 5 5.6 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2008.11.007
46885502 14481 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 504 6 1 4 3.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088847 14481 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 504 6 1 4 3.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
46885649 14738 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 582 6 1 4 6.5 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090507 14738 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 582 6 1 4 6.5 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
46885734 15139 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1093124 15139 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
46885690 15228 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 516 6 2 5 4.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1093791 15228 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 516 6 2 5 4.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
1883 9856 75 None -1 24 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 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 9856 75 None -1 24 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 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 9856 75 None -1 24 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 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 9856 75 None -1 24 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 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 9856 75 None -1 24 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 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 9856 75 None -1 24 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 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
46879758 12952 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 585 6 1 6 8.1 Cc1cn(Cc2ccc3ccccc3c2)c2c(-c3cc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1081185 12952 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 585 6 1 6 8.1 Cc1cn(Cc2ccc3ccccc3c2)c2c(-c3cc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
46879894 12953 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 565 6 1 5 7.2 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1081186 12953 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 565 6 1 5 7.2 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
46879895 12954 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 547 6 1 5 7.0 Cc1cn(Cc2ccc3ccccc3c2)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1081187 12954 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 547 6 1 5 7.0 Cc1cn(Cc2ccc3ccccc3c2)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
46879859 13022 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 597 6 1 5 8.2 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4ccc(Cl)c(Cl)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1081545 13022 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 597 6 1 5 8.2 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4ccc(Cl)c(Cl)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44627718 205724 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 514 7 1 5 4.9 COc1cccc(Cn2cc(C)c3cc(F)cc(/C=C/C(=O)NS(=O)(=O)c4ccc(F)c(F)c4)c32)c1 10.1021/jm9005912
CHEMBL584904 205724 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 514 7 1 5 4.9 COc1cccc(Cn2cc(C)c3cc(F)cc(/C=C/C(=O)NS(=O)(=O)c4ccc(F)c(F)c4)c32)c1 10.1021/jm9005912
46885656 15141 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 564 6 1 5 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1093133 15141 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 564 6 1 5 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
44627395 203651 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL565992 203651 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44627395 203651 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL565992 203651 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
46885840 14887 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 570 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1091606 14887 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 570 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.02.028
25181432 198425 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL519598 198425 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570147 190854 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 548 9 2 7 5.4 COc1ccc(OC)c(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(Sc4ccc5ccccc5c4)c23)c1 10.1016/j.bmcl.2008.11.007
CHEMBL482379 190854 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 548 9 2 7 5.4 COc1ccc(OC)c(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(Sc4ccc5ccccc5c4)c23)c1 10.1016/j.bmcl.2008.11.007
46885386 15230 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 568 6 1 4 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1093797 15230 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 568 6 1 4 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
44570281 197599 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 540 7 2 6 6.2 Cc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c(C)c1 10.1016/j.bmcl.2008.11.007
CHEMBL518396 197599 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 540 7 2 6 6.2 Cc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c(C)c1 10.1016/j.bmcl.2008.11.007
25181432 198425 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL519598 198425 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
45488100 203686 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 562 6 1 7 5.7 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL566202 203686 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 562 6 1 7 5.7 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
46885387 14469 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 556 6 1 5 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1088785 14469 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 556 6 1 5 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
46886028 14888 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 540 6 1 4 4.4 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1091621 14888 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 540 6 1 4 4.4 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
46886029 14889 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 572 6 1 4 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1091622 14889 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 572 6 1 4 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
44570148 190855 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 522 7 2 5 6.0 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1Cl 10.1016/j.bmcl.2008.11.007
CHEMBL482380 190855 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 522 7 2 5 6.0 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1Cl 10.1016/j.bmcl.2008.11.007
44570950 190209 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 536 6 1 4 4.6 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL479868 190209 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 536 6 1 4 4.6 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
46885655 14722 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 514 6 1 5 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1090455 14722 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 514 6 1 5 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
46885691 15229 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 534 6 2 5 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1093792 15229 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 534 6 2 5 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
44570398 199150 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 572 9 2 8 5.6 COc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1OC 10.1016/j.bmcl.2008.11.007
CHEMBL520741 199150 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 572 9 2 8 5.6 COc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1OC 10.1016/j.bmcl.2008.11.007
44570604 189845 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 594 7 2 7 5.4 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL479427 189845 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 594 7 2 7 5.4 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570314 190320 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 564 7 2 6 6.4 O=C(COc1cccc2[nH]cc(Sc3ccc(F)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480011 190320 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 564 7 2 6 6.4 O=C(COc1cccc2[nH]cc(Sc3ccc(F)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570870 190614 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 542 7 1 4 4.8 CC12CCCC(CCC(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL480635 190614 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 542 7 1 4 4.8 CC12CCCC(CCC(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44564890 186815 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 519 6 1 6 5.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ncccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL474751 186815 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 519 6 1 6 5.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ncccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
46885984 15249 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 552 6 1 4 5.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1093897 15249 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 552 6 1 4 5.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
44570280 184536 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 548 7 2 6 5.9 O=C(COc1cccc2[nH]cc(Sc3ccc(F)cc3F)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL464271 184536 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 548 7 2 6 5.9 O=C(COc1cccc2[nH]cc(Sc3ccc(F)cc3F)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
11657311 12669 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 604 6 1 7 7.7 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1079555 12669 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 604 6 1 7 7.7 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44570232 184362 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 488 7 2 5 5.4 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.11.007
CHEMBL464063 184362 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 488 7 2 5 5.4 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.11.007
46885432 14472 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1088815 14472 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
44570445 185185 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 566 7 2 8 5.5 Cn1c(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)nc2ccccc21 10.1016/j.bmcl.2008.11.007
CHEMBL465923 185185 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 566 7 2 8 5.5 Cn1c(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)nc2ccccc21 10.1016/j.bmcl.2008.11.007
44570004 185605 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 596 7 2 7 5.0 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(F)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL469303 185605 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 596 7 2 7 5.0 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(F)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570950 190209 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 536 6 1 4 4.6 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL479868 190209 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 536 6 1 4 4.6 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
44564771 197692 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 512 7 1 6 5.7 COc1ccc(S(=O)(=O)NC(=O)/C=C/c2cn(C)c3cccc(Oc4ccc5ccccc5c4)c23)cc1 10.1016/j.bmcl.2008.12.112
CHEMBL518522 197692 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 512 7 1 6 5.7 COc1ccc(S(=O)(=O)NC(=O)/C=C/c2cn(C)c3cccc(Oc4ccc5ccccc5c4)c23)cc1 10.1016/j.bmcl.2008.12.112
10047541 139288 0 None - 0 Human 6.0 pIC50 = 6 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
ChEMBL 416 13 4 6 3.8 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccs1 10.1021/jm990542v
CHEMBL369797 139288 0 None - 0 Human 6.0 pIC50 = 6 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
ChEMBL 416 13 4 6 3.8 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccs1 10.1021/jm990542v
44627070 203547 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 437 6 1 6 4.0 Cc1cn(Cc2ccccn2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc12 10.1021/jm9005912
CHEMBL565384 203547 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 437 6 1 6 4.0 Cc1cn(Cc2ccccn2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc12 10.1021/jm9005912
46880037 14269 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 530 5 1 5 7.0 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NC(=O)c4ccc(F)cc4F)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1087149 14269 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 530 5 1 5 7.0 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NC(=O)c4ccc(F)cc4F)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
46879858 12637 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 579 6 1 5 8.1 Cc1cn(Cc2ccc3ccccc3c2)c2c(-c3cc(NS(=O)(=O)c4ccc(Cl)c(Cl)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1079381 12637 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 579 6 1 5 8.1 Cc1cn(Cc2ccc3ccccc3c2)c2c(-c3cc(NS(=O)(=O)c4ccc(Cl)c(Cl)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
11296282 8191 32 None - 1 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
5822 8191 32 None - 1 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
CHEMBL565591 8191 32 None - 1 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
44570911 186128 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 616 7 1 6 4.8 COC(=O)C12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL473655 186128 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 616 7 1 6 4.8 COC(=O)C12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
44570191 196627 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 604 9 2 9 4.3 COc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1OC 10.1016/j.bmcl.2008.11.007
CHEMBL516686 196627 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 604 9 2 9 4.3 COc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1OC 10.1016/j.bmcl.2008.11.007
46885541 14544 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 578 8 3 6 3.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(CO)CO)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1089313 14544 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 578 8 3 6 3.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(CO)CO)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
46885882 15160 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 592 6 1 5 6.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1093240 15160 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 592 6 1 5 6.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44570152 199326 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 595 7 2 8 4.8 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL521103 199326 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 595 7 2 8 4.8 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44564804 183479 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL459885 183479 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
44564649 183534 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL460322 183534 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44570047 196169 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 574 8 2 8 4.3 COc1ccccc1S(=O)(=O)c1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
CHEMBL512993 196169 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 574 8 2 8 4.3 COc1ccccc1S(=O)(=O)c1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
44564726 183703 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL461980 183703 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
1884 9857 52 None -11 22 Human 7.0 pIC50 = 7.0 Binding
In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand
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 10.1021/jm010264b
5280363 9857 52 None -11 22 Human 7.0 pIC50 = 7.0 Binding
In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand
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 10.1021/jm010264b
912 9857 52 None -11 22 Human 7.0 pIC50 = 7.0 Binding
In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand
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 10.1021/jm010264b
CHEMBL815 9857 52 None -11 22 Human 7.0 pIC50 = 7.0 Binding
In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand
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 10.1021/jm010264b
DB12789 9857 52 None -11 22 Human 7.0 pIC50 = 7.0 Binding
In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand
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 10.1021/jm010264b
44564770 184625 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)cc2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL464411 184625 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)cc2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44627173 205745 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 506 7 1 5 5.8 Cc1cn(Cc2ccc3ccccc3c2)c2c(CCC(=O)NS(=O)(=O)c3cccs3)cc(F)cc12 10.1021/jm9005912
CHEMBL585100 205745 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 506 7 1 5 5.8 Cc1cn(Cc2ccc3ccccc3c2)c2c(CCC(=O)NS(=O)(=O)c3cccs3)cc(F)cc12 10.1021/jm9005912
44564686 184171 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)cc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL463816 184171 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)cc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44564725 183702 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cccc(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL461979 183702 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cccc(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
46879998 12642 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 551 6 1 5 6.3 Cc1cn(Cc2ccc(F)c(F)c2)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4F)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1079409 12642 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 551 6 1 5 6.3 Cc1cn(Cc2ccc(F)c(F)c2)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4F)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
46885654 14721 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 570 6 1 6 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1090454 14721 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 570 6 1 6 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44564571 193594 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL489310 193594 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
46885656 15141 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 564 6 1 5 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1093133 15141 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 564 6 1 5 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
44571354 190848 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 516 7 1 5 4.2 COc1cccc(CN2C(=O)CC3(C)CCCC(/C=C/C(=O)NS(=O)(=O)c4ccc(F)c(F)c4)=C23)c1 10.1016/j.bmcl.2008.12.027
CHEMBL482330 190848 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 516 7 1 5 4.2 COc1cccc(CN2C(=O)CC3(C)CCCC(/C=C/C(=O)NS(=O)(=O)c4ccc(F)c(F)c4)=C23)c1 10.1016/j.bmcl.2008.12.027
44570604 189845 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 594 7 2 7 5.4 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL479427 189845 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 594 7 2 7 5.4 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570188 199164 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 507 7 2 7 5.0 Cc1noc(C)c1S(=O)(=O)NC(=O)COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12 10.1016/j.bmcl.2008.11.007
CHEMBL520757 199164 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 507 7 2 7 5.0 Cc1noc(C)c1S(=O)(=O)NC(=O)COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12 10.1016/j.bmcl.2008.11.007
44190762 183659 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of prostanoid EP3 receptorInhibition of prostanoid EP3 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
CHEMBL461571 183659 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of prostanoid EP3 receptorInhibition of prostanoid EP3 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
44564841 187143 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475152 187143 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
46885986 14815 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 552 6 1 4 5.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1090889 14815 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 552 6 1 4 5.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.02.028
11495634 21677 13 None - 4 Human 5.9 pIC50 = 5.9 Binding
Inhibition of EP3 receptor by FLIPR assayInhibition of EP3 receptor by FLIPR assay
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2009.02.112
CHEMBL1207972 21677 13 None - 4 Human 5.9 pIC50 = 5.9 Binding
Inhibition of EP3 receptor by FLIPR assayInhibition of EP3 receptor by FLIPR assay
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2009.02.112
CHEMBL467114 21677 13 None - 4 Human 5.9 pIC50 = 5.9 Binding
Inhibition of EP3 receptor by FLIPR assayInhibition of EP3 receptor by FLIPR assay
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2009.02.112
44565044 199847 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 538 6 1 7 4.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3cnc4ccccc4n3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL522435 199847 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 538 6 1 7 4.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3cnc4ccccc4n3)cccc21 10.1016/j.bmcl.2008.12.112
44564890 186815 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 519 6 1 6 5.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ncccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL474751 186815 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 519 6 1 6 5.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ncccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
46885577 14572 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 546 6 1 7 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C21OCCO1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
CHEMBL1089446 14572 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 546 6 1 7 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C21OCCO1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
44570316 190818 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 542 8 2 7 5.6 COc1ccccc1Sc1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
CHEMBL482177 190818 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 542 8 2 7 5.6 COc1ccccc1Sc1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
44571292 190791 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 558 6 1 5 5.9 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)s3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL481987 190791 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 558 6 1 5 5.9 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)s3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
44570315 190323 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 546 7 2 6 6.2 O=C(COc1cccc2[nH]cc(Sc3ccccc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480012 190323 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 546 7 2 6 6.2 O=C(COc1cccc2[nH]cc(Sc3ccccc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
46885653 14668 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 502 6 1 6 4.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
CHEMBL1090102 14668 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 502 6 1 6 4.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
44570640 185182 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 580 7 2 7 4.5 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(F)cc3F)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL465915 185182 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 580 7 2 7 4.5 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(F)cc3F)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44627622 203614 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 570 6 1 4 6.4 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cc(F)cc12 10.1021/jm9005912
CHEMBL565791 203614 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 570 6 1 4 6.4 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cc(F)cc12 10.1021/jm9005912
44564842 186015 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL472758 186015 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
44570607 190763 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 520 7 2 6 4.0 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.11.007
CHEMBL481783 190763 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 520 7 2 6 4.0 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.11.007
46880001 12737 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 562 5 1 5 8.1 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NC(=O)c4ccc(Cl)cc4Cl)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1079937 12737 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 562 5 1 5 8.1 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NC(=O)c4ccc(Cl)cc4Cl)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44570147 190854 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 548 9 2 7 5.4 COc1ccc(OC)c(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(Sc4ccc5ccccc5c4)c23)c1 10.1016/j.bmcl.2008.11.007
CHEMBL482379 190854 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 548 9 2 7 5.4 COc1ccc(OC)c(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(Sc4ccc5ccccc5c4)c23)c1 10.1016/j.bmcl.2008.11.007
46885606 14580 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 588 6 1 6 5.6 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2=O)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1089481 14580 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 588 6 1 6 5.6 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2=O)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44626882 203657 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 466 6 1 7 4.0 O=C(/C=C/c1cccc2ccn(Cc3ccc4c(c3)OCO4)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL566015 203657 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 466 6 1 7 4.0 O=C(/C=C/c1cccc2ccn(Cc3ccc4c(c3)OCO4)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44627399 203757 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 504 6 1 5 5.9 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cc(F)cc12 10.1021/jm9005912
CHEMBL566631 203757 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 504 6 1 5 5.9 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cc(F)cc12 10.1021/jm9005912
44626975 203578 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 504 6 1 5 5.9 Cc1cn(Cc2ccc(Cl)c(Cl)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc12 10.1021/jm9005912
CHEMBL565597 203578 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 504 6 1 5 5.9 Cc1cn(Cc2ccc(Cl)c(Cl)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc12 10.1021/jm9005912
44570193 184940 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 578 7 2 7 4.9 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)cc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL464905 184940 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 578 7 2 7 4.9 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)cc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44627719 203758 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 503 6 1 6 4.5 Cc1noc(C)c1Cn1cc(C)c2cc(F)cc(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)c21 10.1021/jm9005912
CHEMBL566643 203758 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 503 6 1 6 4.5 Cc1noc(C)c1Cn1cc(C)c2cc(F)cc(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)c21 10.1021/jm9005912
44570525 196630 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 588 7 2 6 5.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2008.11.007
CHEMBL516708 196630 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 588 7 2 6 5.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2008.11.007
44627398 203828 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 599 6 2 6 5.2 CN1C(=O)C(NC(=O)c2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
CHEMBL567266 203828 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 599 6 2 6 5.2 CN1C(=O)C(NC(=O)c2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
44564842 186015 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL472758 186015 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
44627718 205724 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 514 7 1 5 4.9 COc1cccc(Cn2cc(C)c3cc(F)cc(/C=C/C(=O)NS(=O)(=O)c4ccc(F)c(F)c4)c32)c1 10.1021/jm9005912
CHEMBL584904 205724 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 514 7 1 5 4.9 COc1cccc(Cn2cc(C)c3cc(F)cc(/C=C/C(=O)NS(=O)(=O)c4ccc(F)c(F)c4)c32)c1 10.1021/jm9005912
46885654 14721 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 570 6 1 6 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1090454 14721 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 570 6 1 6 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44571319 190812 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 536 6 1 4 5.4 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)cc3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL482156 190812 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 536 6 1 4 5.4 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)cc3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
25181432 198425 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptorDisplacement of [3H]PGE2 from mouse EP3 receptor
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL519598 198425 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptorDisplacement of [3H]PGE2 from mouse EP3 receptor
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44564572 193785 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cccc(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL490692 193785 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cccc(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44157014 199396 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL521609 199396 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44564650 196641 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)cc2Cl)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL516789 196641 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)cc2Cl)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44564991 193813 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL490896 193813 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
44627283 203859 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 524 6 1 6 4.2 O=C(/C=C/c1cccc2c1N(S(=O)(=O)c1ccc3ccccc3c1)CC2)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL567484 203859 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 524 6 1 6 4.2 O=C(/C=C/c1cccc2c1N(S(=O)(=O)c1ccc3ccccc3c1)CC2)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44564687 184767 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)ccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL464618 184767 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)ccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44564724 196873 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)cc(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL517282 196873 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)cc(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44570485 196815 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 556 7 2 6 4.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2008.11.007
CHEMBL517180 196815 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 556 7 2 6 4.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2008.11.007
46886027 15125 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 558 6 1 4 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1092991 15125 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 558 6 1 4 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
44570235 184376 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 544 7 2 7 4.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccccc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL464074 184376 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 544 7 2 7 4.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccccc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44564893 187302 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475349 187302 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
44565043 200005 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 537 6 1 6 5.5 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc4ncccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL523608 200005 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 537 6 1 6 5.5 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc4ncccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44564648 183533 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccccc2Cl)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL460321 183533 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccccc2Cl)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44627285 205782 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 584 6 2 7 5.9 Cn1nc(NC(=O)c2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
CHEMBL585582 205782 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 584 6 2 7 5.9 Cn1nc(NC(=O)c2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
46885689 15227 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 550 6 1 5 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1093790 15227 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 550 6 1 5 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
44564725 183702 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cccc(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL461979 183702 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cccc(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
10045223 158746 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 378 10 3 4 3.3 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1CC#CCCCC(=O)O nan
CHEMBL3966610 158746 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 378 10 3 4 3.3 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1CC#CCCCC(=O)O nan
45488095 203831 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 390 6 1 6 3.4 O=C(Cc1csc(/C=C/c2ccccc2)n1)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL567273 203831 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 390 6 1 6 3.4 O=C(Cc1csc(/C=C/c2ccccc2)n1)NS(=O)(=O)c1cccs1 10.1021/jm9005912
46880091 14423 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 435 5 1 5 4.4 Cc1cn(Cc2ccc(F)cc2F)c2c(-c3cc(NS(C)(=O)=O)on3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1088322 14423 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 435 5 1 5 4.4 Cc1cn(Cc2ccc(F)cc2F)c2c(-c3cc(NS(C)(=O)=O)on3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44564992 193814 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL490897 193814 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
44570280 184536 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 548 7 2 6 5.9 O=C(COc1cccc2[nH]cc(Sc3ccc(F)cc3F)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL464271 184536 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 548 7 2 6 5.9 O=C(COc1cccc2[nH]cc(Sc3ccc(F)cc3F)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44564648 183533 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccccc2Cl)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL460321 183533 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccccc2Cl)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44564807 184630 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 504 6 1 5 5.0 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL464414 184630 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 504 6 1 5 5.0 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
44570486 184510 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 580 9 2 8 4.1 COc1ccc(OC)c(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(S(=O)(=O)c4ccc5ccccc5c4)c23)c1 10.1016/j.bmcl.2008.11.007
CHEMBL464237 184510 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 580 9 2 8 4.1 COc1ccc(OC)c(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(S(=O)(=O)c4ccc5ccccc5c4)c23)c1 10.1016/j.bmcl.2008.11.007
44570152 199326 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 595 7 2 8 4.8 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL521103 199326 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 595 7 2 8 4.8 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570995 190857 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 540 6 1 5 6.2 Cc1cn(Cc2ccc(F)cc2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL482390 190857 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 540 6 1 5 6.2 Cc1cn(Cc2ccc(F)cc2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
44564647 183286 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)cc2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL459688 183286 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)cc2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
46885541 14544 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 578 8 3 6 3.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(CO)CO)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1089313 14544 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 578 8 3 6 3.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(CO)CO)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
46885690 15228 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 516 6 2 5 4.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1093791 15228 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 516 6 2 5 4.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
44570047 196169 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 574 8 2 8 4.3 COc1ccccc1S(=O)(=O)c1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
CHEMBL512993 196169 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 574 8 2 8 4.3 COc1ccccc1S(=O)(=O)c1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
44564806 184626 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 504 6 1 5 5.0 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL464413 184626 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 504 6 1 5 5.0 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
46879759 12990 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 584 6 1 6 7.0 Cc1cn(Cc2ccc(F)c(F)c2)c2c(-c3cc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)nn3C)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1081360 12990 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 584 6 1 6 7.0 Cc1cn(Cc2ccc(F)c(F)c2)c2c(-c3cc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)nn3C)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44570638 190573 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 566 7 2 10 3.4 Cc1nnc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480416 190573 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 566 7 2 10 3.4 Cc1nnc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)s1 10.1016/j.bmcl.2008.11.007
46879802 12760 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 584 6 1 6 6.7 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NS(=O)(=O)c4cc(F)c(F)cc4F)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1080106 12760 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 584 6 1 6 6.7 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NS(=O)(=O)c4cc(F)c(F)cc4F)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
46879718 12840 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 613 6 1 5 8.7 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3ccc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)nc3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1080619 12840 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 613 6 1 5 8.7 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3ccc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)nc3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44570189 184327 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 522 7 2 5 6.0 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2008.11.007
CHEMBL464031 184327 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 522 7 2 5 6.0 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2008.11.007
44570036 185228 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 524 7 2 5 5.6 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2008.11.007
CHEMBL466184 185228 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 524 7 2 5 5.6 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2008.11.007
44627621 203652 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 552 6 1 4 6.2 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)cc(F)cc12 10.1021/jm9005912
CHEMBL566005 203652 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 552 6 1 4 6.2 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)cc(F)cc12 10.1021/jm9005912
44626877 205781 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 490 6 1 5 5.6 O=C(/C=C/c1cccc2ccn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL585581 205781 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 490 6 1 5 5.6 O=C(/C=C/c1cccc2ccn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44626877 205781 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting
ChEMBL 490 6 1 5 5.6 O=C(/C=C/c1cccc2ccn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL585581 205781 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting
ChEMBL 490 6 1 5 5.6 O=C(/C=C/c1cccc2ccn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
25181438 190634 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptorDisplacement of [3H]PGE2 from mouse EP3 receptor
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480809 190634 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptorDisplacement of [3H]PGE2 from mouse EP3 receptor
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570232 184362 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 488 7 2 5 5.4 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.11.007
CHEMBL464063 184362 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 488 7 2 5 5.4 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.11.007
44571245 189725 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 558 6 1 5 5.9 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1cccc(Cl)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479275 189725 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 558 6 1 5 5.9 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1cccc(Cl)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44627174 203658 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 576 7 1 6 7.3 Cc1cn(CCC(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)c2c(Oc3ccc4ccccc4c3)cc(F)cc12 10.1021/jm9005912
CHEMBL566016 203658 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 576 7 1 6 7.3 Cc1cn(CCC(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)c2c(Oc3ccc4ccccc4c3)cc(F)cc12 10.1021/jm9005912
44570189 184327 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 522 7 2 5 6.0 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2008.11.007
CHEMBL464031 184327 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 522 7 2 5 6.0 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2008.11.007
44571244 190415 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 592 6 1 5 6.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL480251 190415 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 592 6 1 5 6.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
44627720 203684 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 524 6 1 6 4.6 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cc(F)cc12 10.1021/jm9005912
CHEMBL566197 203684 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 524 6 1 6 4.6 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cc(F)cc12 10.1021/jm9005912
46885540 14620 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 616 8 3 7 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(CO)CO)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1089780 14620 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 616 8 3 7 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(CO)CO)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44570150 190732 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 556 7 2 5 6.7 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2008.11.007
CHEMBL481589 190732 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 556 7 2 5 6.7 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2008.11.007
44627073 203934 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 542 7 2 4 6.7 O=C(CCc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL567905 203934 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 542 7 2 4 6.7 O=C(CCc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
46885602 14627 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 520 6 1 5 5.2 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089806 14627 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 520 6 1 5 5.2 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc21 10.1016/j.bmcl.2010.02.028
44570445 185185 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 566 7 2 8 5.5 Cn1c(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)nc2ccccc21 10.1016/j.bmcl.2008.11.007
CHEMBL465923 185185 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 566 7 2 8 5.5 Cn1c(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)nc2ccccc21 10.1016/j.bmcl.2008.11.007
44570667 190770 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 504 6 1 4 4.3 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(F)cc1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL481823 190770 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 504 6 1 4 4.3 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(F)cc1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44627071 205686 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 540 6 2 4 6.8 O=C(/C=C/c1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL584492 205686 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 540 6 2 4 6.8 O=C(/C=C/c1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44627074 205799 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 556 7 1 5 6.7 Cn1cc(Cc2ccc3ccccc3c2)c2c(CCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
CHEMBL585766 205799 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 556 7 1 5 6.7 Cn1cc(Cc2ccc3ccccc3c2)c2c(CCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
44564892 187301 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475348 187301 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
44570314 190320 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 564 7 2 6 6.4 O=C(COc1cccc2[nH]cc(Sc3ccc(F)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480011 190320 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 564 7 2 6 6.4 O=C(COc1cccc2[nH]cc(Sc3ccc(F)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44627072 203727 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 554 6 1 5 6.8 Cn1cc(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
CHEMBL566421 203727 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 554 6 1 5 6.8 Cn1cc(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
46885985 14814 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 536 6 1 4 5.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1090888 14814 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 536 6 1 4 5.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
44570353 190730 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 513 7 2 7 5.0 O=C(COc1cccc2[nH]cc(Sc3ccccn3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL481582 190730 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 513 7 2 7 5.0 O=C(COc1cccc2[nH]cc(Sc3ccccn3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
46885732 14573 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 530 6 1 4 5.7 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089454 14573 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 530 6 1 4 5.7 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
46885341 14938 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 574 6 1 5 6.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1091893 14938 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 574 6 1 5 6.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
46879896 12783 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 566 6 1 6 6.6 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NS(=O)(=O)c4ccc(F)c(F)c4)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1080281 12783 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 566 6 1 6 6.6 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NS(=O)(=O)c4ccc(F)c(F)c4)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
46885687 14724 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 532 6 1 4 5.3 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090459 14724 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 532 6 1 4 5.3 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2010.02.028
44570004 185605 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 596 7 2 7 5.0 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(F)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL469303 185605 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 596 7 2 7 5.0 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(F)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570910 196326 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 598 7 1 6 4.7 COC(=O)C12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL514311 196326 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 598 7 1 6 4.7 COC(=O)C12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
46885882 15160 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 592 6 1 5 6.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1093240 15160 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 592 6 1 5 6.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44409910 147687 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(-c3ccccc3)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL382197 147687 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(-c3ccccc3)c2)s1 10.1016/j.bmcl.2006.01.018
46885883 14603 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 524 6 1 5 5.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
CHEMBL1089555 14603 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 524 6 1 5 5.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
44627830 203729 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 524 6 1 6 4.6 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)cc(F)cc12 10.1021/jm9005912
CHEMBL566429 203729 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 524 6 1 6 4.6 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)cc(F)cc12 10.1021/jm9005912
44564935 186973 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 522 6 1 5 5.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL474949 186973 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 522 6 1 5 5.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
44564770 184625 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)cc2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL464411 184625 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)cc2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44564891 196596 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 7 4.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3cnc4ccccc4n3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL516394 196596 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 7 4.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3cnc4ccccc4n3)cccc21 10.1016/j.bmcl.2008.12.112
44627173 205745 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 506 7 1 5 5.8 Cc1cn(Cc2ccc3ccccc3c2)c2c(CCC(=O)NS(=O)(=O)c3cccs3)cc(F)cc12 10.1021/jm9005912
CHEMBL585100 205745 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 506 7 1 5 5.8 Cc1cn(Cc2ccc3ccccc3c2)c2c(CCC(=O)NS(=O)(=O)c3cccs3)cc(F)cc12 10.1021/jm9005912
44570401 189853 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 542 8 2 7 5.6 COc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
CHEMBL479434 189853 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 542 8 2 7 5.6 COc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
44626882 203657 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 466 6 1 7 4.0 O=C(/C=C/c1cccc2ccn(Cc3ccc4c(c3)OCO4)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL566015 203657 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 466 6 1 7 4.0 O=C(/C=C/c1cccc2ccn(Cc3ccc4c(c3)OCO4)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44627398 203828 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 599 6 2 6 5.2 CN1C(=O)C(NC(=O)c2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
CHEMBL567266 203828 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 599 6 2 6 5.2 CN1C(=O)C(NC(=O)c2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
44564840 187142 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475151 187142 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
46885431 14471 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 488 6 1 5 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
CHEMBL1088814 14471 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 488 6 1 5 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
44564804 183479 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL459885 183479 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
46885603 14628 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 588 6 1 5 6.5 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089807 14628 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 588 6 1 5 6.5 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1016/j.bmcl.2010.02.028
30897313 128376 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [3H]-PGE2 from human EP3 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP3 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 128376 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [3H]-PGE2 from human EP3 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP3 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
44570153 190633 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 535 7 3 9 2.4 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3nc[nH]n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480808 190633 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 535 7 3 9 2.4 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3nc[nH]n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
46885785 14736 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 542 6 1 5 5.2 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
CHEMBL1090500 14736 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 542 6 1 5 5.2 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
46879719 12698 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 604 6 1 7 7.7 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1079732 12698 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 604 6 1 7 7.7 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44570316 190818 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 542 8 2 7 5.6 COc1ccccc1Sc1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
CHEMBL482177 190818 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 542 8 2 7 5.6 COc1ccccc1Sc1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
44570282 184535 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 572 9 2 8 5.6 COc1ccc(OC)c(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
CHEMBL464270 184535 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 572 9 2 8 5.6 COc1ccc(OC)c(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
44570282 184535 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 572 9 2 8 5.6 COc1ccc(OC)c(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
CHEMBL464270 184535 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 572 9 2 8 5.6 COc1ccc(OC)c(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
46885540 14620 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 616 8 3 7 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(CO)CO)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1089780 14620 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 616 8 3 7 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(CO)CO)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
46880039 14208 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 574 5 1 7 7.1 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NC(=O)c4ccc5c(c4)OC(F)(F)O5)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1086634 14208 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 574 5 1 7 7.1 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NC(=O)c4ccc5c(c4)OC(F)(F)O5)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44626976 205741 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 490 6 1 5 5.3 O=C(/C=C/c1cccc2ccn(Cc3cccc(C(F)(F)F)c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL585091 205741 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 490 6 1 5 5.3 O=C(/C=C/c1cccc2ccn(Cc3cccc(C(F)(F)F)c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
46885840 14887 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 570 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1091606 14887 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 570 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.02.028
46886028 14888 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 540 6 1 4 4.4 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1091621 14888 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 540 6 1 4 4.4 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
46880040 14226 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 468 5 1 6 4.9 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NS(C)(=O)=O)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1086762 14226 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 468 5 1 6 4.9 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NS(C)(=O)=O)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44565193 183639 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL461390 183639 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
46885653 14668 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 502 6 1 6 4.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
CHEMBL1090102 14668 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 502 6 1 6 4.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
44570993 190338 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 532 7 1 5 5.1 COc1cccc(Cn2cc(C)c3cc(F)cc(/C=C/C(=O)NS(=O)(=O)c4cc(F)c(F)cc4F)c32)c1 10.1021/jm9005912
CHEMBL480029 190338 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 532 7 1 5 5.1 COc1cccc(Cn2cc(C)c3cc(F)cc(/C=C/C(=O)NS(=O)(=O)c4cc(F)c(F)cc4F)c32)c1 10.1021/jm9005912
44570912 190686 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 538 6 1 4 5.4 Cc1cn(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cc(F)cc12 10.1021/jm9005912
CHEMBL481228 190686 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 538 6 1 4 5.4 Cc1cn(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cc(F)cc12 10.1021/jm9005912
44627284 203580 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 504 7 1 7 4.1 O=C(COc1cccc2ccc(=O)n(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL565604 203580 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 504 7 1 7 4.1 O=C(COc1cccc2ccc(=O)n(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44570562 190649 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 556 7 2 6 4.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2008.11.007
CHEMBL480992 190649 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 556 7 2 6 4.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2008.11.007
46885985 14814 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 536 6 1 4 5.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1090888 14814 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 536 6 1 4 5.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
44564805 197492 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 502 6 1 5 5.4 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL518237 197492 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 502 6 1 5 5.4 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3)cccc21 10.1016/j.bmcl.2008.12.112
44570149 198863 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 494 7 2 6 5.4 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2008.11.007
CHEMBL520290 198863 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 494 7 2 6 5.4 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2008.11.007
44570279 185119 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL465122 185119 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 580 7 2 6 6.9 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44627285 205782 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 584 6 2 7 5.9 Cn1nc(NC(=O)c2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
CHEMBL585582 205782 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 584 6 2 7 5.9 Cn1nc(NC(=O)c2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
44570192 184345 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 601 9 3 8 3.3 NC(=O)Cc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
CHEMBL464042 184345 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 601 9 3 8 3.3 NC(=O)Cc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
44626977 205666 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 490 6 1 5 5.3 O=C(/C=C/c1cccc2ccn(Cc3ccccc3C(F)(F)F)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL584279 205666 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 490 6 1 5 5.3 O=C(/C=C/c1cccc2ccn(Cc3ccccc3C(F)(F)F)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44627174 203658 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 576 7 1 6 7.3 Cc1cn(CCC(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)c2c(Oc3ccc4ccccc4c3)cc(F)cc12 10.1021/jm9005912
CHEMBL566016 203658 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 576 7 1 6 7.3 Cc1cn(CCC(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)c2c(Oc3ccc4ccccc4c3)cc(F)cc12 10.1021/jm9005912
44627282 203798 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 595 7 1 8 5.7 O=C(COc1cccc2occ(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL567051 203798 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 595 7 1 8 5.7 O=C(COc1cccc2occ(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44129707 183535 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL460325 183535 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44626877 205781 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 490 6 1 5 5.6 O=C(/C=C/c1cccc2ccn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL585581 205781 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 490 6 1 5 5.6 O=C(/C=C/c1cccc2ccn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44627172 203728 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 437 6 1 6 4.0 Cc1cn(Cc2cccnc2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc12 10.1021/jm9005912
CHEMBL566423 203728 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 437 6 1 6 4.0 Cc1cn(Cc2cccnc2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc12 10.1021/jm9005912
44570872 190045 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 604 7 1 7 4.7 COC(=O)C12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479657 190045 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 604 7 1 7 4.7 COC(=O)C12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
45488096 203692 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 521 6 1 4 6.5 CC1=CC(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cc(F)cc21 10.1021/jm9005912
CHEMBL566221 203692 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 521 6 1 4 6.5 CC1=CC(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cc(F)cc21 10.1021/jm9005912
46879801 12759 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 583 6 1 5 7.3 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4cc(F)c(F)cc4F)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1080105 12759 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 583 6 1 5 7.3 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4cc(F)c(F)cc4F)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44570000 185429 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL467632 185429 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570149 198863 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 494 7 2 6 5.4 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2008.11.007
CHEMBL520290 198863 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 494 7 2 6 5.4 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2008.11.007
44570000 185429 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL467632 185429 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44627175 203650 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 572 7 1 5 5.9 CN1C(=O)C(Cc2ccc3ccccc3c2)c2c(CCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
CHEMBL565991 203650 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 572 7 1 5 5.9 CN1C(=O)C(Cc2ccc3ccccc3c2)c2c(CCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
45488096 203692 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 521 6 1 4 6.5 CC1=CC(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cc(F)cc21 10.1021/jm9005912
CHEMBL566221 203692 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 521 6 1 4 6.5 CC1=CC(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cc(F)cc21 10.1021/jm9005912
44570000 185429 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL467632 185429 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44564934 186969 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL474948 186969 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3)cccc21 10.1016/j.bmcl.2008.12.112
44564893 187302 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475349 187302 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
46885686 14723 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 570 6 1 5 6.4 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090458 14723 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 570 6 1 5 6.4 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1016/j.bmcl.2010.02.028
46885385 14670 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1090113 14670 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
46885604 14846 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1091164 14846 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2010.02.028
46885386 15230 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 568 6 1 4 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1093797 15230 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 568 6 1 4 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
44570400 189850 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 546 7 2 6 6.2 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)cc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL479433 189850 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 546 7 2 6 6.2 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)cc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570665 197330 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL517994 197330 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
44571355 198096 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL519137 198096 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
46885603 14628 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 588 6 1 5 6.5 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089807 14628 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 588 6 1 5 6.5 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1016/j.bmcl.2010.02.028
44571289 190020 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 560 6 1 5 5.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479632 190020 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 560 6 1 5 5.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44564686 184171 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)cc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL463816 184171 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)cc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
46885652 14698 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 502 6 1 5 5.1 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090342 14698 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 502 6 1 5 5.1 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc21 10.1016/j.bmcl.2010.02.028
44570399 189854 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 569 9 3 7 4.6 NC(=O)Cc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
CHEMBL479435 189854 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 569 9 3 7 4.6 NC(=O)Cc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
44570150 190732 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 556 7 2 5 6.7 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2008.11.007
CHEMBL481589 190732 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 556 7 2 5 6.7 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2008.11.007
44570485 196815 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 556 7 2 6 4.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2008.11.007
CHEMBL517180 196815 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 556 7 2 6 4.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2008.11.007
44627830 203729 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 524 6 1 6 4.6 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)cc(F)cc12 10.1021/jm9005912
CHEMBL566429 203729 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 524 6 1 6 4.6 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)cc(F)cc12 10.1021/jm9005912
25181438 190634 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480809 190634 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570231 196798 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 528 7 2 6 6.1 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL517165 196798 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 528 7 2 6 6.1 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2008.11.007
44570712 189857 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 572 6 1 4 5.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479439 189857 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 572 6 1 4 5.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
44594042 203653 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 547 6 1 6 5.9 Cc1cn(Cc2cccc(C#N)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL566006 203653 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 547 6 1 6 5.9 Cc1cn(Cc2cccc(C#N)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
44571321 185940 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL472145 185940 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
44571290 190021 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 542 6 1 5 5.4 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc(F)cc1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479633 190021 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 542 6 1 5 5.4 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc(F)cc1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44564935 186973 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 522 6 1 5 5.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL474949 186973 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 522 6 1 5 5.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
46885576 14532 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 632 6 1 7 5.6 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C21OCCO1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1089115 14532 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 632 6 1 7 5.6 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C21OCCO1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
46885784 14735 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 610 6 1 5 6.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1090499 14735 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 610 6 1 5 6.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44570562 190649 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 556 7 2 6 4.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2008.11.007
CHEMBL480992 190649 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 556 7 2 6 4.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2008.11.007
44570354 199295 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 563 7 2 7 6.1 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL520933 199295 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 563 7 2 7 6.1 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570194 184943 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 574 8 2 8 4.3 COc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
CHEMBL464906 184943 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 574 8 2 8 4.3 COc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
10339756 149863 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
CHEMBL3895324 149863 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
44570193 184940 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 578 7 2 7 4.9 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)cc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL464905 184940 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 578 7 2 7 4.9 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)cc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
1955 6805 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
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 10.1021/jm990542v
5311240 6805 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
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 10.1021/jm990542v
CHEMBL36041 6805 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
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 10.1021/jm990542v
44570953 199285 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 520 6 1 4 5.2 Cc1cn(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)cc(F)cc12 10.1021/jm9005912
CHEMBL520918 199285 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 520 6 1 4 5.2 Cc1cn(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)cc(F)cc12 10.1021/jm9005912
44564992 193814 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL490897 193814 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
44564685 184170 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL463815 184170 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
1884 9857 52 None -11 22 Human 6.5 pIC50 = 6.5 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
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 10.1021/jm990542v
5280363 9857 52 None -11 22 Human 6.5 pIC50 = 6.5 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
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 10.1021/jm990542v
912 9857 52 None -11 22 Human 6.5 pIC50 = 6.5 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
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 10.1021/jm990542v
CHEMBL815 9857 52 None -11 22 Human 6.5 pIC50 = 6.5 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
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 10.1021/jm990542v
DB12789 9857 52 None -11 22 Human 6.5 pIC50 = 6.5 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
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 10.1021/jm990542v
44626978 203615 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 498 7 1 5 5.9 O=C(/C=C/c1cccc2ccn(Cc3ccccc3-c3ccccc3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL565797 203615 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 498 7 1 5 5.9 O=C(/C=C/c1cccc2ccn(Cc3ccccc3-c3ccccc3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44570641 197405 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 572 7 2 7 4.9 Cc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c(C)c1 10.1016/j.bmcl.2008.11.007
CHEMBL518109 197405 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 572 7 2 7 4.9 Cc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c(C)c1 10.1016/j.bmcl.2008.11.007
44570484 184359 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 574 8 2 8 4.3 COc1cccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
CHEMBL464059 184359 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 574 8 2 8 4.3 COc1cccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
46885655 14722 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 514 6 1 5 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1090455 14722 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 514 6 1 5 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2=O)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
44626979 205687 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 452 7 1 6 4.3 COc1ccc(Cn2ccc3cccc(/C=C/C(=O)NS(=O)(=O)c4cccs4)c32)cc1 10.1021/jm9005912
CHEMBL584495 205687 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 452 7 1 6 4.3 COc1ccc(Cn2ccc3cccc(/C=C/C(=O)NS(=O)(=O)c4cccs4)c32)cc1 10.1021/jm9005912
44570444 197406 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 512 7 2 6 5.6 O=C(COc1cccc2[nH]cc(Sc3ccccc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL518110 197406 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 512 7 2 6 5.6 O=C(COc1cccc2[nH]cc(Sc3ccccc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
45488090 203656 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 415 7 1 5 4.6 CC(C)c1cccc(COc2cccc(C(=O)NS(=O)(=O)c3cccs3)c2)c1 10.1021/jm9005912
CHEMBL566014 203656 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 415 7 1 5 4.6 CC(C)c1cccc(COc2cccc(C(=O)NS(=O)(=O)c3cccs3)c2)c1 10.1021/jm9005912
44564572 193785 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cccc(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL490692 193785 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 516 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cccc(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
46885504 14482 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 502 6 1 4 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088848 14482 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 502 6 1 4 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
44626877 205781 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 490 6 1 5 5.6 O=C(/C=C/c1cccc2ccn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL585581 205781 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 490 6 1 5 5.6 O=C(/C=C/c1cccc2ccn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44627283 203859 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 524 6 1 6 4.2 O=C(/C=C/c1cccc2c1N(S(=O)(=O)c1ccc3ccccc3c1)CC2)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL567484 203859 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 524 6 1 6 4.2 O=C(/C=C/c1cccc2c1N(S(=O)(=O)c1ccc3ccccc3c1)CC2)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44627515 203616 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL565799 203616 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
44570233 196898 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 534 7 2 9 4.7 Cc1nnc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)s1 10.1016/j.bmcl.2008.11.007
CHEMBL517316 196898 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 534 7 2 9 4.7 Cc1nnc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)s1 10.1016/j.bmcl.2008.11.007
46880038 14207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 484 5 1 6 6.3 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NC(=O)c4ccco4)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1086633 14207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 484 5 1 6 6.3 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NC(=O)c4ccco4)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44570355 190606 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 503 7 3 8 3.7 O=C(COc1cccc2[nH]cc(Sc3nc[nH]n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480604 190606 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 503 7 3 8 3.7 O=C(COc1cccc2[nH]cc(Sc3nc[nH]n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
10001608 107125 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE-2 from human Prostaglandin E receptor EP3 expressed in CHO-KI cellsDisplacement of [3H]PGE-2 from human Prostaglandin E receptor EP3 expressed in CHO-KI cells
ChEMBL 410 13 4 4 3.7 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCc1cccc(F)c1 10.1016/s0960-894x(00)00273-0
CHEMBL289568 107125 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE-2 from human Prostaglandin E receptor EP3 expressed in CHO-KI cellsDisplacement of [3H]PGE-2 from human Prostaglandin E receptor EP3 expressed in CHO-KI cells
ChEMBL 410 13 4 4 3.7 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCc1cccc(F)c1 10.1016/s0960-894x(00)00273-0
44626787 203832 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 472 6 1 5 5.4 O=C(/C=C/c1cccc2ccn(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL567274 203832 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 472 6 1 5 5.4 O=C(/C=C/c1cccc2ccn(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
46885783 14734 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 516 6 1 4 4.8 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090498 14734 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 516 6 1 4 4.8 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
44564934 186969 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL474948 186969 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3)cccc21 10.1016/j.bmcl.2008.12.112
44627720 203684 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 524 6 1 6 4.6 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cc(F)cc12 10.1021/jm9005912
CHEMBL566197 203684 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 524 6 1 6 4.6 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)cc(F)cc12 10.1021/jm9005912
46879860 13055 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 598 6 1 6 7.6 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NS(=O)(=O)c4ccc(Cl)c(Cl)c4)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1081724 13055 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 598 6 1 6 7.6 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NS(=O)(=O)c4ccc(Cl)c(Cl)c4)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
46885783 14734 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 516 6 1 4 4.8 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090498 14734 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 516 6 1 4 4.8 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
44570000 185429 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL467632 185429 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44627395 203651 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL565992 203651 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
46885733 14574 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 564 6 1 4 6.3 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089455 14574 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 564 6 1 4 6.3 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
44570400 189850 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 546 7 2 6 6.2 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)cc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL479433 189850 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 546 7 2 6 6.2 O=C(COc1cccc2[nH]cc(Sc3ccc(Cl)cc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570187 190656 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 524 7 2 5 5.6 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2008.11.007
CHEMBL481004 190656 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 524 7 2 5 5.6 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2008.11.007
44570668 190796 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 572 6 1 4 5.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL482018 190796 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 572 6 1 4 5.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
46885651 14585 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 568 6 1 4 5.6 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089491 14585 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 568 6 1 4 5.6 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
44571243 196635 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 592 6 1 5 6.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL516765 196635 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 592 6 1 5 6.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1cccc(Cl)c1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
44564843 186043 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 498 7 1 6 4.8 COc1cccc(Oc2cccc3c2c(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)cn3C)c1 10.1016/j.bmcl.2008.12.112
CHEMBL472957 186043 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 498 7 1 6 4.8 COc1cccc(Oc2cccc3c2c(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)cn3C)c1 10.1016/j.bmcl.2008.12.112
44564991 193813 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL490896 193813 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
46885686 14723 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 570 6 1 5 6.4 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090458 14723 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 570 6 1 5 6.4 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1016/j.bmcl.2010.02.028
46885384 14669 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 554 6 1 4 5.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1090112 14669 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 554 6 1 4 5.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
44570231 196798 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 528 7 2 6 6.1 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL517165 196798 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 528 7 2 6 6.1 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2008.11.007
46885947 14688 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 586 6 1 4 6.3 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1090222 14688 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 586 6 1 4 6.3 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
11296282 8191 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1016/j.bmcl.2009.09.084
5822 8191 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1016/j.bmcl.2009.09.084
CHEMBL565591 8191 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1016/j.bmcl.2009.09.084
11296282 8191 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
5822 8191 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
CHEMBL565591 8191 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
11296282 8191 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
5822 8191 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
CHEMBL565591 8191 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
44564573 193786 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 556 6 1 6 7.0 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL490693 193786 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 556 6 1 6 7.0 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
25181438 190634 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480809 190634 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570354 199295 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 563 7 2 7 6.1 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL520933 199295 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 563 7 2 7 6.1 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4n3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44564806 184626 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 504 6 1 5 5.0 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL464413 184626 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 504 6 1 5 5.0 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
44627397 205771 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 647 6 2 7 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C21NCCS1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL585507 205771 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 647 6 2 7 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C21NCCS1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44627397 205771 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 647 6 2 7 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C21NCCS1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL585507 205771 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 647 6 2 7 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C21NCCS1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44570524 185157 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 526 7 2 7 4.1 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2008.11.007
CHEMBL465298 185157 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 526 7 2 7 4.1 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2008.11.007
44570606 190762 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 560 7 2 7 4.8 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL481782 190762 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 560 7 2 7 4.8 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2008.11.007
44626980 205684 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 423 6 1 6 3.7 O=C(/C=C/c1cccc2ccn(Cc3cccnc3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL584484 205684 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 423 6 1 6 3.7 O=C(/C=C/c1cccc2ccn(Cc3cccnc3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44626976 205741 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 490 6 1 5 5.3 O=C(/C=C/c1cccc2ccn(Cc3cccc(C(F)(F)F)c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL585091 205741 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 490 6 1 5 5.3 O=C(/C=C/c1cccc2ccn(Cc3cccc(C(F)(F)F)c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44570563 190680 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 539 7 2 8 3.6 Cc1noc(C)c1S(=O)(=O)NC(=O)COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1016/j.bmcl.2008.11.007
CHEMBL481183 190680 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 539 7 2 8 3.6 Cc1noc(C)c1S(=O)(=O)NC(=O)COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1016/j.bmcl.2008.11.007
46885340 14937 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 538 6 1 4 4.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1091892 14937 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 538 6 1 4 4.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
44626977 205666 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 490 6 1 5 5.3 O=C(/C=C/c1cccc2ccn(Cc3ccccc3C(F)(F)F)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL584279 205666 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 490 6 1 5 5.3 O=C(/C=C/c1cccc2ccn(Cc3ccccc3C(F)(F)F)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
46885538 14839 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 522 6 1 4 4.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1091145 14839 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 522 6 1 4 4.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
44626878 205767 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 490 6 1 5 5.6 O=C(/C=C/c1cccc2ccn(Cc3c(Cl)cccc3Cl)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL585483 205767 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 490 6 1 5 5.6 O=C(/C=C/c1cccc2ccn(Cc3c(Cl)cccc3Cl)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44626880 203649 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 450 6 1 5 4.9 Cc1ccc(Cn2ccc3cccc(/C=C/C(=O)NS(=O)(=O)c4cccs4)c32)cc1C 10.1021/jm9005912
CHEMBL565988 203649 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 450 6 1 5 4.9 Cc1ccc(Cn2ccc3cccc(/C=C/C(=O)NS(=O)(=O)c4cccs4)c32)cc1C 10.1021/jm9005912
44570005 185606 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 578 7 2 7 4.9 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccccc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL469304 185606 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 578 7 2 7 4.9 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccccc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570399 189854 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 569 9 3 7 4.6 NC(=O)Cc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
CHEMBL479435 189854 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 569 9 3 7 4.6 NC(=O)Cc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
46879999 12705 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 533 6 1 5 6.1 Cc1cn(Cc2ccc(F)c(F)c2)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1079767 12705 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 533 6 1 5 6.1 Cc1cn(Cc2ccc(F)c(F)c2)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44570003 196203 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 601 7 2 9 4.9 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3nc4ccccc4s3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL513305 196203 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 601 7 2 9 4.9 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3nc4ccccc4s3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570639 190608 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480609 190608 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44564724 196873 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)cc(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL517282 196873 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)cc(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44564892 187301 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475348 187301 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
46885575 14531 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 564 8 3 6 2.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(CO)CO)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1089114 14531 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 564 8 3 6 2.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(CO)CO)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
44627721 203655 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 506 6 1 6 4.4 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)cc3)cc(F)cc12 10.1021/jm9005912
CHEMBL566013 203655 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 506 6 1 6 4.4 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)cc3)cc(F)cc12 10.1021/jm9005912
44594042 203653 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 547 6 1 6 5.9 Cc1cn(Cc2cccc(C#N)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL566006 203653 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 547 6 1 6 5.9 Cc1cn(Cc2cccc(C#N)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
46885502 14481 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 504 6 1 4 3.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088847 14481 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 504 6 1 4 3.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
10479215 153239 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 456 10 3 5 4.8 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)Cc2cc3ccccc3s2)[C@@H]1O nan
CHEMBL3922155 153239 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 456 10 3 5 4.8 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)Cc2cc3ccccc3s2)[C@@H]1O nan
44627719 203758 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 503 6 1 6 4.5 Cc1noc(C)c1Cn1cc(C)c2cc(F)cc(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)c21 10.1021/jm9005912
CHEMBL566643 203758 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 503 6 1 6 4.5 Cc1noc(C)c1Cn1cc(C)c2cc(F)cc(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)c21 10.1021/jm9005912
44570148 190855 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 522 7 2 5 6.0 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1Cl 10.1016/j.bmcl.2008.11.007
CHEMBL482380 190855 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 522 7 2 5 6.0 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1Cl 10.1016/j.bmcl.2008.11.007
46879757 13127 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 603 6 1 6 8.3 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1082084 13127 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 603 6 1 6 8.3 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
44626879 205744 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 504 6 1 5 5.9 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc12 10.1021/jm9005912
CHEMBL585099 205744 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 504 6 1 5 5.9 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc12 10.1021/jm9005912
44570000 185429 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL467632 185429 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
46885340 14937 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 538 6 1 4 4.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1091892 14937 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 538 6 1 4 4.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
46885946 15239 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 554 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1093843 15239 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 554 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
44570192 184345 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 601 9 3 8 3.3 NC(=O)Cc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
CHEMBL464042 184345 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 601 9 3 8 3.3 NC(=O)Cc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1 10.1016/j.bmcl.2008.11.007
44627515 203616 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL565799 203616 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
44564993 193595 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 516 7 1 6 4.9 COc1cccc(Oc2cccc3c2c(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)cn3C)c1 10.1016/j.bmcl.2008.12.112
CHEMBL489315 193595 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 516 7 1 6 4.9 COc1cccc(Oc2cccc3c2c(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)cn3C)c1 10.1016/j.bmcl.2008.12.112
44564772 196626 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 572 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2c(F)c(F)c(F)c(F)c2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL516673 196626 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 572 6 1 5 6.3 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2c(F)c(F)c(F)c(F)c2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44570444 197406 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 512 7 2 6 5.6 O=C(COc1cccc2[nH]cc(Sc3ccccc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL518110 197406 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 512 7 2 6 5.6 O=C(COc1cccc2[nH]cc(Sc3ccccc3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
46885434 14476 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 550 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088823 14476 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 550 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
44570281 197599 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 540 7 2 6 6.2 Cc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c(C)c1 10.1016/j.bmcl.2008.11.007
CHEMBL518396 197599 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 540 7 2 6 6.2 Cc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c(C)c1 10.1016/j.bmcl.2008.11.007
46885387 14469 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 556 6 1 5 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1088785 14469 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 556 6 1 5 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
46885688 14725 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090460 14725 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)cccc21 10.1016/j.bmcl.2010.02.028
46885986 14815 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 552 6 1 4 5.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1090889 14815 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 552 6 1 4 5.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.02.028
46885838 14524 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 604 6 1 4 6.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1089094 14524 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 604 6 1 4 6.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
44570827 189715 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 534 7 1 5 4.4 COc1cccc(CN2C(=O)CC3(C)CCCC(/C=C/C(=O)NS(=O)(=O)c4cc(F)c(F)cc4F)=C23)c1 10.1016/j.bmcl.2008.12.027
CHEMBL479264 189715 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 534 7 1 5 4.4 COc1cccc(CN2C(=O)CC3(C)CCCC(/C=C/C(=O)NS(=O)(=O)c4cc(F)c(F)cc4F)=C23)c1 10.1016/j.bmcl.2008.12.027
44570829 190736 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)cc(Cl)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL481614 190736 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 6 1 4 5.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)cc(Cl)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44571353 190814 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 516 7 1 5 4.2 COc1cccc(CN2C(=O)CC3(C)CCCC(/C=C/C(=O)NS(=O)(=O)c4cc(F)cc(F)c4)=C23)c1 10.1016/j.bmcl.2008.12.027
CHEMBL482159 190814 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 516 7 1 5 4.2 COc1cccc(CN2C(=O)CC3(C)CCCC(/C=C/C(=O)NS(=O)(=O)c4cc(F)cc(F)c4)=C23)c1 10.1016/j.bmcl.2008.12.027
46885786 14737 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 590 6 1 4 5.6 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1090501 14737 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 590 6 1 4 5.6 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
44570639 190608 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480609 190608 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 612 7 2 7 5.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570187 190656 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 524 7 2 5 5.6 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2008.11.007
CHEMBL481004 190656 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 524 7 2 5 5.6 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2008.11.007
44570641 197405 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 572 7 2 7 4.9 Cc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c(C)c1 10.1016/j.bmcl.2008.11.007
CHEMBL518109 197405 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 572 7 2 7 4.9 Cc1ccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c(C)c1 10.1016/j.bmcl.2008.11.007
44570993 190338 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 532 7 1 5 5.1 COc1cccc(Cn2cc(C)c3cc(F)cc(/C=C/C(=O)NS(=O)(=O)c4cc(F)c(F)cc4F)c32)c1 10.1021/jm9005912
CHEMBL480029 190338 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 532 7 1 5 5.1 COc1cccc(Cn2cc(C)c3cc(F)cc(/C=C/C(=O)NS(=O)(=O)c4cc(F)c(F)cc4F)c32)c1 10.1021/jm9005912
44570315 190323 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 546 7 2 6 6.2 O=C(COc1cccc2[nH]cc(Sc3ccccc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL480012 190323 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 546 7 2 6 6.2 O=C(COc1cccc2[nH]cc(Sc3ccccc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44570564 198965 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 7 2 6 4.7 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2008.11.007
CHEMBL520425 198965 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 7 2 6 4.7 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2008.11.007
44564723 183689 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2c(F)cccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL461807 183689 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2c(F)cccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44564571 193594 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL489310 193594 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
44627829 203693 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 558 6 1 5 6.3 Cc1cn(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL566226 203693 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 558 6 1 5 6.3 Cc1cn(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
44570607 190763 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 520 7 2 6 4.0 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.11.007
CHEMBL481783 190763 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 520 7 2 6 4.0 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.11.007
44564990 199429 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL521777 199429 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
44564650 196641 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)cc2Cl)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL516789 196641 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)cc2Cl)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44570605 198749 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 550 8 2 7 4.0 COc1ccc(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(S(=O)(=O)c4ccc5ccccc5c4)c23)cc1 10.1016/j.bmcl.2008.11.007
CHEMBL520108 198749 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 550 8 2 7 4.0 COc1ccc(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(S(=O)(=O)c4ccc5ccccc5c4)c23)cc1 10.1016/j.bmcl.2008.11.007
44570001 185276 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 558 7 2 6 5.8 O=C(COc1cccc2[nH]cc(C(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL466594 185276 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 558 7 2 6 5.8 O=C(COc1cccc2[nH]cc(C(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
46885539 14840 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 542 6 1 5 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1091146 14840 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 542 6 1 5 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
46885503 15107 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1092871 15107 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 536 6 1 4 4.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.028
44570871 186077 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 544 7 1 4 4.6 C[C@]12CCC[C@@H](CCC(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)[C@H]1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL473242 186077 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 544 7 1 4 4.6 C[C@]12CCC[C@@H](CCC(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)[C@H]1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44626979 205687 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 452 7 1 6 4.3 COc1ccc(Cn2ccc3cccc(/C=C/C(=O)NS(=O)(=O)c4cccs4)c32)cc1 10.1021/jm9005912
CHEMBL584495 205687 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 452 7 1 6 4.3 COc1ccc(Cn2ccc3cccc(/C=C/C(=O)NS(=O)(=O)c4cccs4)c32)cc1 10.1021/jm9005912
46885342 14985 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 506 6 1 5 4.7 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
CHEMBL1092229 14985 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 506 6 1 5 4.7 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
44571318 190811 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 524 6 1 5 5.3 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cccs3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL482155 190811 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 524 6 1 5 5.3 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cccs3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
44570443 190790 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 518 7 2 10 3.1 Cn1nnnc1Sc1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
CHEMBL481984 190790 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 518 7 2 10 3.1 Cn1nnnc1Sc1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
46879756 13097 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 571 6 1 6 7.2 Cc1cn(Cc2ccc(F)c(F)c2)c2c(-c3cc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1081902 13097 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 571 6 1 6 7.2 Cc1cn(Cc2ccc(F)c(F)c2)c2c(-c3cc(NS(=O)(=O)c4cc(Cl)c(Cl)s4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
15486805 172832 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
ChEMBL 394 13 4 5 3.0 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)COc1ccccc1 10.1021/jm990542v
CHEMBL425681 172832 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
ChEMBL 394 13 4 5 3.0 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)COc1ccccc1 10.1021/jm990542v
44627513 205685 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 547 6 1 6 5.9 Cc1cn(Cc2ccc(C#N)cc2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL584488 205685 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 547 6 1 6 5.9 Cc1cn(Cc2ccc(C#N)cc2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
45488091 205798 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 498 5 1 6 3.5 O=C(NS(=O)(=O)c1cccs1)C1Cc2ccccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm9005912
CHEMBL585765 205798 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 498 5 1 6 3.5 O=C(NS(=O)(=O)c1cccs1)C1Cc2ccccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm9005912
11296282 8191 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
5822 8191 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
CHEMBL565591 8191 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
44570002 185277 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 604 9 2 9 4.3 COc1ccc(OC)c(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
CHEMBL466595 185277 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 604 9 2 9 4.3 COc1ccc(OC)c(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
44564891 196596 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 7 4.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3cnc4ccccc4n3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL516394 196596 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 7 4.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3cnc4ccccc4n3)cccc21 10.1016/j.bmcl.2008.12.112
44571291 196935 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 7 1 6 5.3 COc1cccc(CN2C(=O)CC3(C)CCCC(/C=C/C(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)=C23)c1 10.1016/j.bmcl.2008.12.027
CHEMBL517377 196935 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 7 1 6 5.3 COc1cccc(CN2C(=O)CC3(C)CCCC(/C=C/C(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)=C23)c1 10.1016/j.bmcl.2008.12.027
44564687 184767 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)ccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL464618 184767 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)ccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
46885606 14580 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 588 6 1 6 5.6 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2=O)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1089481 14580 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 588 6 1 6 5.6 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2=O)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
46885837 14468 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 572 6 1 4 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088780 14468 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 572 6 1 4 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
44627513 205685 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 547 6 1 6 5.9 Cc1cn(Cc2ccc(C#N)cc2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL584488 205685 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 547 6 1 6 5.9 Cc1cn(Cc2ccc(C#N)cc2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
44564990 199429 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL521777 199429 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
44571206 190768 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 574 6 1 5 6.4 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc3ccccc3c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL481813 190768 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 574 6 1 5 6.4 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc3ccccc3c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
46885650 14537 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 548 6 1 4 5.8 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089161 14537 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 548 6 1 4 5.8 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccc(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
46885433 14475 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 518 6 1 4 4.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088822 14475 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 518 6 1 4 4.7 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
44564937 186014 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL472754 186014 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
44564840 187142 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475151 187142 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
44626788 203688 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 422 6 1 5 4.3 O=C(/C=C/c1cccc2ccn(Cc3ccccc3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL566211 203688 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 422 6 1 5 4.3 O=C(/C=C/c1cccc2ccn(Cc3ccccc3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44627399 203757 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 504 6 1 5 5.9 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cc(F)cc12 10.1021/jm9005912
CHEMBL566631 203757 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 504 6 1 5 5.9 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cc(F)cc12 10.1021/jm9005912
1894 7744 41 None -1 5 Human 6.2 pIC50 = 6.2 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
5311053 7744 41 None -1 5 Human 6.2 pIC50 = 6.2 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
CHEMBL37853 7744 41 None -1 5 Human 6.2 pIC50 = 6.2 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
DB11507 7744 41 None -1 5 Human 6.2 pIC50 = 6.2 Binding
Affinity for Prostanoid EP3 receptor expressed in CHO cell lineAffinity for Prostanoid EP3 receptor expressed in CHO cell line
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
44627175 203650 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 572 7 1 5 5.9 CN1C(=O)C(Cc2ccc3ccccc3c2)c2c(CCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
CHEMBL565991 203650 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 572 7 1 5 5.9 CN1C(=O)C(Cc2ccc3ccccc3c2)c2c(CCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
46885784 14735 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 610 6 1 5 6.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1090499 14735 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 610 6 1 5 6.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
46885881 15159 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 554 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
CHEMBL1093239 15159 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 554 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2010.02.028
45488089 203827 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 569 7 1 6 4.4 O=C(NS(=O)(=O)c1cccs1)c1cccc(CN2CCCCN(Cc3ccc4ccccc4c3)S2(=O)=O)c1 10.1021/jm9005912
CHEMBL567265 203827 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 569 7 1 6 4.4 O=C(NS(=O)(=O)c1cccs1)c1cccc(CN2CCCCN(Cc3ccc4ccccc4c3)S2(=O)=O)c1 10.1021/jm9005912
44564726 183703 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL461980 183703 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
45488094 205709 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 505 7 2 7 5.8 O=C(NS(=O)(=O)c1cccs1)c1ccc(-c2csc(NCc3ccc4ccccc4c3)n2)cc1 10.1021/jm9005912
CHEMBL584705 205709 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 505 7 2 7 5.8 O=C(NS(=O)(=O)c1cccs1)c1ccc(-c2csc(NCc3ccc4ccccc4c3)n2)cc1 10.1021/jm9005912
44627396 203892 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 593 7 2 7 5.4 CN1C(=O)C(Nc2ccc(Cl)c(Cl)c2)c2c(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
CHEMBL567690 203892 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 593 7 2 7 5.4 CN1C(=O)C(Nc2ccc(Cl)c(Cl)c2)c2c(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cccc21 10.1021/jm9005912
44570230 185199 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 518 8 2 6 5.4 COc1ccc(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(Sc4ccc5ccccc5c4)c23)cc1 10.1016/j.bmcl.2008.11.007
CHEMBL465947 185199 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 518 8 2 6 5.4 COc1ccc(S(=O)(=O)NC(=O)COc2cccc3[nH]cc(Sc4ccc5ccccc5c4)c23)cc1 10.1016/j.bmcl.2008.11.007
44570446 197592 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 502 7 3 7 4.3 O=C(COc1cccc2[nH]cc(Sc3ncc[nH]3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL518387 197592 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 502 7 3 7 4.3 O=C(COc1cccc2[nH]cc(Sc3ncc[nH]3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
46885602 14627 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 520 6 1 5 5.2 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1089806 14627 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 520 6 1 5 5.2 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc21 10.1016/j.bmcl.2010.02.028
10432730 154047 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 428 11 2 5 4.0 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1ccccc1 nan
CHEMBL3928703 154047 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 428 11 2 5 4.0 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1ccccc1 nan
46880000 12736 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 530 5 1 5 7.0 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NC(=O)c4ccc(F)c(F)c4)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1079936 12736 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 530 5 1 5 7.0 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3nnc(NC(=O)c4ccc(F)c(F)c4)o3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
46885577 14572 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 546 6 1 7 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C21OCCO1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
CHEMBL1089446 14572 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 546 6 1 7 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C21OCCO1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2010.02.028
45488100 203686 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 562 6 1 7 5.7 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL566202 203686 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 562 6 1 7 5.7 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
44627721 203655 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 506 6 1 6 4.4 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)cc3)cc(F)cc12 10.1021/jm9005912
CHEMBL566013 203655 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 506 6 1 6 4.4 Cc1cn(Cc2cn3ccccc3n2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(F)cc3)cc(F)cc12 10.1021/jm9005912
44627515 203616 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL565799 203616 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
44627515 203616 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL565799 203616 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
44564841 187143 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475152 187143 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
44565044 199847 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 538 6 1 7 4.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3cnc4ccccc4n3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL522435 199847 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 538 6 1 7 4.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3cnc4ccccc4n3)cccc21 10.1016/j.bmcl.2008.12.112
46886026 15124 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 578 6 1 5 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1092990 15124 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 578 6 1 5 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44157014 199396 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL521609 199396 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44570313 196940 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 569 7 2 8 6.2 O=C(COc1cccc2[nH]cc(Sc3nc4ccccc4s3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL517385 196940 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 569 7 2 8 6.2 O=C(COc1cccc2[nH]cc(Sc3nc4ccccc4s3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
46885691 15229 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 534 6 2 5 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1093792 15229 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 534 6 2 5 4.2 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.028
44570003 196203 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 601 7 2 9 4.9 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3nc4ccccc4s3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL513305 196203 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 601 7 2 9 4.9 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3nc4ccccc4s3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
25195248 189714 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 540 6 1 4 4.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479263 189714 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 540 6 1 4 4.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
46885839 14525 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 570 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1089095 14525 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 570 6 1 4 5.8 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2(F)F)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
46885605 14847 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 614 6 1 7 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C21OCCO1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1091165 14847 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in bufferDisplacement of [3H]PGE2 from human EP3 receptor in buffer
ChEMBL 614 6 1 7 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C21OCCO1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44570002 185277 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 604 9 2 9 4.3 COc1ccc(OC)c(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
CHEMBL466595 185277 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 604 9 2 9 4.3 COc1ccc(OC)c(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
44564723 183689 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2c(F)cccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL461807 183689 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2c(F)cccc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44626880 203649 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 450 6 1 5 4.9 Cc1ccc(Cn2ccc3cccc(/C=C/C(=O)NS(=O)(=O)c4cccs4)c32)cc1C 10.1021/jm9005912
CHEMBL565988 203649 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 450 6 1 5 4.9 Cc1ccc(Cn2ccc3cccc(/C=C/C(=O)NS(=O)(=O)c4cccs4)c32)cc1C 10.1021/jm9005912
44626975 203578 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 504 6 1 5 5.9 Cc1cn(Cc2ccc(Cl)c(Cl)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc12 10.1021/jm9005912
CHEMBL565597 203578 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 504 6 1 5 5.9 Cc1cn(Cc2ccc(Cl)c(Cl)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc12 10.1021/jm9005912
46886027 15125 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 558 6 1 4 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1092991 15125 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 558 6 1 4 4.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
45488088 205134 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 387 7 1 5 3.6 O=C(/C=C/c1ccc(CCc2ccccc2)o1)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL576509 205134 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 387 7 1 5 3.6 O=C(/C=C/c1ccc(CCc2ccccc2)o1)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44627284 203580 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 504 7 1 7 4.1 O=C(COc1cccc2ccc(=O)n(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL565604 203580 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 504 7 1 7 4.1 O=C(COc1cccc2ccc(=O)n(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
44564805 197492 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 502 6 1 5 5.4 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL518237 197492 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 502 6 1 5 5.4 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3)cccc21 10.1016/j.bmcl.2008.12.112
44627395 203651 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL565992 203651 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44570523 185156 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 7 2 6 4.7 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1Cl 10.1016/j.bmcl.2008.11.007
CHEMBL465297 185156 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 554 7 2 6 4.7 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccccc1Cl 10.1016/j.bmcl.2008.11.007
46879800 12886 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 565 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(-c3cc(NS(=O)(=O)c4cc(F)c(F)cc4F)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1080819 12886 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 565 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(-c3cc(NS(=O)(=O)c4cc(F)c(F)cc4F)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
46885501 14480 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 516 6 1 4 5.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1088846 14480 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 516 6 1 4 5.1 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
44570443 190790 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 518 7 2 10 3.1 Cn1nnnc1Sc1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
CHEMBL481984 190790 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 518 7 2 10 3.1 Cn1nnnc1Sc1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
44565043 200005 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 537 6 1 6 5.5 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc4ncccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL523608 200005 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 537 6 1 6 5.5 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc4ncccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44564685 184170 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL463815 184170 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44570525 196630 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 588 7 2 6 5.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2008.11.007
CHEMBL516708 196630 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 588 7 2 6 5.3 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2008.11.007
44627282 203798 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 595 7 1 8 5.7 O=C(COc1cccc2occ(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL567051 203798 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 595 7 1 8 5.7 O=C(COc1cccc2occ(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44565193 183639 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL461390 183639 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 520 6 1 5 5.6 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(F)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
46885605 14847 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 614 6 1 7 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C21OCCO1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1091165 14847 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 614 6 1 7 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C21OCCO1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44571352 190813 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 504 6 1 4 4.3 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)=C1N(Cc1ccc(F)cc1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL482158 190813 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 504 6 1 4 4.3 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)=C1N(Cc1ccc(F)cc1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44564936 196392 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 522 6 1 5 5.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL514808 196392 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 522 6 1 5 5.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)cc3F)cccc21 10.1016/j.bmcl.2008.12.112
44626881 203579 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 482 8 1 7 4.3 COc1cc(Cn2ccc3cccc(/C=C/C(=O)NS(=O)(=O)c4cccs4)c32)cc(OC)c1 10.1021/jm9005912
CHEMBL565598 203579 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 482 8 1 7 4.3 COc1cc(Cn2ccc3cccc(/C=C/C(=O)NS(=O)(=O)c4cccs4)c32)cc(OC)c1 10.1021/jm9005912
44570234 184375 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 550 7 2 11 1.8 Cn1nnnc1S(=O)(=O)c1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
CHEMBL464073 184375 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 550 7 2 11 1.8 Cn1nnnc1S(=O)(=O)c1c[nH]c2cccc(OCC(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)c12 10.1016/j.bmcl.2008.11.007
44627397 205771 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 647 6 2 7 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C21NCCS1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL585507 205771 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum
ChEMBL 647 6 2 7 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C21NCCS1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44627397 205771 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 647 6 2 7 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C21NCCS1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL585507 205771 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 647 6 2 7 5.9 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C21NCCS1)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44627286 203830 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 561 7 1 7 6.5 O=C(CCc1csc2ncc(/C=C/c3ccc4ccccc4c3)n12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL567272 203830 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 561 7 1 7 6.5 O=C(CCc1csc2ncc(/C=C/c3ccc4ccccc4c3)n12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44564573 193786 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 556 6 1 6 7.0 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL490693 193786 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 556 6 1 6 7.0 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44570606 190762 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 560 7 2 7 4.8 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL481782 190762 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 560 7 2 7 4.8 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccc4ccccc4c3)c12)NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2008.11.007
44571320 190842 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 522 6 1 4 4.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL482318 190842 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 522 6 1 4 4.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)cc(F)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44129707 183535 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL460325 183535 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44570398 199150 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 572 9 2 8 5.6 COc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1OC 10.1016/j.bmcl.2008.11.007
CHEMBL520741 199150 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 572 9 2 8 5.6 COc1ccc(Sc2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1OC 10.1016/j.bmcl.2008.11.007
46885945 15199 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 572 6 1 4 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1093559 15199 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 572 6 1 4 5.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
44570484 184359 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 574 8 2 8 4.3 COc1cccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
CHEMBL464059 184359 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 574 8 2 8 4.3 COc1cccc(S(=O)(=O)c2c[nH]c3cccc(OCC(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)c1 10.1016/j.bmcl.2008.11.007
44570666 190049 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 522 6 1 4 4.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479664 190049 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 522 6 1 4 4.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44564647 183286 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)cc2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL459688 183286 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 500 6 1 5 5.8 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)cc2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
46885343 14986 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 534 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
CHEMBL1092230 14986 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 534 6 1 4 5.3 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.02.028
46885735 15140 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 552 6 2 5 4.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
CHEMBL1093125 15140 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 552 6 2 5 4.4 O=C(/C=C/c1cccc2c1N(Cc1ccc3ccccc3c1)C(=O)C2O)NS(=O)(=O)c1cc(F)c(F)cc1F 10.1016/j.bmcl.2010.02.028
44571246 196931 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 542 6 1 5 5.4 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1cccc(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL517369 196931 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 542 6 1 5 5.4 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1cccc(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
44570190 184330 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 562 7 2 6 6.7 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL464032 184330 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 562 7 2 6 6.7 O=C(COc1cccc2[nH]cc(Sc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
44564937 186014 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL472754 186014 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal bufferDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of normal buffer
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(F)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
44570828 189879 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 586 6 1 4 6.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)cc(Cl)c3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479454 189879 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 586 6 1 4 6.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)cc(Cl)c3)=C1N(Cc1ccc(Cl)cc1Cl)C(=O)C2 10.1016/j.bmcl.2008.12.027
46885649 14738 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 582 6 1 4 6.5 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090507 14738 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 582 6 1 4 6.5 CC1C(=O)N(Cc2ccc(Cl)cc2Cl)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
44570313 196940 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 569 7 2 8 6.2 O=C(COc1cccc2[nH]cc(Sc3nc4ccccc4s3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL517385 196940 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 569 7 2 8 6.2 O=C(COc1cccc2[nH]cc(Sc3nc4ccccc4s3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
46885341 14938 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 574 6 1 5 6.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1091893 14938 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 574 6 1 5 6.0 O=C(/C=C/c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C2)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44564649 183534 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL460322 183534 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor at 20 uM in presence of 10% human serum
ChEMBL 550 6 1 5 6.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
44570151 190733 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 545 7 2 8 3.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccccn3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
CHEMBL481590 190733 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 receptor
ChEMBL 545 7 2 8 3.6 O=C(COc1cccc2[nH]cc(S(=O)(=O)c3ccccn3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2008.11.007
46885734 15139 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1093124 15139 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 550 6 1 4 5.4 CC1C(=O)N(Cc2ccc(F)c(F)c2)c2c(/C=C/C(=O)NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2010.02.028
46885652 14698 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 502 6 1 5 5.1 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc21 10.1016/j.bmcl.2010.02.028
CHEMBL1090342 14698 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 502 6 1 5 5.1 CC1C(=O)N(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cccs3)cccc21 10.1016/j.bmcl.2010.02.028
46886026 15124 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 578 6 1 5 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
CHEMBL1092990 15124 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serumDisplacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
ChEMBL 578 6 1 5 5.5 O=C(/C=C/c1cccc2c1N(Cc1ccc(F)c(F)c1)C(=O)C2(F)F)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2010.02.028
44626788 203688 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 422 6 1 5 4.3 O=C(/C=C/c1cccc2ccn(Cc3ccccc3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
CHEMBL566211 203688 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting
ChEMBL 422 6 1 5 4.3 O=C(/C=C/c1cccc2ccn(Cc3ccccc3)c12)NS(=O)(=O)c1cccs1 10.1021/jm9005912
23016838 14907 0 None - 1 Mouse 10.2 pKi = 10.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 564 11 1 7 5.0 N#Cc1cccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091742 14907 0 None - 1 Mouse 10.2 pKi = 10.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 564 11 1 7 5.0 N#Cc1cccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2010.02.034
11620429 15289 0 None 3388 2 Mouse 10.2 pKi = 10.2 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094161 15289 0 None 3388 2 Mouse 10.2 pKi = 10.2 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23017788 14906 0 None 24547 3 Mouse 10.1 pKi = 10.1 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 575 11 1 6 5.4 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091741 14906 0 None 24547 3 Mouse 10.1 pKi = 10.1 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 575 11 1 6 5.4 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
23017083 207075 0 None - 1 Mouse 10.1 pKi = 10.1 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3Cl)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597348 207075 0 None - 1 Mouse 10.1 pKi = 10.1 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3Cl)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
11752564 207082 0 None 2290 2 Mouse 10.0 pKi = 10 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597375 207082 0 None 2290 2 Mouse 10.0 pKi = 10 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017429 208038 0 None - 1 Mouse 10.0 pKi = 10 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL603881 208038 0 None - 1 Mouse 10.0 pKi = 10 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017762 207371 0 None - 1 Mouse 10.0 pKi = 10.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 487 11 2 3 6.7 Cc1cccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2009.12.068
CHEMBL599203 207371 0 None - 1 Mouse 10.0 pKi = 10.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 487 11 2 3 6.7 Cc1cccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2009.12.068
23017557 207458 0 None 645 2 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599812 207458 0 None 645 2 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017255 14818 0 None 2187 3 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 554 12 1 7 4.2 CN(CCOc1cc(Cn2cccn2)ccc1CCC(=O)NS(=O)(=O)c1ccc(F)c(F)c1)c1ccccc1 10.1016/j.bmcl.2010.02.034
CHEMBL1090937 14818 0 None 2187 3 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 554 12 1 7 4.2 CN(CCOc1cc(Cn2cccn2)ccc1CCC(=O)NS(=O)(=O)c1ccc(F)c(F)c1)c1ccccc1 10.1016/j.bmcl.2010.02.034
23016850 207047 0 None 1479 2 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597146 207047 0 None 1479 2 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017339 207167 0 None - 1 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 500 12 2 5 5.7 COc1cccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597974 207167 0 None - 1 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 500 12 2 5 5.7 COc1cccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017359 207974 0 None - 1 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 475 12 2 4 5.8 COc1cccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL603497 207974 0 None - 1 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 475 12 2 4 5.8 COc1cccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
46886451 14908 0 None 13803 3 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 576 11 2 7 4.9 O=C(CCc1ccc(Cn2cccn2)cc1ONCc1cccc2ccccc12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091743 14908 0 None 13803 3 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 576 11 2 7 4.9 O=C(CCc1ccc(Cn2cccn2)cc1ONCc1cccc2ccccc12)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
23017033 208455 0 None - 1 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 493 12 2 4 5.9 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1F 10.1016/j.bmc.2009.12.068
CHEMBL606195 208455 0 None - 1 Mouse 9.9 pKi = 9.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 493 12 2 4 5.9 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1F 10.1016/j.bmc.2009.12.068
23016978 207374 0 None - 1 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(F)c3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599213 207374 0 None - 1 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(F)c3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017690 207263 0 None - 1 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 489 12 2 4 6.1 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1C 10.1016/j.bmc.2009.12.068
CHEMBL598613 207263 0 None - 1 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 489 12 2 4 6.1 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1C 10.1016/j.bmc.2009.12.068
23017295 208193 0 None 3981 2 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 477 11 2 3 6.2 Cc1cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)ccc1F 10.1016/j.bmc.2009.12.068
CHEMBL604708 208193 0 None 3981 2 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 477 11 2 3 6.2 Cc1cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)ccc1F 10.1016/j.bmc.2009.12.068
23017414 15030 0 None 4466 3 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 602 12 1 6 6.2 O=C(CCc1ccc(COc2cccnc2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1092432 15030 0 None 4466 3 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 602 12 1 6 6.2 O=C(CCc1ccc(COc2cccnc2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
46887058 15286 0 None 5011 3 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(Cl)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094156 15286 0 None 5011 3 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(Cl)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23016737 206993 0 None 7079 2 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 487 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL596745 206993 0 None 7079 2 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 487 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017457 207201 0 None - 1 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 488 11 2 4 5.8 CC(C)CC(NC(=O)c1cc(COc2cccc(C#N)c2)ccc1CCC(=O)O)c1ccc(F)cc1 10.1016/j.bmc.2009.12.068
CHEMBL598174 207201 0 None - 1 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 488 11 2 4 5.8 CC(C)CC(NC(=O)c1cc(COc2cccc(C#N)c2)ccc1CCC(=O)O)c1ccc(F)cc1 10.1016/j.bmc.2009.12.068
23017153 207233 0 None - 1 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 473 11 2 3 6.4 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1C 10.1016/j.bmc.2009.12.068
CHEMBL598410 207233 0 None - 1 Mouse 9.8 pKi = 9.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 473 11 2 3 6.4 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1C 10.1016/j.bmc.2009.12.068
23017771 208429 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 479 11 2 3 6.5 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(Cl)c1 10.1016/j.bmc.2009.12.068
CHEMBL605991 208429 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 479 11 2 3 6.5 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(Cl)c1 10.1016/j.bmc.2009.12.068
23017080 207021 0 None 4073 2 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 473 11 2 3 6.4 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL596956 207021 0 None 4073 2 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 473 11 2 3 6.4 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017556 207466 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599836 207466 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017299 208426 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL605974 208426 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
46887059 15287 2 None 524 2 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 487 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094157 15287 2 None 524 2 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 487 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23017600 207298 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 484 11 2 4 6.0 Cc1cccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL598802 207298 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 484 11 2 4 6.0 Cc1cccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23016874 207595 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(F)c1 10.1016/j.bmc.2009.12.068
CHEMBL600831 207595 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(F)c1 10.1016/j.bmc.2009.12.068
23017321 208113 2 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 477 11 2 3 6.2 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1F 10.1016/j.bmc.2009.12.068
CHEMBL604297 208113 2 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 477 11 2 3 6.2 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1F 10.1016/j.bmc.2009.12.068
23017462 208485 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 502 11 2 4 6.1 Cc1cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)ccc1F 10.1016/j.bmc.2009.12.068
CHEMBL606393 208485 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 502 11 2 4 6.1 Cc1cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)ccc1F 10.1016/j.bmc.2009.12.068
23017297 15235 0 None 6456 3 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 525 11 1 6 4.3 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccccc1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1093820 15235 0 None 6456 3 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 525 11 1 6 4.3 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccccc1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
23017484 207456 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(Cl)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599810 207456 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3cccc(Cl)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017311 14905 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 591 11 1 6 5.9 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091740 14905 0 None - 1 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 591 11 1 6 5.9 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2010.02.034
46201043 207361 0 None 457 3 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL599154 207361 0 None 457 3 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
10413147 15852 0 None 1318 3 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 486 10 3 3 7.2 Cc1cc(C)cc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1099047 15852 0 None 1318 3 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 486 10 3 3 7.2 Cc1cc(C)cc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
23017697 207048 0 None - 1 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597147 207048 0 None - 1 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017331 207143 0 None - 1 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 497 11 2 3 6.6 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2009.12.068
CHEMBL597786 207143 0 None - 1 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 497 11 2 3 6.6 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2009.12.068
23017699 207406 0 None - 1 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 503 12 2 4 6.4 COc1cccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2009.12.068
CHEMBL599405 207406 0 None - 1 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 503 12 2 4 6.4 COc1cccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2009.12.068
23016842 15122 0 None 10471 2 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 541 12 1 7 4.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCOc1ccccc1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1092976 15122 0 None 10471 2 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 541 12 1 7 4.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCOc1ccccc1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
23017561 207519 0 None - 1 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 479 11 2 3 6.5 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(Cl)cc1 10.1016/j.bmc.2009.12.068
CHEMBL600219 207519 0 None - 1 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 479 11 2 3 6.5 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(Cl)cc1 10.1016/j.bmc.2009.12.068
10028427 15398 0 None 426 2 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 487 10 2 3 7.2 Cc1cc(C)cc(Oc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095064 15398 0 None 426 2 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 487 10 2 3 7.2 Cc1cc(C)cc(Oc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
10368064 15399 0 None 151 2 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 10 2 4 6.5 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095065 15399 0 None 151 2 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 10 2 4 6.5 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
46887091 15472 0 None 257 2 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095767 15472 0 None 257 2 Mouse 9.6 pKi = 9.6 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
46887092 15288 0 None 380 2 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094160 15288 0 None 380 2 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(F)cc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
46887057 15321 0 None 446 3 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3Cl)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094464 15321 0 None 446 3 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3Cl)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23017043 207297 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 459 11 2 3 6.1 Cc1cccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL598796 207297 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 459 11 2 3 6.1 Cc1cccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017223 207300 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 481 11 2 3 6.1 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cc(F)cc(F)c1 10.1016/j.bmc.2009.12.068
CHEMBL598813 207300 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 481 11 2 3 6.1 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cc(F)cc(F)c1 10.1016/j.bmc.2009.12.068
1883 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 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 10.1016/j.bmcl.2007.11.020
1916 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 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 10.1016/j.bmcl.2007.11.020
5280360 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 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 10.1016/j.bmcl.2007.11.020
913 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 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 10.1016/j.bmcl.2007.11.020
CHEMBL548 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 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 10.1016/j.bmcl.2007.11.020
DB00917 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptorDisplacement of [3H]PGE2 from human EP3 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 10.1016/j.bmcl.2007.11.020
1883 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
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 10.1016/j.bmcl.2007.05.025
1916 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
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 10.1016/j.bmcl.2007.05.025
5280360 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
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 10.1016/j.bmcl.2007.05.025
913 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
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 10.1016/j.bmcl.2007.05.025
CHEMBL548 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
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 10.1016/j.bmcl.2007.05.025
DB00917 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
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 10.1016/j.bmcl.2007.05.025
11562422 15367 0 None 275 2 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 501 11 2 3 7.0 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cc(C)ccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094813 15367 0 None 275 2 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 501 11 2 3 7.0 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cc(C)ccc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23016869 207465 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)c(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599835 207465 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(F)c(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017224 207013 0 None 794 2 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL596903 207013 0 None 794 2 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
23016733 207457 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3C#N)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL599811 207457 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3C#N)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017402 15234 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 560 11 1 8 4.9 Cc1csc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)n1 10.1016/j.bmcl.2010.02.034
CHEMBL1093819 15234 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 560 11 1 8 4.9 Cc1csc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)n1 10.1016/j.bmcl.2010.02.034
23017728 207841 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 475 12 2 4 5.8 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1 10.1016/j.bmc.2009.12.068
CHEMBL602687 207841 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 475 12 2 4 5.8 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1 10.1016/j.bmc.2009.12.068
10413031 15722 0 None 602 3 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 483 10 3 4 6.5 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Nc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1098047 15722 0 None 602 3 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 483 10 3 4 6.5 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Nc3cccc(C#N)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
46887056 15285 0 None 457 2 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094155 15285 0 None 457 2 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 491 11 2 3 6.6 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23017610 208453 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 513 11 2 3 6.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(C(F)(F)F)c1 10.1016/j.bmc.2009.12.068
CHEMBL606181 208453 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 513 11 2 3 6.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc(C(F)(F)F)c1 10.1016/j.bmc.2009.12.068
46887240 15526 0 None 457 3 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 472 10 3 3 6.9 Cc1cccc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1096382 15526 0 None 457 3 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 472 10 3 3 6.9 Cc1cccc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL5092858 222171 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(-c3ccc(C(F)(F)F)cc3)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
23017440 207408 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 481 11 2 3 6.1 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)c(F)c1 10.1016/j.bmc.2009.12.068
CHEMBL599419 207408 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 481 11 2 3 6.1 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)c(F)c1 10.1016/j.bmc.2009.12.068
46887719 15316 0 None 186 2 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 473 11 2 3 6.4 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094419 15316 0 None 186 2 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 473 11 2 3 6.4 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23016900 14903 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 587 11 1 6 6.1 Cc1ccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)cc1Cl 10.1016/j.bmcl.2010.02.034
CHEMBL1091738 14903 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 587 11 1 6 6.1 Cc1ccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)cc1Cl 10.1016/j.bmcl.2010.02.034
23017116 208053 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 503 11 2 5 5.6 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc2c(c1)OCCO2 10.1016/j.bmc.2009.12.068
CHEMBL603969 208053 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 503 11 2 5 5.6 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc2c(c1)OCCO2 10.1016/j.bmc.2009.12.068
23017669 207142 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 531 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.12.068
CHEMBL597785 207142 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 531 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.12.068
23017638 14904 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 607 11 1 6 6.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091739 14904 0 None - 1 Mouse 9.4 pKi = 9.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 607 11 1 6 6.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.02.034
23017438 206992 0 None - 1 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(C#N)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL596738 206992 0 None - 1 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 498 11 2 4 6.3 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(C#N)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
10051189 15361 0 None 1258 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 488 11 2 4 6.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(C)nc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094789 15361 0 None 1258 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 488 11 2 4 6.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(C)nc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL5086191 221792 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
23016858 207054 0 None - 1 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 505 13 2 5 5.8 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1OC 10.1016/j.bmc.2009.12.068
CHEMBL597160 207054 0 None - 1 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 505 13 2 5 5.8 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1OC 10.1016/j.bmc.2009.12.068
23017347 14997 0 None - 1 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 539 11 1 6 5.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.02.034
CHEMBL1092266 14997 0 None - 1 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 539 11 1 6 5.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.02.034
9982348 15368 0 None 912 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 474 11 2 4 5.8 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccnc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094814 15368 0 None 912 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 474 11 2 4 5.8 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccnc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23017332 15029 0 None 4466 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 626 12 1 6 6.6 N#Cc1cccc(OCc2ccc(CCC(=O)NS(=O)(=O)c3ccc(F)c(F)c3)c(OCCc3ccc4ccccc4c3)c2)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1092431 15029 0 None 4466 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 626 12 1 6 6.6 N#Cc1cccc(OCc2ccc(CCC(=O)NS(=O)(=O)c3ccc(F)c(F)c3)c(OCCc3ccc4ccccc4c3)c2)c1 10.1016/j.bmcl.2010.02.034
23017529 14909 0 None 1047 3 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 610 12 1 8 4.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1cccc(N2CCOCC2)c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1091744 14909 0 None 1047 3 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 610 12 1 8 4.1 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1cccc(N2CCOCC2)c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
10480657 15578 0 None 831 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 488 11 2 4 6.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccnc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1096750 15578 0 None 831 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 488 11 2 4 6.1 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3cccnc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23017539 15238 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 543 11 1 7 5.0 Cc1ccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)o1 10.1016/j.bmcl.2010.02.034
CHEMBL1093842 15238 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 543 11 1 7 5.0 Cc1ccc(S(=O)(=O)NC(=O)CCc2ccc(Cn3cccn3)cc2OCCc2ccc3ccccc3c2)o1 10.1016/j.bmcl.2010.02.034
15551229 9038 41 None 446 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 10.1016/j.bmcl.2006.08.025
1941 9038 41 None 446 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 10.1016/j.bmcl.2006.08.025
CHEMBL218071 9038 41 None 446 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 10.1016/j.bmcl.2006.08.025
10302378 89554 0 None 912 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 539 9 1 5 6.6 O=C(/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL217991 89554 0 None 912 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 539 9 1 5 6.6 O=C(/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
23016744 207116 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(Cl)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL597552 207116 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 507 11 2 3 7.1 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3ccc(Cl)cc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017126 207327 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 459 11 2 3 6.1 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1 10.1016/j.bmc.2009.12.068
CHEMBL598995 207327 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 459 11 2 3 6.1 Cc1ccc(C(CC(C)C)NC(=O)c2cc(COc3ccccc3)ccc2CCC(=O)O)cc1 10.1016/j.bmc.2009.12.068
23017423 207080 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 530 13 2 6 5.7 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)cc1OC 10.1016/j.bmc.2009.12.068
CHEMBL597367 207080 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 530 13 2 6 5.7 COc1ccc(C(CC(C)C)NC(=O)c2cc(COc3cccc(C#N)c3)ccc2CCC(=O)O)cc1OC 10.1016/j.bmc.2009.12.068
23017221 207372 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 487 11 2 3 6.7 Cc1ccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)cc1 10.1016/j.bmc.2009.12.068
CHEMBL599204 207372 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 487 11 2 3 6.7 Cc1ccc(OCc2ccc(CCC(=O)O)c(C(=O)NC(CC(C)C)c3cc(C)cc(C)c3)c2)cc1 10.1016/j.bmc.2009.12.068
46887090 15325 0 None 81 3 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 503 12 2 4 6.4 COc1ccccc1OCc1ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c2cc(C)cc(C)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094470 15325 0 None 81 3 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 503 12 2 4 6.4 COc1ccccc1OCc1ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c2cc(C)cc(C)c2)c1 10.1016/j.bmc.2010.03.028
15551228 89431 0 None 10000 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 641 10 1 5 7.3 COc1ccc(Br)cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1 10.1016/j.bmcl.2006.08.025
CHEMBL217941 89431 0 None 10000 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 641 10 1 5 7.3 COc1ccc(Br)cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1 10.1016/j.bmcl.2006.08.025
23017081 207410 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 531 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(C(F)(F)F)c(F)c1 10.1016/j.bmc.2009.12.068
CHEMBL599420 207410 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 531 11 2 3 7.0 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(C(F)(F)F)c(F)c1 10.1016/j.bmc.2009.12.068
23017731 207807 0 None 2238 2 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 445 11 2 3 5.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.12.068
CHEMBL602337 207807 0 None 2238 2 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 445 11 2 3 5.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.12.068
23017731 207807 0 None 2238 2 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 445 11 2 3 5.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL602337 207807 0 None 2238 2 Mouse 9.2 pKi = 9.2 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 445 11 2 3 5.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
23017621 207232 0 None - 1 Mouse 9.1 pKi = 9.1 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 513 11 2 3 6.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.12.068
CHEMBL598409 207232 0 None - 1 Mouse 9.1 pKi = 9.1 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 513 11 2 3 6.8 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.12.068
46887210 15400 0 None 549 2 Mouse 9.1 pKi = 9.1 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 494 10 3 3 6.9 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Nc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095066 15400 0 None 549 2 Mouse 9.1 pKi = 9.1 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 494 10 3 3 6.9 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Nc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
10368531 15403 0 None 478 2 Mouse 9.1 pKi = 9.1 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 495 10 2 3 6.9 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095117 15403 0 None 478 2 Mouse 9.1 pKi = 9.1 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 495 10 2 3 6.9 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3cc(F)cc(F)c3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
15551228 89431 0 None 10000 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 641 10 1 5 7.3 COc1ccc(Br)cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1 10.1016/j.bmcl.2006.08.025
CHEMBL217941 89431 0 None 10000 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 641 10 1 5 7.3 COc1ccc(Br)cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1 10.1016/j.bmcl.2006.08.025
23016797 207616 0 None - 1 Mouse 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)cc1 10.1016/j.bmc.2009.12.068
CHEMBL601029 207616 0 None - 1 Mouse 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccc(F)cc1 10.1016/j.bmc.2009.12.068
23017343 207296 0 None - 1 Mouse 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 459 11 2 3 6.1 Cc1ccccc1C(CC(C)C)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.12.068
CHEMBL598795 207296 0 None - 1 Mouse 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 459 11 2 3 6.1 Cc1ccccc1C(CC(C)C)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.12.068
137477812 189611 0 None 8 2 Rat 9.0 pKi = 9 Binding
Binding affinity to rat EP3Binding affinity to rat EP3
ChEMBL 406 4 2 4 4.2 CC(C)C(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4791261 189611 0 None 8 2 Rat 9.0 pKi = 9 Binding
Binding affinity to rat EP3Binding affinity to rat EP3
ChEMBL 406 4 2 4 4.2 CC(C)C(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL5078847 221369 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
CHEMBL5080528 221469 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None CS(=O)(=O)c1ccc(-n2ncc3c2/C(=C/CNC(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)CCC3)cc1 10.1021/acsmedchemlett.1c00594
CHEMBL5093140 222190 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(C3CCN(c4ccc(F)cc4)CC3)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
CHEMBL5094127 222253 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NS(=O)(=O)c1cc(Cl)c(Cl)s1)OC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21 10.1021/acsmedchemlett.1c00594
137487344 192019 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 392 5 2 2 4.6 CC(C)[C@H](C[C@H]1CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4858203 192019 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 392 5 2 2 4.6 CC(C)[C@H](C[C@H]1CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017606 15237 0 None - 1 Mouse 9.0 pKi = 9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 540 11 1 7 4.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1cccnc1 10.1016/j.bmcl.2010.02.034
CHEMBL1093841 15237 0 None - 1 Mouse 9.0 pKi = 9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 540 11 1 7 4.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1cccnc1 10.1016/j.bmcl.2010.02.034
137478210 192843 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 380 5 2 2 4.6 CC(C)NC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
CHEMBL4871125 192843 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 380 5 2 2 4.6 CC(C)NC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
23017216 205938 0 None 309 4 Mouse 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL589411 205938 0 None 309 4 Mouse 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
9954562 90912 0 None 72 4 Human 9.0 pKi = 9.0 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL220802 90912 0 None 72 4 Human 9.0 pKi = 9.0 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
44304389 209932 0 None 1 4 Mouse 8.9 pKi = 8.9 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCSCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL64188 209932 0 None 1 4 Mouse 8.9 pKi = 8.9 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCSCC(=O)O 10.1016/s0960-894x(01)00365-1
23016807 207517 0 None - 1 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 475 12 2 4 5.8 COc1ccccc1C(CC(C)C)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.12.068
CHEMBL600209 207517 0 None - 1 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 475 12 2 4 5.8 COc1ccccc1C(CC(C)C)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.12.068
23016804 14967 0 None 4168 2 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 11 1 6 5.0 O=C(CCc1ccc(CN2CCOCC2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1092097 14967 0 None 4168 2 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 11 1 6 5.0 O=C(CCc1ccc(CN2CCOCC2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2010.02.034
9954562 90912 0 None 72 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL220802 90912 0 None 72 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
23017225 208456 0 None - 1 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3c(F)cccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
CHEMBL606197 208456 0 None - 1 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc(C(CC(C)C)NC(=O)c2cc(COc3c(F)cccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2009.12.068
23017660 207842 0 None - 1 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1F 10.1016/j.bmc.2009.12.068
CHEMBL602688 207842 0 None - 1 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membraneDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cell membrane
ChEMBL 463 11 2 3 5.9 CC(C)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1F 10.1016/j.bmc.2009.12.068
46887126 15473 0 None 2137 2 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@H](CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095768 15473 0 None 2137 2 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 509 11 2 3 6.7 Cc1cc(C)cc([C@H](CC(C)C)NC(=O)c2cc(COc3cc(F)ccc3F)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
10345923 15474 0 None 60 2 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 501 11 2 3 7.0 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(C)cc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1095769 15474 0 None 60 2 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 501 11 2 3 7.0 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(COc3ccc(C)cc3C)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
22009008 89932 0 None 524 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL218280 89932 0 None 524 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
22009004 148529 0 None 1202 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL385955 148529 0 None 1202 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
23017463 15198 0 None - 1 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 540 11 1 7 4.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccn1 10.1016/j.bmcl.2010.02.034
CHEMBL1093537 15198 0 None - 1 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 540 11 1 7 4.5 O=C(CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccn1 10.1016/j.bmcl.2010.02.034
44304388 209931 0 None -3 5 Mouse 8.7 pKi = 8.7 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL64187 209931 0 None -3 5 Mouse 8.7 pKi = 8.7 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O 10.1016/s0960-894x(01)00365-1
9965922 70651 0 None 158 4 Human 8.0 pKi = 8 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 294 5 2 2 4.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1O 10.1016/j.bmcl.2004.11.051
CHEMBL180389 70651 0 None 158 4 Human 8.0 pKi = 8 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 294 5 2 2 4.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1O 10.1016/j.bmcl.2004.11.051
22009011 70847 0 None 93 4 Human 8.0 pKi = 8 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(/C=C/C(O)c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL180742 70847 0 None 93 4 Human 8.0 pKi = 8 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(/C=C/C(O)c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
44419380 89854 0 None 95 4 Human 8.0 pKi = 8 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
CHEMBL218178 89854 0 None 95 4 Human 8.0 pKi = 8 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
44419384 89855 0 None 95 4 Human 8.0 pKi = 8 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
CHEMBL218179 89855 0 None 95 4 Human 8.0 pKi = 8 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
49850345 68194 6 None 1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
CHEMBL1770317 68194 6 None 1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
137477780 190064 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 407 5 3 3 3.7 CC(C)C(CC1NC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4796825 190064 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 407 5 3 3 3.7 CC(C)C(CC1NC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL5092711 222162 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None COc1ccc(S(=O)(=O)NC(=O)NC/C=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)cc1 10.1021/acsmedchemlett.1c00594
137477876 191332 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 412 7 4 4 2.5 CC(C)C(C(=O)NC(CO)CO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4848264 191332 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 412 7 4 4 2.5 CC(C)C(C(=O)NC(CO)CO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137487318 191352 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 376 5 2 3 4.4 CC(C)C(Cc1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4848523 191352 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 376 5 2 3 4.4 CC(C)C(Cc1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
127046441 146696 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 474 5 2 8 3.0 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CCN(C(=O)C(C)(C)O)CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3799530 146696 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 474 5 2 8 3.0 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CCN(C(=O)C(C)(C)O)CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
52947851 23317 0 None 14 3 Human 7.0 pKi = 7 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237315 23317 0 None 14 3 Human 7.0 pKi = 7 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2004.11.051
52947851 23317 0 None 14 3 Human 7.0 pKi = 7 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL1237315 23317 0 None 14 3 Human 7.0 pKi = 7 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
9813912 144660 0 None 14 3 Human 7.0 pKi = 7 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 264 5 1 1 4.0 O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL376282 144660 0 None 14 3 Human 7.0 pKi = 7 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 264 5 1 1 4.0 O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
10410111 109618 0 None -52 3 Mouse 7.0 pKi = 7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL305568 109618 0 None -52 3 Mouse 7.0 pKi = 7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
2114670 202501 5 None - 1 Human 7.0 pKi = 7 Binding
Inhibition of human EP3 receptorInhibition of human EP3 receptor
ChEMBL 333 5 1 6 3.5 CCC(CC)c1nnc(NC(=O)c2ccc3c(c2)OCCO3)s1 10.1016/j.bmcl.2009.05.074
CHEMBL557109 202501 5 None - 1 Human 7.0 pKi = 7 Binding
Inhibition of human EP3 receptorInhibition of human EP3 receptor
ChEMBL 333 5 1 6 3.5 CCC(CC)c1nnc(NC(=O)c2ccc3c(c2)OCCO3)s1 10.1016/j.bmcl.2009.05.074
71452690 85400 0 None -15 4 Human 6.0 pKi = 6 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 400 9 1 4 5.1 c1ccc(CCSCc2ccc(-c3ccccc3CCc3nnn[nH]3)cc2)cc1 10.1016/s0960-894x(02)00518-8
CHEMBL2112332 85400 0 None -15 4 Human 6.0 pKi = 6 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 400 9 1 4 5.1 c1ccc(CCSCc2ccc(-c3ccccc3CCc3nnn[nH]3)cc2)cc1 10.1016/s0960-894x(02)00518-8
9975502 101264 0 None -74 4 Human 5.0 pKi = 5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251504 101264 0 None -74 4 Human 5.0 pKi = 5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
44442331 101265 0 None -2511 4 Human 5.0 pKi = 5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251505 101265 0 None -2511 4 Human 5.0 pKi = 5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
44269544 42026 0 None -25118 3 Human 4.0 pKi = 4 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 359 11 2 3 3.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)Cc1ccccc1 10.1016/j.bmcl.2004.01.063
CHEMBL14359 42026 0 None -25118 3 Human 4.0 pKi = 4 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 359 11 2 3 3.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)Cc1ccccc1 10.1016/j.bmcl.2004.01.063
44269568 105576 0 None -169 2 Human 5.0 pKi = 5.0 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 387 11 2 3 3.9 CC(C)(c1ccccc1)C(O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL278451 105576 0 None -169 2 Human 5.0 pKi = 5.0 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 387 11 2 3 3.9 CC(C)(c1ccccc1)C(O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
127047602 146483 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 299 3 1 6 2.6 Cn1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3798145 146483 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 299 3 1 6 2.6 Cn1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
71519482 93288 0 None -2 2 Mouse 7.0 pKi = 7.0 Binding
Antagonist activity at mouse EP3 receptorAntagonist activity at mouse EP3 receptor
ChEMBL 578 8 1 5 6.5 O=C(NS(=O)(=O)c1ccc(Cl)cc1)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
CHEMBL2315055 93288 0 None -2 2 Mouse 7.0 pKi = 7.0 Binding
Antagonist activity at mouse EP3 receptorAntagonist activity at mouse EP3 receptor
ChEMBL 578 8 1 5 6.5 O=C(NS(=O)(=O)c1ccc(Cl)cc1)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
52945419 23306 0 None 162 4 Human 8.0 pKi = 8.0 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 772 16 4 6 10.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(O)c1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237296 23306 0 None 162 4 Human 8.0 pKi = 8.0 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 772 16 4 6 10.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(O)c1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
137487348 189119 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 406 4 2 4 4.2 CC(C)[C@H](/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4784483 189119 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 406 4 2 4 4.2 CC(C)[C@H](/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL5082682 221598 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NS(=O)(=O)c1ccc(Cl)cc1)OC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21 10.1021/acsmedchemlett.1c00594
137477890 191337 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 375 5 2 2 5.0 CC(C)C(Cc1ncc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4848372 191337 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 375 5 2 2 5.0 CC(C)C(Cc1ncc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
44304058 209956 0 None -4 5 Mouse 8.0 pKi = 8.0 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 374 13 3 6 2.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCOCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64254 209956 0 None -4 5 Mouse 8.0 pKi = 8.0 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 374 13 3 6 2.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCOCC(=O)O 10.1016/s0960-894x(01)00364-x
117993157 167686 1 None - 1 Human 8.0 pKi = 8.0 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 335 2 2 3 2.7 Cn1ccc2ccc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 nan
CHEMBL4115257 167686 1 None - 1 Human 8.0 pKi = 8.0 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 335 2 2 3 2.7 Cn1ccc2ccc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 nan
91827668 146433 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 430 4 1 7 3.2 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CCN(C(C)=O)CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3797819 146433 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 430 4 1 7 3.2 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CCN(C(C)=O)CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
117993289 167413 0 None - 1 Human 7.9 pKi = 7.9 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 339 2 2 3 2.5 Cn1ccc2cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc(F)c21 nan
CHEMBL4113141 167413 0 None - 1 Human 7.9 pKi = 7.9 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 339 2 2 3 2.5 Cn1ccc2cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc(F)c21 nan
21362845 113680 0 None 257 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 556 7 1 5 7.3 O=C(/C=C/c1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL314616 113680 0 None 257 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 556 7 1 5 7.3 O=C(/C=C/c1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
10295336 208225 0 None 20 4 Mouse 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 415 8 1 3 4.7 O=C(O)/C=C/c1ccc(CN2CCCC2=O)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL604897 208225 0 None 20 4 Mouse 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 415 8 1 3 4.7 O=C(O)/C=C/c1ccc(CN2CCCC2=O)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
23016939 206300 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 389 9 2 3 4.2 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL592056 206300 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 389 9 2 3 4.2 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1ccccc1 10.1016/j.bmc.2009.11.023
44304011 209587 0 None -34 3 Mouse 6.0 pKi = 6.0 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL62305 209587 0 None -34 3 Mouse 6.0 pKi = 6.0 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
10291963 91483 0 None -6456 6 Human 5.0 pKi = 5.0 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
CHEMBL222715 91483 0 None -6456 6 Human 5.0 pKi = 5.0 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
44289922 170303 0 None -707 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
CHEMBL42027 170303 0 None -707 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
137477766 192980 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 375 4 2 2 5.2 Cc1c[nH]c(C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C(C)C)n1 10.1016/j.bmcl.2021.128172
CHEMBL4872962 192980 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 375 4 2 2 5.2 Cc1c[nH]c(C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C(C)C)n1 10.1016/j.bmcl.2021.128172
137477709 193012 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 362 4 2 3 4.2 CC(C)C(c1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4873446 193012 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 362 4 2 3 4.2 CC(C)C(c1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
10294290 206832 0 None 56 4 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595632 206832 0 None 56 4 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
10157813 208395 0 None 69 4 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL605833 208395 0 None 69 4 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
117992889 166626 1 None - 1 Human 7.9 pKi = 7.9 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 335 2 2 3 2.7 Cn1ccc2cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)ccc21 nan
CHEMBL4106568 166626 1 None - 1 Human 7.9 pKi = 7.9 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 335 2 2 3 2.7 Cn1ccc2cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)ccc21 nan
10144273 212613 0 None 131 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 558 8 1 5 7.2 O=C(CCc1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL83450 212613 0 None 131 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 558 8 1 5 7.2 O=C(CCc1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
44320126 213191 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 537 11 1 7 6.2 Cc1cccc(OCCCOc2ccc(-c3ccccc3COC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87816 213191 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 537 11 1 7 6.2 Cc1cccc(OCCCOc2ccc(-c3ccccc3COC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
162650924 187043 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 444 6 2 4 5.5 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cccc(C(C)C)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4750495 187043 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 444 6 2 4 5.5 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cccc(C(C)C)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
162658087 187830 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 438 6 2 6 3.8 CCn1ncc2cc(F)c(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
CHEMBL4759511 187830 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 438 6 2 6 3.8 CCn1ncc2cc(F)c(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
21974331 133324 0 None -19 4 Mouse 5.9 pKi = 5.9 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 399 6 1 4 4.8 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL365243 133324 0 None -19 4 Mouse 5.9 pKi = 5.9 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 399 6 1 4 4.8 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
9959673 213245 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 567 5 2 4 6.1 CC(C)(C)NC(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL88154 213245 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 567 5 2 4 6.1 CC(C)(C)NC(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
11269563 148388 0 None -1096 5 Human 5.9 pKi = 5.9 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
ChEMBL 399 5 1 3 5.2 CC(=O)c1cc(F)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
CHEMBL385126 148388 0 None -1096 5 Human 5.9 pKi = 5.9 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
ChEMBL 399 5 1 3 5.2 CC(=O)c1cc(F)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
10363130 107812 1 None -3 2 Mouse 5.9 pKi = 5.9 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL294585 107812 1 None -3 2 Mouse 5.9 pKi = 5.9 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
10048720 76136 0 None -1230 2 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 437 13 2 5 4.2 CCCc1cccc(C[C@H](O)/C=C/[C@H]2CSC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929541 76136 0 None -1230 2 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 437 13 2 5 4.2 CCCc1cccc(C[C@H](O)/C=C/[C@H]2CSC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
57393340 76250 0 None -851 4 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 530 12 2 7 4.2 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(COCC(F)(F)F)c2)n1 10.1016/j.bmcl.2011.10.109
CHEMBL1933726 76250 0 None -851 4 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 530 12 2 7 4.2 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(COCC(F)(F)F)c2)n1 10.1016/j.bmcl.2011.10.109
9846782 107682 7 None -389 3 Mouse 5.9 pKi = 5.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 454 13 3 7 2.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL293856 107682 7 None -389 3 Mouse 5.9 pKi = 5.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 454 13 3 7 2.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
44289968 107292 0 None -1621 2 Human 4.9 pKi = 4.9 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 415 11 2 3 4.5 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
CHEMBL291182 107292 0 None -1621 2 Human 4.9 pKi = 4.9 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 415 11 2 3 4.5 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
44289792 175941 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 427 11 2 3 4.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
CHEMBL440474 175941 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 427 11 2 3 4.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
44269542 45436 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 339 13 2 3 3.5 CCCCCC(O)/C=C/[C@@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL14655 45436 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 339 13 2 3 3.5 CCCCCC(O)/C=C/[C@@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
71462286 88659 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 742 13 5 8 7.7 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCNC(=S)Nc1ccc(C(=O)O)c(-c2c3ccc(=O)cc-3oc3cc(O)ccc23)c1 10.1021/ml300191g
CHEMBL2164614 88659 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 742 13 5 8 7.7 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCNC(=S)Nc1ccc(C(=O)O)c(-c2c3ccc(=O)cc-3oc3cc(O)ccc23)c1 10.1021/ml300191g
52944193 23305 0 None 63 4 Human 7.9 pKi = 7.9 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237295 23305 0 None 63 4 Human 7.9 pKi = 7.9 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
52944194 23315 0 None 57 4 Human 7.9 pKi = 7.9 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 936 18 4 6 12.8 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(CO)c1OCc1c(Cl)cccc1Cl.O=C(O)/C=C/c1ccccc1C/C=C/c1cccc(CO)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL1237305 23315 0 None 57 4 Human 7.9 pKi = 7.9 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 936 18 4 6 12.8 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(CO)c1OCc1c(Cl)cccc1Cl.O=C(O)/C=C/c1ccccc1C/C=C/c1cccc(CO)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
10271490 172672 0 None 29 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 386 9 1 2 5.8 Cc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL424975 172672 0 None 29 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 386 9 1 2 5.8 Cc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
137477918 188295 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 434 6 2 4 5.0 CCC(CC)C(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4765017 188295 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 434 6 2 4 5.0 CCC(CC)C(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
162661390 188298 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 420 5 2 4 4.5 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4765027 188298 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 420 5 2 4 4.5 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137477983 189722 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 422 4 2 4 4.9 CC(C)C(/C=C1\SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4792728 189722 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 422 4 2 4 4.9 CC(C)C(/C=C1\SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL5079457 221398 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(C3CCN(c4ccc(F)cc4)CC3)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
23016909 206301 0 None - 1 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 403 9 2 3 4.8 CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL592061 206301 0 None - 1 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 403 9 2 3 4.8 CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
117993541 167485 0 None - 1 Human 7.9 pKi = 7.9 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 354 2 2 4 2.2 Cn1ncc2c(F)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 nan
CHEMBL4113622 167485 0 None - 1 Human 7.9 pKi = 7.9 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 354 2 2 4 2.2 Cn1ncc2c(F)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 nan
10273914 206451 0 None 20 3 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(COc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL593041 206451 0 None 20 3 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(COc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
10136146 208003 0 None 16 2 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 408 8 1 2 6.2 O=C(O)/C=C/c1ccc(Cc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL603653 208003 0 None 16 2 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 408 8 1 2 6.2 O=C(O)/C=C/c1ccc(Cc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
44304008 210021 0 None -18 4 Mouse 6.9 pKi = 6.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 410 11 3 6 2.4 O=C(O)CSCCCS[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/s0960-894x(01)00364-x
CHEMBL64542 210021 0 None -18 4 Mouse 6.9 pKi = 6.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 410 11 3 6 2.4 O=C(O)CSCCCS[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/s0960-894x(01)00364-x
9939791 168697 0 None -107 8 Human 5.9 pKi = 5.9 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
CHEMBL415310 168697 0 None -107 8 Human 5.9 pKi = 5.9 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
162672070 189754 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 438 6 2 6 3.8 CCn1ncc2c(F)c(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)ccc21 10.1021/acsmedchemlett.0c00667
CHEMBL4793202 189754 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 438 6 2 6 3.8 CCn1ncc2c(F)c(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)ccc21 10.1021/acsmedchemlett.0c00667
9916766 213562 0 None -64 2 Human 4.9 pKi = 4.9 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 601 7 2 4 6.5 O=C(NCc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL90226 213562 0 None -64 2 Human 4.9 pKi = 4.9 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 601 7 2 4 6.5 O=C(NCc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
10202765 179466 0 None -8128 3 Human 4.9 pKi = 4.9 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 427 11 2 3 4.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
CHEMBL45008 179466 0 None -8128 3 Human 4.9 pKi = 4.9 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 427 11 2 3 4.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
11955315 150569 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 mins
ChEMBL 394 9 3 3 4.6 CC(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3901088 150569 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 mins
ChEMBL 394 9 3 3 4.6 CC(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
71458758 127640 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 615 14 1 4 7.8 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
CHEMBL2164612 127640 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 615 14 1 4 7.8 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
CHEMBL3558858 127640 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 615 14 1 4 7.8 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
137477794 191248 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 393 5 3 3 3.2 CC(C)C(C(=O)NC1CNC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4846915 191248 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 393 5 3 3 3.2 CC(C)C(C(=O)NC1CNC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137487367 192078 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 428 4 1 3 4.5 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCCCS1(=O)=O 10.1016/j.bmcl.2021.128172
CHEMBL4859300 192078 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 428 4 1 3 4.5 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCCCS1(=O)=O 10.1016/j.bmcl.2021.128172
127047729 146434 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 347 4 1 6 3.7 CCn1ncc2c(Cl)cc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3797824 146434 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 347 4 1 6 3.7 CCn1ncc2c(Cl)cc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
117992929 167681 0 None - 1 Human 7.9 pKi = 7.9 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 356 2 2 4 2.4 Cn1ncc2c(Cl)cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc21 nan
CHEMBL4115231 167681 0 None - 1 Human 7.9 pKi = 7.9 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 356 2 2 4 2.4 Cn1ncc2c(Cl)cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc21 nan
127046263 146594 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 446 5 2 8 2.2 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CCN(C(=O)CO)CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3798872 146594 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 446 5 2 8 2.2 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CCN(C(=O)CO)CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
137477597 189501 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 392 3 2 4 4.0 CC(C)/C(=C1/OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4789676 189501 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 392 3 2 4 4.0 CC(C)/C(=C1/OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
23017213 14950 0 None - 1 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 539 11 1 6 5.0 O=C(NS(=O)(=O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.02.034
CHEMBL1091959 14950 0 None - 1 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 539 11 1 6 5.0 O=C(NS(=O)(=O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.02.034
44304258 109133 0 None -6 3 Mouse 6.9 pKi = 6.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL303787 109133 0 None -6 3 Mouse 6.9 pKi = 6.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
11210487 71068 0 None -177 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 356 7 1 2 5.5 O=C(O)/C=C/c1ccccc1/C=C/c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL181035 71068 0 None -177 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 356 7 1 2 5.5 O=C(O)/C=C/c1ccccc1/C=C/c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
71460570 88654 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 353 9 2 4 3.4 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCN 10.1021/ml300191g
CHEMBL2164607 88654 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 353 9 2 4 3.4 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCN 10.1021/ml300191g
CHEMBL5087700 221891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cccs1 10.1021/acsmedchemlett.1c00594
57396825 76248 0 None -30 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2011.10.109
CHEMBL1933724 76248 0 None -30 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2011.10.109
57396825 76248 0 None -30 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2012.02.018
CHEMBL1933724 76248 0 None -30 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2012.02.018
137478100 192429 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 379 4 2 4 3.8 CC(C)C(c1noc(=O)[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4864589 192429 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 379 4 2 4 3.8 CC(C)C(c1noc(=O)[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137477893 192435 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 471 6 1 4 3.7 CC(C)C(CN1CCN(S(C)(=O)=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4864757 192435 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 471 6 1 4 3.7 CC(C)C(CN1CCN(S(C)(=O)=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
46886376 14998 0 None - 1 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 540 10 2 6 4.9 O=C(NCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.02.034
CHEMBL1092267 14998 0 None - 1 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 540 10 2 6 4.9 O=C(NCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.02.034
44320388 213187 0 None 19 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 536 11 2 6 5.8 Cc1cccc(OCCCOc2ccc(-c3ccccc3CNC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87797 213187 0 None 19 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 536 11 2 6 5.8 Cc1cccc(OCCCOc2ccc(-c3ccccc3CNC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
23017746 206628 0 None 13 3 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 8 1 3 6.2 O=C(O)/C=C/c1ccc(Cc2cccs2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL594365 206628 0 None 13 3 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 8 1 3 6.2 O=C(O)/C=C/c1ccc(Cc2cccs2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
21362863 25231 0 None 13 2 Human 5.8 pKi = 5.8 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccc(OCc3ccccc3)cc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL127204 25231 0 None 13 2 Human 5.8 pKi = 5.8 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccc(OCc3ccccc3)cc2)c1 10.1016/s0960-894x(03)00794-7
9867899 209903 0 None -47 3 Mouse 5.8 pKi = 5.8 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 440 13 3 5 3.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2CCSCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL64072 209903 0 None -47 3 Mouse 5.8 pKi = 5.8 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 440 13 3 5 3.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2CCSCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
10113842 90363 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 435 6 1 5 5.2 O=C(/C=C/c1ccccc1Oc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL2204336 90363 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 435 6 1 5 5.2 O=C(/C=C/c1ccccc1Oc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
59465571 153063 0 None -21 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 mins
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3920796 153063 0 None -21 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 mins
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
10113842 90363 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 435 6 1 5 5.2 O=C(/C=C/c1ccccc1Oc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL2204336 90363 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 435 6 1 5 5.2 O=C(/C=C/c1ccccc1Oc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
52946883 25170 0 None -3 2 Rat 6.8 pKi = 6.8 Binding
Inhibition of rat EP3 receptorInhibition of rat EP3 receptor
ChEMBL 381 5 2 3 4.8 CCc1cccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
CHEMBL1271476 25170 0 None -3 2 Rat 6.8 pKi = 6.8 Binding
Inhibition of rat EP3 receptorInhibition of rat EP3 receptor
ChEMBL 381 5 2 3 4.8 CCc1cccc(NC(=O)Nc2cccn(Cc3ccccc3Cl)c2=O)c1 10.1016/j.bmcl.2010.08.137
44349503 175169 0 None 100 4 Human 7.8 pKi = 7.8 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 553 10 1 5 7.1 O=C(CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
CHEMBL434637 175169 0 None 100 4 Human 7.8 pKi = 7.8 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 553 10 1 5 7.1 O=C(CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
10168694 213128 0 None 309 4 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 671 17 1 7 8.2 O=C(CCc1ccccc1-c1ccc(OCCCOc2cccc(CSCCc3ccccc3)c2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL87366 213128 0 None 309 4 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 671 17 1 7 8.2 O=C(CCc1ccccc1-c1ccc(OCCCOc2cccc(CSCCc3ccccc3)c2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
137478269 192295 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 393 4 2 4 5.2 CC(C)C(c1cnc(N)s1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4862628 192295 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 393 4 2 4 5.2 CC(C)C(c1cnc(N)s1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
10294289 206950 0 None 138 2 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL596515 206950 0 None 138 2 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
127046264 146622 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 460 5 2 8 2.6 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CCN(C(=O)C(C)O)CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3799118 146622 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 460 5 2 8 2.6 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CCN(C(=O)C(C)O)CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
15907747 213802 0 None -31 4 Human 5.8 pKi = 5.8 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
CHEMBL91537 213802 0 None -31 4 Human 5.8 pKi = 5.8 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
22990263 23565 0 None 4 3 Human 5.8 pKi = 5.8 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 292 3 1 1 4.8 O=C(O)/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(03)00794-7
CHEMBL124574 23565 0 None 4 3 Human 5.8 pKi = 5.8 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 292 3 1 1 4.8 O=C(O)/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(03)00794-7
9981052 76128 0 None -794 2 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 447 11 2 5 3.6 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929533 76128 0 None -794 2 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 447 11 2 5 3.6 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmc.2011.12.009
10112412 76243 0 None -2630 3 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933719 76243 0 None -2630 3 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmcl.2011.10.109
10112412 76243 0 None -2630 3 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933719 76243 0 None -2630 3 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
9895436 113793 0 None -891 7 Human 4.8 pKi = 4.8 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 628 8 1 4 7.4 CC(C)(Cc1ccccc1)C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL315391 113793 0 None -891 7 Human 4.8 pKi = 4.8 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 628 8 1 4 7.4 CC(C)(Cc1ccccc1)C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
44289921 171150 0 None -2089 3 Human 4.8 pKi = 4.8 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 365 11 2 3 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)CC1CCCCC1 10.1016/j.bmcl.2004.01.063
CHEMBL42129 171150 0 None -2089 3 Human 4.8 pKi = 4.8 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 365 11 2 3 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)CC1CCCCC1 10.1016/j.bmcl.2004.01.063
137478093 186974 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 421 5 2 3 4.0 CC(C)C(CC1C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4749494 186974 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 421 5 2 3 4.0 CC(C)C(CC1C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137478196 187760 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 420 4 2 4 4.6 C/C(=C1/OC(=O)NC1=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1021/acsmedchemlett.0c00667
CHEMBL4758663 187760 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 420 4 2 4 4.6 C/C(=C1/OC(=O)NC1=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1021/acsmedchemlett.0c00667
137487333 189238 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 430 6 2 4 5.0 CCc1cccc2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc12 10.1021/acsmedchemlett.0c00667
CHEMBL4786317 189238 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 430 6 2 4 5.0 CCc1cccc2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc12 10.1021/acsmedchemlett.0c00667
CHEMBL5087384 221871 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00594
137477590 191555 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 394 6 2 5 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL4851298 191555 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 394 6 2 5 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
10139917 90365 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 467 6 1 5 4.6 O=C(/C=C/c1ccccc1[S+]([O-])c1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL2204338 90365 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 467 6 1 5 4.6 O=C(/C=C/c1ccccc1[S+]([O-])c1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
10206535 73346 0 None -323 4 Mouse 5.8 pKi = 5.8 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 488 6 1 6 4.7 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccc(F)cc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL185251 73346 0 None -323 4 Mouse 5.8 pKi = 5.8 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 488 6 1 6 4.7 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccc(F)cc3O2)cc1 10.1016/j.bmcl.2004.07.039
10116114 132664 0 None -489 8 Mouse 5.8 pKi = 5.8 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL364841 132664 0 None -489 8 Mouse 5.8 pKi = 5.8 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
44349531 23337 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 394 7 1 2 6.2 O=C(O)Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL123844 23337 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 394 7 1 2 6.2 O=C(O)Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
10457106 76132 0 None -58 2 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 463 12 2 6 3.5 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1cccc(OC(F)(F)F)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929537 76132 0 None -58 2 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 463 12 2 6 3.5 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1cccc(OC(F)(F)F)c1 10.1016/j.bmc.2011.12.009
10000670 76144 0 None -2454 2 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 393 11 2 3 4.1 O=C(O)CCCCCCN1C(=S)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(F)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929549 76144 0 None -2454 2 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 393 11 2 3 4.1 O=C(O)CCCCCCN1C(=S)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(F)c1 10.1016/j.bmc.2011.12.009
10116116 71185 0 None -218 5 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1c(CC(=O)O)c2ccccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813115 71185 0 None -218 5 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1c(CC(=O)O)c2ccccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
10116114 132664 0 None -489 8 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL364841 132664 0 None -489 8 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
57464006 81943 0 None -14125 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 534 10 2 7 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3cc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036322 81943 0 None -14125 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 534 10 2 7 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3cc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
56672018 71581 0 None -2 3 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 446 7 1 5 3.9 CN1C[C@@H](COc2ccc(C(=O)N(C)c3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819606 71581 0 None -2 3 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 446 7 1 5 3.9 CN1C[C@@H](COc2ccc(C(=O)N(C)c3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
10116114 132664 0 None -489 8 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.08.007
CHEMBL364841 132664 0 None -489 8 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.08.007
71461205 90367 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 449 7 1 5 5.0 O=C(/C=C/c1ccccc1OCc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL2204340 90367 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 449 7 1 5 5.0 O=C(/C=C/c1ccccc1OCc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL5089190 221976 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cccc(Cl)c1 10.1021/acsmedchemlett.1c00594
137478241 192900 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 320 4 2 2 3.4 CC(C)C(C(N)=O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4871834 192900 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 320 4 2 2 3.4 CC(C)C(C(N)=O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
71462285 88655 0 None 177 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 478 10 1 5 6.0 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
CHEMBL2164608 88655 0 None 177 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 478 10 1 5 6.0 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
23017322 207012 0 None 107 2 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 459 12 2 3 5.7 CC(C)CC(Cc1ccccc1)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.11.023
CHEMBL596902 207012 0 None 107 2 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 459 12 2 3 5.7 CC(C)CC(Cc1ccccc1)NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O 10.1016/j.bmc.2009.11.023
10001791 76138 0 None -1174 2 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 413 11 2 5 3.4 O=C(O)CCCSCCN1C(=O)SC[C@@H]1/C=C/[C@@H](O)Cc1cccc(F)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929543 76138 0 None -1174 2 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 413 11 2 5 3.4 O=C(O)CCCSCCN1C(=O)SC[C@@H]1/C=C/[C@@H](O)Cc1cccc(F)c1 10.1016/j.bmc.2011.12.009
44390782 71377 0 None 57 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 402 10 1 3 5.5 COc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL181691 71377 0 None 57 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 402 10 1 3 5.5 COc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
164619977 192321 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 376 5 2 3 4.6 CCC(CC)(c1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4863000 192321 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 376 5 2 3 4.6 CCC(CC)(c1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
117993506 167246 0 None - 1 Human 7.7 pKi = 7.7 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 335 3 2 3 2.8 CCn1ccc2ccc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc21 nan
CHEMBL4111788 167246 0 None - 1 Human 7.7 pKi = 7.7 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 335 3 2 3 2.8 CCn1ccc2ccc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc21 nan
9845064 76123 0 None -79 3 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 420 13 2 5 3.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)[C@@H]2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929528 76123 0 None -79 3 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 420 13 2 5 3.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)[C@@H]2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
9885106 91548 0 None -954 6 Human 5.7 pKi = 5.7 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1021/jm049290a
CHEMBL223151 91548 0 None -954 6 Human 5.7 pKi = 5.7 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1021/jm049290a
10320021 76127 0 None -794 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 421 13 2 5 3.5 CCCc1cccc(C[C@H](O)/C=C/[C@H]2COC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929532 76127 0 None -794 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 421 13 2 5 3.5 CCCc1cccc(C[C@H](O)/C=C/[C@H]2COC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
10228100 71188 0 None -331 5 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 488 6 1 6 4.7 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813118 71188 0 None -331 5 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 488 6 1 6 4.7 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
11545879 21678 3 None -794 3 Human 5.7 pKi = 5.7 Binding
Activity at EP3 receptor by FLIPR methodActivity at EP3 receptor by FLIPR method
ChEMBL 381 6 1 3 5.8 CC(C)COc1ccc(Cl)cc1-c1ccccc1-c1cccc(C(=O)O)n1 10.1016/j.bmcl.2008.11.032
CHEMBL1207973 21678 3 None -794 3 Human 5.7 pKi = 5.7 Binding
Activity at EP3 receptor by FLIPR methodActivity at EP3 receptor by FLIPR method
ChEMBL 381 6 1 3 5.8 CC(C)COc1ccc(Cl)cc1-c1ccccc1-c1cccc(C(=O)O)n1 10.1016/j.bmcl.2008.11.032
CHEMBL467510 21678 3 None -794 3 Human 5.7 pKi = 5.7 Binding
Activity at EP3 receptor by FLIPR methodActivity at EP3 receptor by FLIPR method
ChEMBL 381 6 1 3 5.8 CC(C)COc1ccc(Cl)cc1-c1ccccc1-c1cccc(C(=O)O)n1 10.1016/j.bmcl.2008.11.032
44304334 208355 0 None 4 5 Mouse 8.7 pKi = 8.7 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL60555 208355 0 None 4 5 Mouse 8.7 pKi = 8.7 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL5080602 221474 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None Cc1nc(C)c(S(=O)(=O)NC(=O)NC/C=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)s1 10.1021/acsmedchemlett.1c00594
CHEMBL5084190 221679 3 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None Cc1cc(S(=O)(=O)NC(=O)NC/C(F)=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)sc1Cl 10.1021/acsmedchemlett.1c00594
CHEMBL5091517 222091 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None COc1ccc(-n2ncc3c2/C(=C/CNC(=O)NS(=O)(=O)c2cc(Cl)c(Cl)s2)CCC3)cn1 10.1021/acsmedchemlett.1c00594
91668213 128535 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assayDisplacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assay
ChEMBL 368 3 2 4 2.7 CCn1ncc2c(F)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.5b00188
CHEMBL3589082 128535 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assayDisplacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assay
ChEMBL 368 3 2 4 2.7 CCn1ncc2c(F)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.5b00188
137487375 192549 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 499 6 2 4 3.6 CC(C)C(C(=O)NC1CCN(S(C)(=O)=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4866485 192549 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 499 6 2 4 3.6 CC(C)C(C(=O)NC1CCN(S(C)(=O)=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
91668213 128535 0 None - 1 Human 8.7 pKi = 8.7 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 368 3 2 4 2.7 CCn1ncc2c(F)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 nan
CHEMBL3589082 128535 0 None - 1 Human 8.7 pKi = 8.7 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 368 3 2 4 2.7 CCn1ncc2c(F)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 nan
9913176 90366 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 483 6 1 6 4.3 O=C(/C=C/c1ccccc1S(=O)(=O)c1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL2204339 90366 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 483 6 1 6 4.3 O=C(/C=C/c1ccccc1S(=O)(=O)c1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
1883 9856 75 None -1 24 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
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/acs.jmedchem.9b00336
1916 9856 75 None -1 24 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
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/acs.jmedchem.9b00336
5280360 9856 75 None -1 24 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
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/acs.jmedchem.9b00336
913 9856 75 None -1 24 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
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/acs.jmedchem.9b00336
CHEMBL548 9856 75 None -1 24 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
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/acs.jmedchem.9b00336
DB00917 9856 75 None -1 24 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
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/acs.jmedchem.9b00336
137477910 191415 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 390 4 2 2 4.5 CC(C)C(/C=C1\CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4849504 191415 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 390 4 2 2 4.5 CC(C)C(/C=C1\CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
22008967 89924 0 None 416 4 Human 8.6 pKi = 8.6 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL218228 89924 0 None 416 4 Human 8.6 pKi = 8.6 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
22008966 89925 0 None 416 4 Human 8.6 pKi = 8.6 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL218229 89925 0 None 416 4 Human 8.6 pKi = 8.6 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
10302378 89554 0 None 912 4 Human 8.6 pKi = 8.6 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 539 9 1 5 6.6 O=C(/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL217991 89554 0 None 912 4 Human 8.6 pKi = 8.6 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 539 9 1 5 6.6 O=C(/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
137477985 191211 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 422 5 2 3 4.4 CC(C)C(C(=O)NC1CCOCC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4846309 191211 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 422 5 2 3 4.4 CC(C)C(C(=O)NC1CCOCC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137477920 192643 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 406 5 1 2 5.1 CC(C)C(CN1CCCCC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4867987 192643 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 406 5 1 2 5.1 CC(C)C(CN1CCCCC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137477950 193153 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 470 5 2 4 3.8 CC(C)C(C(=O)NC1CCS(=O)(=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4875575 193153 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 470 5 2 4 3.8 CC(C)C(C(=O)NC1CCS(=O)(=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137477644 191874 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 368 5 2 3 3.8 CONC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
CHEMBL4856048 191874 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 368 5 2 3 3.8 CONC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
21362912 177954 0 None 3 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 535 12 1 5 6.7 O=C(CCCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL445895 177954 0 None 3 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 535 12 1 5 6.7 O=C(CCCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
10139917 90365 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 467 6 1 5 4.6 O=C(/C=C/c1ccccc1[S+]([O-])c1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL2204338 90365 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 467 6 1 5 4.6 O=C(/C=C/c1ccccc1[S+]([O-])c1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
52950151 23309 0 None -3 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1.Cc1cccc(C/C=C/c2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237299 23309 0 None -3 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1.Cc1cccc(C/C=C/c2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44269516 50407 30 None -57 3 Human 5.7 pKi = 5.7 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CCC1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL15096 50407 30 None -57 3 Human 5.7 pKi = 5.7 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CCC1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
44303711 109129 0 None -46 3 Mouse 5.7 pKi = 5.7 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 406 13 3 4 4.4 CCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL303763 109129 0 None -46 3 Mouse 5.7 pKi = 5.7 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 406 13 3 4 4.4 CCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
10319835 76142 0 None -5011 3 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 417 13 2 3 4.9 CCCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929547 76142 0 None -5011 3 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 417 13 2 3 4.9 CCCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
11696697 105808 0 None -676 3 Human 4.7 pKi = 4.7 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 385 11 2 3 3.7 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)C1(c2ccccc2)CC1 10.1016/j.bmcl.2004.01.063
CHEMBL280223 105808 0 None -676 3 Human 4.7 pKi = 4.7 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 385 11 2 3 3.7 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)C1(c2ccccc2)CC1 10.1016/j.bmcl.2004.01.063
44269596 105837 0 None -19 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 373 12 2 3 3.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)CCc1ccccc1 10.1016/s0960-894x(03)00042-8
CHEMBL280442 105837 0 None -19 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 373 12 2 3 3.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)CCc1ccccc1 10.1016/s0960-894x(03)00042-8
71517030 93289 0 None -3 2 Mouse 6.7 pKi = 6.7 Binding
Antagonist activity at mouse EP3 receptorAntagonist activity at mouse EP3 receptor
ChEMBL 612 8 1 5 7.1 O=C(NS(=O)(=O)c1cc(Cl)ccc1Cl)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
CHEMBL2315056 93289 0 None -3 2 Mouse 6.7 pKi = 6.7 Binding
Antagonist activity at mouse EP3 receptorAntagonist activity at mouse EP3 receptor
ChEMBL 612 8 1 5 7.1 O=C(NS(=O)(=O)c1cc(Cl)ccc1Cl)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
10227492 23670 0 None 52 4 Human 7.7 pKi = 7.7 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 476 8 1 2 7.9 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2c(Cl)cccc2Cl)c1 10.1016/s0960-894x(03)00794-7
CHEMBL125087 23670 0 None 52 4 Human 7.7 pKi = 7.7 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 476 8 1 2 7.9 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2c(Cl)cccc2Cl)c1 10.1016/s0960-894x(03)00794-7
10157813 208395 0 None 69 4 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmcl.2010.02.034
CHEMBL605833 208395 0 None 69 4 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmcl.2010.02.034
46230201 207395 0 None 52 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL599355 207395 0 None 52 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
23017109 206853 0 None 6 2 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 416 10 1 5 4.3 O=C(O)COCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595830 206853 0 None 6 2 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 416 10 1 5 4.3 O=C(O)COCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
56658143 71579 0 None -1 6 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 468 8 2 6 3.4 CN1C[C@@H](COc2ccc(S(=O)(=O)Nc3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819604 71579 0 None -1 6 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 468 8 2 6 3.4 CN1C[C@@H](COc2ccc(S(=O)(=O)Nc3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
23017563 206170 0 None - 1 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 403 10 2 3 4.3 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCCc1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL591034 206170 0 None - 1 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 403 10 2 3 4.3 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCCc1ccccc1 10.1016/j.bmc.2009.11.023
71519330 93282 0 None 1 2 Mouse 6.7 pKi = 6.7 Binding
Antagonist activity at mouse EP3 receptorAntagonist activity at mouse EP3 receptor
ChEMBL 460 8 1 3 6.1 CC(C)CNC(=O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
CHEMBL2315049 93282 0 None 1 2 Mouse 6.7 pKi = 6.7 Binding
Antagonist activity at mouse EP3 receptorAntagonist activity at mouse EP3 receptor
ChEMBL 460 8 1 3 6.1 CC(C)CNC(=O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
71456905 127639 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 589 13 1 4 7.3 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
CHEMBL2164611 127639 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 589 13 1 4 7.3 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
CHEMBL3558857 127639 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 589 13 1 4 7.3 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
137477703 187073 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 404 4 2 4 4.0 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4750905 187073 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 404 4 2 4 4.0 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CC2)O1 10.1021/acsmedchemlett.0c00667
137487342 188220 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 408 3 2 4 4.7 CC(C)/C(=C1/SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4764161 188220 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 408 3 2 4 4.7 CC(C)/C(=C1/SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137477572 192838 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 377 5 3 4 4.3 CC(C)C(Nc1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4871021 192838 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 377 5 3 4 4.3 CC(C)C(Nc1nnc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017476 15252 0 None - 1 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 477 10 1 6 3.7 CS(=O)(=O)NC(=O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmcl.2010.02.034
CHEMBL1093911 15252 0 None - 1 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 477 10 1 6 3.7 CS(=O)(=O)NC(=O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmcl.2010.02.034
10271818 207926 0 None - 1 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 392 11 1 5 4.3 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCCCOc1ccccc1 10.1016/j.bmc.2009.08.007
CHEMBL603227 207926 0 None - 1 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 392 11 1 5 4.3 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCCCOc1ccccc1 10.1016/j.bmc.2009.08.007
44304051 109537 0 None -30 4 Mouse 6.7 pKi = 6.7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
CHEMBL305126 109537 0 None -30 4 Mouse 6.7 pKi = 6.7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
9886718 209942 0 None -309 4 Mouse 6.7 pKi = 6.7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64217 209942 0 None -309 4 Mouse 6.7 pKi = 6.7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
11315933 130072 4 None -1202 5 Mouse 5.7 pKi = 5.7 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 413 7 1 4 4.9 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL361457 130072 4 None -1202 5 Mouse 5.7 pKi = 5.7 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 413 7 1 4 4.9 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
9938995 118483 0 None -21 2 Human 5.7 pKi = 5.7 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 621 8 2 5 6.6 O=C(NCCc1cccs1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL328697 118483 0 None -21 2 Human 5.7 pKi = 5.7 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 621 8 2 5 6.6 O=C(NCCc1cccs1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
44304335 209757 0 None -281 4 Mouse 5.7 pKi = 5.7 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 422 10 4 4 4.0 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
CHEMBL63061 209757 0 None -281 4 Mouse 5.7 pKi = 5.7 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 422 10 4 4 4.0 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
10158725 23600 0 None 28 4 Human 7.6 pKi = 7.6 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL124738 23600 0 None 28 4 Human 7.6 pKi = 7.6 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
137477752 187018 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 420 4 2 4 4.5 Cc1cc(C(/C=C2\OC(=O)NC2=O)C(C)C)c(=O)[nH]c1-c1ccc2cccc(F)c2c1 10.1021/acsmedchemlett.0c00667
CHEMBL4750135 187018 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 420 4 2 4 4.5 Cc1cc(C(/C=C2\OC(=O)NC2=O)C(C)C)c(=O)[nH]c1-c1ccc2cccc(F)c2c1 10.1021/acsmedchemlett.0c00667
137487355 189712 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 440 4 2 4 4.6 O=C1NC(=O)/C(=C/C(c2ccccc2)c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4792611 189712 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 440 4 2 4 4.6 O=C1NC(=O)/C(=C/C(c2ccccc2)c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)O1 10.1021/acsmedchemlett.0c00667
137477714 192028 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 403 4 2 3 3.8 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCN/C1=N\C#N 10.1016/j.bmcl.2021.128172
CHEMBL4858376 192028 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 403 4 2 3 3.8 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCN/C1=N\C#N 10.1016/j.bmcl.2021.128172
71458756 88657 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 519 13 2 8 5.4 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCNc1ccc([N+](=O)[O-])cc1[N+](=O)[O-] 10.1021/ml300191g
CHEMBL2164610 88657 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 519 13 2 8 5.4 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCNc1ccc([N+](=O)[O-])cc1[N+](=O)[O-] 10.1021/ml300191g
137487319 189073 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 470 5 2 4 5.4 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cccc(C(F)(F)F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4784048 189073 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 470 5 2 4 5.4 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cccc(C(F)(F)F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
18973764 23419 0 None -15 4 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 346 8 1 2 5.1 O=C(O)c1ccc(CCCc2ccccc2OCc2ccccc2)cc1 10.1016/s0960-894x(03)00794-7
CHEMBL124199 23419 0 None -15 4 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 346 8 1 2 5.1 O=C(O)c1ccc(CCCc2ccccc2OCc2ccccc2)cc1 10.1016/s0960-894x(03)00794-7
10384865 76140 0 None -1513 2 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 375 11 2 3 4.0 O=C(O)CCCCCCN1C(=S)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/j.bmc.2011.12.009
CHEMBL1929545 76140 0 None -1513 2 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 375 11 2 3 4.0 O=C(O)CCCCCCN1C(=S)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/j.bmc.2011.12.009
10431288 76141 0 None -2754 3 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 403 12 2 3 4.5 CCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929546 76141 0 None -2754 3 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 403 12 2 3 4.5 CCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
44269464 41251 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL14286 41251 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
162657359 187756 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 437 6 2 6 3.5 CCN1CCOc2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
CHEMBL4758607 187756 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 437 6 2 6 3.5 CCN1CCOc2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
164615533 191419 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 362 4 1 3 5.1 CC(C)C(c1ncco1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4849556 191419 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 362 4 1 3 5.1 CC(C)C(c1ncco1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
21362867 113879 0 None 104 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 417 7 1 5 4.6 CSc1cccc(-c2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL315974 113879 0 None 104 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 417 7 1 5 4.6 CSc1cccc(-c2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/s0960-894x(02)00518-8
9873528 213709 0 None -15 4 Human 5.6 pKi = 5.6 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 602 7 1 5 6.9 O=C(NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)OCc1ccccc1 10.1016/s0960-894x(99)00465-5
CHEMBL91063 213709 0 None -15 4 Human 5.6 pKi = 5.6 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 602 7 1 5 6.9 O=C(NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)OCc1ccccc1 10.1016/s0960-894x(99)00465-5
11418818 73436 0 None -12 4 Mouse 5.6 pKi = 5.6 Binding
Binding affinity for mouse Prostanoid EP3 receptorBinding affinity for mouse Prostanoid EP3 receptor
ChEMBL 423 10 1 5 5.2 CCCCOc1ccc(C(=O)n2c(C)c(CCCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL185369 73436 0 None -12 4 Mouse 5.6 pKi = 5.6 Binding
Binding affinity for mouse Prostanoid EP3 receptorBinding affinity for mouse Prostanoid EP3 receptor
ChEMBL 423 10 1 5 5.2 CCCCOc1ccc(C(=O)n2c(C)c(CCCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
10181606 213130 0 None 33 7 Human 7.6 pKi = 7.6 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
CHEMBL87371 213130 0 None 33 7 Human 7.6 pKi = 7.6 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
10181606 213130 0 None 33 7 Human 7.6 pKi = 7.6 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL87371 213130 0 None 33 7 Human 7.6 pKi = 7.6 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
52943000 23307 0 None 26 4 Human 7.6 pKi = 7.6 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237297 23307 0 None 26 4 Human 7.6 pKi = 7.6 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
137477697 187264 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 410 4 2 4 4.4 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1SC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4753054 187264 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 410 4 2 4 4.4 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1SC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
137478136 192926 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 442 8 5 5 1.9 CC(C)C(C(=O)NC(CO)(CO)CO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4872246 192926 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 442 8 5 5 1.9 CC(C)C(C(=O)NC(CO)(CO)CO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
117993490 166708 0 None - 1 Human 7.6 pKi = 7.6 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 350 2 2 4 2.4 Cc1cc(-c2ccc([C@@]3(C)CCCNC3=O)c(=O)[nH]2)cc2c1cnn2C nan
CHEMBL4107193 166708 0 None - 1 Human 7.6 pKi = 7.6 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 350 2 2 4 2.4 Cc1cc(-c2ccc([C@@]3(C)CCCNC3=O)c(=O)[nH]2)cc2c1cnn2C nan
10185382 71189 0 None -251 5 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 500 7 1 7 4.6 COc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813119 71189 0 None -251 5 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 500 7 1 7 4.6 COc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
12521 8978 0 None -1071 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
72722131 8978 0 None -1071 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
CHEMBL3918816 8978 0 None -1071 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
CHEMBL5083509 221647 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None COc1ccc(Cl)cc1S(=O)(=O)NC(=O)NC/C(F)=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21 10.1021/acsmedchemlett.1c00594
9885106 91548 0 None -13 6 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmcl.2011.10.109
CHEMBL223151 91548 0 None -13 6 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmcl.2011.10.109
9885106 91548 0 None -13 6 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmc.2012.02.018
CHEMBL223151 91548 0 None -13 6 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmc.2012.02.018
137477568 191814 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 356 4 2 2 3.6 CC(C)C(F)(C(N)=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4855134 191814 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 356 4 2 2 3.6 CC(C)C(F)(C(N)=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
71455094 88656 0 None 354 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 623 12 1 8 6.4 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
CHEMBL2164609 88656 0 None 354 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 623 12 1 8 6.4 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
52945423 23313 0 None 3 4 Human 6.6 pKi = 6.6 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 824 18 2 6 11.6 CC(=O)c1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1.CC(=O)c1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2004.11.051
CHEMBL1237303 23313 0 None 3 4 Human 6.6 pKi = 6.6 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 824 18 2 6 11.6 CC(=O)c1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1.CC(=O)c1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2004.11.051
10272453 208000 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 402 9 1 5 4.2 O=C(O)COc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL603633 208000 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 402 9 1 5 4.2 O=C(O)COc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
137487352 187383 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 436 5 2 5 4.4 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3c(c2)OC(C)(C)CC3)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4754488 187383 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 436 5 2 5 4.4 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3c(c2)OC(C)(C)CC3)[nH]c1=O 10.1021/acsmedchemlett.0c00667
9954562 90912 0 None 72 4 Human 6.6 pKi = 6.6 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL220802 90912 0 None 72 4 Human 6.6 pKi = 6.6 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
21362879 23340 0 None 28 4 Human 7.6 pKi = 7.6 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1cc(-c2ccccc2OCc2ccccc2)cs1 10.1016/s0960-894x(03)00794-7
CHEMBL123855 23340 0 None 28 4 Human 7.6 pKi = 7.6 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1cc(-c2ccccc2OCc2ccccc2)cs1 10.1016/s0960-894x(03)00794-7
10118889 213052 0 None 30 4 Human 7.6 pKi = 7.6 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1cccc(CSCCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL86933 213052 0 None 30 4 Human 7.6 pKi = 7.6 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1cccc(CSCCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
137487290 188477 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 394 4 2 4 3.7 CC(C)[C@@H](c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)[C@H]1OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4776714 188477 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 394 4 2 4 3.7 CC(C)[C@@H](c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)[C@H]1OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
162651616 187065 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 434 6 2 6 3.9 CCn1nc(C)c2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
CHEMBL4750762 187065 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 434 6 2 6 3.9 CCn1nc(C)c2ccc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
162668445 189458 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 392 3 2 4 4.0 CC(C)/C(=C1\NC(=O)OC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4789221 189458 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 392 3 2 4 4.0 CC(C)/C(=C1\NC(=O)OC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
52943002 23311 0 None 2 4 Human 5.6 pKi = 5.6 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 716 14 2 4 11.1 Cc1cccc(/C=C\Cc2ccccc2C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237301 23311 0 None 2 4 Human 5.6 pKi = 5.6 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 716 14 2 4 11.1 Cc1cccc(/C=C\Cc2ccccc2C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
1932 9716 5 None -1584 6 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP3 receptor (unknown origin)Binding affinity to EP3 receptor (unknown origin)
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
5311228 9716 5 None -1584 6 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP3 receptor (unknown origin)Binding affinity to EP3 receptor (unknown origin)
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
CHEMBL3286796 9716 5 None -1584 6 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP3 receptor (unknown origin)Binding affinity to EP3 receptor (unknown origin)
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
15947857 162292 7 None -2398 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
ChEMBL 767 12 1 9 6.3 COc1cccc(OC)c1C1(C(=O)NS(=O)(=O)Cc2ccc(N3Cc4c(c(OCC(F)(F)F)c5cccnc5c4OCC(F)(F)F)C3=O)c(C)c2)CC1 10.1016/j.bmcl.2008.01.103
CHEMBL404199 162292 7 None -2398 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
ChEMBL 767 12 1 9 6.3 COc1cccc(OC)c1C1(C(=O)NS(=O)(=O)Cc2ccc(N3Cc4c(c(OCC(F)(F)F)c5cccnc5c4OCC(F)(F)F)C3=O)c(C)c2)CC1 10.1016/j.bmcl.2008.01.103
10092823 76126 0 None -338 3 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 407 12 2 5 3.1 CCc1cccc(C[C@H](O)/C=C/[C@H]2COC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929531 76126 0 None -338 3 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 407 12 2 5 3.1 CCc1cccc(C[C@H](O)/C=C/[C@H]2COC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
162654507 187443 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 390 3 2 4 3.5 O=C1NC(=O)/C(=C/C2(c3ccc(-c4ccc5cccc(F)c5c4)[nH]c3=O)CC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4755147 187443 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 390 3 2 4 3.5 O=C1NC(=O)/C(=C/C2(c3ccc(-c4ccc5cccc(F)c5c4)[nH]c3=O)CC2)O1 10.1021/acsmedchemlett.0c00667
162662909 188740 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 438 5 2 4 4.7 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cc(F)cc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4780007 188740 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 438 5 2 4 4.7 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3cc(F)cc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL5075763 221177 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1ccc(Cl)cc1 10.1021/acsmedchemlett.1c00594
137477803 191693 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 421 5 2 4 5.2 CC(C)C(C(=O)Nc1nccs1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4853296 191693 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 421 5 2 4 5.2 CC(C)C(C(=O)Nc1nccs1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
9954562 90912 0 None 72 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL220802 90912 0 None 72 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
10004602 76137 0 None -288 2 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 463 11 2 5 4.3 O=C(O)CCCSCCN1C(=O)SC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929542 76137 0 None -288 2 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 463 11 2 5 4.3 O=C(O)CCCSCCN1C(=O)SC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmc.2011.12.009
10199656 206944 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 378 10 1 5 3.9 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCCOc1ccccc1 10.1016/j.bmc.2009.08.007
CHEMBL596499 206944 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 378 10 1 5 3.9 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCCOc1ccccc1 10.1016/j.bmc.2009.08.007
9808508 118337 0 None -48 3 Human 5.6 pKi = 5.6 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 586 7 1 4 6.3 O=C(Cc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL328067 118337 0 None -48 3 Human 5.6 pKi = 5.6 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 586 7 1 4 6.3 O=C(Cc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
10023506 76125 0 None -1122 3 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 393 11 2 5 2.9 Cc1cccc(C[C@H](O)/C=C/[C@H]2COC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929530 76125 0 None -1122 3 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 393 11 2 5 2.9 Cc1cccc(C[C@H](O)/C=C/[C@H]2COC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
10277744 71186 0 None -100 7 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813116 71186 0 None -100 7 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
53358921 71215 0 None -588 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 482 7 1 5 5.4 CCN1c2ccccc2C[C@@H]1COc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)c(C)c1 10.1016/j.bmc.2011.06.014
CHEMBL1813287 71215 0 None -588 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 482 7 1 5 5.4 CCN1c2ccccc2C[C@@H]1COc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)c(C)c1 10.1016/j.bmc.2011.06.014
117992976 167456 0 None - 1 Human 7.5 pKi = 7.5 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 380 3 3 3 3.1 C[C@]1(c2ccc(-c3cc(F)c4[nH]nc(C5CC5)c4c3)[nH]c2=O)CCCNC1=O nan
CHEMBL4113451 167456 0 None - 1 Human 7.5 pKi = 7.5 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 380 3 3 3 3.1 C[C@]1(c2ccc(-c3cc(F)c4[nH]nc(C5CC5)c4c3)[nH]c2=O)CCCNC1=O nan
162658086 187829 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 438 5 2 4 4.7 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3c(F)cc(F)cc3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4759510 187829 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 438 5 2 4 4.7 CCC(/C=C1\OC(=O)NC1=O)(CC)c1ccc(-c2ccc3c(F)cc(F)cc3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
9910141 107652 0 None -588 3 Mouse 5.5 pKi = 5.5 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 422 11 4 6 2.7 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCSCCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
CHEMBL293647 107652 0 None -588 3 Mouse 5.5 pKi = 5.5 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 422 11 4 6 2.7 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCSCCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
52947847 23310 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1.Cc1cccc(C/C=C\c2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237300 23310 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1.Cc1cccc(C/C=C\c2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
11743212 23936 0 None 100 7 Human 8.5 pKi = 8.5 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 426 7 1 3 6.8 O=C(O)C1CC1c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL125588 23936 0 None 100 7 Human 8.5 pKi = 8.5 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 426 7 1 3 6.8 O=C(O)C1CC1c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
11155228 72880 0 None 204 4 Human 8.5 pKi = 8.5 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 452 8 1 2 7.2 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL183919 72880 0 None 204 4 Human 8.5 pKi = 8.5 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 452 8 1 2 7.2 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
44419347 89550 0 None 204 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 452 8 1 2 7.2 Cc1ccc(OCc2c(Cl)cccc2Cl)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL217988 89550 0 None 204 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 452 8 1 2 7.2 Cc1ccc(OCc2c(Cl)cccc2Cl)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
137477676 188682 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 438 6 2 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
CHEMBL4779295 188682 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 438 6 2 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
CHEMBL5072303 221057 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(-c3ccc(C(F)(F)F)cc3)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
CHEMBL5076035 221189 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None COc1ccc(Cl)cc1S(=O)(=O)NC(=O)NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21 10.1021/acsmedchemlett.1c00594
CHEMBL5083128 221622 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None COc1ccc(S(=O)(=O)NC(=O)NC/C(F)=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)cc1Cl 10.1021/acsmedchemlett.1c00594
21198692 89930 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 394 7 1 2 6.1 O=C(O)/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1 10.1016/j.bmcl.2006.08.025
CHEMBL218263 89930 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 394 7 1 2 6.1 O=C(O)/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1 10.1016/j.bmcl.2006.08.025
23017035 206213 0 None - 1 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 431 11 2 3 5.6 CCCC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL591299 206213 0 None - 1 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 431 11 2 3 5.6 CCCC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
44304057 210038 0 None 8 4 Mouse 8.5 pKi = 8.5 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.6 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64598 210038 0 None 8 4 Mouse 8.5 pKi = 8.5 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.6 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL5074870 221116 0 None 1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to rat EP3 receptor assessed as inhibition constantBinding affinity to rat EP3 receptor assessed as inhibition constant
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1ccc(Cl)cc1 10.1021/acsmedchemlett.1c00594
117993400 128536 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assayDisplacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assay
ChEMBL 370 2 2 4 2.8 Cn1ncc2c(Cl)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.5b00188
CHEMBL3589083 128536 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assayDisplacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assay
ChEMBL 370 2 2 4 2.8 Cn1ncc2c(Cl)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.5b00188
137477971 191298 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 468 5 2 4 5.6 CC(C)C(C(=O)Nc1ccc2c(c1)ncn2C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4847629 191298 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 468 5 2 4 5.6 CC(C)C(C(=O)Nc1ccc2c(c1)ncn2C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
117993400 128536 0 None - 1 Human 8.4 pKi = 8.4 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 370 2 2 4 2.8 Cn1ncc2c(Cl)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 nan
CHEMBL3589083 128536 0 None - 1 Human 8.4 pKi = 8.4 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 370 2 2 4 2.8 Cn1ncc2c(Cl)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 nan
44304474 209710 0 None 2 5 Mouse 8.4 pKi = 8.4 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCSCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL62868 209710 0 None 2 5 Mouse 8.4 pKi = 8.4 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCSCCC(=O)O 10.1016/s0960-894x(01)00365-1
137477849 193065 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 382 6 3 3 3.2 CC(C)C(C(=O)NCCO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4874159 193065 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 382 6 3 3 3.2 CC(C)C(C(=O)NCCO)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
44289922 170303 0 None -707 5 Human 5.5 pKi = 5.5 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/j.bmcl.2004.01.063
CHEMBL42027 170303 0 None -707 5 Human 5.5 pKi = 5.5 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/j.bmcl.2004.01.063
44304009 107512 0 None -575 3 Mouse 5.5 pKi = 5.5 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 482 15 3 7 3.3 CCCOCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL292717 107512 0 None -575 3 Mouse 5.5 pKi = 5.5 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 482 15 3 7 3.3 CCCOCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
44303590 209690 0 None -354 3 Mouse 5.5 pKi = 5.5 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 468 14 3 7 2.6 COCCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL62779 209690 0 None -354 3 Mouse 5.5 pKi = 5.5 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 468 14 3 7 2.6 COCCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
11955317 153250 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 mins
ChEMBL 396 10 3 3 4.9 CC(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3922270 153250 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 mins
ChEMBL 396 10 3 3 4.9 CC(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
117993349 128538 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assayDisplacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assay
ChEMBL 350 3 2 4 2.5 CCn1ncc2c(C)cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.5b00188
CHEMBL3589085 128538 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assayDisplacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assay
ChEMBL 350 3 2 4 2.5 CCn1ncc2c(C)cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.5b00188
117993349 128538 0 None - 1 Human 7.5 pKi = 7.5 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 350 3 2 4 2.5 CCn1ncc2c(C)cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc21 nan
CHEMBL3589085 128538 0 None - 1 Human 7.5 pKi = 7.5 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 350 3 2 4 2.5 CCn1ncc2c(C)cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc21 nan
127047604 146361 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 313 4 1 6 3.0 CCn1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3797362 146361 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 313 4 1 6 3.0 CCn1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL5074974 221124 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None Cc1nc(C)c(S(=O)(=O)NC(=O)NC/C(F)=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)s1 10.1021/acsmedchemlett.1c00594
53358922 71204 0 None -602 6 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 522 6 1 6 5.3 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1Cl 10.1016/j.bmc.2011.06.014
CHEMBL1813276 71204 0 None -602 6 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 522 6 1 6 5.3 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1Cl 10.1016/j.bmc.2011.06.014
11519006 109263 0 None -512 6 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptorInhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptor
ChEMBL 481 8 1 5 6.1 O=C(O)COc1cccc(C[C@@H]2CCC[C@H]3O[C@]23c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
CHEMBL2373410 109263 0 None -512 6 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptorInhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptor
ChEMBL 481 8 1 5 6.1 O=C(O)COc1cccc(C[C@@H]2CCC[C@H]3O[C@]23c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
CHEMBL3040272 109263 0 None -512 6 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptorInhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptor
ChEMBL 481 8 1 5 6.1 O=C(O)COc1cccc(C[C@@H]2CCC[C@H]3O[C@]23c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
162656122 187692 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 454 5 2 4 4.8 O=C1NC(=O)/C(=C/C(Cc2ccccc2)c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4757838 187692 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 454 5 2 4 4.8 O=C1NC(=O)/C(=C/C(Cc2ccccc2)c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)O1 10.1021/acsmedchemlett.0c00667
137478289 192217 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 409 7 2 3 3.8 CC(C)C(C(=O)NCCN(C)C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4861530 192217 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 409 7 2 3 3.8 CC(C)C(C(=O)NCCN(C)C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
44320272 213041 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 507 10 1 5 5.9 O=C(Cc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL86886 213041 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 507 10 1 5 5.9 O=C(Cc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
10361472 71982 0 None -331 3 Mouse 5.5 pKi = 5.5 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)cc3c(CC(=O)O)cccc32)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL182555 71982 0 None -331 3 Mouse 5.5 pKi = 5.5 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)cc3c(CC(=O)O)cccc32)cc1 10.1016/j.bmcl.2004.07.039
21974464 73778 0 None -19 4 Mouse 5.5 pKi = 5.5 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 427 8 1 4 5.3 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL186925 73778 0 None -19 4 Mouse 5.5 pKi = 5.5 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 427 8 1 4 5.3 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
11187675 71988 0 None -100 4 Mouse 5.5 pKi = 5.5 Binding
Binding affinity for mouse Prostanoid EP3 receptorBinding affinity for mouse Prostanoid EP3 receptor
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL182572 71988 0 None -100 4 Mouse 5.5 pKi = 5.5 Binding
Binding affinity for mouse Prostanoid EP3 receptorBinding affinity for mouse Prostanoid EP3 receptor
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)cc1 10.1016/j.bmcl.2004.06.006
24952929 9332 42 None -5248 5 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from rat EP3 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP3 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
4041 9332 42 None -5248 5 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from rat EP3 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP3 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
CHEMBL597997 9332 42 None -5248 5 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from rat EP3 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP3 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
11696697 105808 0 None -676 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 385 11 2 3 3.7 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)C1(c2ccccc2)CC1 10.1016/s0960-894x(03)00042-8
CHEMBL280223 105808 0 None -676 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 385 11 2 3 3.7 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)C1(c2ccccc2)CC1 10.1016/s0960-894x(03)00042-8
137477657 191265 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 377 5 2 4 3.8 CC(C)C(Cc1nnn[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4847115 191265 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 377 5 2 4 3.8 CC(C)C(Cc1nnn[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137477673 192583 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 408 6 2 5 4.1 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc(C)[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL4866965 192583 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 408 6 2 5 4.1 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc(C)[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
137477942 193183 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 393 5 2 4 4.0 CC(C)C(Cc1noc(=O)[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4875937 193183 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 393 5 2 4 4.0 CC(C)C(Cc1noc(=O)[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
12112239 113337 0 None 3 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 549 12 1 6 6.3 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL314200 113337 0 None 3 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 549 12 1 6 6.3 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
52941777 23312 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 744 16 2 4 10.9 Cc1cccc(/C=C/Cc2ccccc2CC(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2CC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237302 23312 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 744 16 2 4 10.9 Cc1cccc(/C=C/Cc2ccccc2CC(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2CC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44349528 120578 0 None 31 4 Human 7.5 pKi = 7.5 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 7.2 CC(CC(=O)O)c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL332446 120578 0 None 31 4 Human 7.5 pKi = 7.5 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 7.2 CC(CC(=O)O)c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
57403612 78080 0 None -436 3 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 9 2 4 4.2 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmc.2012.02.018
CHEMBL1957434 78080 0 None -436 3 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 9 2 4 4.2 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmc.2012.02.018
72950089 157370 0 None -1698 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
CHEMBL3955128 157370 0 None -1698 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
10275762 90364 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 451 6 1 5 5.6 O=C(/C=C/c1ccccc1Sc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL2204337 90364 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 451 6 1 5 5.6 O=C(/C=C/c1ccccc1Sc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
9938625 213563 0 None -77 3 Human 5.4 pKi = 5.4 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 600 8 1 4 6.7 O=C(CCc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL90227 213563 0 None -77 3 Human 5.4 pKi = 5.4 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 600 8 1 4 6.7 O=C(CCc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
10299717 71191 0 None -1047 6 Mouse 5.4 pKi = 5.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1cc(OC[C@@H]2CN(C)c3ccccc3O2)ccc1C(=O)n1c(C)c(CC(=O)O)c2ccccc21 10.1016/j.bmc.2011.06.014
CHEMBL1813120 71191 0 None -1047 6 Mouse 5.4 pKi = 5.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1cc(OC[C@@H]2CN(C)c3ccccc3O2)ccc1C(=O)n1c(C)c(CC(=O)O)c2ccccc21 10.1016/j.bmc.2011.06.014
137477903 189809 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 392 3 2 4 3.8 CC(C)(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4793929 189809 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 392 3 2 4 3.8 CC(C)(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
127048124 146367 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 331 4 1 6 3.2 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3797387 146367 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 331 4 1 6 3.2 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
137478179 188246 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 440 4 2 4 4.9 CC(C)C(/C=C1\OC(=O)NC1=O)c1cc(Cl)c(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4764526 188246 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 440 4 2 4 4.9 CC(C)C(/C=C1\OC(=O)NC1=O)c1cc(Cl)c(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
10322469 108288 15 None -12302 2 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 469 11 2 3 5.9 Cc1cc(Cl)ccc1-c1cccc(C(O)/C=C/[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2004.01.063
CHEMBL298026 108288 15 None -12302 2 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 469 11 2 3 5.9 Cc1cc(Cl)ccc1-c1cccc(C(O)/C=C/[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2004.01.063
10113454 184280 0 None -2398 3 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 429 12 2 3 4.4 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
CHEMBL46395 184280 0 None -2398 3 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 429 12 2 3 4.4 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
10363310 76134 0 None -60 2 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 395 11 2 5 3.3 O=C(O)CCCSCCN1C(=O)SC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/j.bmc.2011.12.009
CHEMBL1929539 76134 0 None -60 2 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 395 11 2 5 3.3 O=C(O)CCCSCCN1C(=O)SC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/j.bmc.2011.12.009
44289922 170303 0 None -14 5 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/j.bmcl.2011.10.109
CHEMBL42027 170303 0 None -14 5 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/j.bmcl.2011.10.109
44289922 170303 0 None -14 5 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/j.bmc.2012.02.018
CHEMBL42027 170303 0 None -14 5 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/j.bmc.2012.02.018
137477947 192464 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 408 6 1 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4ncn(C)n4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL4865168 192464 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 408 6 1 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4ncn(C)n4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
23017362 206757 0 None 36 4 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 10 1 4 5.1 O=C(O)CCCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595157 206757 0 None 36 4 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 10 1 4 5.1 O=C(O)CCCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
1050 8683 94 None -1 2 Human 6.4 pKi = 6.4 Binding
Activity at EP3 receptorActivity at EP3 receptor
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.12.084
11595431 8683 94 None -1 2 Human 6.4 pKi = 6.4 Binding
Activity at EP3 receptorActivity at EP3 receptor
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.12.084
CHEMBL207881 8683 94 None -1 2 Human 6.4 pKi = 6.4 Binding
Activity at EP3 receptorActivity at EP3 receptor
ChEMBL 347 8 2 3 5.1 OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 10.1016/j.bmcl.2006.12.084
137477635 187630 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 446 4 2 4 5.1 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CCCCC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4757179 187630 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 446 4 2 4 5.1 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CCCCC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL5074870 221116 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1ccc(Cl)cc1 10.1021/acsmedchemlett.1c00594
137477638 192590 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 394 5 1 3 4.4 CC(C)C(CN1CCOCC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4867086 192590 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 394 5 1 3 4.4 CC(C)C(CN1CCOCC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
23017142 208572 0 None - 1 Mouse 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 443 11 2 3 5.6 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NC(CC1CC1)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL606857 208572 0 None - 1 Mouse 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 443 11 2 3 5.6 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NC(CC1CC1)c1ccccc1 10.1016/j.bmc.2009.11.023
44250281 203286 0 None 2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 434 4 1 6 5.0 CCN1CCOc2ccc(C(=O)Nc3nnc(-c4c(Cl)cccc4Cl)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL563480 203286 0 None 2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 434 4 1 6 5.0 CCN1CCOc2ccc(C(=O)Nc3nnc(-c4c(Cl)cccc4Cl)s3)cc21 10.1016/j.bmcl.2016.04.009
44304055 109500 0 None -1 4 Mouse 8.4 pKi = 8.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCSCCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL304887 109500 0 None -1 4 Mouse 8.4 pKi = 8.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCSCCC(=O)O 10.1016/s0960-894x(01)00364-x
13231966 107728 0 None -6 5 Mouse 8.4 pKi = 8.4 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL294108 107728 0 None -6 5 Mouse 8.4 pKi = 8.4 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
13231966 107728 0 None -6 5 Mouse 8.4 pKi = 8.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL294108 107728 0 None -6 5 Mouse 8.4 pKi = 8.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
9817405 172182 5 None 7 6 Human 6.4 pKi = 6.4 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2006.08.025
CHEMBL423815 172182 5 None 7 6 Human 6.4 pKi = 6.4 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2006.08.025
9809136 113666 0 None -398 8 Human 5.4 pKi = 5.4 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 614 7 1 4 7.1 CC(C)(C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
CHEMBL314533 113666 0 None -398 8 Human 5.4 pKi = 5.4 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 614 7 1 4 7.1 CC(C)(C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
15948325 9304 45 None -3235 6 Human 5.4 pKi = 5.4 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
ChEMBL 603 11 1 8 4.7 CCOc1c2CN(C(=O)c2c(c2c1nccc2)OCC)c1ccc(cc1C)CS(=O)(=O)NC(=O)Cc1ccccc1OC 10.1016/j.bmcl.2008.01.103
5856 9304 45 None -3235 6 Human 5.4 pKi = 5.4 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
ChEMBL 603 11 1 8 4.7 CCOc1c2CN(C(=O)c2c(c2c1nccc2)OCC)c1ccc(cc1C)CS(=O)(=O)NC(=O)Cc1ccccc1OC 10.1016/j.bmcl.2008.01.103
CHEMBL402162 9304 45 None -3235 6 Human 5.4 pKi = 5.4 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
ChEMBL 603 11 1 8 4.7 CCOc1c2CN(C(=O)c2c(c2c1nccc2)OCC)c1ccc(cc1C)CS(=O)(=O)NC(=O)Cc1ccccc1OC 10.1016/j.bmcl.2008.01.103
10046356 76129 0 None -199 3 Mouse 5.4 pKi = 5.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 397 11 2 5 2.7 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1cccc(F)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929534 76129 0 None -199 3 Mouse 5.4 pKi = 5.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 397 11 2 5 2.7 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1cccc(F)c1 10.1016/j.bmc.2011.12.009
44390806 70852 0 None 24 3 Human 7.4 pKi = 7.4 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 386 8 1 2 5.9 Cc1cccc(C2CC2c2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL180752 70852 0 None 24 3 Human 7.4 pKi = 7.4 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 386 8 1 2 5.9 Cc1cccc(C2CC2c2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
9913176 90366 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 483 6 1 6 4.3 O=C(/C=C/c1ccccc1S(=O)(=O)c1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL2204339 90366 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of EP3 receptor in presence of 0.005 % HASInhibition of EP3 receptor in presence of 0.005 % HAS
ChEMBL 483 6 1 6 4.3 O=C(/C=C/c1ccccc1S(=O)(=O)c1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
13230981 41841 0 None -69 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 339 13 2 3 3.5 CCCCCC(O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL14334 41841 0 None -69 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 339 13 2 3 3.5 CCCCCC(O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
162673365 189789 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 405 4 3 3 3.8 CC(C)C(/C=C1\NC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4793698 189789 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 405 4 3 3 3.8 CC(C)C(/C=C1\NC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
44303709 209979 0 None -70 3 Mouse 6.4 pKi = 6.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 470 13 3 7 3.3 CSCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL64338 209979 0 None -70 3 Mouse 6.4 pKi = 6.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 470 13 3 7 3.3 CSCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
57394893 78081 0 None -4570 4 Mouse 5.4 pKi = 5.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957435 78081 0 None -4570 4 Mouse 5.4 pKi = 5.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.02.018
57394893 78081 0 None -4570 4 Mouse 5.4 pKi = 5.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957435 78081 0 None -4570 4 Mouse 5.4 pKi = 5.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.04.008
10200281 206605 1 None 97 2 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 388 8 1 5 4.4 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCc1cc2ccccc2o1 10.1016/j.bmc.2009.08.007
CHEMBL594210 206605 1 None 97 2 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 388 8 1 5 4.4 O=C(O)/C=C/c1ccc(Cn2ccnc2)cc1OCCc1cc2ccccc2o1 10.1016/j.bmc.2009.08.007
44320321 213213 0 None 2 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 563 12 1 6 6.6 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87975 213213 0 None 2 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 563 12 1 6 6.6 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
11744126 76143 0 None -1174 2 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 443 11 2 3 5.0 O=C(O)CCCCCCN1C(=S)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929548 76143 0 None -1174 2 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 443 11 2 3 5.0 O=C(O)CCCCCCN1C(=S)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmc.2011.12.009
10367369 210026 0 None -478 2 Mouse 5.4 pKi = 5.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 468 14 3 7 2.9 CCOCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL64557 210026 0 None -478 2 Mouse 5.4 pKi = 5.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 468 14 3 7 2.9 CCOCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
21362900 212619 0 None 23 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL83518 212619 0 None 23 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
21198692 89930 0 None 6 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 394 7 1 2 6.1 O=C(O)/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1 10.1016/j.bmcl.2006.08.025
CHEMBL218263 89930 0 None 6 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 394 7 1 2 6.1 O=C(O)/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1 10.1016/j.bmcl.2006.08.025
137477755 187515 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 407 4 2 3 3.6 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1C(=O)NC(=O)N1C 10.1021/acsmedchemlett.0c00667
CHEMBL4755933 187515 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 407 4 2 3 3.6 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1C(=O)NC(=O)N1C 10.1021/acsmedchemlett.0c00667
117993109 167468 1 None - 1 Human 7.3 pKi = 7.3 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 321 2 2 3 2.3 Cn1ccc2cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)ccc21 nan
CHEMBL4113525 167468 1 None - 1 Human 7.3 pKi = 7.3 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 321 2 2 3 2.3 Cn1ccc2cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)ccc21 nan
44324368 103293 0 None 3 4 Human 5.3 pKi = 5.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 587 6 2 4 6.8 O=C(Nc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL262690 103293 0 None 3 4 Human 5.3 pKi = 5.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 587 6 2 4 6.8 O=C(Nc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
9817405 172182 5 None 7 6 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2006.08.025
CHEMBL423815 172182 5 None 7 6 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2006.08.025
11597294 172955 4 None -562 8 Human 6.3 pKi = 6.3 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
ChEMBL 435 4 1 2 5.7 O=C(O)C[C@H]1CCc2c1n(Cc1ccc(Cl)cc1)c1c(Br)cc(F)cc21 10.1021/jm0603668
CHEMBL426387 172955 4 None -562 8 Human 6.3 pKi = 6.3 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
ChEMBL 435 4 1 2 5.7 O=C(O)C[C@H]1CCc2c1n(Cc1ccc(Cl)cc1)c1c(Br)cc(F)cc21 10.1021/jm0603668
15907748 118241 0 None -33 4 Human 5.3 pKi = 5.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 615 7 2 4 7.0 C[C@H](NC(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
CHEMBL327597 118241 0 None -33 4 Human 5.3 pKi = 5.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 615 7 2 4 7.0 C[C@H](NC(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
9938669 174837 0 None -33 4 Human 5.3 pKi = 5.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 602 8 1 5 6.2 O=C(COc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL432380 174837 0 None -33 4 Human 5.3 pKi = 5.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 602 8 1 5 6.2 O=C(COc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
44320405 112942 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 521 11 1 5 6.2 O=C(NS(=O)(=O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL313700 112942 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 521 11 1 5 6.2 O=C(NS(=O)(=O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)c1cccs1 10.1016/s0960-894x(02)00518-8
57398586 76251 0 None -63 3 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 422 9 2 7 3.0 Cc1ccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)o1 10.1016/j.bmcl.2011.10.109
CHEMBL1933727 76251 0 None -63 3 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 422 9 2 7 3.0 Cc1ccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)o1 10.1016/j.bmcl.2011.10.109
44290314 180753 0 None -489 3 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 403 10 2 4 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccc(C(F)(F)F)o1 10.1016/j.bmcl.2004.01.063
CHEMBL45418 180753 0 None -489 3 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 403 10 2 4 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccc(C(F)(F)F)o1 10.1016/j.bmcl.2004.01.063
138 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
149351 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
1882 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
5280723 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
CHEMBL495 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
DB00770 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
22009006 148342 0 None 301 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1/C=C/Cc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL384878 148342 0 None 301 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1/C=C/Cc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
9953337 148438 0 None 301 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1C/C=C/c1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL385396 148438 0 None 301 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1C/C=C/c1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
1883 9856 75 None -1 24 Human 8.3 pKi = 8.3 Binding
Binding affinity to EP3 receptor (unknown origin)Binding affinity to EP3 receptor (unknown origin)
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/jm401431x
1916 9856 75 None -1 24 Human 8.3 pKi = 8.3 Binding
Binding affinity to EP3 receptor (unknown origin)Binding affinity to EP3 receptor (unknown origin)
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/jm401431x
5280360 9856 75 None -1 24 Human 8.3 pKi = 8.3 Binding
Binding affinity to EP3 receptor (unknown origin)Binding affinity to EP3 receptor (unknown origin)
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/jm401431x
913 9856 75 None -1 24 Human 8.3 pKi = 8.3 Binding
Binding affinity to EP3 receptor (unknown origin)Binding affinity to EP3 receptor (unknown origin)
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/jm401431x
CHEMBL548 9856 75 None -1 24 Human 8.3 pKi = 8.3 Binding
Binding affinity to EP3 receptor (unknown origin)Binding affinity to EP3 receptor (unknown origin)
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/jm401431x
DB00917 9856 75 None -1 24 Human 8.3 pKi = 8.3 Binding
Binding affinity to EP3 receptor (unknown origin)Binding affinity to EP3 receptor (unknown origin)
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/jm401431x
138 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
149351 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
1882 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
5280723 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
CHEMBL495 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
DB00770 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
5283086 210089 24 None -35 5 Mouse 8.3 pKi = 8.3 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
CHEMBL64804 210089 24 None -35 5 Mouse 8.3 pKi = 8.3 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
CHEMBL5077079 221255 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21)NS(=O)(=O)c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00594
1883 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
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 10.1016/j.bmcl.2011.10.109
1916 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
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 10.1016/j.bmcl.2011.10.109
5280360 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
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 10.1016/j.bmcl.2011.10.109
913 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
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 10.1016/j.bmcl.2011.10.109
CHEMBL548 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
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 10.1016/j.bmcl.2011.10.109
DB00917 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
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 10.1016/j.bmcl.2011.10.109
1883 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
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 10.1016/j.bmc.2012.02.018
1916 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
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 10.1016/j.bmc.2012.02.018
5280360 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
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 10.1016/j.bmc.2012.02.018
913 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
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 10.1016/j.bmc.2012.02.018
CHEMBL548 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
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 10.1016/j.bmc.2012.02.018
DB00917 9856 75 None -2 24 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
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 10.1016/j.bmc.2012.02.018
117993349 128538 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 350 3 2 4 2.5 CCn1ncc2c(C)cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL3589085 128538 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 350 3 2 4 2.5 CCn1ncc2c(C)cc(-c3ccc([C@@]4(C)CCNC4=O)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
137478225 192631 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 484 13 2 5 3.9 COCCOCCOCCNC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
CHEMBL4867692 192631 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 484 13 2 5 3.9 COCCOCCOCCNC(=O)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
137478254 192976 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 352 5 2 2 3.9 CC(C)C(CC(N)=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4872930 192976 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 352 5 2 2 3.9 CC(C)C(CC(N)=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
138 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
149351 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
1882 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
5280723 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
CHEMBL495 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
DB00770 9855 88 None -2 18 Mouse 8.3 pKi = 8.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
49850345 68194 6 None 1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human EP3Binding affinity to human EP3
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
CHEMBL1770317 68194 6 None 1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human EP3Binding affinity to human EP3
ChEMBL 362 3 2 4 3.3 CC(C)C1(c2ccc(-c3ccc4ccccc4c3)[nH]c2=O)OC(=O)NC1=O 10.1021/ml100077x
23016747 206212 0 None - 1 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 417 10 2 3 5.2 CCC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL591298 206212 0 None - 1 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 417 10 2 3 5.2 CCC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
137478205 191794 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 390 4 2 2 4.5 CC(C)C(/C=C1/CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4854881 191794 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 390 4 2 2 4.5 CC(C)C(/C=C1/CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137477997 192627 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 415 5 2 3 5.1 CC(C)C(C(=O)Nc1ccncc1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4867652 192627 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 415 5 2 3 5.1 CC(C)C(C(=O)Nc1ccncc1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137478217 192668 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 394 6 2 2 5.0 CC(C)NC(=O)CC(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
CHEMBL4868434 192668 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 394 6 2 2 5.0 CC(C)NC(=O)CC(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C(C)C 10.1016/j.bmcl.2021.128172
52945421 23308 0 None -2 4 Human 7.3 pKi = 7.3 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(OCc2ccccc2)c1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(OCc2ccccc2)c1 10.1016/j.bmcl.2004.11.051
CHEMBL1237298 23308 0 None -2 4 Human 7.3 pKi = 7.3 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(OCc2ccccc2)c1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(OCc2ccccc2)c1 10.1016/j.bmcl.2004.11.051
162674113 189939 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 418 3 2 4 4.3 O=C1NC(=O)/C(=C/C2(c3ccc(-c4ccc5cccc(F)c5c4)[nH]c3=O)CCCC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4795369 189939 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 418 3 2 4 4.3 O=C1NC(=O)/C(=C/C2(c3ccc(-c4ccc5cccc(F)c5c4)[nH]c3=O)CCCC2)O1 10.1021/acsmedchemlett.0c00667
137478002 190243 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 393 4 3 3 3.3 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1NC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4799069 190243 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 393 4 3 3 3.3 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)C1NC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
137478051 192682 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 336 4 3 3 2.5 CC(C)C(O)(C(N)=O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4868701 192682 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 336 4 3 3 2.5 CC(C)C(O)(C(N)=O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
9938626 213612 0 None -316 7 Human 5.3 pKi = 5.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 600 7 1 4 6.9 CC(C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
CHEMBL90491 213612 0 None -316 7 Human 5.3 pKi = 5.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 600 7 1 4 6.9 CC(C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
9874010 213969 0 None -295 8 Human 5.3 pKi = 5.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 629 8 1 4 6.9 CN(CCc1ccccc1)C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL92539 213969 0 None -295 8 Human 5.3 pKi = 5.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 629 8 1 4 6.9 CN(CCc1ccccc1)C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
11476788 168053 0 None -35 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 463 5 1 5 4.4 CS(=O)(=O)c1cc(F)cc2c1c(C(=O)c1ccc(Cl)cc1)c1n2CCC[C@@H]1CC(=O)O 10.1016/j.bmcl.2008.03.015
CHEMBL412070 168053 0 None -35 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 463 5 1 5 4.4 CS(=O)(=O)c1cc(F)cc2c1c(C(=O)c1ccc(Cl)cc1)c1n2CCC[C@@H]1CC(=O)O 10.1016/j.bmcl.2008.03.015
44320433 174722 0 None -6 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccccc1CSCCc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL431612 174722 0 None -6 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccccc1CSCCc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
44304052 209716 0 None -51 2 Mouse 6.3 pKi = 6.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL62888 209716 0 None -51 2 Mouse 6.3 pKi = 6.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
9830442 213570 0 None -426 2 Human 4.3 pKi = 4.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 615 8 2 4 6.5 O=C(NCCc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL90269 213570 0 None -426 2 Human 4.3 pKi = 4.3 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 615 8 2 4 6.5 O=C(NCCc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
44349551 23586 0 None 8 4 Human 7.3 pKi = 7.3 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 415 8 2 4 6.2 O=C(O)CNc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL124675 23586 0 None 8 4 Human 7.3 pKi = 7.3 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 415 8 2 4 6.2 O=C(O)CNc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
10112486 23673 0 None 2 4 Human 6.3 pKi = 6.3 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1ccc(-c2ccccc2OCc2ccccc2)s1 10.1016/s0960-894x(03)00794-7
CHEMBL125110 23673 0 None 2 4 Human 6.3 pKi = 6.3 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1ccc(-c2ccccc2OCc2ccccc2)s1 10.1016/s0960-894x(03)00794-7
132836 66469 23 None -1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL1722929 66469 23 None -1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP3 receptor expressed in HEK293 cells membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
21362893 213106 0 None 30 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 535 12 1 6 6.0 Cc1cccc(OCCCOc2ccc(-c3ccccc3CCC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87263 213106 0 None 30 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 535 12 1 6 6.0 Cc1cccc(OCCCOc2ccc(-c3ccccc3CCC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
127047210 146387 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 416 4 1 7 2.8 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CCN(C(C)=O)C4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3797483 146387 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 416 4 1 7 2.8 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CCN(C(C)=O)C4)s3)cc21 10.1016/j.bmcl.2016.04.009
50898361 63647 0 None -416 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 549 7 2 5 5.4 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(C)cc(C)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
CHEMBL1644003 63647 0 None -416 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 549 7 2 5 5.4 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(C)cc(C)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
44520989 206543 0 None 2 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 396 6 2 4 5.0 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1ccccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
CHEMBL593764 206543 0 None 2 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 396 6 2 4 5.0 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1ccccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
137477756 191417 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 408 6 1 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nncn4C)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL4849526 191417 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 408 6 1 6 3.8 CCn1ncc2c(F)cc(-c3ccc(C(CC)(CC)c4nncn4C)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
56835070 76246 0 None -1318 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933722 76246 0 None -1318 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmcl.2011.10.109
56835070 76246 0 None -1318 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933722 76246 0 None -1318 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
56835070 76246 0 None -1318 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.04.008
CHEMBL1933722 76246 0 None -1318 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.04.008
12137443 91478 0 None -57543 4 Human 4.3 pKi = 4.3 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 491 9 2 3 6.1 Cc1cc(Cl)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
CHEMBL222677 91478 0 None -57543 4 Human 4.3 pKi = 4.3 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 491 9 2 3 6.1 Cc1cc(Cl)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
164616453 192084 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 337 4 3 3 3.1 CC(C)C(O)(C(=O)O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4859363 192084 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 337 4 3 3 3.1 CC(C)C(O)(C(=O)O)c1ccc(-c2ccc3ccccc3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
21362851 123682 0 None 32 4 Human 7.3 pKi = 7.3 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL338388 123682 0 None 32 4 Human 7.3 pKi = 7.3 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
23017687 206315 0 None - 1 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 461 11 3 4 4.9 CC(C)(O)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL592212 206315 0 None - 1 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 461 11 3 4 4.9 CC(C)(O)CC(NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1ccccc1 10.1016/j.bmc.2009.11.023
8541 9718 2 None -141 4 Mouse 7.3 pKi = 7.3 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
9824353 9718 2 None -141 4 Mouse 7.3 pKi = 7.3 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
CHEMBL292964 9718 2 None -141 4 Mouse 7.3 pKi = 7.3 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
44419351 90918 0 None 17 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 533 12 1 5 6.2 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
CHEMBL220821 90918 0 None 17 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 533 12 1 5 6.2 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
1930 10106 25 None -89 3 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse EP3 receptor by competitive binding assayBinding affinity to mouse EP3 receptor by competitive binding assay
ChEMBL 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 10.1021/jm9018756
9803828 10106 25 None -89 3 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse EP3 receptor by competitive binding assayBinding affinity to mouse EP3 receptor by competitive binding assay
ChEMBL 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 10.1021/jm9018756
CHEMBL303960 10106 25 None -89 3 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse EP3 receptor by competitive binding assayBinding affinity to mouse EP3 receptor by competitive binding assay
ChEMBL 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 10.1021/jm9018756
DB16315 10106 25 None -89 3 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse EP3 receptor by competitive binding assayBinding affinity to mouse EP3 receptor by competitive binding assay
ChEMBL 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 10.1021/jm9018756
8541 9718 2 None -141 4 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/j.bmc.2011.12.009
9824353 9718 2 None -141 4 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/j.bmc.2011.12.009
CHEMBL292964 9718 2 None -141 4 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/j.bmc.2011.12.009
44290267 168974 0 None -13489 2 Human 4.3 pKi = 4.3 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 337 11 2 3 3.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)CC1CCC1 10.1016/j.bmcl.2004.01.063
CHEMBL416262 168974 0 None -13489 2 Human 4.3 pKi = 4.3 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 337 11 2 3 3.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)CC1CCC1 10.1016/j.bmcl.2004.01.063
57396659 78076 0 None -724 3 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 431 9 2 5 4.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1957430 78076 0 None -724 3 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 431 9 2 5 4.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
162650038 186839 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 434 6 2 6 3.9 CCn1ncc2cc(C)c(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
CHEMBL4747822 186839 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 434 6 2 6 3.9 CCn1ncc2cc(C)c(-c3ccc(C(/C=C4\OC(=O)NC4=O)(CC)CC)c(=O)[nH]3)cc21 10.1021/acsmedchemlett.0c00667
12002526 76241 0 None -3162 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 391 11 2 4 3.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933717 76241 0 None -3162 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 391 11 2 4 3.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmcl.2011.10.109
12002526 76241 0 None -3162 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 391 11 2 4 3.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933717 76241 0 None -3162 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 391 11 2 4 3.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2012.02.018
12002526 76241 0 None -3162 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 391 11 2 4 3.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2012.04.008
CHEMBL1933717 76241 0 None -3162 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 391 11 2 4 3.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2012.04.008
127047605 146627 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 327 4 1 6 3.6 CC(C)n1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3799153 146627 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 327 4 1 6 3.6 CC(C)n1ncc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
127047603 146644 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 299 3 1 6 2.6 Cn1ncc2cc(C(=O)Nc3nnc(C4CC4)s3)ccc21 10.1016/j.bmcl.2016.04.009
CHEMBL3799257 146644 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 299 3 1 6 2.6 Cn1ncc2cc(C(=O)Nc3nnc(C4CC4)s3)ccc21 10.1016/j.bmcl.2016.04.009
21362910 23697 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 9 1 2 7.0 O=C(O)CCCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL125269 23697 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 9 1 2 7.0 O=C(O)CCCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
21362869 213033 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 449 7 1 6 3.3 CS(=O)(=O)c1cccc(-c2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL86820 213033 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 449 7 1 6 3.3 CS(=O)(=O)c1cccc(-c2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/s0960-894x(02)00518-8
137477872 186978 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 419 4 2 3 4.1 CC(C)C(/C=C1/C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4749557 186978 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 419 4 2 3 4.1 CC(C)C(/C=C1/C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137487263 187225 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 408 5 2 4 4.1 CC(C)[C@H](C[C@H]1OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4752588 187225 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 408 5 2 4 4.1 CC(C)[C@H](C[C@H]1OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137487338 189985 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 424 5 2 4 4.8 CC(C)[C@@H](C[C@H]1SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4795879 189985 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 424 5 2 4 4.8 CC(C)[C@@H](C[C@H]1SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
44304436 210099 0 None -15 5 Mouse 8.2 pKi = 8.2 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 400 14 3 5 3.8 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64854 210099 0 None -15 5 Mouse 8.2 pKi = 8.2 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 400 14 3 5 3.8 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
44250281 203286 0 None -2 2 Rat 8.2 pKi = 8.2 Binding
Inhibition of rat EP3 receptorInhibition of rat EP3 receptor
ChEMBL 434 4 1 6 5.0 CCN1CCOc2ccc(C(=O)Nc3nnc(-c4c(Cl)cccc4Cl)s3)cc21 10.1016/j.bmcl.2009.05.074
CHEMBL563480 203286 0 None -2 2 Rat 8.2 pKi = 8.2 Binding
Inhibition of rat EP3 receptorInhibition of rat EP3 receptor
ChEMBL 434 4 1 6 5.0 CCN1CCOc2ccc(C(=O)Nc3nnc(-c4c(Cl)cccc4Cl)s3)cc21 10.1016/j.bmcl.2009.05.074
137477747 191449 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 392 4 1 2 5.0 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCCCC1=O 10.1016/j.bmcl.2021.128172
CHEMBL4849811 191449 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 392 4 1 2 5.0 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCCCC1=O 10.1016/j.bmcl.2021.128172
10275762 90364 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 451 6 1 5 5.6 O=C(/C=C/c1ccccc1Sc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL2204337 90364 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 451 6 1 5 5.6 O=C(/C=C/c1ccccc1Sc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
15551229 9038 41 None 446 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 10.1016/j.bmcl.2006.08.025
1941 9038 41 None 446 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 10.1016/j.bmcl.2006.08.025
CHEMBL218071 9038 41 None 446 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to EP3 receptor in presence of HSABinding affinity to EP3 receptor in presence of HSA
ChEMBL 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 10.1016/j.bmcl.2006.08.025
52941778 23314 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 712 14 2 4 11.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1Oc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1Oc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237304 23314 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 712 14 2 4 11.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1Oc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1Oc1ccccc1 10.1016/j.bmcl.2004.11.051
9872741 213741 0 None -27 2 Human 5.2 pKi = 5.2 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 567 8 2 4 6.1 CCCCNC(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL91270 213741 0 None -27 2 Human 5.2 pKi = 5.2 Binding
Affinity at human EP3 receptor.Affinity at human EP3 receptor.
ChEMBL 567 8 2 4 6.1 CCCCNC(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
44320294 112784 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 557 12 1 6 5.7 O=S(=O)(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL313266 112784 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 557 12 1 6 5.7 O=S(=O)(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL5081848 221551 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None COc1ccccc1S(=O)(=O)NC(=O)NC/C=C1\CCCc2cnn(Cc3ccc(Cl)cc3Cl)c21 10.1021/acsmedchemlett.1c00594
21362905 178086 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 6.9 CC(Cc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
CHEMBL446098 178086 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 6.9 CC(Cc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
23016963 206514 0 None - 1 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 476 8 2 6 5.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1cc(Cn3ccnc3)ccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
CHEMBL593526 206514 0 None - 1 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 476 8 2 6 5.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1cc(Cn3ccnc3)ccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
11338951 76130 0 None -416 2 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 413 11 2 5 3.2 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1cccc(Cl)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929535 76130 0 None -416 2 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 413 11 2 5 3.2 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1cccc(Cl)c1 10.1016/j.bmc.2011.12.009
57394140 76146 0 None -3162 3 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 419 13 2 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929550 76146 0 None -3162 3 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 419 13 2 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
127046040 146580 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 402 4 1 7 2.4 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CN(C(C)=O)C4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3798781 146580 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 402 4 1 7 2.4 CCn1ncc2c(F)cc(C(=O)Nc3nnc(C4(C)CN(C(C)=O)C4)s3)cc21 10.1016/j.bmcl.2016.04.009
10362346 76124 0 None -1548 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 379 11 2 5 2.6 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/j.bmc.2011.12.009
CHEMBL1929529 76124 0 None -1548 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 379 11 2 5 2.6 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/j.bmc.2011.12.009
9865111 70639 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 388 10 1 2 5.8 Cc1cccc(CCCc2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL180343 70639 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 388 10 1 2 5.8 Cc1cccc(CCCc2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44419350 90917 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 388 10 1 2 5.8 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL220820 90917 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 388 10 1 2 5.8 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)O)c1 10.1016/j.bmcl.2006.08.025
10093793 76135 0 None -74 3 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 423 12 2 5 3.8 CCc1cccc(C[C@H](O)/C=C/[C@H]2CSC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929540 76135 0 None -74 3 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 423 12 2 5 3.8 CCc1cccc(C[C@H](O)/C=C/[C@H]2CSC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
71517032 93291 0 None 3 2 Mouse 7.2 pKi = 7.2 Binding
Antagonist activity at mouse EP3 receptorAntagonist activity at mouse EP3 receptor
ChEMBL 612 8 1 5 7.1 O=C(NS(=O)(=O)c1ccc(Cl)c(Cl)c1)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
CHEMBL2315059 93291 0 None 3 2 Mouse 7.2 pKi = 7.2 Binding
Antagonist activity at mouse EP3 receptorAntagonist activity at mouse EP3 receptor
ChEMBL 612 8 1 5 7.1 O=C(NS(=O)(=O)c1ccc(Cl)c(Cl)c1)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
71451558 88658 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 742 13 5 8 7.7 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCNC(=S)Nc1ccc(-c2c3ccc(=O)cc-3oc3cc(O)ccc23)c(C(=O)O)c1 10.1021/ml300191g
CHEMBL2164613 88658 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP3R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 742 13 5 8 7.7 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCNC(=S)Nc1ccc(-c2c3ccc(=O)cc-3oc3cc(O)ccc23)c(C(=O)O)c1 10.1021/ml300191g
52947852 23318 0 None 37 3 Human 7.2 pKi = 7.2 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237316 23318 0 None 37 3 Human 7.2 pKi = 7.2 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2004.11.051
52947852 23318 0 None 37 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL1237316 23318 0 None 37 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
44419388 90190 0 None 37 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 294 6 1 2 4.0 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL219590 90190 0 None 37 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 294 6 1 2 4.0 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
10028418 21444 3 None -117 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE-2 from human Prostanoid EP3 receptorDisplacement of [3H]PGE-2 from human Prostanoid EP3 receptor
ChEMBL 465 8 1 4 6.9 O=C(O)COc1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.047
CHEMBL1205677 21444 3 None -117 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE-2 from human Prostanoid EP3 receptorDisplacement of [3H]PGE-2 from human Prostanoid EP3 receptor
ChEMBL 465 8 1 4 6.9 O=C(O)COc1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.047
CHEMBL132589 21444 3 None -117 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE-2 from human Prostanoid EP3 receptorDisplacement of [3H]PGE-2 from human Prostanoid EP3 receptor
ChEMBL 465 8 1 4 6.9 O=C(O)COc1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.047
10028418 21444 3 None -117 3 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptorInhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptor
ChEMBL 465 8 1 4 6.9 O=C(O)COc1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
CHEMBL1205677 21444 3 None -117 3 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptorInhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptor
ChEMBL 465 8 1 4 6.9 O=C(O)COc1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
CHEMBL132589 21444 3 None -117 3 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptorInhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptor
ChEMBL 465 8 1 4 6.9 O=C(O)COc1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
10178073 23331 0 None 269 4 Human 8.2 pKi = 8.2 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/s0960-894x(03)00794-7
CHEMBL123794 23331 0 None 269 4 Human 8.2 pKi = 8.2 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/s0960-894x(03)00794-7
10178073 23331 0 None 269 4 Human 8.2 pKi = 8.2 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL123794 23331 0 None 269 4 Human 8.2 pKi = 8.2 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44390831 70411 0 None 338 4 Human 8.2 pKi = 8.2 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 402 8 1 2 6.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccc(F)cc1 10.1016/j.bmcl.2004.11.051
CHEMBL180089 70411 0 None 338 4 Human 8.2 pKi = 8.2 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 402 8 1 2 6.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccc(F)cc1 10.1016/j.bmcl.2004.11.051
137487349 188195 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 406 4 2 4 4.2 CC(C)[C@@H](/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4763806 188195 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 406 4 2 4 4.2 CC(C)[C@@H](/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL5077024 221254 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None Cc1ncc(S(=O)(=O)NC(=O)NC/C=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)s1 10.1021/acsmedchemlett.1c00594
CHEMBL5086151 221791 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None O=C(NC/C(F)=C1\CCCc2cnn(Cc3ccc(C(F)(F)F)cc3)c21)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.1c00594
137477779 191951 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 389 4 2 2 5.5 Cc1nc(C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C(C)C)[nH]c1C 10.1016/j.bmcl.2021.128172
CHEMBL4857240 191951 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 389 4 2 2 5.5 Cc1nc(C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C(C)C)[nH]c1C 10.1016/j.bmcl.2021.128172
164620081 192469 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 392 5 2 2 4.6 CC(C)[C@@H](C[C@H]1CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4865327 192469 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 392 5 2 2 4.6 CC(C)[C@@H](C[C@H]1CCNC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
137477566 192451 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 361 4 2 2 4.8 CC(C)C(c1ncc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4864985 192451 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 361 4 2 2 4.8 CC(C)C(c1ncc[nH]1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
46887177 15362 0 None 33 2 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 459 10 2 3 6.6 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
CHEMBL1094790 15362 0 None 33 2 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 459 10 2 3 6.6 Cc1cc(C)cc([C@@H](CC(C)C)NC(=O)c2cc(Oc3ccccc3)ccc2CCC(=O)O)c1 10.1016/j.bmc.2010.03.028
23017739 206316 0 None - 1 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 465 10 2 3 5.8 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.11.023
CHEMBL592213 206316 0 None - 1 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE3alpha from mouse EP3alpha receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 465 10 2 3 5.8 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.11.023
117993413 128537 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assayDisplacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assay
ChEMBL 370 2 2 4 2.8 Cn1cnc2cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc(Cl)c21 10.1021/acsmedchemlett.5b00188
CHEMBL3589084 128537 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assayDisplacement of [3H]PGE2 from human EP3 receptor by MicroBeta plate-based scintillation counting/SPA binding assay
ChEMBL 370 2 2 4 2.8 Cn1cnc2cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc(Cl)c21 10.1021/acsmedchemlett.5b00188
117993413 128537 0 None - 1 Human 8.1 pKi = 8.1 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 370 2 2 4 2.8 Cn1cnc2cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc(Cl)c21 nan
CHEMBL3589084 128537 0 None - 1 Human 8.1 pKi = 8.1 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 370 2 2 4 2.8 Cn1cnc2cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc(Cl)c21 nan
44269486 173621 0 None -24 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL428524 173621 0 None -24 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
56668527 71582 0 None 1 4 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 8 1 5 4.3 CCN(C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1)c1cccc(CC(=O)O)c1 10.1016/j.bmc.2011.08.007
CHEMBL1819607 71582 0 None 1 4 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP3alpha receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 8 1 5 4.3 CCN(C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1)c1cccc(CC(=O)O)c1 10.1016/j.bmc.2011.08.007
9830839 113708 0 None -151 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 640 10 1 8 6.3 CCCCc1nn(-c2ccccc2C(F)(F)F)c(=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)NC(=O)c2cccs2)cc1 10.1016/s0960-894x(02)00518-8
CHEMBL314812 113708 0 None -151 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 640 10 1 8 6.3 CCCCc1nn(-c2ccccc2C(F)(F)F)c(=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)NC(=O)c2cccs2)cc1 10.1016/s0960-894x(02)00518-8
24765153 191308 0 None -1096 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
CHEMBL484778 191308 0 None -1096 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
44304034 207373 0 None -10 3 Mouse 7.1 pKi = 7.1 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
CHEMBL59921 207373 0 None -10 3 Mouse 7.1 pKi = 7.1 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
44304417 208889 0 None -275 4 Mouse 6.1 pKi = 6.1 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 438 13 3 4 4.3 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL60894 208889 0 None -275 4 Mouse 6.1 pKi = 6.1 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 438 13 3 4 4.3 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
44320373 213029 0 None -5 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 376 9 1 2 5.8 O=C(O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1 10.1016/s0960-894x(02)00518-8
CHEMBL86799 213029 0 None -5 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human Prostanoid EP3 receptor.Binding affinity at human Prostanoid EP3 receptor.
ChEMBL 376 9 1 2 5.8 O=C(O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1 10.1016/s0960-894x(02)00518-8
25003075 13610 18 None -26302 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from human prostanoid EP3 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP3 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 478 6 2 3 5.8 O=C(O)c1ccc(C2(NC(=O)c3cccc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1084009 13610 18 None -26302 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from human prostanoid EP3 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP3 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 478 6 2 3 5.8 O=C(O)c1ccc(C2(NC(=O)c3cccc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.065
21974328 73044 0 None -81 5 Mouse 6.1 pKi = 6.1 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 443 6 1 6 4.4 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Oc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL184684 73044 0 None -81 5 Mouse 6.1 pKi = 6.1 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 443 6 1 6 4.4 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Oc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
9944231 24807 0 None 7 4 Human 6.1 pKi = 6.1 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 302 5 1 1 5.0 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL126472 24807 0 None 7 4 Human 6.1 pKi = 6.1 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 302 5 1 1 5.0 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2)c1 10.1016/s0960-894x(03)00794-7
127047601 146552 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 330 4 1 6 2.9 CCN1CCOc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
CHEMBL3798598 146552 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assayDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in human Chem1 cell membrane by scintillation proximity assay
ChEMBL 330 4 1 6 2.9 CCN1CCOc2ccc(C(=O)Nc3nnc(C4CC4)s3)cc21 10.1016/j.bmcl.2016.04.009
57395059 76249 0 None -512 3 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmcl.2011.10.109
CHEMBL1933725 76249 0 None -512 3 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmcl.2011.10.109
57395059 76249 0 None -512 3 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1933725 76249 0 None -512 3 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmc.2012.02.018
11337782 91718 0 None -4365 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 373 10 2 3 3.6 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2CC[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
CHEMBL223744 91718 0 None -4365 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 373 10 2 3 3.6 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2CC[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
11440167 91493 0 None -79432 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 371 9 2 3 3.4 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
CHEMBL222782 91493 0 None -79432 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 371 9 2 3 3.4 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
52945294 23319 0 None 77 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237317 23319 0 None 77 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
52945294 23319 0 None 77 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL1237317 23319 0 None 77 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
10111602 90003 0 None 77 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 400 9 1 3 5.6 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL218626 90003 0 None 77 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 400 9 1 3 5.6 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
44290266 168487 0 None -10 4 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 353 12 3 4 2.3 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)N1C/C=C/CCCC(=O)O 10.1016/j.bmcl.2004.01.063
CHEMBL413509 168487 0 None -10 4 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined against prostanoid EP3 receptorBinding affinity was determined against prostanoid EP3 receptor
ChEMBL 353 12 3 4 2.3 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)N1C/C=C/CCCC(=O)O 10.1016/j.bmcl.2004.01.063
137487264 186235 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 408 5 2 4 4.1 CC(C)[C@H](C[C@@H]1OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4740657 186235 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 408 5 2 4 4.1 CC(C)[C@H](C[C@@H]1OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137490797 188141 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 424 5 2 4 4.8 CC(C)[C@H](C[C@H]1SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4763179 188141 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 424 5 2 4 4.8 CC(C)[C@H](C[C@H]1SC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
23017168 14819 0 None - 1 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 552 11 1 5 5.2 CN(C)Cc1ccc(CCC(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c(OCCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2010.02.034
CHEMBL1090938 14819 0 None - 1 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counterDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 552 11 1 5 5.2 CN(C)Cc1ccc(CCC(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c(OCCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2010.02.034
137477601 191559 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 442 5 1 4 3.8 CC(C)C(CN1CCS(=O)(=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4851344 191559 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 442 5 1 4 3.8 CC(C)C(CN1CCS(=O)(=O)CC1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
132836 66469 23 None -1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to EP3 receptor (unknown origin)Binding affinity to EP3 receptor (unknown origin)
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 10.1021/jm401431x
CHEMBL1722929 66469 23 None -1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to EP3 receptor (unknown origin)Binding affinity to EP3 receptor (unknown origin)
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 10.1021/jm401431x
21362849 175107 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 8 1 2 6.9 CC(Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
CHEMBL434247 175107 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 8 1 2 6.9 CC(Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
5855 8426 7 None -912 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE-2 from human Prostanoid EP3 receptorDisplacement of [3H]PGE-2 from human Prostanoid EP3 receptor
ChEMBL 447 7 2 5 4.3 OC(=O)COc1cccc2c1CC[C@](C2)(O)COC(=O)N(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2005.04.047
9911469 8426 7 None -912 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE-2 from human Prostanoid EP3 receptorDisplacement of [3H]PGE-2 from human Prostanoid EP3 receptor
ChEMBL 447 7 2 5 4.3 OC(=O)COc1cccc2c1CC[C@](C2)(O)COC(=O)N(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2005.04.047
CHEMBL196779 8426 7 None -912 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE-2 from human Prostanoid EP3 receptorDisplacement of [3H]PGE-2 from human Prostanoid EP3 receptor
ChEMBL 447 7 2 5 4.3 OC(=O)COc1cccc2c1CC[C@](C2)(O)COC(=O)N(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2005.04.047
11488860 26063 0 None -1949 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to prostanoid receptor EP3 receptorBinding affinity to prostanoid receptor EP3 receptor
ChEMBL 497 5 1 4 5.7 C[C@@H](c1ccc(C(F)(F)F)cc1)n1c2c(c3cc(F)cc(S(C)(=O)=O)c31)CCC[C@@H]2CC(=O)O 10.1016/j.bmcl.2010.10.018
CHEMBL1290413 26063 0 None -1949 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to prostanoid receptor EP3 receptorBinding affinity to prostanoid receptor EP3 receptor
ChEMBL 497 5 1 4 5.7 C[C@@H](c1ccc(C(F)(F)F)cc1)n1c2c(c3cc(F)cc(S(C)(=O)=O)c31)CCC[C@@H]2CC(=O)O 10.1016/j.bmcl.2010.10.018
44303952 107663 0 None -41 4 Mouse 6.1 pKi = 6.1 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 420 14 3 4 4.8 CCCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL293697 107663 0 None -41 4 Mouse 6.1 pKi = 6.1 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
ChEMBL 420 14 3 4 4.8 CCCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
12112238 124849 0 None 10 4 Human 7.1 pKi = 7.1 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 406 7 1 2 6.7 O=C(O)/C=C/c1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL340501 124849 0 None 10 4 Human 7.1 pKi = 7.1 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 406 7 1 2 6.7 O=C(O)/C=C/c1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
162647817 186612 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 405 3 2 3 3.9 CC(C)/C(=C1\C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4745085 186612 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 405 3 2 3 3.9 CC(C)/C(=C1\C(=O)NC(=O)N1C)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137487291 187909 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 394 4 2 4 3.7 CC(C)[C@@H](c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)[C@@H]1OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4760599 187909 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 394 4 2 4 3.7 CC(C)[C@@H](c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)[C@@H]1OC(=O)NC1=O 10.1021/acsmedchemlett.0c00667
57400249 76252 0 None -6 3 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 410 9 2 6 3.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CC2CCCC2)n1 10.1016/j.bmcl.2011.10.109
CHEMBL1933728 76252 0 None -6 3 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 410 9 2 6 3.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CC2CCCC2)n1 10.1016/j.bmcl.2011.10.109
23016719 207999 0 None 1 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(OCc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL603625 207999 0 None 1 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(OCc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
44138108 191064 0 None -2630 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
CHEMBL483991 191064 0 None -2630 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
10291963 91483 0 None -50 6 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.10.109
CHEMBL222715 91483 0 None -50 6 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.10.109
10291963 91483 0 None -50 6 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmc.2012.02.018
CHEMBL222715 91483 0 None -50 6 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmc.2012.02.018
72706947 181443 20 None -371 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 363 11 2 3 3.4 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
CHEMBL4558749 181443 20 None -371 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 363 11 2 3 3.4 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
21362853 25304 0 None 11 4 Human 7.1 pKi = 7.1 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2COc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL127482 25304 0 None 11 4 Human 7.1 pKi = 7.1 Binding
Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP3 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2COc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
137478291 191198 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 394 5 2 3 4.7 CCC(CC)(c1nnc[nH]1)c1ccc(-c2ccc3cc(F)cc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4846132 191198 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 394 5 2 3 4.7 CCC(CC)(c1nnc[nH]1)c1ccc(-c2ccc3cc(F)cc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
3356 9060 73 None -131 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
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 9060 73 None -131 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
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
9867642 9060 73 None -131 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
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
CHEMBL426559 9060 73 None -131 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
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
DB11629 9060 73 None -131 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
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
52944193 23305 0 None 63 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237295 23305 0 None 63 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
22009003 129394 0 None 112 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(C(O)/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL360290 129394 0 None 112 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human prostanoid EP3 receptorBinding affinity for human prostanoid EP3 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(C(O)/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
44419374 89770 0 None 95 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL218123 89770 0 None 95 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
44419379 144641 0 None 95 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL376053 144641 0 None 95 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to EP3 receptorBinding affinity to EP3 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
137477812 189611 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 406 4 2 4 4.2 CC(C)C(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
CHEMBL4791261 189611 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 406 4 2 4 4.2 CC(C)C(/C=C1\OC(=O)NC1=O)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1021/acsmedchemlett.0c00667
137478131 189878 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 432 4 2 4 4.8 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CCCC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL4794537 189878 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysisDisplacement of [3H]-PGE2 from human EP3 expressed in Chem-1 cell membranes incubated for 2 hrs by TopCount scintillation plate reader analysis
ChEMBL 432 4 2 4 4.8 O=C1NC(=O)/C(=C/C(c2ccc(-c3ccc4cccc(F)c4c3)[nH]c2=O)C2CCCC2)O1 10.1021/acsmedchemlett.0c00667
CHEMBL5085586 221753 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting methodDisplacement of [3H]-PGE2 from human EP3 receptor assessed as inhibition constant incubated for 2 hrs by TopCount scintillation counting method
ChEMBL None None None Cn1cc(S(=O)(=O)NC(=O)NC/C=C2\CCCc3cnn(Cc4ccc(Cl)cc4Cl)c32)cn1 10.1021/acsmedchemlett.1c00594
137477851 193104 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 379 4 2 2 4.1 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCNC1=O 10.1016/j.bmcl.2021.128172
CHEMBL4874814 193104 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 379 4 2 2 4.1 CC(C)C(c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O)N1CCNC1=O 10.1016/j.bmcl.2021.128172
137477995 192468 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 393 5 2 4 5.6 CC(C)C(Nc1nccs1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
CHEMBL4865321 192468 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 393 5 2 4 5.6 CC(C)C(Nc1nccs1)c1ccc(-c2ccc3cccc(F)c3c2)[nH]c1=O 10.1016/j.bmcl.2021.128172
117992916 167136 0 None - 1 Human 8.0 pKi = 8.0 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 364 3 2 4 2.9 CCn1ncc2c(C)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 nan
CHEMBL4110846 167136 0 None - 1 Human 8.0 pKi = 8.0 Binding
EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.EP3 Radioligand SPA Binding Assay: Test compounds were half log serially diluted in 100% DMSO (J. T. Baker #922401). 1 uL of each compound was added to appropriate wells of a 384-well plate (Matrix Cat #4322). Unlabeled PGE2 (Tocris Cat #2296) at a final concentration of 1 uM was used to determine non-specific binding. 1 uL of 100% DMSO (J. T. Baker #922401) was used to determine total binding. Millipore EP3 Chem1 membranes (prepared in-house from cell paste derived from the Millipore ChemiSCREEN Human Recombinant EP3 Prostanoid Receptor Calcium-Optimized Stable Cell Line (Millipore Cat #HTS092C. http://www.millipore.com/catalogue/item/hts092c)) were thawed and diluted in binding buffer (50 mM Hepes pH 7.4 (Lonza Cat #17-737), 5 mM MgCl2 (Sigma-M1028), and 0.1% BSA (Sigma A-7409)) to a final concentration of 1 ug/25 uL. 25 uL of diluted membranes were added to prepared compound plates. WGA coated PVT SPA Beads (Perkin Elmer Cat #RPNQ0060) were diluted in binding buffer to a concentration of 4 ug/ul, and 25 uL of the SPA bead mixture was then added to each well for a final assay concentration of 100 ug/well. [3H]-PGE2 (Perkin Elmer Cat #NET428) was diluted in binding buffer to a concentration of 3.375 pM, and 25 uL was added to all wells for a final assay concentration of 1.125 nM. Plates were incubated for 30 minutes at r.t. (approximately 25° C.) with shaking. Radioactivity associated with each well was measured after a 10 hour incubation using a Wallac Trilux MicroBeta plate-based scintillation counter and a normalized protocol at 1 minute read/well.
ChEMBL 364 3 2 4 2.9 CCn1ncc2c(C)cc(-c3ccc([C@@]4(C)CCCNC4=O)c(=O)[nH]3)cc21 nan
71461205 90367 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 449 7 1 5 5.0 O=C(/C=C/c1ccccc1OCc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
CHEMBL2204340 90367 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of EP3 receptorInhibition of EP3 receptor
ChEMBL 449 7 1 5 5.0 O=C(/C=C/c1ccccc1OCc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1021/jm1013693
44442327 101234 0 None -5623 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251294 101234 0 None -5623 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
11405770 144686 0 None -5370 3 Human 4.0 pKi = 4.0 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 361 11 2 3 3.6 CCCCC[C@H](O)CC[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
CHEMBL376347 144686 0 None -5370 3 Human 4.0 pKi = 4.0 Binding
Binding affinity to human EP3 receptorBinding affinity to human EP3 receptor
ChEMBL 361 11 2 3 3.6 CCCCC[C@H](O)CC[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
44304404 107357 0 None -181 4 Mouse 7.0 pKi = 7.0 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 436 12 3 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL291630 107357 0 None -181 4 Mouse 7.0 pKi = 7.0 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 436 12 3 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
44304403 175876 0 None -27 4 Mouse 7.0 pKi = 7.0 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 420 12 3 4 3.8 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL439934 175876 0 None -27 4 Mouse 7.0 pKi = 7.0 Binding
Affinity for mouse Prostanoid EP3 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP3 receptor expressed in CHO cells
ChEMBL 420 12 3 4 3.8 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
44520990 206632 0 None 2 3 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 410 6 2 4 5.3 Cc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
CHEMBL594423 206632 0 None 2 3 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 410 6 2 4 5.3 Cc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
137477592 191482 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 411 6 2 5 3.6 CCN1CCOc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
CHEMBL4850242 191482 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assayDisplacement of [3H]PGE2 from human EP3 receptor expressed in CHO cells by radioligand competition binding assay
ChEMBL 411 6 2 5 3.6 CCN1CCOc2c(F)cc(-c3ccc(C(CC)(CC)c4nnc[nH]4)c(=O)[nH]3)cc21 10.1016/j.bmcl.2021.128172
21974528 131228 0 None -48 5 Mouse 6.0 pKi = 6.0 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 441 6 1 5 4.6 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Cc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL363984 131228 0 None -48 5 Mouse 6.0 pKi = 6.0 Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
ChEMBL 441 6 1 5 4.6 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Cc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
56949973 76147 0 None -1949 4 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 407 11 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929551 76147 0 None -1949 4 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 407 11 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
44520992 206759 0 None 28 2 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 396 6 1 4 4.1 O=C(O)C#Cc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595159 206759 0 None 28 2 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP3 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 396 6 1 4 4.1 O=C(O)C#Cc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
1884 9857 52 None -11 22 Human 8.2 pIC50 = 8.2 Binding
In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand
Drug Central 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 None
5280363 9857 52 None -11 22 Human 8.2 pIC50 = 8.2 Binding
In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand
Drug Central 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 None
912 9857 52 None -11 22 Human 8.2 pIC50 = 8.2 Binding
In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand
Drug Central 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 None
CHEMBL815 9857 52 None -11 22 Human 8.2 pIC50 = 8.2 Binding
In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand
Drug Central 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 None
DB12789 9857 52 None -11 22 Human 8.2 pIC50 = 8.2 Binding
In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand
Drug Central 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 None
1883 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
1883 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8076679
1916 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
1916 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8076679
5280360 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
5280360 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8076679
913 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
913 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8076679
CHEMBL548 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
CHEMBL548 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8076679
DB00917 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
DB00917 9856 75 None -1 24 Rat 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8076679
1883 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
1883 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
1883 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22480736
1916 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
1916 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
1916 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22480736
5280360 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
5280360 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
5280360 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22480736
913 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
913 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
913 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22480736
CHEMBL548 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
CHEMBL548 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
CHEMBL548 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22480736
DB00917 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
DB00917 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
DB00917 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22480736
1883 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
1916 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
5280360 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
913 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
CHEMBL548 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
DB00917 9856 75 None -1 24 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
1883 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
1883 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
1883 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
1916 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
1916 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
1916 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
5280360 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
5280360 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
5280360 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
913 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
913 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
913 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
CHEMBL548 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
CHEMBL548 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
CHEMBL548 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
DB00917 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 15937517
DB00917 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
DB00917 9856 75 None -1 24 Rat 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
1883 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
1883 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
1916 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
1916 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
5280360 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
5280360 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
913 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
913 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
CHEMBL548 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
CHEMBL548 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
DB00917 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
DB00917 9856 75 None -1 24 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 16604093
1883 9856 75 None -2 24 Mouse 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
1916 9856 75 None -2 24 Mouse 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
5280360 9856 75 None -2 24 Mouse 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
913 9856 75 None -2 24 Mouse 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
CHEMBL548 9856 75 None -2 24 Mouse 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
DB00917 9856 75 None -2 24 Mouse 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
1883 9856 75 None -1 24 Rat 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
1916 9856 75 None -1 24 Rat 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
5280360 9856 75 None -1 24 Rat 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
913 9856 75 None -1 24 Rat 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
CHEMBL548 9856 75 None -1 24 Rat 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
DB00917 9856 75 None -1 24 Rat 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18632791
1883 9856 75 None -1 24 Rat 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
1916 9856 75 None -1 24 Rat 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
5280360 9856 75 None -1 24 Rat 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
913 9856 75 None -1 24 Rat 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
CHEMBL548 9856 75 None -1 24 Rat 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
DB00917 9856 75 None -1 24 Rat 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
1913 9242 0 3H-PGE2 4 15 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O None
5311223 9242 0 3H-PGE2 4 15 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O None
1883 9856 75 3H-PGE2 -1 24 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 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 None
1916 9856 75 3H-PGE2 -1 24 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 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 None
5280360 9856 75 3H-PGE2 -1 24 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 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 None
913 9856 75 3H-PGE2 -1 24 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 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 None
CHEMBL548 9856 75 3H-PGE2 -1 24 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 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 None
DB00917 9856 75 3H-PGE2 -1 24 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 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 None
134689669 222829 0 3H-PGE2 1 12 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 465 12 3 7 1.7 CS(=O)(=O)NC(=O)CCCC=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
134689669 222829 0 3H-PGE2 -1 12 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 465 12 3 7 1.7 CS(=O)(=O)NC(=O)CCCC=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
1913 9242 0 3H-PGE2 -4 15 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O None
5311223 9242 0 3H-PGE2 -4 15 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O None
1883 9856 75 3H-PGE2 -2 24 Mouse 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 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 None
1916 9856 75 3H-PGE2 -2 24 Mouse 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 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 None
5280360 9856 75 3H-PGE2 -2 24 Mouse 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 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 None
913 9856 75 3H-PGE2 -2 24 Mouse 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 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 None
CHEMBL548 9856 75 3H-PGE2 -2 24 Mouse 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 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 None
DB00917 9856 75 3H-PGE2 -2 24 Mouse 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 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 None
138 9855 88 3H-PGE2 -2 18 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
149351 9855 88 3H-PGE2 -2 18 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 9855 88 3H-PGE2 -2 18 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 9855 88 3H-PGE2 -2 18 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 9855 88 3H-PGE2 -2 18 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 9855 88 3H-PGE2 -2 18 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
None 222830 0 3H-PGE2 4 4 Mouse 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 587 15 3 8 4.7 C1C(C(C(C1=O)CCC=CCCC(=O)OC2=CC=C(C=C2)NC(=O)C3=CC=CC=C3)OCC(COC4=CC=CC=C4)O)O None
None 222828 0 3H-PGE2 1 3 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 512 11 2 4 4.6 C1CC2C(C(C1O2)CC=CCCCC(=O)O)C=CC(COC3=CC=C(C=C3)I)O None
179 7188 115 3H-PGE2 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 3H-PGE2 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 3H-PGE2 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 3H-PGE2 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 3H-PGE2 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
242 7258 124 3H-PGE2 -7244 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-PGE2 -7244 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-PGE2 -7244 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-PGE2 -7244 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-PGE2 -7244 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
119304 7539 0 3H-PGE2 -14125 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 368 11 3 4 2.7 OC(=O)CCCCCCC1C(=O)NC(=O)N1CCC(C1CCCCC1)O None
1878 7539 0 3H-PGE2 -14125 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 368 11 3 4 2.7 OC(=O)CCCCCCC1C(=O)NC(=O)N1CCC(C1CCCCC1)O None
40481312 7539 0 3H-PGE2 -14125 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 368 11 3 4 2.7 OC(=O)CCCCCCC1C(=O)NC(=O)N1CCC(C1CCCCC1)O None
CHEMBL575504 7539 0 3H-PGE2 -14125 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 368 11 3 4 2.7 OC(=O)CCCCCCC1C(=O)NC(=O)N1CCC(C1CCCCC1)O None
122021 7543 0 3H-PGE1 -7585 4 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 459 13 3 5 3.7 OC(=O)CCCCCCC1N(NCC(C2CCCCC2)O)C(=O)N(C1=O)Cc1ccccc1 None
122021 7543 0 3H-PGE2 -7585 4 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 459 13 3 5 3.7 OC(=O)CCCCCCC1N(NCC(C2CCCCC2)O)C(=O)N(C1=O)Cc1ccccc1 None
1897 7543 0 3H-PGE1 -7585 4 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 459 13 3 5 3.7 OC(=O)CCCCCCC1N(NCC(C2CCCCC2)O)C(=O)N(C1=O)Cc1ccccc1 None
1897 7543 0 3H-PGE2 -7585 4 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 459 13 3 5 3.7 OC(=O)CCCCCCC1N(NCC(C2CCCCC2)O)C(=O)N(C1=O)Cc1ccccc1 None
1899 7543 0 3H-PGE1 -7585 4 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 459 13 3 5 3.7 OC(=O)CCCCCCC1N(NCC(C2CCCCC2)O)C(=O)N(C1=O)Cc1ccccc1 None
1899 7543 0 3H-PGE2 -7585 4 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 459 13 3 5 3.7 OC(=O)CCCCCCC1N(NCC(C2CCCCC2)O)C(=O)N(C1=O)Cc1ccccc1 None
2726 7706 68 3H-PGE2 -5888 72 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-PGE2 -5888 72 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-PGE2 -5888 72 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-PGE2 -5888 72 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-PGE2 -5888 72 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 7745 93 3H-PGE2 -4168 90 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-PGE2 -4168 90 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-PGE2 -4168 90 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-PGE2 -4168 90 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-PGE2 -4168 90 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1212 8443 50 3H-PGE2 -19952 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-PGE2 -19952 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-PGE2 -19952 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-PGE2 -19952 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-PGE2 -19952 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1353 8692 93 3H-PGE2 -6918 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-PGE2 -6918 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-PGE2 -6918 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-PGE2 -6918 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-PGE2 -6918 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135409468 8816 69 3H-PGE2 -3548 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 8816 69 3H-PGE2 -3548 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 8816 69 3H-PGE2 -3548 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
1551 9066 0 3H-PGE2 -97 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
1961 9066 0 3H-PGE2 -97 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
5311221 9066 0 3H-PGE2 -97 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
CHEMBL1051 9066 0 3H-PGE2 -97 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
DB00654 9066 0 3H-PGE2 -97 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
1613 9127 53 3H-PGE2 -2754 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-PGE2 -2754 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-PGE2 -2754 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-PGE2 -2754 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-PGE2 -2754 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
134 9292 24 3H-PGE2 -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-PGE2 -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-PGE2 -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-PGE2 -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-PGE2 -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
15897 9637 0 3H-PGE2 -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-PGE2 -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-PGE2 -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
135398745 9688 112 3H-PGE2 -5128 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-PGE2 -5128 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-PGE2 -5128 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-PGE2 -5128 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2337 10030 77 3H-PGE2 -1122 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-PGE2 -1122 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-PGE2 -1122 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-PGE2 -1122 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-PGE2 -1122 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2389 10104 118 3H-PGE2 -26915 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-PGE2 -26915 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-PGE2 -26915 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-PGE2 -26915 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-PGE2 -26915 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1922 10310 38 3H-PGE2 4 3 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 0 2 3 3.2 CC(=O)NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2 None
4336830 10310 38 3H-PGE2 4 3 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 0 2 3 3.2 CC(=O)NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL112816 10310 38 3H-PGE2 4 3 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 0 2 3 3.2 CC(=O)NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2 None
1980 10434 0 3H-PGE2 -10000 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 387 10 4 4 3.3 O=C(Nc1ccccc1)NNC[C@@H]1[C@@H]2CC[C@H]([C@@H]1C/C=C\CCCC(=O)O)O2 None
1985 10434 0 3H-PGE2 -10000 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 387 10 4 4 3.3 O=C(Nc1ccccc1)NNC[C@@H]1[C@@H]2CC[C@H]([C@@H]1C/C=C\CCCC(=O)O)O2 None
6437074 10434 0 3H-PGE2 -10000 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 387 10 4 4 3.3 O=C(Nc1ccccc1)NNC[C@@H]1[C@@H]2CC[C@H]([C@@H]1C/C=C\CCCC(=O)O)O2 None
100 10577 58 3H-PGE2 -4897 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-PGE2 -4897 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-PGE2 -4897 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-PGE2 -4897 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-PGE2 -4897 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
213 10625 55 3H-PGE2 -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 10625 55 3H-PGE2 -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 10625 55 3H-PGE2 -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 10625 55 3H-PGE2 -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 10625 55 3H-PGE2 -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
1888 10672 29 3H-PGE1 -398 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
1888 10672 29 3H-PGE2 -398 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
1888 10672 29 3H-PGE2 -446 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
1974 10672 29 3H-PGE1 -398 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
1974 10672 29 3H-PGE2 -398 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
1974 10672 29 3H-PGE2 -446 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
5311493 10672 29 3H-PGE1 -398 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
5311493 10672 29 3H-PGE2 -398 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
5311493 10672 29 3H-PGE2 -446 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
CHEMBL521784 10672 29 3H-PGE1 -398 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
CHEMBL521784 10672 29 3H-PGE2 -398 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
CHEMBL521784 10672 29 3H-PGE2 -446 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O None
185 10778 60 3H-PGE2 -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 10778 60 3H-PGE2 -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 10778 60 3H-PGE2 -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 10778 60 3H-PGE2 -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2865 10915 73 3H-PGE2 -20417 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-PGE2 -20417 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-PGE2 -20417 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-PGE2 -20417 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-PGE2 -20417 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
103 10925 61 3H-PGE2 -8317 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-PGE2 -8317 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-PGE2 -8317 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-PGE2 -8317 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-PGE2 -8317 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
115237 62359 119 3H-PGE2 -954 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-PGE2 -954 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 62359 119 3H-PGE2 -954 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
5311035 104579 29 3H-PGE2 -91 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 None
5311035 104579 29 3H-PGE2 -37 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 None
CHEMBL271896 104579 29 3H-PGE2 -91 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 None
CHEMBL271896 104579 29 3H-PGE2 -37 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 None
3036780 114308 20 3H-PGE2 -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 114308 20 3H-PGE2 -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-PGE2 -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-PGE2 -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-PGE2 -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 114308 20 3H-PGE2 -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 114308 20 3H-PGE2 -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1615 174570 24 3H-PGE2 -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 174570 24 3H-PGE2 -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
4054 212280 72 3H-PGE2 -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 212280 72 3H-PGE2 -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 212280 72 3H-PGE2 -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
3337 213146 27 3H-PGE2 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 3H-PGE2 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 3H-PGE2 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 3H-PGE2 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 3H-PGE2 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 213146 27 3H-PGE2 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
11954224 222732 0 3H-PGE2 -141253 59 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954259 222758 0 3H-PGE2 -33113 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
None 222845 0 3H-PGE1 -91 2 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 390 12 4 4 3.3 C1C(C(C(C1O)CC=CCCCC(=O)O)CCC(CCC2=CC=CC=C2)O)O None
None 222847 0 3H-PGE1 -1 2 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 424 16 2 5 5.1 CCCCCCCC(=O)CCC1C(CC(C1CC=CCCCC(=O)OC(C)C)O)O None
None 222847 0 3H-PGE2 -1 2 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 424 16 2 5 5.1 CCCCCCCC(=O)CCC1C(CC(C1CC=CCCCC(=O)OC(C)C)O)O None
None 222848 0 3H-PGE2 -147 6 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 16 2 2 5.2 CCCCCC=CCC=CCC=CCC=CCCCC(=O)NCCO None
None 222849 0 3H-PGE1 -1 2 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 150 1 0 4 1.3 C1N(CSCS1)N=O None
None 222849 0 3H-PGE2 -1 2 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 150 1 0 4 1.3 C1N(CSCS1)N=O None
None 222850 0 3H-PGE2 -2 2 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 13 3 5 4.2 CC(C)OC(=O)CCCC=CCC1C(CC(C1CCC(CCC2=CC=CC=C2)O)O)O None
132748 223191 0 3H-PGE2 -7 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 3 2 4 4.6 C1C2=CC=CC=C2OC3=C(N1C(=O)NNC(=O)CCC4=CC=NC=C4)C=C(C=C3)Cl.Cl None
134689669 222829 0 3H-PGE2 -8 12 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 465 12 3 7 1.7 CS(=O)(=O)NC(=O)CCCC=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
None 222830 0 3H-PGE2 -4 4 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 587 15 3 8 4.7 C1C(C(C(C1=O)CCC=CCCC(=O)OC2=CC=C(C=C2)NC(=O)C3=CC=CC=C3)OCC(COC4=CC=CC=C4)O)O None
None 222826 0 3H-PGE2 -6 2 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 398 8 3 4 3.3 CC#CCC(C)C(C=CC1C(CC2C1C3=C(O2)C(=CC=C3)CCCC(=O)O)O)O None
1881 9853 0 3H-PGE2 -602 21 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
1891 9853 0 3H-PGE2 -602 21 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
448457 9853 0 3H-PGE2 -602 21 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
CHEMBL1235252 9853 0 3H-PGE2 -602 21 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
DB02056 9853 0 3H-PGE2 -602 21 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
91798918 222842 0 3H-PGE1 -2 10 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 400 10 2 6 2.6 COC(=O)CCC=C=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
91798918 222842 0 3H-PGE2 -1 10 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 400 10 2 6 2.6 COC(=O)CCC=C=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
133126726 222824 0 3H-PGE2 -1 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
24868263 222824 0 3H-PGE2 -1 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
1881 9853 0 3H-PGE1 -602 21 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
1891 9853 0 3H-PGE1 -602 21 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
448457 9853 0 3H-PGE1 -602 21 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
CHEMBL1235252 9853 0 3H-PGE1 -602 21 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
DB02056 9853 0 3H-PGE1 -602 21 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
119461 7108 72 3H-PGE2 -4 10 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C None
1896 7108 72 3H-PGE2 -4 10 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C None
CHEMBL1317823 7108 72 3H-PGE2 -4 10 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C None
5311035 104579 29 3H-PGE2 -37 9 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 None
CHEMBL271896 104579 29 3H-PGE2 -37 9 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 None
1917 7714 0 3H-PGE2 -3 9 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
5311044 7714 0 3H-PGE2 -3 9 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
631 7714 0 3H-PGE2 -3 9 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
CHEMBL160629 7714 0 3H-PGE2 -3 9 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
138 9855 88 3H-PGE1 -2 18 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
149351 9855 88 3H-PGE1 -2 18 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 9855 88 3H-PGE1 -2 18 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 9855 88 3H-PGE1 -2 18 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 9855 88 3H-PGE1 -2 18 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 9855 88 3H-PGE1 -2 18 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
124936 224471 0 3H-EP2 3 6 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 268 3 1 5 4.8 CNC1=CC=C(C=C1)N=NC2=CC3=C(C=C2)N=CS3 None
134689669 222829 0 3H-PGE1 -8 12 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 465 12 3 7 1.7 CS(=O)(=O)NC(=O)CCCC=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
89077401 222823 0 3H-PGE2 -1 12 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 360 8 3 3 3.5 CC#CCC(C)C(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
None 222822 0 3H-PGE2 4 5 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 366 12 2 3 5.2 CCCCCC(C=CC1CC2CC(C1CC=CCCCC(=O)O)S2)O None
1884 9857 52 3H-PGE2 -8 22 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 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 None
5280363 9857 52 3H-PGE2 -8 22 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 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 None
912 9857 52 3H-PGE2 -8 22 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 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 None
CHEMBL815 9857 52 3H-PGE2 -8 22 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 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 None
DB12789 9857 52 3H-PGE2 -8 22 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 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 None
1817 9320 68 3H-PGE1 1 12 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1936 9320 68 3H-PGE1 1 12 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
5282381 9320 68 3H-PGE1 1 12 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
CHEMBL606 9320 68 3H-PGE1 1 12 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
DB00929 9320 68 3H-PGE1 1 12 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
91798918 222842 0 3H-PGE2 -2 10 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 400 10 2 6 2.6 COC(=O)CCC=C=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
1917 7714 0 3H-PGE2 -4 9 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
5311044 7714 0 3H-PGE2 -4 9 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
631 7714 0 3H-PGE2 -4 9 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
CHEMBL160629 7714 0 3H-PGE2 -4 9 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
89077401 222823 0 3H-PGE2 -23 12 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 360 8 3 3 3.5 CC#CCC(C)C(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
1881 9853 0 3H-PGE2 -128 21 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
1891 9853 0 3H-PGE2 -128 21 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
448457 9853 0 3H-PGE2 -128 21 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
CHEMBL1235252 9853 0 3H-PGE2 -128 21 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
DB02056 9853 0 3H-PGE2 -128 21 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
None 222843 0 3H-PGE2 - 1 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 416 11 2 5 4.2 CC(CC=CC1C(CC(=O)C1CCC=CCCC(=O)OC)O)(C=CC2=CCCC2)O None
1883 9856 75 3H-PGE2 -3 24 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 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 None
1916 9856 75 3H-PGE2 -3 24 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 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 None
5280360 9856 75 3H-PGE2 -3 24 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 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 None
913 9856 75 3H-PGE2 -3 24 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 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 None
CHEMBL548 9856 75 3H-PGE2 -3 24 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 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 None
DB00917 9856 75 3H-PGE2 -3 24 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 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 None
1922 10310 38 3H-PGE1 4 3 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 331 0 2 3 3.2 CC(=O)NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2 None
4336830 10310 38 3H-PGE1 4 3 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 331 0 2 3 3.2 CC(=O)NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL112816 10310 38 3H-PGE1 4 3 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 331 0 2 3 3.2 CC(=O)NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2 None
133126726 222824 0 3H-PGE2 -2 14 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
24868263 222824 0 3H-PGE2 -2 14 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
None 222825 0 3H-PGE2 -2 3 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 350 11 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=C2)CCCCC(=O)O)O)O None
1940 8444 41 3H-PGE1 -1380 10 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
3417 8444 41 3H-PGE1 -1380 10 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
5311100 8444 41 3H-PGE1 -1380 10 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
CHEMBL1201379 8444 41 3H-PGE1 -1380 10 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
DB11519 8444 41 3H-PGE1 -1380 10 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
1817 9320 68 3H-PGE2 -1 12 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1936 9320 68 3H-PGE2 -1 12 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
5282381 9320 68 3H-PGE2 -1 12 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
CHEMBL606 9320 68 3H-PGE2 -1 12 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
DB00929 9320 68 3H-PGE2 -1 12 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1940 8444 41 3H-PGE2 -1380 10 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
3417 8444 41 3H-PGE2 -1380 10 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
5311100 8444 41 3H-PGE2 -1380 10 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
CHEMBL1201379 8444 41 3H-PGE2 -1380 10 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
DB11519 8444 41 3H-PGE2 -1380 10 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
1884 9857 52 3H-PGE1 -8 22 Bovine 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 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 None
5280363 9857 52 3H-PGE1 -8 22 Bovine 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 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 None
912 9857 52 3H-PGE1 -8 22 Bovine 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 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 None
CHEMBL815 9857 52 3H-PGE1 -8 22 Bovine 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 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 None
DB12789 9857 52 3H-PGE1 -8 22 Bovine 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 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 None
1884 9857 52 3H-PGE2 -11 22 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 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 None
5280363 9857 52 3H-PGE2 -11 22 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 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 None
912 9857 52 3H-PGE2 -11 22 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 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 None
CHEMBL815 9857 52 3H-PGE2 -11 22 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 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 None
DB12789 9857 52 3H-PGE2 -11 22 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 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 None
138 9855 88 3H-PGE2 -2 18 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
149351 9855 88 3H-PGE2 -2 18 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 9855 88 3H-PGE2 -2 18 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 9855 88 3H-PGE2 -2 18 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 9855 88 3H-PGE2 -2 18 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 9855 88 3H-PGE2 -2 18 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1883 9856 75 3H-PGE1 -3 24 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 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 None
1916 9856 75 3H-PGE1 -3 24 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 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 None
5280360 9856 75 3H-PGE1 -3 24 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 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 None
913 9856 75 3H-PGE1 -3 24 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 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 None
CHEMBL548 9856 75 3H-PGE1 -3 24 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 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 None
DB00917 9856 75 3H-PGE1 -3 24 Bovine 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 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 None
656511 224495 0 None -1 7 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 539 6 3 8 -0.2 CC1(C)S[C@@H]2[C@H](NC(=O)[C@H](NC(=O)N3CCN(C3=O)S(C)(=O)=O)C3=CC=CC=C3)C(=O)N2[C@H]1C(O)=O None
67861203 222844 0 3H-PGE2 -9 8 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 424 11 4 5 3.2 C1C(C(C(C1O)C=CC(COC2=CC(=CC=C2)Cl)O)CC=CCCCC(=O)O)O None
None 223192 0 3H-PGE2 -1318 6 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 384 9 3 3 4.3 C1CCC(CC1)C(C=CC2C(CC(C2CC=CCCCC(=O)O)Cl)O)O None
None 223193 0 3H-PGE2 -4 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 477 11 1 5 5.1 C1CC(=O)CC1CCC(=CCC(C(=O)O)N2CCOCC2)OCC3=CC=C(C=C3)C4=CC=CC=C4 None
1881 9853 0 3H-PGE2 -190 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
1891 9853 0 3H-PGE2 -190 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
448457 9853 0 3H-PGE2 -190 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
CHEMBL1235252 9853 0 3H-PGE2 -190 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
DB02056 9853 0 3H-PGE2 -190 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
None 223193 0 3H-PGE2 -4 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 477 11 1 5 5.1 C1CC(=O)CC1CCC(=CCC(C(=O)O)N2CCOCC2)OCC3=CC=C(C=C3)C4=CC=CC=C4 None
133126726 222824 0 3H-PGE1 -489 14 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
24868263 222824 0 3H-PGE1 -489 14 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
115237 62359 119 None -954 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 None -954 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 62359 119 None -954 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
5282226 224508 0 None 1 2 Human 8.3 pKi = 8.3 Binding
inhibition of [3H]AL-5848 binding to prostaglandin EP3 receptorinhibition of [3H]AL-5848 binding to prostaglandin EP3 receptor
Drug Central 500 12 3 6 4.4 CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)COC1=CC(=CC=C1)C(F)(F)F None
CHEMBL1200799 224508 0 None 1 2 Human 8.3 pKi = 8.3 Binding
inhibition of [3H]AL-5848 binding to prostaglandin EP3 receptorinhibition of [3H]AL-5848 binding to prostaglandin EP3 receptor
Drug Central 500 12 3 6 4.4 CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)COC1=CC(=CC=C1)C(F)(F)F None
DB00287 224508 0 None 1 2 Human 8.3 pKi = 8.3 Binding
inhibition of [3H]AL-5848 binding to prostaglandin EP3 receptorinhibition of [3H]AL-5848 binding to prostaglandin EP3 receptor
Drug Central 500 12 3 6 4.4 CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)COC1=CC(=CC=C1)C(F)(F)F None
2720 10626 59 None -20 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 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 None
5820 10626 59 None -20 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 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 None
6918140 10626 59 None -20 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 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 None
CHEMBL1237119 10626 59 None -20 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 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 None
DB00374 10626 59 None -20 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 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 None
133126726 222824 0 3H-PGE2 -489 14 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
24868263 222824 0 3H-PGE2 -489 14 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
1817 9320 68 3H-PGE2 1 12 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1936 9320 68 3H-PGE2 1 12 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
5282381 9320 68 3H-PGE2 1 12 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
CHEMBL606 9320 68 3H-PGE2 1 12 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
DB00929 9320 68 3H-PGE2 1 12 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
89077401 222823 0 3H-PGE2 -5 12 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 360 8 3 3 3.5 CC#CCC(C)C(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
3356 9060 73 None -131 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
4326 9060 73 None -131 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
9867642 9060 73 None -131 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
CHEMBL426559 9060 73 None -131 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
DB11629 9060 73 None -131 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP3 receptor expressed in HEK293 cellsBinding affinity to human EP3 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
69658829 224476 0 None -1 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 398 8 3 4 3.3 CC#CCC(C)[C@H](O)\C=C\[C@H]1[C@H](O)C[C@@H]2OC3=C(C=CC=C3CCCC(O)=O)[C@H]12 None
1917 7714 0 None -4 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
5311044 7714 0 None -4 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
631 7714 0 None -4 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
CHEMBL160629 7714 0 None -4 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
1917 7714 0 None -3 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
5311044 7714 0 None -3 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
631 7714 0 None -3 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
CHEMBL160629 7714 0 None -3 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
1551 9066 0 3H-PGE2 -97 7 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
1961 9066 0 3H-PGE2 -97 7 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
5311221 9066 0 3H-PGE2 -97 7 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
CHEMBL1051 9066 0 3H-PGE2 -97 7 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
DB00654 9066 0 3H-PGE2 -97 7 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
1817 9320 68 3H-PGE2 -1 12 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1936 9320 68 3H-PGE2 -1 12 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
5282381 9320 68 3H-PGE2 -1 12 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
CHEMBL606 9320 68 3H-PGE2 -1 12 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
DB00929 9320 68 3H-PGE2 -1 12 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1884 9857 52 None -7 22 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None
5280363 9857 52 None -7 22 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None
912 9857 52 None -7 22 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None
CHEMBL815 9857 52 None -7 22 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None
DB12789 9857 52 None -7 22 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None
91798918 222842 0 None -1 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 400 10 2 6 2.6 COC(=O)CCC=C=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
138107701 194243 46 None -7 15 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 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 None
5311181 194243 46 None -7 15 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 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 None
CHEMBL494 194243 46 None -7 15 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 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 None
DB01088 194243 46 None -7 15 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 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 None
1817 9320 68 3H-PGE2 -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1936 9320 68 3H-PGE2 -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
5282381 9320 68 3H-PGE2 -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
CHEMBL606 9320 68 3H-PGE2 -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
DB00929 9320 68 3H-PGE2 -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1940 8444 41 3H-PGE2 -295 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
3417 8444 41 3H-PGE2 -295 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
5311100 8444 41 3H-PGE2 -295 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
CHEMBL1201379 8444 41 3H-PGE2 -295 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
DB11519 8444 41 3H-PGE2 -295 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O None
None 222827 0 3H-PGE2 -15 2 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 442 9 1 5 5.1 CC1=C(C2=C(CC1)C(=CC=C2)OCC(=O)O)CCON=C(C3=CC=CC=C3)C4=CN=CC=C4 None
1884 9857 52 3H-PGE2 -7 22 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 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 None
5280363 9857 52 3H-PGE2 -7 22 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 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 None
912 9857 52 3H-PGE2 -7 22 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 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 None
CHEMBL815 9857 52 3H-PGE2 -7 22 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 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 None
DB12789 9857 52 3H-PGE2 -7 22 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 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 None
None 222845 0 3H-PGE2 -91 2 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 390 12 4 4 3.3 C1C(C(C(C1O)CC=CCCCC(=O)O)CCC(CCC2=CC=CC=C2)O)O None
None 222830 0 3H-PGE1 -4 4 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 587 15 3 8 4.7 C1C(C(C(C1=O)CCC=CCCC(=O)OC2=CC=C(C=C2)NC(=O)C3=CC=CC=C3)OCC(COC4=CC=CC=C4)O)O None
1817 9320 68 None -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1936 9320 68 None -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
5282381 9320 68 None -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
CHEMBL606 9320 68 None -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
DB00929 9320 68 None -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
138 9855 88 None -2 18 Mouse 8.1 pKi = 8.1 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
149351 9855 88 None -2 18 Mouse 8.1 pKi = 8.1 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 9855 88 None -2 18 Mouse 8.1 pKi = 8.1 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 9855 88 None -2 18 Mouse 8.1 pKi = 8.1 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 9855 88 None -2 18 Mouse 8.1 pKi = 8.1 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 9855 88 None -2 18 Mouse 8.1 pKi = 8.1 Binding
Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells.
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1883 9856 75 None -2 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 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 None
1916 9856 75 None -2 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 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 None
5280360 9856 75 None -2 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 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 None
913 9856 75 None -2 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 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 None
CHEMBL548 9856 75 None -2 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 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 None
DB00917 9856 75 None -2 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 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 None
1928 7105 0 3H-PGE2 3 3 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O None
5310998 7105 0 3H-PGE2 3 3 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O None
None 222846 0 3H-PGE2 1 2 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 400 9 3 4 3.4 CC1CCCCC1C(C=CC2C(CC(C2CC=CCOCC(=O)O)Cl)O)O None
134689669 222829 0 None -1 12 Mouse 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 465 12 3 7 1.7 CS(=O)(=O)NC(=O)CCCC=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
134689669 222829 0 None 1 12 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 465 12 3 7 1.7 CS(=O)(=O)NC(=O)CCCC=CCC1C(C(CC1=O)O)C=CC(COC2=CC=CC=C2)O None
1883 9856 75 None -1 24 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
Drug Central 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 None
1916 9856 75 None -1 24 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
Drug Central 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 None
5280360 9856 75 None -1 24 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
Drug Central 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 None
913 9856 75 None -1 24 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
Drug Central 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 None
CHEMBL548 9856 75 None -1 24 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
Drug Central 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 None
DB00917 9856 75 None -1 24 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
Drug Central 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 None
67861203 222844 0 3H-PGE1 -194 8 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 424 11 4 5 3.2 C1C(C(C(C1O)C=CC(COC2=CC(=CC=C2)Cl)O)CC=CCCCC(=O)O)O None
67861203 222844 0 3H-PGE2 -194 8 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 424 11 4 5 3.2 C1C(C(C(C1O)C=CC(COC2=CC(=CC=C2)Cl)O)CC=CCCCC(=O)O)O None
11296282 8191 32 None - 1 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 18632791
5822 8191 32 None - 1 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 18632791
CHEMBL565591 8191 32 None - 1 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 18632791
1888 10672 29 None -645 17 Rat 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
1974 10672 29 None -645 17 Rat 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
5311493 10672 29 None -645 17 Rat 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
CHEMBL521784 10672 29 None -645 17 Rat 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
1892 7534 20 None -186 9 Rat 4.9 pKi = 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
25886893 7534 20 None -186 9 Rat 4.9 pKi = 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
CHEMBL1628262 7534 20 None -186 9 Rat 4.9 pKi = 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
2720 10626 59 None -20 6 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22480736
5820 10626 59 None -20 6 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22480736
6918140 10626 59 None -20 6 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22480736
CHEMBL1237119 10626 59 None -20 6 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22480736
DB00374 10626 59 None -20 6 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22480736
1892 7534 20 None -26 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10634944
25886893 7534 20 None -26 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10634944
CHEMBL1628262 7534 20 None -26 9 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10634944
119461 7108 72 None -4 10 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10634944
1896 7108 72 None -4 10 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10634944
CHEMBL1317823 7108 72 None -4 10 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10634944
1933 9717 0 None -120 3 Mouse 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 14 3 7 2.9 COCc1ccccc1CC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O)O 10746663
5311230 9717 0 None -120 3 Mouse 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 14 3 7 2.9 COCc1ccccc1CC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O)O 10746663
1940 8444 41 None -295 10 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O 10634944
3417 8444 41 None -295 10 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O 10634944
5311100 8444 41 None -295 10 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O 10634944
CHEMBL1201379 8444 41 None -295 10 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O 10634944
DB11519 8444 41 None -295 10 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 11 4 5 3.6 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)C(F)(F)F)O)O 10634944
1924 10315 39 None -89 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 457 5 2 5 5.1 O=C(NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2)CCSCc1ccco1 10634944
9933831 10315 39 None -89 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 457 5 2 5 5.1 O=C(NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2)CCSCc1ccco1 10634944
CHEMBL358653 10315 39 None -89 3 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 457 5 2 5 5.1 O=C(NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2)CCSCc1ccco1 10634944
1967 7388 0 None -42 5 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 398 8 3 4 3.3 CC#CCC(C(/C=C/C1C(O)CC2C1c1cccc(c1O2)CCCC(=O)O)O)C 17545310
5282428 7388 0 None -42 5 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 398 8 3 4 3.3 CC#CCC(C(/C=C/C1C(O)CC2C1c1cccc(c1O2)CCCC(=O)O)O)C 17545310
1817 9320 68 None -1 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
1936 9320 68 None -1 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
5282381 9320 68 None -1 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
CHEMBL606 9320 68 None -1 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
DB00929 9320 68 None -1 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
1881 9853 0 None -128 21 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9313928
1891 9853 0 None -128 21 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9313928
448457 9853 0 None -128 21 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9313928
CHEMBL1235252 9853 0 None -128 21 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9313928
DB02056 9853 0 None -128 21 Mouse 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9313928
1917 7714 0 None -4 9 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 10634944
5311044 7714 0 None -4 9 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 10634944
631 7714 0 None -4 9 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 10634944
CHEMBL160629 7714 0 None -4 9 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 10634944
1884 9857 52 None -64 22 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
5280363 9857 52 None -64 22 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
912 9857 52 None -64 22 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
CHEMBL815 9857 52 None -64 22 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
DB12789 9857 52 None -64 22 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
1895 8788 0 None -10 16 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 22480736
6435378 8788 0 None -10 16 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 22480736
CHEMBL236025 8788 0 None -10 16 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 22480736
DB01088 8788 0 None -10 16 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 22480736
1917 7714 0 None -3 9 Mouse 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
5311044 7714 0 None -3 9 Mouse 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
631 7714 0 None -3 9 Mouse 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
CHEMBL160629 7714 0 None -3 9 Mouse 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
1938 8750 18 None -199 4 Mouse 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 512 11 2 4 4.6 OC(=O)CCC/C=C\C[C@H]1[C@@H]2CC[C@H]([C@@H]1/C=C/[C@H](COc1ccc(cc1)I)O)O2 9313928
5311175 8750 18 None -199 4 Mouse 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 512 11 2 4 4.6 OC(=O)CCC/C=C\C[C@H]1[C@@H]2CC[C@H]([C@@H]1/C=C/[C@H](COc1ccc(cc1)I)O)O2 9313928
CHEMBL2113346 8750 18 None -199 4 Mouse 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 512 11 2 4 4.6 OC(=O)CCC/C=C\C[C@H]1[C@@H]2CC[C@H]([C@@H]1/C=C/[C@H](COc1ccc(cc1)I)O)O2 9313928
1884 9857 52 None -7 22 Mouse 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
5280363 9857 52 None -7 22 Mouse 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
912 9857 52 None -7 22 Mouse 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
CHEMBL815 9857 52 None -7 22 Mouse 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
DB12789 9857 52 None -7 22 Mouse 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
1918 8348 0 None -6 6 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 400 10 2 6 2.6 COC(=O)CCC=C=CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
5311225 8348 0 None -6 6 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 400 10 2 6 2.6 COC(=O)CCC=C=CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
CHEMBL2104194 8348 0 None -6 6 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 400 10 2 6 2.6 COC(=O)CCC=C=CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
1937 8634 0 None -38 3 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 587 15 3 8 4.7 O[C@H](CO[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)Oc1ccc(cc1)NC(=O)c1ccccc1)COc1ccccc1 9537820
5311224 8634 0 None -38 3 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 587 15 3 8 4.7 O[C@H](CO[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)Oc1ccc(cc1)NC(=O)c1ccccc1)COc1ccccc1 9537820
1920 9711 0 None -107 4 Mouse 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 9 2 3 4.8 OC(=O)CCC/C=C\[C@H]1C2CCC([C@@H]1CNS(=O)(=O)c1ccc(cc1C)Cl)CC2 10840160
9824507 9711 0 None -107 4 Mouse 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 9 2 3 4.8 OC(=O)CCC/C=C\[C@H]1C2CCC([C@@H]1CNS(=O)(=O)c1ccc(cc1C)Cl)CC2 10840160
CHEMBL1628612 9711 0 None -107 4 Mouse 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 9 2 3 4.8 OC(=O)CCC/C=C\[C@H]1C2CCC([C@@H]1CNS(=O)(=O)c1ccc(cc1C)Cl)CC2 10840160
1895 8788 0 None -10 16 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
6435378 8788 0 None -10 16 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
CHEMBL236025 8788 0 None -10 16 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
DB01088 8788 0 None -10 16 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
1930 10106 25 None -89 3 Mouse 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
9803828 10106 25 None -89 3 Mouse 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
CHEMBL303960 10106 25 None -89 3 Mouse 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
DB16315 10106 25 None -89 3 Mouse 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
1895 8788 0 None -4 16 Rat 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
6435378 8788 0 None -4 16 Rat 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
CHEMBL236025 8788 0 None -4 16 Rat 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
DB01088 8788 0 None -4 16 Rat 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
1884 9857 52 None -11 22 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
5280363 9857 52 None -11 22 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
912 9857 52 None -11 22 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
CHEMBL815 9857 52 None -11 22 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
DB12789 9857 52 None -11 22 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
1893 7582 0 None -2 13 Mouse 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 9313928
5311242 7582 0 None -2 13 Mouse 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 9313928
CHEMBL148319 7582 0 None -2 13 Mouse 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 9313928
1934 8871 0 None -1 3 Mouse 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 11 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1CC(=C2)CCCCC(=O)O)O 9313928
5311244 8871 0 None -1 3 Mouse 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 11 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1CC(=C2)CCCCC(=O)O)O 9313928
CHEMBL4522827 8871 0 None -1 3 Mouse 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 11 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1CC(=C2)CCCCC(=O)O)O 9313928
10111831 9721 0 None -23 3 Mouse 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 3 5.0 N#Cc1ccc(c(c1)NC(=O)C(c1ccc(c2c1cccc2)F)C)CCCC(=O)O 11927615
1942 9721 0 None -23 3 Mouse 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 3 5.0 N#Cc1ccc(c(c1)NC(=O)C(c1ccc(c2c1cccc2)F)C)CCCC(=O)O 11927615
1939 10460 0 None -1 2 Mouse 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 12 2 3 5.2 CCCCC[C@H](/C=C/[C@H]1C[C@H]2C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)S2)O 9313928
5311453 10460 0 None -1 2 Mouse 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 12 2 3 5.2 CCCCC[C@H](/C=C/[C@H]1C[C@H]2C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)S2)O 9313928
1895 8788 0 None -2 16 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
6435378 8788 0 None -2 16 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
CHEMBL236025 8788 0 None -2 16 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
DB01088 8788 0 None -2 16 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
5311232 9719 13 None -7 3 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 6 2 2 5.9 O=C(C(c1cccc2c1cccc2)C)Nc1ccccc1Cc1ccccc1C(=O)O 11782353
5824 9719 13 None -7 3 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 6 2 2 5.9 O=C(C(c1cccc2c1cccc2)C)Nc1ccccc1Cc1ccccc1C(=O)O 11782353
CHEMBL3260772 9719 13 None -7 3 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 6 2 2 5.9 O=C(C(c1cccc2c1cccc2)C)Nc1ccccc1Cc1ccccc1C(=O)O 11782353
1893 7582 0 None 1 13 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 10634944
5311242 7582 0 None 1 13 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 10634944
CHEMBL148319 7582 0 None 1 13 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 10634944
1918 8348 0 None 2 6 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 400 10 2 6 2.6 COC(=O)CCC=C=CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 10634944
5311225 8348 0 None 2 6 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 400 10 2 6 2.6 COC(=O)CCC=C=CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 10634944
CHEMBL2104194 8348 0 None 2 6 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 400 10 2 6 2.6 COC(=O)CCC=C=CC[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 10634944
5821 9725 0 None - 1 Mouse 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 9 2 3 5.1 O=C(NC(c1ccccc1)c1ccccc1)CCc1cccc2c1cccc2OCC(=O)O 9863659
9867828 9725 0 None - 1 Mouse 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 9 2 3 5.1 O=C(NC(c1ccccc1)c1ccccc1)CCc1cccc2c1cccc2OCC(=O)O 9863659
1931 9720 0 None 371 2 Mouse 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 10479656
1931 9720 0 None 371 2 Mouse 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 10746663
5311229 9720 0 None 371 2 Mouse 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 10479656
5311229 9720 0 None 371 2 Mouse 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 10746663
1935 9319 0 None 3 3 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 13 3 4 3.9 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)(O)C 10634944
6436406 9319 0 None 3 3 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 13 3 4 3.9 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)(O)C 10634944
CHEMBL1201377 9319 0 None 3 3 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 13 3 4 3.9 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)(O)C 10634944
1937 8634 0 None -2 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 587 15 3 8 4.7 O[C@H](CO[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)Oc1ccc(cc1)NC(=O)c1ccccc1)COc1ccccc1 10634944
5311224 8634 0 None -2 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 587 15 3 8 4.7 O[C@H](CO[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)Oc1ccc(cc1)NC(=O)c1ccccc1)COc1ccccc1 10634944
1894 7744 41 None -1 5 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10634944
5311053 7744 41 None -1 5 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10634944
CHEMBL37853 7744 41 None -1 5 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10634944
DB11507 7744 41 None -1 5 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10634944
1912 6815 0 None -1 6 Rat 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9537820
5283068 6815 0 None -1 6 Rat 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9537820
CHEMBL1879970 6815 0 None -1 6 Rat 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9537820
11296282 8191 32 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 19486006
5822 8191 32 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 19486006
CHEMBL565591 8191 32 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 19486006
1912 6815 0 None 1 6 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9313928
5283068 6815 0 None 1 6 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9313928
CHEMBL1879970 6815 0 None 1 6 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9313928
1921 9712 0 None -10 4 Rat 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 523 10 1 5 5.8 CC(CN(S(=O)(=O)c1ccco1)c1ccc(cc1OCc1ccc(cc1)/C=C/C(=O)O)C(F)(F)F)C 9537820
9936595 9712 0 None -10 4 Rat 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 523 10 1 5 5.8 CC(CN(S(=O)(=O)c1ccco1)c1ccc(cc1OCc1ccc(cc1)/C=C/C(=O)O)C(F)(F)F)C 9537820
5844 9041 0 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 569 7 1 4 6.4 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1cc(Cl)ccc1Cc1ccc2c(c1)cccc2)Br 18287210
5844 9041 0 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 569 7 1 4 6.4 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1cc(Cl)ccc1Cc1ccc2c(c1)cccc2)Br 20973775
9808643 9041 0 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 569 7 1 4 6.4 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1cc(Cl)ccc1Cc1ccc2c(c1)cccc2)Br 18287210
9808643 9041 0 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 569 7 1 4 6.4 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1cc(Cl)ccc1Cc1ccc2c(c1)cccc2)Br 20973775
1926 6813 0 None 8 3 Mouse 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 12 3 4 3.9 CCCCC([C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O)(C)C 9313928
5283066 6813 0 None 8 3 Mouse 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 12 3 4 3.9 CCCCC([C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O)(C)C 9313928
CHEMBL1221529 6813 0 None 8 3 Mouse 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 12 3 4 3.9 CCCCC([C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O)(C)C 9313928
1937 8634 0 None 2 3 Mouse 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 587 15 3 8 4.7 O[C@H](CO[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)Oc1ccc(cc1)NC(=O)c1ccccc1)COc1ccccc1 9313928
5311224 8634 0 None 2 3 Mouse 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 587 15 3 8 4.7 O[C@H](CO[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)Oc1ccc(cc1)NC(=O)c1ccccc1)COc1ccccc1 9313928
15551229 9038 41 None 446 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 11504634
15551229 9038 41 None 446 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 18632791
15551229 9038 41 None 446 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 19486006
1941 9038 41 None 446 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 11504634
1941 9038 41 None 446 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 18632791
1941 9038 41 None 446 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 19486006
CHEMBL218071 9038 41 None 446 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 11504634
CHEMBL218071 9038 41 None 446 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 18632791
CHEMBL218071 9038 41 None 446 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 535 7 1 4 5.7 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1ccccc1Cc1ccc2c(c1)cccc2)Br 19486006
1925 6796 0 None -1 6 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
5283055 6796 0 None -1 6 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
CHEMBL3246389 6796 0 None -1 6 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
1881 9853 0 None -18 21 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
1891 9853 0 None -18 21 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
448457 9853 0 None -18 21 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
CHEMBL1235252 9853 0 None -18 21 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
DB02056 9853 0 None -18 21 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
138 9855 88 None -2 18 Mouse 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
138 9855 88 None 1 18 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
149351 9855 88 None -2 18 Mouse 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
149351 9855 88 None 1 18 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
1882 9855 88 None -2 18 Mouse 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
1882 9855 88 None 1 18 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
5280723 9855 88 None -2 18 Mouse 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
5280723 9855 88 None 1 18 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
CHEMBL495 9855 88 None -2 18 Mouse 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
CHEMBL495 9855 88 None 1 18 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
DB00770 9855 88 None -2 18 Mouse 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
DB00770 9855 88 None 1 18 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
1883 9856 75 None -1 24 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
1916 9856 75 None -1 24 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
5280360 9856 75 None -1 24 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
913 9856 75 None -1 24 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
CHEMBL548 9856 75 None -1 24 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
DB00917 9856 75 None -1 24 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9537820
1883 9856 75 None -2 24 Mouse 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
1916 9856 75 None -2 24 Mouse 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
5280360 9856 75 None -2 24 Mouse 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
913 9856 75 None -2 24 Mouse 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
CHEMBL548 9856 75 None -2 24 Mouse 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
DB00917 9856 75 None -2 24 Mouse 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 9313928
5844 9041 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 569 7 1 4 6.4 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1cc(Cl)ccc1Cc1ccc2c(c1)cccc2)Br 11504634
9808643 9041 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 569 7 1 4 6.4 COc1ccc(cc1S(=O)(=O)NC(=O)/C=C/c1cc(Cl)ccc1Cc1ccc2c(c1)cccc2)Br 11504634
1913 9242 0 None -4 15 Mouse 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 9313928
5311223 9242 0 None -4 15 Mouse 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 9313928
1919 10476 0 None -2 7 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
2538 10476 0 None -2 7 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
5312153 10476 0 None -2 7 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
CHEMBL1472830 10476 0 None -2 7 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
DB12708 10476 0 None -2 7 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9537820
1919 10476 0 None -1 7 Mouse 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9313928
2538 10476 0 None -1 7 Mouse 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9313928
5312153 10476 0 None -1 7 Mouse 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9313928
CHEMBL1472830 10476 0 None -1 7 Mouse 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9313928
DB12708 10476 0 None -1 7 Mouse 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 9313928
1919 10476 0 None 1 7 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 10634944
2538 10476 0 None 1 7 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 10634944
5312153 10476 0 None 1 7 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 10634944
CHEMBL1472830 10476 0 None 1 7 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 10634944
DB12708 10476 0 None 1 7 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 12 3 7 1.7 O=C(NS(=O)(=O)C)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](COc1ccccc1)O)O 10634944
1883 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
1916 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
5280360 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
913 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
CHEMBL548 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
DB00917 9856 75 None -1 24 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10634944
11296282 8191 32 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 18632791
5822 8191 32 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 18632791
CHEMBL565591 8191 32 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 18632791
15984632 9723 0 None 229 2 Mouse 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 531 10 2 4 7.1 CC(CC(c1cccc2c1cccc2)C(=O)Nc1cc(ccc1Cc1ccccc1C(=O)O)Cn1cccn1)C 12538661
1943 9723 0 None 229 2 Mouse 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 531 10 2 4 7.1 CC(CC(c1cccc2c1cccc2)C(=O)Nc1cc(ccc1Cc1ccccc1C(=O)O)Cn1cccn1)C 12538661
1913 9242 0 None 4 15 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 10634944
5311223 9242 0 None 4 15 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 10634944
11296282 8191 32 None - 1 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 18632791
5822 8191 32 None - 1 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 18632791
CHEMBL565591 8191 32 None - 1 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 18632791
1921 9712 0 None -31622 4 Mouse 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 523 10 1 5 5.8 CC(CN(S(=O)(=O)c1ccco1)c1ccc(cc1OCc1ccc(cc1)/C=C/C(=O)O)C(F)(F)F)C 10840160
9936595 9712 0 None -31622 4 Mouse 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 523 10 1 5 5.8 CC(CN(S(=O)(=O)c1ccco1)c1ccc(cc1OCc1ccc(cc1)/C=C/C(=O)O)C(F)(F)F)C 10840160
1551 9066 0 None -97 7 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
1961 9066 0 None -97 7 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
5311221 9066 0 None -97 7 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
CHEMBL1051 9066 0 None -97 7 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
DB00654 9066 0 None -97 7 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 432 13 3 5 4.2 O[C@@H](CCc1ccccc1)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)OC(C)C)O None
1888 10672 29 None -446 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
1974 10672 29 None -446 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
5311493 10672 29 None -446 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
CHEMBL521784 10672 29 None -446 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
1881 9853 0 None -18 21 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
1891 9853 0 None -18 21 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
448457 9853 0 None -18 21 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
CHEMBL1235252 9853 0 None -18 21 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
DB02056 9853 0 None -18 21 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
1925 6796 0 None -2 6 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
5283055 6796 0 None -2 6 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
CHEMBL3246389 6796 0 None -2 6 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820