Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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8541 2944 None 1 Human Functional pEC50 = 11 11.0 38 4
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 10.1021/acs.jmedchem.9b00336
9824353 2944 None 1 Human Functional pEC50 = 11 11.0 38 4
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 10.1021/acs.jmedchem.9b00336
CHEMBL292964 2944 None 1 Human Functional pEC50 = 11 11.0 38 4
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 10.1021/acs.jmedchem.9b00336
72948479 153122 None 0 Human Functional pEC50 = 11 11.0 512 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3975743 153122 None 0 Human Functional pEC50 = 11 11.0 512 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
90054537 148491 None 0 Human Functional pEC50 = 10.8 10.8 213 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3937596 148491 None 0 Human Functional pEC50 = 10.8 10.8 213 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
10269841 196998 None 0 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 359 11 2 3 3.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/j.bmcl.2023.129351
CHEMBL5436415 196998 None 0 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 359 11 2 3 3.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/j.bmcl.2023.129351
10291963 84742 None 0 Human Functional pEC50 = 10.7 10.7 6 4
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
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.2007.11.020
CHEMBL222715 84742 None 0 Human Functional pEC50 = 10.7 10.7 6 4
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
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.2007.11.020
1883 3082 None 47 Human Functional pEC50 = 10.7 10.7 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 3082 None 47 Human Functional pEC50 = 10.7 10.7 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 3082 None 47 Human Functional pEC50 = 10.7 10.7 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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
5280360.0 3082 None 47 Human Functional pEC50 = 10.7 10.7 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 3082 None 47 Human Functional pEC50 = 10.7 10.7 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 3082 None 47 Human Functional pEC50 = 10.7 10.7 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 3082 None 47 Human Functional pEC50 = 10.7 10.7 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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
72950089 150679 None 0 Human Functional pEC50 = 10.7 10.7 4365 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 150679 None 0 Human Functional pEC50 = 10.7 10.7 4365 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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
72949915 143420 None 0 Human Functional pEC50 = 10.6 10.6 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 451 14 2 3 4.8 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3897335 143420 None 0 Human Functional pEC50 = 10.6 10.6 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 451 14 2 3 4.8 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
44455046 95780 None 0 Human Functional pEC50 = 10.5 10.5 8317 2
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL258332 95780 None 0 Human Functional pEC50 = 10.5 10.5 8317 2
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
9821171 97919 None 0 Human Functional pEC50 = 10.5 10.5 14454 2
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL272276 97919 None 0 Human Functional pEC50 = 10.5 10.5 14454 2
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
90054482 144004 None 0 Human Functional pEC50 = 10.4 10.4 26302 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 463 10 2 4 4.4 C[C@@H](Cc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3902065 144004 None 0 Human Functional pEC50 = 10.4 10.4 26302 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 463 10 2 4 4.4 C[C@@H](Cc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
44442327 94512 None 0 Human Functional pEC50 = 10.4 10.4 891 2
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
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.2007.11.020
CHEMBL251294 94512 None 0 Human Functional pEC50 = 10.4 10.4 891 2
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
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.2007.11.020
12137443 84737 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 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 84737 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 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
92135977 152985 None 0 Human Functional pEC50 = 10.4 10.4 141 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 152985 None 0 Human Functional pEC50 = 10.4 10.4 141 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
72950425 143137 None 0 Human Functional pEC50 = 10.3 10.3 19952 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3895047 143137 None 0 Human Functional pEC50 = 10.3 10.3 19952 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
172447178 195021 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 512 14 2 5 3.7 O=C(CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1)NS(=O)(=O)Cc1ccccc1 10.1016/j.bmcl.2023.129351
CHEMBL5395111 195021 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 512 14 2 5 3.7 O=C(CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1)NS(=O)(=O)Cc1ccccc1 10.1016/j.bmcl.2023.129351
118517359 144484 None 0 Human Functional pEC50 = 10.3 10.3 79 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 144484 None 0 Human Functional pEC50 = 10.3 10.3 79 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
90054392 143005 None 0 Human Functional pEC50 = 10.2 10.2 1348962 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 519 14 2 4 6.0 C[C@@H](CCCCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3893847 143005 None 0 Human Functional pEC50 = 10.2 10.2 1348962 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 519 14 2 4 6.0 C[C@@H](CCCCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
44289922 163619 None 0 Human Functional pEC50 = 10.2 10.2 4 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 163619 None 0 Human Functional pEC50 = 10.2 10.2 4 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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
72948663 145822 None 0 Human Functional pEC50 = 10.1 10.1 2884 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3916499 145822 None 0 Human Functional pEC50 = 10.1 10.1 2884 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
12521 2197 None 0 Human Functional pEC50 = 10.1 10.1 23988 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 2197 None 0 Human Functional pEC50 = 10.1 10.1 23988 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 2197 None 0 Human Functional pEC50 = 10.1 10.1 23988 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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
44442331 94543 None 0 Human Functional pEC50 = 10 10.0 346 2
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
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 94543 None 0 Human Functional pEC50 = 10 10.0 346 2
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
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
44444720 94280 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human prostaglandin EP4 receptorAgonist activity at human prostaglandin EP4 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249953 94280 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human prostaglandin EP4 receptorAgonist activity at human prostaglandin EP4 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
8541 2944 None 1 Human Functional pEC50 = 9.9 9.9 38 4
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 10.1021/acs.jmedchem.9b00336
9824353 2944 None 1 Human Functional pEC50 = 9.9 9.9 38 4
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 10.1021/acs.jmedchem.9b00336
CHEMBL292964 2944 None 1 Human Functional pEC50 = 9.9 9.9 38 4
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 10.1021/acs.jmedchem.9b00336
90054391 142753 None 0 Human Functional pEC50 = 9.8 9.8 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 477 11 2 4 4.8 C[C@@H](CCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3891907 142753 None 0 Human Functional pEC50 = 9.8 9.8 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 477 11 2 4 4.8 C[C@@H](CCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
72949200 153866 None 0 Human Functional pEC50 = 9.8 9.8 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 385 11 2 3 3.2 CC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3982139 153866 None 0 Human Functional pEC50 = 9.8 9.8 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 385 11 2 3 3.2 CC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
10298293 94220 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human prostaglandin EP4 receptorAgonist activity at human prostaglandin EP4 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249538 94220 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human prostaglandin EP4 receptorAgonist activity at human prostaglandin EP4 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
10295421 94250 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human prostaglandin EP4 receptorAgonist activity at human prostaglandin EP4 receptor
ChEMBL 416 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249744 94250 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human prostaglandin EP4 receptorAgonist activity at human prostaglandin EP4 receptor
ChEMBL 416 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.09.074
23660680 57117 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assayAgonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 468 6 2 3 5.5 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(C(F)(F)F)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645138 57117 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assayAgonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 468 6 2 3 5.5 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(C(F)(F)F)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
11440167 84752 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 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 84752 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 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
118517485 142837 None 0 Human Functional pEC50 = 9.7 9.7 3 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 142837 None 0 Human Functional pEC50 = 9.7 9.7 3 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
118517489 143778 None 0 Human Functional pEC50 = 9.7 9.7 18 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 143778 None 0 Human Functional pEC50 = 9.7 9.7 18 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
118517359 144484 None 0 Human Functional pEC50 = 9.7 9.7 79 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 144484 None 0 Human Functional pEC50 = 9.7 9.7 79 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
118517361 153459 None 0 Human Functional pEC50 = 9.7 9.7 107 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
CHEMBL3978590 153459 None 0 Human Functional pEC50 = 9.7 9.7 107 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
118517488 153800 None 0 Human Functional pEC50 = 9.7 9.7 14 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 153800 None 0 Human Functional pEC50 = 9.7 9.7 14 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
5283056 205318 None 28 Human Functional pEC50 = 9.7 9.7 75 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O nan
CHEMBL62570 205318 None 28 Human Functional pEC50 = 9.7 9.7 75 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O nan
12521 2197 None 0 Human Functional pEC50 = 9.6 9.6 23988 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
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 nan
72722131 2197 None 0 Human Functional pEC50 = 9.6 9.6 23988 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
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 nan
CHEMBL3918816 2197 None 0 Human Functional pEC50 = 9.6 9.6 23988 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
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 nan
44455084 97920 None 0 Human Functional pEC50 = 9.5 9.5 10 2
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
ChEMBL 399 10 2 3 4.2 CCCCC1([C@@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.11.020
CHEMBL272277 97920 None 0 Human Functional pEC50 = 9.5 9.5 10 2
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
ChEMBL 399 10 2 3 4.2 CCCCC1([C@@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.11.020
118517483 144359 None 0 Human Functional pEC50 = 9.5 9.5 22 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 144359 None 0 Human Functional pEC50 = 9.5 9.5 22 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
118517490 153244 None 0 Human Functional pEC50 = 9.5 9.5 12 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 153244 None 0 Human Functional pEC50 = 9.5 9.5 12 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
72950089 150679 None 0 Human Functional pEC50 = 9.5 9.5 4365 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 150679 None 0 Human Functional pEC50 = 9.5 9.5 4365 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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
23660678 57121 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assayAgonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 556 6 2 3 6.0 C[C@H](NC(=O)c1cccc2c1N(Cc1cc(Br)cc(Br)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645142 57121 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assayAgonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 556 6 2 3 6.0 C[C@H](NC(=O)c1cccc2c1N(Cc1cc(Br)cc(Br)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
72950089 150679 None 0 Human Functional pEC50 = 9.4 9.4 4365 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3955128 150679 None 0 Human Functional pEC50 = 9.4 9.4 4365 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
90054429 153387 None 0 Human Functional pEC50 = 9.4 9.4 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 505 13 2 4 5.6 C[C@@H](CCCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3977939 153387 None 0 Human Functional pEC50 = 9.4 9.4 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 505 13 2 4 5.6 C[C@@H](CCCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
72706947 174768 None 21 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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 174768 None 21 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
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
5283086 205768 None 20 Human Functional pEC50 = 9.3 9.3 10 4
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
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 nan
CHEMBL64804 205768 None 20 Human Functional pEC50 = 9.3 9.3 10 4
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
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 nan
9934368 139008 None 11 Rat Functional pEC50 = 9.3 9.3 1 3
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL378376 139008 None 11 Rat Functional pEC50 = 9.3 9.3 1 3
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2006.01.018
10452108 94061 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 375 7 1 2 4.6 C/C(=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1)c1ccccc1 10.1016/j.bmcl.2007.05.025
CHEMBL248679 94061 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 375 7 1 2 4.6 C/C(=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1)c1ccccc1 10.1016/j.bmcl.2007.05.025
57395059 69496 None 0 Human Functional pEC50 = 9.3 9.3 11 3
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
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 69496 None 0 Human Functional pEC50 = 9.3 9.3 11 3
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
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
9934368 139008 None 11 Rat Functional pEC50 = 9.3 9.3 1 3
Agonist activity at rat EP4 receptor expressed in HEK293 cells assessed as cAMP activationAgonist activity at rat EP4 receptor expressed in HEK293 cells assessed as cAMP activation
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1021/jm9018756
CHEMBL378376 139008 None 11 Rat Functional pEC50 = 9.3 9.3 1 3
Agonist activity at rat EP4 receptor expressed in HEK293 cells assessed as cAMP activationAgonist activity at rat EP4 receptor expressed in HEK293 cells assessed as cAMP activation
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1021/jm9018756
118517453 151984 None 0 Human Functional pEC50 = 9.3 9.3 134 2
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 151984 None 0 Human Functional pEC50 = 9.3 9.3 134 2
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
1883 3082 None 47 Human Functional pEC50 = 9.2 9.2 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 3082 None 47 Human Functional pEC50 = 9.2 9.2 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 3082 None 47 Human Functional pEC50 = 9.2 9.2 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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
5280360.0 3082 None 47 Human Functional pEC50 = 9.2 9.2 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 3082 None 47 Human Functional pEC50 = 9.2 9.2 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 3082 None 47 Human Functional pEC50 = 9.2 9.2 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 3082 None 47 Human Functional pEC50 = 9.2 9.2 -1 12
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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
44409738 139693 None 0 Rat Functional pEC50 = 9.2 9.2 229 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL379746 139693 None 0 Rat Functional pEC50 = 9.2 9.2 229 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmcl.2006.01.018
57894115 75188 None 0 Rat Functional pEC50 = 9.2 9.2 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 484 14 2 6 3.7 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(OCc2ccccn2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036316 75188 None 0 Rat Functional pEC50 = 9.2 9.2 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 484 14 2 6 3.7 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(OCc2ccccn2)c1 10.1016/j.bmc.2012.04.008
72950929 146670 None 0 Human Functional pEC50 = 9.2 9.2 8912 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3923027 146670 None 0 Human Functional pEC50 = 9.2 9.2 8912 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
1883 3082 None 47 Rat Functional pEC50 = 9.2 9.2 -1 12
Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
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.2009.01.059
1916 3082 None 47 Rat Functional pEC50 = 9.2 9.2 -1 12
Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
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.2009.01.059
5280360 3082 None 47 Rat Functional pEC50 = 9.2 9.2 -1 12
Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
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.2009.01.059
5280360.0 3082 None 47 Rat Functional pEC50 = 9.2 9.2 -1 12
Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
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.2009.01.059
913 3082 None 47 Rat Functional pEC50 = 9.2 9.2 -1 12
Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
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.2009.01.059
CHEMBL548 3082 None 47 Rat Functional pEC50 = 9.2 9.2 -1 12
Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
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.2009.01.059
DB00917 3082 None 47 Rat Functional pEC50 = 9.2 9.2 -1 12
Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
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.2009.01.059
72948294 150045 None 0 Human Functional pEC50 = 9.1 9.1 1174 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 439 9 2 4 4.0 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3949856 150045 None 0 Human Functional pEC50 = 9.1 9.1 1174 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 439 9 2 4 4.0 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
56835070 69493 None 0 Rat Functional pEC50 = 9.1 9.1 112 2
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
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 69493 None 0 Rat Functional pEC50 = 9.1 9.1 112 2
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
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 69493 None 0 Rat Functional pEC50 = 9.1 9.1 112 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69493 None 0 Rat Functional pEC50 = 9.1 9.1 112 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
10322469 101566 None 16 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 101566 None 16 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
23634376 57112 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assayAgonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 434 6 2 3 5.1 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(Cl)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645133 57112 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assayAgonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as potentiation of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 434 6 2 3 5.1 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(Cl)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
118510801 151089 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 428 8 2 3 5.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc3ccccc3c2)cc1 nan
CHEMBL3958395 151089 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 428 8 2 3 5.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc3ccccc3c2)cc1 nan
92135977 152985 None 0 Human Functional pEC50 = 9 9.0 141 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 152985 None 0 Human Functional pEC50 = 9 9.0 141 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
118689427 151941 None 0 Human Functional pEC50 = 9 9.0 8 2
cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
CHEMBL3965497 151941 None 0 Human Functional pEC50 = 9 9.0 8 2
cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
9845064 69370 None 0 Rat Functional pEC50 = 9.0 9.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69370 None 0 Rat Functional pEC50 = 9.0 9.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
72950260 151248 None 0 Human Functional pEC50 = 9.0 9.0 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 437 14 2 3 4.6 O=C(O)CCCCCCN1C(=O)C(F)(F)C[C@@H]1/C=C/[C@@H](O)CCCCc1ccccc1 nan
CHEMBL3959605 151248 None 0 Human Functional pEC50 = 9.0 9.0 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 437 14 2 3 4.6 O=C(O)CCCCCCN1C(=O)C(F)(F)C[C@@H]1/C=C/[C@@H](O)CCCCc1ccccc1 nan
56834112 69369 None 0 Rat Functional pEC50 = 8.9 8.9 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 421 13 2 5 2.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929527 69369 None 0 Rat Functional pEC50 = 8.9 8.9 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 421 13 2 5 2.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
8541 2944 None 1 Rat Functional pEC50 = 8.9 8.9 -38 4
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 2944 None 1 Rat Functional pEC50 = 8.9 8.9 -38 4
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 2944 None 1 Rat Functional pEC50 = 8.9 8.9 -38 4
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
1930 3333 None 24 Mouse Functional pEC50 = 8.8 8.8 - 1
Agonist activity at mouse EP4 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at mouse EP4 receptor expressed in CHO cells assessed as cAMP production
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 3333 None 24 Mouse Functional pEC50 = 8.8 8.8 - 1
Agonist activity at mouse EP4 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at mouse EP4 receptor expressed in CHO cells assessed as cAMP production
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 3333 None 24 Mouse Functional pEC50 = 8.8 8.8 - 1
Agonist activity at mouse EP4 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at mouse EP4 receptor expressed in CHO cells assessed as cAMP production
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 3333 None 24 Mouse Functional pEC50 = 8.8 8.8 - 1
Agonist activity at mouse EP4 receptor expressed in CHO cells assessed as cAMP productionAgonist activity at mouse EP4 receptor expressed in CHO cells assessed as cAMP production
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
58932683 75313 None 0 Rat Functional pEC50 = 8.8 8.8 1995 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2037289 75313 None 0 Rat Functional pEC50 = 8.8 8.8 1995 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
8541 2944 None 1 Mouse Functional pEC50 = 8.8 8.8 -42 4
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 2944 None 1 Mouse Functional pEC50 = 8.8 8.8 -42 4
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 2944 None 1 Mouse Functional pEC50 = 8.8 8.8 -42 4
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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
44409733 140971 None 0 Rat Functional pEC50 = 8.8 8.8 114 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 401 10 2 4 3.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL382029 140971 None 0 Rat Functional pEC50 = 8.8 8.8 114 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 401 10 2 4 3.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2)s1 10.1016/j.bmcl.2006.01.018
44289922 163619 None 0 Human Functional pEC50 = 8.8 8.8 4 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 163619 None 0 Human Functional pEC50 = 8.8 8.8 4 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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
10093793 69382 None 0 Rat Functional pEC50 = 8.7 8.7 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69382 None 0 Rat Functional pEC50 = 8.7 8.7 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
11744126 69390 None 0 Rat Functional pEC50 = 8 8.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69390 None 0 Rat Functional pEC50 = 8 8.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
56839342 149095 None 0 Human Functional pEC50 = 8 8.0 1 7
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 646 13 2 7 6.0 O=C(CCc1ccc(Cl)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
CHEMBL3942394 149095 None 0 Human Functional pEC50 = 8 8.0 1 7
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 646 13 2 7 6.0 O=C(CCc1ccc(Cl)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
44304009 100790 None 0 Mouse Functional pEC50 = 8 8.0 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 100790 None 0 Mouse Functional pEC50 = 8 8.0 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
21079282 165308 None 0 Human Functional pEC50 = 8 8.0 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 435 8 1 5 4.4 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1OC)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4229001 165308 None 0 Human Functional pEC50 = 8 8.0 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 435 8 1 5 4.4 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1OC)C2 10.1016/j.bmcl.2018.03.091
44304334 204033 None 0 Mouse Functional pEC50 = 6 6.0 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 204033 None 0 Mouse Functional pEC50 = 6 6.0 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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
44304474 205389 None 0 Mouse Functional pEC50 = 6 6.0 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 205389 None 0 Mouse Functional pEC50 = 6 6.0 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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
57564500 151299 None 0 Human Functional pEC50 = 5 5.0 -63 3
Agonist activity at human recombinant EP4 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP4 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 151299 None 0 Human Functional pEC50 = 5 5.0 -63 3
Agonist activity at human recombinant EP4 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP4 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
44409920 140452 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 463 10 2 3 4.7 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL380839 140452 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 463 10 2 3 4.7 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2006.01.018
11255960 137952 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 329 11 2 4 2.3 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCC(=O)O 10.1021/jm049290a
CHEMBL376063 137952 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 329 11 2 4 2.3 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCC(=O)O 10.1021/jm049290a
10291963 84742 None 0 Human Functional pEC50 = 8.0 8.0 6 4
Functional activity at human EP4 receptorFunctional activity at human EP4 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 84742 None 0 Human Functional pEC50 = 8.0 8.0 6 4
Functional activity at human EP4 receptorFunctional activity at human EP4 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
44400307 135683 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 467 12 3 4 5.6 Cc1cc(O)ccc1-c1cccc([C@@H](O)CC[C@H]2CCCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2005.03.059
CHEMBL372926 135683 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 467 12 3 4 5.6 Cc1cc(O)ccc1-c1cccc([C@@H](O)CC[C@H]2CCCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2005.03.059
10202765 172790 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 172790 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
9981052 69375 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69375 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
44303590 205369 None 0 Mouse Functional pEC50 = 7.9 7.9 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 205369 None 0 Mouse Functional pEC50 = 7.9 7.9 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
10109445 85177 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 365 10 2 4 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)s1 10.1021/jm049290a
CHEMBL224970 85177 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 365 10 2 4 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)s1 10.1021/jm049290a
118517359 144484 None 0 Human Functional pEC50 = 7.9 7.9 79 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 144484 None 0 Human Functional pEC50 = 7.9 7.9 79 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
44289921 164466 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 164466 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
10181299 165072 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 433 9 1 4 5.2 CCCOc1c2c(c(OCCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4225442 165072 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 433 9 1 4 5.2 CCCOc1c2c(c(OCCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2 10.1016/j.bmcl.2018.03.091
67082748 164458 None 0 Human Functional pEC50 = 6.9 6.9 -338 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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 164458 None 0 Human Functional pEC50 = 6.9 6.9 -338 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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
118517454 154310 None 0 Human Functional pEC50 = 5.9 5.9 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 468 8 2 4 5.9 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2sc3ccccc3c2Cl)cc1 nan
CHEMBL3986027 154310 None 0 Human Functional pEC50 = 5.9 5.9 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 468 8 2 4 5.9 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2sc3ccccc3c2Cl)cc1 nan
10113454 177606 None 0 Rat Functional pEC50 = 7.9 7.9 28 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
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.2006.01.018
CHEMBL46395 177606 None 0 Rat Functional pEC50 = 7.9 7.9 28 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
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.2006.01.018
44290257 170343 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 451 11 3 4 5.0 Cc1cc(O)ccc1-c1cccc(C(O)/C=C/[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2004.01.063
CHEMBL444574 170343 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 451 11 3 4 5.0 Cc1cc(O)ccc1-c1cccc(C(O)/C=C/[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2004.01.063
156015440 177663 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 437 10 2 4 5.1 CCCCCC(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
CHEMBL4640391 177663 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 437 10 2 4 5.1 CCCCCC(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
57894092 75184 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 494 12 2 6 4.5 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036312 75184 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 494 12 2 6 4.5 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
57894053 75196 None 0 Rat Functional pEC50 = 7.9 7.9 208 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036324 75196 None 0 Rat Functional pEC50 = 7.9 7.9 208 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
44289968 100570 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 100570 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
11405770 137995 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 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 137995 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 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
44304403 169200 None 0 Mouse Functional pEC50 = 7.9 7.9 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 169200 None 0 Mouse Functional pEC50 = 7.9 7.9 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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
44269544 35261 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 35261 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
172443967 195304 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 677 17 3 8 4.3 Cc1nn(C)c(C)c1CC(=O)Nc1ccc(CS(=O)(=O)NC(=O)CCCCCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2023.129351
CHEMBL5400373 195304 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 677 17 3 8 4.3 Cc1nn(C)c(C)c1CC(=O)Nc1ccc(CS(=O)(=O)NC(=O)CCCCCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2023.129351
118517451 152958 None 0 Human Functional pEC50 = 6.9 6.9 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 436 8 2 5 3.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc3c(c2)OCCO3)cc1 nan
CHEMBL3974337 152958 None 0 Human Functional pEC50 = 6.9 6.9 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 436 8 2 5 3.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc3c(c2)OCCO3)cc1 nan
66978356 163803 None 0 Human Functional pEC50 = 6.8 6.8 -1698 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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 163803 None 0 Human Functional pEC50 = 6.8 6.8 -1698 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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
44290263 101384 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 453 12 3 4 5.2 Cc1cc(O)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2004.01.063
CHEMBL296715 101384 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 453 12 3 4 5.2 Cc1cc(O)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2004.01.063
9975502 94542 None 0 Human Functional pEC50 = 7.8 7.8 14 2
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
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 94542 None 0 Human Functional pEC50 = 7.8 7.8 14 2
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
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
56949974 69368 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 403 13 2 4 3.3 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929526 69368 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 403 13 2 4 3.3 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
57893982 75190 None 0 Rat Functional pEC50 = 7.8 7.8 25 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
CHEMBL2036318 75190 None 0 Rat Functional pEC50 = 7.8 7.8 25 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
57894063 75191 None 0 Rat Functional pEC50 = 7.8 7.8 301 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 524 11 2 7 4.8 COc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
CHEMBL2036319 75191 None 0 Rat Functional pEC50 = 7.8 7.8 301 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 524 11 2 7 4.8 COc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
11337782 84977 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 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 84977 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 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
118517361 153459 None 0 Human Functional pEC50 = 7.8 7.8 107 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
CHEMBL3978590 153459 None 0 Human Functional pEC50 = 7.8 7.8 107 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
156014700 177305 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 417 13 2 4 5.1 CCCCCC(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCCCCCC(=O)O 10.1016/j.bmcl.2020.127104
CHEMBL4635212 177305 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 417 13 2 4 5.1 CCCCCC(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCCCCCC(=O)O 10.1016/j.bmcl.2020.127104
10457106 69379 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69379 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
10414412 75192 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)c(C)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036320 75192 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)c(C)c1 10.1016/j.bmc.2012.04.008
44304417 204567 None 0 Mouse Functional pEC50 = 6.8 6.8 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 204567 None 0 Mouse Functional pEC50 = 6.8 6.8 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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
44289792 169265 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 169265 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
9885106 84807 None 0 Human Functional pEC50 = 7.8 7.8 -8 2
Functional activity at human EP4 receptorFunctional activity at human EP4 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 84807 None 0 Human Functional pEC50 = 7.8 7.8 -8 2
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1021/jm049290a
44409902 74772 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 377 12 3 4 3.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(O)c1 10.1016/j.bmcl.2006.01.018
CHEMBL203076 74772 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 377 12 3 4 3.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(O)c1 10.1016/j.bmcl.2006.01.018
44290271 179154 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2cccc(Cl)c2)c1 10.1016/j.bmcl.2004.01.063
CHEMBL47138 179154 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2cccc(Cl)c2)c1 10.1016/j.bmcl.2004.01.063
172449813 195946 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 631 16 3 6 5.0 O=C(CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1)NS(=O)(=O)Cc1ccc(NC(=O)c2ccccc2)cc1 10.1016/j.bmcl.2023.129351
CHEMBL5413926 195946 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 631 16 3 6 5.0 O=C(CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1)NS(=O)(=O)Cc1ccc(NC(=O)c2ccccc2)cc1 10.1016/j.bmcl.2023.129351
44304055 102778 None 0 Mouse Functional pEC50 = 6.8 6.8 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 102778 None 0 Mouse Functional pEC50 = 6.8 6.8 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
10002871 68541 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 431 12 3 4 4.4 CC(C)c1cc(C[C@H](O)/C=C/[C@H]2CCCC(=O)N2CCCCCCC(=O)O)ccc1O 10.1016/j.bmcl.2005.03.059
CHEMBL191748 68541 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 431 12 3 4 4.4 CC(C)c1cc(C[C@H](O)/C=C/[C@H]2CCCC(=O)N2CCCCCCC(=O)O)ccc1O 10.1016/j.bmcl.2005.03.059
44409742 76220 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 405 14 2 4 3.5 COCc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
CHEMBL205819 76220 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 405 14 2 4 3.5 COCc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
10092823 69373 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69373 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
118517489 143778 None 0 Human Functional pEC50 = 7.8 7.8 18 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 143778 None 0 Human Functional pEC50 = 7.8 7.8 18 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
11696697 99086 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 99086 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
10159697 136520 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 429 11 2 4 3.0 O=C(O)COCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1021/jm049290a
CHEMBL373558 136520 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 429 11 2 4 3.0 O=C(O)COCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1021/jm049290a
118517454 154310 None 0 Human Functional pEC50 = 6.7 6.7 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 468 8 2 4 5.9 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2sc3ccccc3c2Cl)cc1 nan
CHEMBL3986027 154310 None 0 Human Functional pEC50 = 6.7 6.7 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 468 8 2 4 5.9 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2sc3ccccc3c2Cl)cc1 nan
57894065 75187 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 484 14 2 6 3.7 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(OCc2cccnc2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036315 75187 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 484 14 2 6 3.7 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(OCc2cccnc2)c1 10.1016/j.bmc.2012.04.008
56839536 143256 None 0 Human Functional pEC50 = 7.7 7.7 -1 7
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 604 15 2 7 5.1 CCCCCCCCNC(=O)c1coc([C@@H]2CCCN2Cc2cc(F)ccc2CCC(=O)NS(=O)(=O)C(F)(F)F)n1 nan
CHEMBL3896035 143256 None 0 Human Functional pEC50 = 7.7 7.7 -1 7
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 604 15 2 7 5.1 CCCCCCCCNC(=O)c1coc([C@@H]2CCCN2Cc2cc(F)ccc2CCC(=O)NS(=O)(=O)C(F)(F)F)n1 nan
72706947 174768 None 21 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 174768 None 21 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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
9931112 165096 None 2 Human Functional pEC50 = 7.7 7.7 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 405 7 1 4 4.4 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4225786 165096 None 2 Human Functional pEC50 = 7.7 7.7 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 405 7 1 4 4.4 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2 10.1016/j.bmcl.2018.03.091
24945854 165109 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 433 7 1 5 4.4 CCOc1c2c(c(OCC)c3cc(C)ccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2=O 10.1016/j.bmcl.2018.03.091
CHEMBL4225963 165109 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 433 7 1 5 4.4 CCOc1c2c(c(OCC)c3cc(C)ccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2=O 10.1016/j.bmcl.2018.03.091
9907375 68301 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 369 12 2 4 3.1 O=C(O)CCCSCCN1C(=O)CCC[C@@H]1/C=C/[C@@H](O)CCC1CC1 10.1016/j.bmcl.2005.03.059
CHEMBL191627 68301 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 369 12 2 4 3.1 O=C(O)CCCSCCN1C(=O)CCC[C@@H]1/C=C/[C@@H](O)CCC1CC1 10.1016/j.bmcl.2005.03.059
127052614 140313 None 0 Human Functional pEC50 = 5.7 5.7 -489 6
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 415 7 2 6 4.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805176 140313 None 0 Human Functional pEC50 = 5.7 5.7 -489 6
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
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
44409712 77369 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 437 13 2 3 5.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2006.01.018
CHEMBL208399 77369 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 437 13 2 3 5.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2006.01.018
90054519 152075 None 0 Human Functional pEC50 = 6.7 6.7 3 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 477 11 2 4 4.8 C[C@@H](CCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3966743 152075 None 0 Human Functional pEC50 = 6.7 6.7 3 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 477 11 2 4 4.8 C[C@@H](CCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
10276417 165198 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 461 11 1 4 6.0 CCCCOc1c2c(c(OCCCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4227243 165198 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 461 11 1 4 6.0 CCCCOc1c2c(c(OCCCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2 10.1016/j.bmcl.2018.03.091
21079296 165294 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 391 5 1 5 3.3 COc1c2c(c(OC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2=O 10.1016/j.bmcl.2018.03.091
CHEMBL4228762 165294 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 391 5 1 5 3.3 COc1c2c(c(OC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2=O 10.1016/j.bmcl.2018.03.091
44442332 94580 None 0 Human Functional pEC50 = 8.7 8.7 97 2
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 341 9 1 2 4.2 CCCC/C=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251709 94580 None 0 Human Functional pEC50 = 8.7 8.7 97 2
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 341 9 1 2 4.2 CCCC/C=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
9885106 84807 None 0 Rat Functional pEC50 = 8.7 8.7 8 2
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
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 84807 None 0 Rat Functional pEC50 = 8.7 8.7 8 2
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
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
118517360 144062 None 0 Human Functional pEC50 = 8.7 8.7 61 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 412 8 2 3 4.7 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Cl)c2)cc1 nan
CHEMBL3902700 144062 None 0 Human Functional pEC50 = 8.7 8.7 61 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 412 8 2 3 4.7 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Cl)c2)cc1 nan
118517484 146180 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 458 9 2 4 5.2 COc1ccc2ccc(CC(O)/C=C/[C@H]3CCC(=O)[C@@H]3CCc3ccc(C(=O)O)cc3)cc2c1 nan
CHEMBL3919302 146180 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 458 9 2 4 5.2 COc1ccc2ccc(CC(O)/C=C/[C@H]3CCC(=O)[C@@H]3CCc3ccc(C(=O)O)cc3)cc2c1 nan
57893848 75195 None 0 Rat Functional pEC50 = 8.7 8.7 724 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036323 75195 None 0 Rat Functional pEC50 = 8.7 8.7 724 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
44409917 139337 None 0 Rat Functional pEC50 = 8.6 8.6 102 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(F)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL378968 139337 None 0 Rat Functional pEC50 = 8.6 8.6 102 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(F)c2)s1 10.1016/j.bmcl.2006.01.018
11743927 69386 None 0 Rat Functional pEC50 = 8.6 8.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 439 13 2 6 3.4 COCc1cccc(C[C@H](O)/C=C/[C@H]2CSC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929544 69386 None 0 Rat Functional pEC50 = 8.6 8.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 439 13 2 6 3.4 COCc1cccc(C[C@H](O)/C=C/[C@H]2CSC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
5859 3767 None 24 Human Functional pEC50 = 8.6 8.6 - 1
EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptorEP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptor
ChEMBL 383 11 2 5 2.5 O[C@@H](Cc1ccccc1)/C=C/[C@H]1CCC(=O)N1CCCCCCc1nnn[nH]1 10.1016/s0960-894x(03)00042-8
9864831 3767 None 24 Human Functional pEC50 = 8.6 8.6 - 1
EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptorEP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptor
ChEMBL 383 11 2 5 2.5 O[C@@H](Cc1ccccc1)/C=C/[C@H]1CCC(=O)N1CCCCCCc1nnn[nH]1 10.1016/s0960-894x(03)00042-8
CHEMBL275667 3767 None 24 Human Functional pEC50 = 8.6 8.6 - 1
EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptorEP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptor
ChEMBL 383 11 2 5 2.5 O[C@@H](Cc1ccccc1)/C=C/[C@H]1CCC(=O)N1CCCCCCc1nnn[nH]1 10.1016/s0960-894x(03)00042-8
138 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
149351 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
149351.0 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
1882 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
5280723 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
5280723.0 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
CHEMBL495 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
DB00770 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
138 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
149351.0 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
5280723.0 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 3081 None 57 Mouse Functional pEC50 = 8.6 8.6 -1 10
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
10367369 205705 None 0 Mouse Functional pEC50 = 8.6 8.6 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 205705 None 0 Mouse Functional pEC50 = 8.6 8.6 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
10113129 69338 None 0 Rabbit Functional pEC50 = 8.6 8.6 - 1
Agonist activity at rabbit EP4 receptor assessed as relaxation of Kcl-induced tissue contraction by isometric transducer methodAgonist activity at rabbit EP4 receptor assessed as relaxation of Kcl-induced tissue contraction by isometric transducer method
ChEMBL 424 7 3 6 3.1 O[C@H](/C=C/[C@@H]1[C@H]2c3cccc(CCc4nnn[nH]4)c3O[C@H]2C[C@H]1O)CC1CCCCC1 10.1016/j.bmcl.2011.09.004
CHEMBL1928220 69338 None 0 Rabbit Functional pEC50 = 8.6 8.6 - 1
Agonist activity at rabbit EP4 receptor assessed as relaxation of Kcl-induced tissue contraction by isometric transducer methodAgonist activity at rabbit EP4 receptor assessed as relaxation of Kcl-induced tissue contraction by isometric transducer method
ChEMBL 424 7 3 6 3.1 O[C@H](/C=C/[C@@H]1[C@H]2c3cccc(CCc4nnn[nH]4)c3O[C@H]2C[C@H]1O)CC1CCCCC1 10.1016/j.bmcl.2011.09.004
12521 2197 None 0 Human Functional pEC50 = 8.6 8.6 23988 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 2197 None 0 Human Functional pEC50 = 8.6 8.6 23988 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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 2197 None 0 Human Functional pEC50 = 8.6 8.6 23988 2
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
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
10410111 102896 None 0 Mouse Functional pEC50 = 8.6 8.6 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 102896 None 0 Mouse Functional pEC50 = 8.6 8.6 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
10181504 195836 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 436 12 2 5 2.2 CS(=O)(=O)NC(=O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/j.bmcl.2023.129351
CHEMBL5411667 195836 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 436 12 2 5 2.2 CS(=O)(=O)NC(=O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/j.bmcl.2023.129351
9910141 100929 None 0 Mouse Functional pEC50 = 7.7 7.7 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 100929 None 0 Mouse Functional pEC50 = 7.7 7.7 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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
44290267 162289 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 162289 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
44409910 140996 None 0 Rat Functional pEC50 = 6.7 6.7 1 4
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
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 140996 None 0 Rat Functional pEC50 = 6.7 6.7 1 4
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
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
10089562 154511 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
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
CHEMBL398948 154511 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
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
10481859 75193 None 0 Rat Functional pEC50 = 7.7 7.7 67 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
CHEMBL2036321 75193 None 0 Rat Functional pEC50 = 7.7 7.7 67 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
118510801 151089 None 0 Human Functional pEC50 = 7.7 7.7 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 428 8 2 3 5.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc3ccccc3c2)cc1 nan
CHEMBL3958395 151089 None 0 Human Functional pEC50 = 7.7 7.7 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 428 8 2 3 5.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc3ccccc3c2)cc1 nan
118517490 153244 None 0 Human Functional pEC50 = 7.7 7.7 12 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 153244 None 0 Human Functional pEC50 = 7.7 7.7 12 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
10268898 84598 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 341 13 2 4 2.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCOCC(=O)O 10.1021/jm049290a
CHEMBL222085 84598 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 341 13 2 4 2.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCOCC(=O)O 10.1021/jm049290a
24771583 68665 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 465 12 2 4 5.7 Cc1cc(O)ccc1-c1cccc(C(=O)CC[C@H]2CCCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2005.03.059
CHEMBL191874 68665 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 465 12 2 4 5.7 Cc1cc(O)ccc1-c1cccc(C(=O)CC[C@H]2CCCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2005.03.059
44409907 77078 None 0 Rat Functional pEC50 = 7.7 7.7 30 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2ccc(F)cc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL207237 77078 None 0 Rat Functional pEC50 = 7.7 7.7 30 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2ccc(F)cc2)s1 10.1016/j.bmcl.2006.01.018
11955293 149929 None 0 Human Functional pEC50 = 4.7 4.7 -1 2
Agonist activity at human recombinant EP4 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP4 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 8 2 4 4.3 COC(=O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3O)[C@H](O)C[C@H]1Cl nan
CHEMBL3948932 149929 None 0 Human Functional pEC50 = 4.7 4.7 -1 2
Agonist activity at human recombinant EP4 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP4 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 8 2 4 4.3 COC(=O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3O)[C@H](O)C[C@H]1Cl nan
11338951 69377 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69377 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
10410053 69380 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 423 13 2 6 2.7 COCc1cccc(C[C@H](O)/C=C/[C@H]2COC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929538 69380 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 423 13 2 6 2.7 COCc1cccc(C[C@H](O)/C=C/[C@H]2COC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
10223809 165038 None 5 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 419 7 1 5 4.1 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2=O 10.1016/j.bmcl.2018.03.091
CHEMBL4224936 165038 None 5 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 419 7 1 5 4.1 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2=O 10.1016/j.bmcl.2018.03.091
21079276 165176 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 391 7 1 4 4.8 CCOc1c2c(c(OCC)c3ccccc13)CN(c1ccc(CC(=O)O)cc1)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4226984 165176 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 391 7 1 4 4.8 CCOc1c2c(c(OCC)c3ccccc13)CN(c1ccc(CC(=O)O)cc1)C2 10.1016/j.bmcl.2018.03.091
67082722 164723 None 0 Human Functional pEC50 = 5.6 5.6 -380 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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 164723 None 0 Human Functional pEC50 = 5.6 5.6 -380 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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
10000670 69391 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69391 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
145971909 164795 None 0 Human Functional pEC50 = 7.6 7.6 -389 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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 164795 None 0 Human Functional pEC50 = 7.6 7.6 -389 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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
44400318 69212 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 417 11 2 4 3.6 O=C(O)CCCSCCN1C(=O)CCC[C@@H]1/C=C/C(O)C1(c2ccccc2)CC1 10.1016/j.bmcl.2005.03.059
CHEMBL192655 69212 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 417 11 2 4 3.6 O=C(O)CCCSCCN1C(=O)CCC[C@@H]1/C=C/C(O)C1(c2ccccc2)CC1 10.1016/j.bmcl.2005.03.059
145977227 164102 None 0 Human Functional pEC50 = 5.6 5.6 -2630 4
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 437 10 2 6 5.2 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CC1CCCC1 10.1016/j.bmc.2017.11.035
CHEMBL4208379 164102 None 0 Human Functional pEC50 = 5.6 5.6 -2630 4
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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
57384034 71331 None 0 Rat Functional pEC50 = 7.6 7.6 9 2
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957436 71331 None 0 Rat Functional pEC50 = 7.6 7.6 9 2
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.02.018
10319835 69389 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69389 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
57384034 71331 None 0 Rat Functional pEC50 = 7.6 7.6 9 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957436 71331 None 0 Rat Functional pEC50 = 7.6 7.6 9 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.04.008
9867899 205582 None 0 Mouse Functional pEC50 = 6.6 6.6 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 205582 None 0 Mouse Functional pEC50 = 6.6 6.6 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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
44304034 203050 None 0 Mouse Functional pEC50 = 6.6 6.6 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 203050 None 0 Mouse Functional pEC50 = 6.6 6.6 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
44409693 166193 None 0 Rat Functional pEC50 = 6.6 6.6 6 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 429 11 2 4 4.3 CCc1ccc(CC(O)CC[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL425950 166193 None 0 Rat Functional pEC50 = 6.6 6.6 6 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 429 11 2 4 4.3 CCc1ccc(CC(O)CC[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)cc1 10.1016/j.bmcl.2006.01.018
10269242 155665 None 0 Human Functional pEC50 = 6.6 6.6 54 2
Agonist activity at human prostaglandin EP4 receptorAgonist activity at human prostaglandin EP4 receptor
ChEMBL 348 9 2 4 2.2 CC(C)CC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL404413 155665 None 0 Human Functional pEC50 = 6.6 6.6 54 2
Agonist activity at human prostaglandin EP4 receptorAgonist activity at human prostaglandin EP4 receptor
ChEMBL 348 9 2 4 2.2 CC(C)CC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
57894108 75182 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 494 12 2 5 4.3 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(N2Cc3ccccc3C2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036310 75182 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 494 12 2 5 4.3 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(N2Cc3ccccc3C2)c1 10.1016/j.bmc.2012.04.008
58932678 75314 None 0 Rat Functional pEC50 = 7.6 7.6 301 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
CHEMBL2037290 75314 None 0 Rat Functional pEC50 = 7.6 7.6 301 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
24771582 69527 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 403 11 3 4 3.6 Cc1cc(C[C@H](O)/C=C/[C@H]2CCCC(=O)N2CCCCCCC(=O)O)ccc1O 10.1016/j.bmcl.2005.03.059
CHEMBL193405 69527 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 403 11 3 4 3.6 Cc1cc(C[C@H](O)/C=C/[C@H]2CCCC(=O)N2CCCCCCC(=O)O)ccc1O 10.1016/j.bmcl.2005.03.059
156010583 177183 None 0 Human Functional pEC50 = 7.5 7.5 162 2
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 451 10 2 4 5.4 CCCCCC(C)(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
CHEMBL4633041 177183 None 0 Human Functional pEC50 = 7.5 7.5 162 2
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 451 10 2 4 5.4 CCCCCC(C)(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
10384865 69387 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69387 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
10069539 68650 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 399 13 2 4 4.1 CCCCC(C)(C)C(O)/C=C/[C@H]1CCCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmcl.2005.03.059
CHEMBL191790 68650 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 399 13 2 4 4.1 CCCCC(C)(C)C(O)/C=C/[C@H]1CCCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmcl.2005.03.059
172453672 195767 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 498 13 2 5 3.6 O=C(CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2023.129351
CHEMBL5410348 195767 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at EP4 (unknown origin) assessed as increase in calcium fluxAgonist activity at EP4 (unknown origin) assessed as increase in calcium flux
ChEMBL 498 13 2 5 3.6 O=C(CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1ccccc1)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2023.129351
44442334 94581 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 327 7 1 2 3.8 CC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251710 94581 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 327 7 1 2 3.8 CC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
1883 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
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 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
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 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
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
5280360.0 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
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 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
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 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
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 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
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
44455115 95615 None 0 Human Functional pEC50 = 8.5 8.5 6 2
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
ChEMBL 387 10 2 3 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL257658 95615 None 0 Human Functional pEC50 = 8.5 8.5 6 2
Agonist activity at human EP4 receptor by cAMP assayAgonist activity at human EP4 receptor by cAMP assay
ChEMBL 387 10 2 3 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
1883 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptorEP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 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/s0960-894x(03)00042-8
1916 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptorEP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 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/s0960-894x(03)00042-8
5280360 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptorEP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 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/s0960-894x(03)00042-8
5280360.0 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptorEP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 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/s0960-894x(03)00042-8
913 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptorEP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 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/s0960-894x(03)00042-8
CHEMBL548 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptorEP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 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/s0960-894x(03)00042-8
DB00917 3082 None 47 Human Functional pEC50 = 8.5 8.5 -1 12
EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptorEP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 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/s0960-894x(03)00042-8
10291963 84742 None 0 Rat Functional pEC50 = 8.5 8.5 -6 4
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
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 84742 None 0 Rat Functional pEC50 = 8.5 8.5 -6 4
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
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
9846782 100959 None 6 Mouse Functional pEC50 = 8.5 8.5 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 100959 None 6 Mouse Functional pEC50 = 8.5 8.5 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
72948479 153122 None 0 Human Functional pEC50 = 8.5 8.5 512 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3975743 153122 None 0 Human Functional pEC50 = 8.5 8.5 512 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
57893891 75185 None 0 Rat Functional pEC50 = 8.5 8.5 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 510 12 2 6 5.0 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3s2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036313 75185 None 0 Rat Functional pEC50 = 8.5 8.5 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 510 12 2 6 5.0 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3s2)c1 10.1016/j.bmc.2012.04.008
44304404 100635 None 0 Mouse Functional pEC50 = 8.5 8.5 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 100635 None 0 Mouse Functional pEC50 = 8.5 8.5 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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
1883 3082 None 47 Rat Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 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.bmc.2012.02.018
1916 3082 None 47 Rat Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 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.bmc.2012.02.018
5280360 3082 None 47 Rat Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 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.bmc.2012.02.018
5280360.0 3082 None 47 Rat Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 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.bmc.2012.02.018
913 3082 None 47 Rat Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 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.bmc.2012.02.018
CHEMBL548 3082 None 47 Rat Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 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.bmc.2012.02.018
DB00917 3082 None 47 Rat Functional pEC50 = 8.5 8.5 -1 12
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 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.bmc.2012.02.018
138 3081 None 57 Mouse Functional pEC50 = 8.4 8.4 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
149351 3081 None 57 Mouse Functional pEC50 = 8.4 8.4 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
149351.0 3081 None 57 Mouse Functional pEC50 = 8.4 8.4 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
1882 3081 None 57 Mouse Functional pEC50 = 8.4 8.4 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
5280723 3081 None 57 Mouse Functional pEC50 = 8.4 8.4 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
5280723.0 3081 None 57 Mouse Functional pEC50 = 8.4 8.4 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
CHEMBL495 3081 None 57 Mouse Functional pEC50 = 8.4 8.4 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
DB00770 3081 None 57 Mouse Functional pEC50 = 8.4 8.4 -1 10
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
44304388 205610 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 205610 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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
13231966 101005 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
CHEMBL294108 101005 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 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)00365-1
13231966 101005 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 101005 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
24739203 165057 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 423 7 1 4 4.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1F)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4225243 165057 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 423 7 1 4 4.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1F)C2 10.1016/j.bmcl.2018.03.091
118517488 153800 None 0 Human Functional pEC50 = 7.5 7.5 14 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 153800 None 0 Human Functional pEC50 = 7.5 7.5 14 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
44304051 102815 None 0 Mouse Functional pEC50 = 7.5 7.5 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 102815 None 0 Mouse Functional pEC50 = 7.5 7.5 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
9820333 75397 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 361 12 2 3 3.4 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CCC(O)Cc1ccccc1 10.1016/j.bmcl.2006.01.018
CHEMBL203780 75397 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 361 12 2 3 3.4 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CCC(O)Cc1ccccc1 10.1016/j.bmcl.2006.01.018
127052613 140293 None 0 Human Functional pEC50 = 7.5 7.5 -41 6
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 431 7 3 7 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/[C@@H](O)COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3804978 140293 None 0 Human Functional pEC50 = 7.5 7.5 -41 6
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 431 7 3 7 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/[C@@H](O)COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
10023506 69372 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69372 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
66857988 164217 None 0 Human Functional pEC50 = 5.5 5.5 -1621 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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 164217 None 0 Human Functional pEC50 = 5.5 5.5 -1621 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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
11294085 137339 None 0 Human Functional pEC50 = 6.5 6.5 -186 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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 137339 None 0 Human Functional pEC50 = 6.5 6.5 -186 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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
10000048 135631 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 383 12 2 4 3.5 O=C(O)CCCSCCN1C(=O)CCC[C@@H]1/C=C/[C@@H](O)CCC1CCC1 10.1016/j.bmcl.2005.03.059
CHEMBL372894 135631 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 383 12 2 4 3.5 O=C(O)CCCSCCN1C(=O)CCC[C@@H]1/C=C/[C@@H](O)CCC1CCC1 10.1016/j.bmcl.2005.03.059
44304008 205700 None 0 Mouse Functional pEC50 = 7.5 7.5 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 205700 None 0 Mouse Functional pEC50 = 7.5 7.5 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
10046356 69376 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69376 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
10362346 69371 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69371 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
44290312 179026 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 421 11 2 3 5.0 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.063
CHEMBL47018 179026 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 421 11 2 3 5.0 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.063
156020398 178207 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 505 13 2 4 5.4 CCCCCC(O)/C=C/c1c(Br)cc(Br)c(=O)n1CCCCCCC(=O)O 10.1016/j.bmcl.2020.127104
CHEMBL4647921 178207 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 505 13 2 4 5.4 CCCCCC(O)/C=C/c1c(Br)cc(Br)c(=O)n1CCCCCCC(=O)O 10.1016/j.bmcl.2020.127104
56839343 144367 None 0 Human Functional pEC50 = 7.4 7.4 1 6
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 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 144367 None 0 Human Functional pEC50 = 7.4 7.4 1 6
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 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
44304052 205395 None 0 Mouse Functional pEC50 = 7.4 7.4 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 205395 None 0 Mouse Functional pEC50 = 7.4 7.4 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
56649302 152755 None 0 Human Functional pEC50 = 7.4 7.4 1 6
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 630 13 2 7 5.5 O=C(CCc1ccc(F)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
CHEMBL3972583 152755 None 0 Human Functional pEC50 = 7.4 7.4 1 6
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 630 13 2 7 5.5 O=C(CCc1ccc(F)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
118517485 142837 None 0 Human Functional pEC50 = 7.4 7.4 3 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 142837 None 0 Human Functional pEC50 = 7.4 7.4 3 4
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
10113722 165152 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 433 7 1 4 5.2 CC(C)Oc1c2c(c(OC(C)C)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4226523 165152 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 433 7 1 4 5.2 CC(C)Oc1c2c(c(OC(C)C)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2 10.1016/j.bmcl.2018.03.091
16678098 165313 None 22 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 423 7 1 4 4.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)c(F)c1)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4229058 165313 None 22 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 423 7 1 4 4.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)c(F)c1)C2 10.1016/j.bmcl.2018.03.091
10448293 154510 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 313 6 1 2 3.4 CC(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL398947 154510 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP4 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 313 6 1 2 3.4 CC(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
118517483 144359 None 0 Human Functional pEC50 = 8.4 8.4 22 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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 144359 None 0 Human Functional pEC50 = 8.4 8.4 22 3
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
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
10004602 69384 None 0 Rat Functional pEC50 = 8.4 8.4 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69384 None 0 Rat Functional pEC50 = 8.4 8.4 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
9886718 205621 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 205621 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
10363310 69381 None 0 Rat Functional pEC50 = 8.3 8.3 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69381 None 0 Rat Functional pEC50 = 8.3 8.3 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
44303709 205658 None 0 Mouse Functional pEC50 = 8.3 8.3 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 205658 None 0 Mouse Functional pEC50 = 8.3 8.3 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
156014791 177689 None 0 Human Functional pEC50 = 8.3 8.3 309 2
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 439 11 2 4 5.0 CCCCCC(O)CCc1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
CHEMBL4640635 177689 None 0 Human Functional pEC50 = 8.3 8.3 309 2
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 439 11 2 4 5.0 CCCCCC(O)CCc1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
10348006 75316 None 0 Rat Functional pEC50 = 8.3 8.3 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 569 10 2 8 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2037292 75316 None 0 Rat Functional pEC50 = 8.3 8.3 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 569 10 2 8 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
44409918 166068 None 0 Rat Functional pEC50 = 7.4 7.4 1 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc(Cl)cc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL425243 166068 None 0 Rat Functional pEC50 = 7.4 7.4 1 2
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc(Cl)cc2)s1 10.1016/j.bmcl.2006.01.018
44290272 101498 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2Cl)c1 10.1016/j.bmcl.2004.01.063
CHEMBL297578 101498 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2Cl)c1 10.1016/j.bmcl.2004.01.063
44290314 174078 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 174078 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
44304258 102411 None 0 Mouse Functional pEC50 = 6.4 6.4 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 102411 None 0 Mouse Functional pEC50 = 6.4 6.4 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
44290316 162276 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 421 11 2 3 5.0 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.01.063
CHEMBL416254 162276 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 421 11 2 3 5.0 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.01.063
11339406 141421 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 429 10 2 3 4.3 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL383515 141421 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 429 10 2 3 4.3 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2006.01.018
44304335 205436 None 0 Mouse Functional pEC50 = 7.4 7.4 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 205436 None 0 Mouse Functional pEC50 = 7.4 7.4 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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
10003118 135300 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 435 13 2 5 3.3 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmcl.2005.03.059
CHEMBL372436 135300 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 435 13 2 5 3.3 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmcl.2005.03.059
11742697 161812 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 417 13 2 4 3.7 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2005.03.059
CHEMBL413563 161812 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 417 13 2 4 3.7 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2005.03.059
44303710 102371 None 0 Mouse Functional pEC50 = 7.4 7.4 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptor
ChEMBL 482 15 3 7 3.0 COCCCc1cccc(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
CHEMBL303532 102371 None 0 Mouse Functional pEC50 = 7.4 7.4 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptor
ChEMBL 482 15 3 7 3.0 COCCCc1cccc(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
11351910 77372 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 471 11 2 3 5.4 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL208411 77372 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 471 11 2 3 5.4 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.018
57390636 69378 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 455 12 2 5 4.2 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccccc2)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929536 69378 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 455 12 2 5 4.2 O=C(O)CCCSCCN1C(=O)OC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccccc2)c1 10.1016/j.bmc.2011.12.009
57893957 75189 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 484 14 2 6 3.7 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(OCc2ccncc2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036317 75189 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 484 14 2 6 3.7 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(OCc2ccncc2)c1 10.1016/j.bmc.2012.04.008
44304389 205611 None 0 Mouse Functional pEC50 = 7.3 7.3 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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 205611 None 0 Mouse Functional pEC50 = 7.3 7.3 - 1
Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptorEffective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor
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
10113454 177606 None 0 Human Functional pEC50 = 6.3 6.3 -28 2
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 177606 None 0 Human Functional pEC50 = 6.3 6.3 -28 2
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
69753740 140309 None 0 Human Functional pEC50 = 5.3 5.3 -1258 5
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
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.5b00455
CHEMBL3805134 140309 None 0 Human Functional pEC50 = 5.3 5.3 -1258 5
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
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.5b00455
57396660 71332 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957437 71332 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.02.018
57396660 71332 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957437 71332 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.04.008
9863804 94151 None 0 Human Functional pEC50 = 8.3 8.3 120 2
Agonist activity at human prostaglandin EP4 receptorAgonist activity at human prostaglandin EP4 receptor
ChEMBL 362 11 2 4 2.7 CCCCCC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249136 94151 None 0 Human Functional pEC50 = 8.3 8.3 120 2
Agonist activity at human prostaglandin EP4 receptorAgonist activity at human prostaglandin EP4 receptor
ChEMBL 362 11 2 4 2.7 CCCCCC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
21079275 165218 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 439 7 1 4 5.1 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1Cl)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4227555 165218 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 439 7 1 4 5.1 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1Cl)C2 10.1016/j.bmcl.2018.03.091
21079274 165252 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 483 7 1 4 5.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1Br)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4228070 165252 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 483 7 1 4 5.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1Br)C2 10.1016/j.bmcl.2018.03.091
90054462 145110 None 0 Human Functional pEC50 = 8.3 8.3 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 477 10 1 5 4.5 COC(=O)c1ccc(CCCN2C(=O)C(F)(F)C[C@@H]2/C=C/[C@@H](O)[C@@H](C)Cc2ccccc2)s1 nan
CHEMBL3911081 145110 None 0 Human Functional pEC50 = 8.3 8.3 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 477 10 1 5 4.5 COC(=O)c1ccc(CCCN2C(=O)C(F)(F)C[C@@H]2/C=C/[C@@H](O)[C@@H](C)Cc2ccccc2)s1 nan
57464006 75194 None 0 Rat Functional pEC50 = 8.3 8.3 288 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 75194 None 0 Rat Functional pEC50 = 8.3 8.3 288 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
90054537 148491 None 0 Human Functional pEC50 = 8.3 8.3 213 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3937596 148491 None 0 Human Functional pEC50 = 8.3 8.3 213 2
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
9865732 69339 None 0 Rabbit Functional pEC50 = 8.2 8.2 - 1
Agonist activity at rabbit EP4 receptor assessed as relaxation of Kcl-induced tissue contraction by isometric transducer methodAgonist activity at rabbit EP4 receptor assessed as relaxation of Kcl-induced tissue contraction by isometric transducer method
ChEMBL 400 7 3 4 3.8 O=C(O)CCc1cccc2c1O[C@H]1C[C@@H](O)[C@H](/C=C/[C@@H](O)CC3CCCCC3)[C@@H]21 10.1016/j.bmcl.2011.09.004
CHEMBL1928221 69339 None 0 Rabbit Functional pEC50 = 8.2 8.2 - 1
Agonist activity at rabbit EP4 receptor assessed as relaxation of Kcl-induced tissue contraction by isometric transducer methodAgonist activity at rabbit EP4 receptor assessed as relaxation of Kcl-induced tissue contraction by isometric transducer method
ChEMBL 400 7 3 4 3.8 O=C(O)CCc1cccc2c1O[C@H]1C[C@@H](O)[C@H](/C=C/[C@@H](O)CC3CCCCC3)[C@@H]21 10.1016/j.bmcl.2011.09.004
10001791 69385 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69385 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
12002526 69488 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69488 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
11339240 84762 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 423 10 2 4 3.2 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
CHEMBL222834 84762 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 423 10 2 4 3.2 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
44409717 77386 None 1 Rat Functional pEC50 = 7.3 7.3 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 445 13 2 4 4.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2006.01.018
CHEMBL208510 77386 None 1 Rat Functional pEC50 = 7.3 7.3 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 445 13 2 4 4.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2006.01.018
44290262 178624 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.01.063
CHEMBL46671 178624 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.01.063
24944617 165025 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 473 7 1 4 5.4 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1C(F)(F)F)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4224711 165025 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 473 7 1 4 5.4 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1C(F)(F)F)C2 10.1016/j.bmcl.2018.03.091
90054387 149988 None 0 Human Functional pEC50 = 7.3 7.3 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 505 12 1 5 5.3 COC(=O)c1ccc(CCCN2C(=O)C(F)(F)C[C@@H]2/C=C/[C@H](O)[C@@H](C)CCCc2ccccc2)s1 nan
CHEMBL3949313 149988 None 0 Human Functional pEC50 = 7.3 7.3 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 505 12 1 5 5.3 COC(=O)c1ccc(CCCN2C(=O)C(F)(F)C[C@@H]2/C=C/[C@H](O)[C@@H](C)CCCc2ccccc2)s1 nan
44409737 77371 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 451 10 2 4 4.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc3ccccc3c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL208410 77371 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 451 10 2 4 4.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc3ccccc3c2)s1 10.1016/j.bmcl.2006.01.018
44289977 162854 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 413 10 2 3 4.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
CHEMBL417171 162854 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 413 10 2 3 4.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
10026946 75179 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 453 12 2 4 4.4 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccccc2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036307 75179 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 453 12 2 4 4.4 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccccc2)c1 10.1016/j.bmc.2012.04.008
156022045 178305 None 0 Human Functional pEC50 = 6.3 6.3 4 3
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 351 14 2 4 3.8 CCCCCC(O)CCc1cccc(=O)n1CCCCCCC(=O)O 10.1016/j.bmcl.2020.127104
CHEMBL4649582 178305 None 0 Human Functional pEC50 = 6.3 6.3 4 3
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 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
44289922 163619 None 0 Human Functional pEC50 = 7.3 7.3 4 2
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 163619 None 0 Human Functional pEC50 = 7.3 7.3 4 2
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
44289922 163619 None 0 Human Functional pEC50 = 7.3 7.3 4 2
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/jm049290a
CHEMBL42027 163619 None 0 Human Functional pEC50 = 7.3 7.3 4 2
Functional activity at human EP4 receptorFunctional activity at human EP4 receptor
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/jm049290a
145978309 163847 None 0 Human Functional pEC50 = 6.2 6.2 -5248 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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 163847 None 0 Human Functional pEC50 = 6.2 6.2 -5248 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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
44304011 205266 None 0 Mouse Functional pEC50 = 6.2 6.2 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 205266 None 0 Mouse Functional pEC50 = 6.2 6.2 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
44290266 161802 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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 161802 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
10048720 69383 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69383 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
11755846 69287 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 503 12 2 4 6.1 Cc1cc(Cl)ccc1-c1cccc([C@H](O)CC[C@H]2CCCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmcl.2005.03.059
CHEMBL192743 69287 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 503 12 2 4 6.1 Cc1cc(Cl)ccc1-c1cccc([C@H](O)CC[C@H]2CCCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmcl.2005.03.059
16678098 165313 None 22 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at EP4 receptor in human whole blood assessed as inhibition of LPS-induced TNFalpha productionPartial agonist activity at EP4 receptor in human whole blood assessed as inhibition of LPS-induced TNFalpha production
ChEMBL 423 7 1 4 4.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)c(F)c1)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4229058 165313 None 22 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at EP4 receptor in human whole blood assessed as inhibition of LPS-induced TNFalpha productionPartial agonist activity at EP4 receptor in human whole blood assessed as inhibition of LPS-induced TNFalpha production
ChEMBL 423 7 1 4 4.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)c(F)c1)C2 10.1016/j.bmcl.2018.03.091
156015440 177663 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 437 10 2 4 5.1 CCCCCC(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
CHEMBL4640391 177663 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 437 10 2 4 5.1 CCCCCC(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
44289980 168911 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
CHEMBL43766 168911 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
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
90054460 154339 None 0 Human Functional pEC50 = 7.2 7.2 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 449 9 2 4 4.3 C[C@@H](c1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3986266 154339 None 0 Human Functional pEC50 = 7.2 7.2 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 449 9 2 4 4.3 C[C@@H](c1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
23654359 68611 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 437 11 2 5 4.1 O=C(O)CCCSCCN1C(=O)CCC[C@@H]1CC[C@@H](O)c1ccc(C(F)(F)F)o1 10.1016/j.bmcl.2005.03.059
CHEMBL191770 68611 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Effective concentration required for prostanoid EP4 receptor activity was determinedEffective concentration required for prostanoid EP4 receptor activity was determined
ChEMBL 437 11 2 5 4.1 O=C(O)CCCSCCN1C(=O)CCC[C@@H]1CC[C@@H](O)c1ccc(C(F)(F)F)o1 10.1016/j.bmcl.2005.03.059
156015440 177663 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 437 10 2 4 5.1 CCCCCC(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
CHEMBL4640391 177663 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP4 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 437 10 2 4 5.1 CCCCCC(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
12002527 75186 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 493 12 2 5 5.1 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2cc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036314 75186 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 493 12 2 5 5.1 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2cc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
56839344 152140 None 0 Human Functional pEC50 = 8.2 8.2 -23 8
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 656 13 2 9 5.1 O=C(CCc1cc2c(cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC3CCCCC3)co1)OCO2)NS(=O)(=O)C(F)(F)F nan
CHEMBL3967284 152140 None 0 Human Functional pEC50 = 8.2 8.2 -23 8
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 656 13 2 9 5.1 O=C(CCc1cc2c(cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC3CCCCC3)co1)OCO2)NS(=O)(=O)C(F)(F)F nan
57394140 69393 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69393 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
1883 3082 None 47 Human Functional pEC50 = 8.1 8.1 -1 12
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF 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/acsmedchemlett.5b00455
1916 3082 None 47 Human Functional pEC50 = 8.1 8.1 -1 12
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF 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/acsmedchemlett.5b00455
5280360 3082 None 47 Human Functional pEC50 = 8.1 8.1 -1 12
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF 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/acsmedchemlett.5b00455
5280360.0 3082 None 47 Human Functional pEC50 = 8.1 8.1 -1 12
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF 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/acsmedchemlett.5b00455
913 3082 None 47 Human Functional pEC50 = 8.1 8.1 -1 12
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF 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/acsmedchemlett.5b00455
CHEMBL548 3082 None 47 Human Functional pEC50 = 8.1 8.1 -1 12
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF 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/acsmedchemlett.5b00455
DB00917 3082 None 47 Human Functional pEC50 = 8.1 8.1 -1 12
Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF 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/acsmedchemlett.5b00455
56949973 69394 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69394 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
10076580 75315 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 563 10 2 8 5.5 Cc1cc(C)c2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2037291 75315 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 563 10 2 8 5.5 Cc1cc(C)c2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
44304058 205635 None 0 Mouse Functional pEC50 = 8.1 8.1 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 205635 None 0 Mouse Functional pEC50 = 8.1 8.1 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
21079283 165112 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 419 7 1 4 4.7 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1C)C2 10.1016/j.bmcl.2018.03.091
CHEMBL4225980 165112 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 419 7 1 4 4.7 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC(=O)O)cc1C)C2 10.1016/j.bmcl.2018.03.091
118517452 148299 None 0 Human Functional pEC50 = 6.1 6.1 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 458 9 2 4 5.2 COc1ccc2cc(CC(O)/C=C/[C@H]3CCC(=O)[C@@H]3CCc3ccc(C(=O)O)cc3)ccc2c1 nan
CHEMBL3935958 148299 None 0 Human Functional pEC50 = 6.1 6.1 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 458 9 2 4 5.2 COc1ccc2cc(CC(O)/C=C/[C@H]3CCC(=O)[C@@H]3CCc3ccc(C(=O)O)cc3)ccc2c1 nan
44304057 205717 None 0 Mouse Functional pEC50 = 5.1 5.1 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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 205717 None 0 Mouse Functional pEC50 = 5.1 5.1 - 1
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 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
17747304 165234 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 437 7 1 5 4.2 CCOc1c2c(c(OCC)c3cc(F)ccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2=O 10.1016/j.bmcl.2018.03.091
CHEMBL4227838 165234 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Partial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assayPartial agonist activity at human EP4 receptor expressed in HEK293-AEQ17 cells assessed as cAMP accumulation by aequorin luminescence assay
ChEMBL 437 7 1 5 4.2 CCOc1c2c(c(OCC)c3cc(F)ccc13)C(=O)N(c1ccc(CC(=O)O)cc1)C2=O 10.1016/j.bmcl.2018.03.091
57394893 71330 None 0 Rat Functional pEC50 = 8.1 8.1 223 2
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
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 71330 None 0 Rat Functional pEC50 = 8.1 8.1 223 2
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
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 71330 None 0 Rat Functional pEC50 = 8.1 8.1 223 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 71330 None 0 Rat Functional pEC50 = 8.1 8.1 223 2
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
118517451 152958 None 0 Human Functional pEC50 = 8.1 8.1 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 436 8 2 5 3.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc3c(c2)OCCO3)cc1 nan
CHEMBL3974337 152958 None 0 Human Functional pEC50 = 8.1 8.1 - 1
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 436 8 2 5 3.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc3c(c2)OCCO3)cc1 nan
90054486 152810 None 0 Human Functional pEC50 = 8.1 8.1 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 491 11 1 5 4.9 COC(=O)c1ccc(CCCN2C(=O)C(F)(F)C[C@@H]2/C=C/[C@@H](O)[C@@H](C)CCc2ccccc2)s1 nan
CHEMBL3973091 152810 None 0 Human Functional pEC50 = 8.1 8.1 - 1
cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.cAMP Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 uL of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing 500 uM IBMX (an inhibitor of cAMP phosphodiesterase) and different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. Incubate the cells in a cell culture incubator for 30 minutes. 5. Centrifuge the plate at 1,000x rpm for 10 minutes. 6. Aspirate the supernatant.
ChEMBL 491 11 1 5 4.9 COC(=O)c1ccc(CCCN2C(=O)C(F)(F)C[C@@H]2/C=C/[C@@H](O)[C@@H](C)CCc2ccccc2)s1 nan
44289922 163619 None 0 Rat Functional pEC50 = 8.1 8.1 -4 2
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
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 163619 None 0 Rat Functional pEC50 = 8.1 8.1 -4 2
Agonist activity at rat EP4 receptorAgonist activity at rat EP4 receptor
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
22394738 75440 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 395 12 2 3 4.1 O=C(O)CCCCCCN1C(=O)CCC1CCC(O)Cc1cccc(Cl)c1 10.1016/j.bmcl.2006.01.018
CHEMBL204058 75440 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 395 12 2 3 4.1 O=C(O)CCCCCCN1C(=O)CCC1CCC(O)Cc1cccc(Cl)c1 10.1016/j.bmcl.2006.01.018
58932681 75198 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1ccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2036326 75198 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1ccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
44290494 100329 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 437 12 2 4 5.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2004.01.063
CHEMBL288978 100329 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cellsAgonist activity against recombinant prostanoid EP4 receptor stably transfected in CHO cells
ChEMBL 437 12 2 4 5.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2004.01.063
57893867 75183 None 0 Rat Functional pEC50 = 7.1 7.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 492 12 3 4 4.9 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3[nH]ccc3c2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036311 75183 None 0 Rat Functional pEC50 = 7.1 7.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 492 12 3 4 4.9 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3[nH]ccc3c2)c1 10.1016/j.bmc.2012.04.008
57893916 75181 None 0 Rat Functional pEC50 = 7.1 7.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 454 12 2 5 3.8 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccccn2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036309 75181 None 0 Rat Functional pEC50 = 7.1 7.1 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 454 12 2 5 3.8 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccccn2)c1 10.1016/j.bmc.2012.04.008
10431288 69388 None 0 Rat Functional pEC50 = 8.0 8.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69388 None 0 Rat Functional pEC50 = 8.0 8.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
10348321 75197 None 0 Rat Functional pEC50 = 8.0 8.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 585 10 2 8 6.0 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036325 75197 None 0 Rat Functional pEC50 = 8.0 8.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 585 10 2 8 6.0 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
15979081 163935 None 0 Human Functional pEC50 = 7.0 7.0 -190 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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 163935 None 0 Human Functional pEC50 = 7.0 7.0 -190 3
Agonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
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
44409743 141386 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 419 15 2 4 3.6 COCCc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
CHEMBL383339 141386 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 419 15 2 4 3.6 COCCc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
10320021 69374 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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 69374 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
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
44409923 166098 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 386 12 2 4 3.3 N#Cc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
CHEMBL425409 166098 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Activity at rat EP4 transfected in HEK293 cells by cAMP accumulationActivity at rat EP4 transfected in HEK293 cells by cAMP accumulation
ChEMBL 386 12 2 4 3.3 N#Cc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
57894081 75180 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 503 12 2 4 5.6 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036308 75180 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 503 12 2 4 5.6 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2012.04.008
78319379 137564 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 389 5 3 3 4.7 Cc1ccc(-c2cccc(CO)c2)cc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2015.12.057
CHEMBL3753860 137564 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 389 5 3 3 4.7 Cc1ccc(-c2cccc(CO)c2)cc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2015.12.057
156073557 191137 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 435 6 2 4 4.9 Cc1ccc(Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5186935 191137 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 435 6 2 4 4.9 Cc1ccc(Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)cc1 10.1021/acs.jmedchem.2c00448
118191094 137441 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 444 5 3 4 4.8 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1nc(-c2cccc(CO)c2)ccc1C(F)(F)F 10.1016/j.bmcl.2015.12.057
CHEMBL3752948 137441 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 444 5 3 4 4.8 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1nc(-c2cccc(CO)c2)ccc1C(F)(F)F 10.1016/j.bmcl.2015.12.057
118191092 137560 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2015.12.057
CHEMBL3753835 137560 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2015.12.057
118190924 137529 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 393 5 3 3 4.6 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)ccc1F 10.1016/j.bmcl.2015.12.057
CHEMBL3753567 137529 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 393 5 3 3 4.6 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)ccc1F 10.1016/j.bmcl.2015.12.057
171361355 196742 None 1 Human Functional pIC50 = 9.1 9.1 -1 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced beta-arrestin recruitment preincubated with compound for 20 mins followed by PGE2 stimulation and measured after 12 hrs by Tango assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced beta-arrestin recruitment preincubated with compound for 20 mins followed by PGE2 stimulation and measured after 12 hrs by Tango assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5431224 196742 None 1 Human Functional pIC50 = 9.1 9.1 -1 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced beta-arrestin recruitment preincubated with compound for 20 mins followed by PGE2 stimulation and measured after 12 hrs by Tango assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced beta-arrestin recruitment preincubated with compound for 20 mins followed by PGE2 stimulation and measured after 12 hrs by Tango assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
23661014 57114 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 434 6 2 3 5.1 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(Cl)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645135 57114 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 434 6 2 3 5.1 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(Cl)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
138671614 190093 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 455 6 2 4 5.3 C[C@H](NC(=O)c1c(Cc2ccc(Cl)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5171006 190093 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 455 6 2 4 5.3 C[C@H](NC(=O)c1c(Cc2ccc(Cl)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
156073540 192315 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 501 6 2 4 5.5 O=C(O)c1ccc(C2(NC(=O)c3c(Cc4cccc(C(F)(F)F)c4)sc4c3CCOC4)CC2)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5204626 192315 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 501 6 2 4 5.5 O=C(O)c1ccc(C2(NC(=O)c3c(Cc4cccc(C(F)(F)F)c4)sc4c3CCOC4)CC2)cc1 10.1021/acs.jmedchem.2c00448
171361355 196742 None 1 Human Functional pIC50 = 9.0 9.0 -1 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5431224 196742 None 1 Human Functional pIC50 = 9.0 9.0 -1 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
23661189 57113 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 468 6 2 3 5.7 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(Cl)c(Cl)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645134 57113 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 468 6 2 3 5.7 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(Cl)c(Cl)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
118191077 136887 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 425 5 3 3 5.6 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3741430 136887 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 425 5 3 3 5.6 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
46890660 6660 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 500 6 2 3 6.6 C[C@H](NC(=O)c1cc(Cl)cc2ccn(Cc3ccc(C(F)(F)F)cc3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1083400 6660 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 500 6 2 3 6.6 C[C@H](NC(=O)c1cc(Cl)cc2ccn(Cc3ccc(C(F)(F)F)cc3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
50898361 56889 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human EP4 receptor in HEK293 cells by cell-based functional assayAntagonist activity at human EP4 receptor in HEK293 cells by cell-based functional assay
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 56889 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human EP4 receptor in HEK293 cells by cell-based functional assayAntagonist activity at human EP4 receptor in HEK293 cells by cell-based functional assay
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
25002382 7397 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 512 6 2 3 6.5 O=C(O)c1ccc(C2(NC(=O)c3cc(Cl)cc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1086490 7397 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 512 6 2 3 6.5 O=C(O)c1ccc(C2(NC(=O)c3cc(Cl)cc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.065
141730900 171217 None 0 Human Functional pIC50 = 8.9 8.9 104 2
Antagonist activity at human EP4 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 EP4 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 524 9 2 6 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1CCOc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4457944 171217 None 0 Human Functional pIC50 = 8.9 8.9 104 2
Antagonist activity at human EP4 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 EP4 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 524 9 2 6 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1CCOc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
25003075 6840 None 21 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
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 6840 None 21 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
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
53317509 57120 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 476 7 2 3 6.1 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(-c3ccccc3)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645141 57120 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 476 7 2 3 6.1 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(-c3ccccc3)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
46890658 6960 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 516 7 2 4 6.4 C[C@H](NC(=O)c1cccc2ccn(Cc3cc(Cl)cc(OC(F)(F)F)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1084552 6960 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 516 7 2 4 6.4 C[C@H](NC(=O)c1cccc2ccn(Cc3cc(Cl)cc(OC(F)(F)F)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
24765768 7087 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 466 6 2 3 6.2 C[C@H](NC(=O)c1cc(Cl)cc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1085040 7087 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 466 6 2 3 6.2 C[C@H](NC(=O)c1cc(Cl)cc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
118174960 137507 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 394 4 2 3 5.3 Cc1ccc(-c2cccc(Cl)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
CHEMBL3753372 137507 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 394 4 2 3 5.3 Cc1ccc(-c2cccc(Cl)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
24953285 203326 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 453 6 2 3 5.9 O=C(O)c1ccc(CNC(=O)c2c(Cl)sc(Cl)c2Cc2cccc(Cl)c2)cc1 10.1021/jm901771h
CHEMBL601299 203326 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 453 6 2 3 5.9 O=C(O)c1ccc(CNC(=O)c2c(Cl)sc(Cl)c2Cc2cccc(Cl)c2)cc1 10.1021/jm901771h
171361355 196742 None 1 Mouse Functional pIC50 = 8.8 8.8 1 3
Antagonist activity at mouse EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at mouse EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5431224 196742 None 1 Mouse Functional pIC50 = 8.8 8.8 1 3
Antagonist activity at mouse EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at mouse EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
86707361 139444 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 403 4 2 4 4.2 Cc1ccc(N2CCC(F)(F)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
CHEMBL3793002 139444 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 403 4 2 4 4.2 Cc1ccc(N2CCC(F)(F)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
138671623 191327 None 0 Human Functional pIC50 = 8.8 8.8 1 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 489 6 2 4 5.6 C[C@H](NC(=O)c1c(Cc2cccc(C(F)(F)F)c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5189703 191327 None 0 Human Functional pIC50 = 8.8 8.8 1 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 489 6 2 4 5.6 C[C@H](NC(=O)c1c(Cc2cccc(C(F)(F)F)c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
172462136 196599 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 437 6 2 4 4.5 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(Cl)c(F)c2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5427544 196599 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 437 6 2 4 4.5 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(Cl)c(F)c2)cc1 10.1021/acs.jmedchem.2c02058
24953283 201904 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 467 6 2 3 6.5 C[C@@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
CHEMBL591431 201904 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 467 6 2 3 6.5 C[C@@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
172446201 194990 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 471 6 2 4 4.9 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)c(F)c2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5394484 194990 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 471 6 2 4 4.9 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)c(F)c2)cc1 10.1021/acs.jmedchem.2c02058
25003075 6840 None 21 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
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 6840 None 21 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
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
138671613 190655 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 469 7 2 5 4.7 COc1ccc(Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)cc1F 10.1021/acs.jmedchem.2c00448
CHEMBL5179874 190655 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 469 7 2 5 4.7 COc1ccc(Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)cc1F 10.1021/acs.jmedchem.2c00448
156073538 191520 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 451 7 2 5 4.6 COc1cccc(Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)c1 10.1021/acs.jmedchem.2c00448
CHEMBL5192663 191520 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 451 7 2 5 4.6 COc1cccc(Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)c1 10.1021/acs.jmedchem.2c00448
118191093 137494 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 444 5 3 4 4.8 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1nc(-c2cccc(CO)c2)ccc1C(F)(F)F 10.1016/j.bmcl.2015.12.057
CHEMBL3753286 137494 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 444 5 3 4 4.8 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1nc(-c2cccc(CO)c2)ccc1C(F)(F)F 10.1016/j.bmcl.2015.12.057
56944705 129281 None 39 Human Functional pIC50 = 8 8.0 11 3
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
CHEMBL3670685 129281 None 39 Human Functional pIC50 = 8 8.0 11 3
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
138670958 190780 None 0 Human Functional pIC50 = 8.0 8.0 1 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 437 7 2 3 5.4 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5181722 190780 None 0 Human Functional pIC50 = 8.0 8.0 1 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 437 7 2 3 5.4 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
155524726 171071 None 0 Human Functional pIC50 = 8.0 8.0 12 2
Antagonist activity at human EP4 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 EP4 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 444 7 2 5 4.0 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NCc1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4455965 171071 None 0 Human Functional pIC50 = 8.0 8.0 12 2
Antagonist activity at human EP4 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 EP4 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 444 7 2 5 4.0 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NCc1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
57396195 67871 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay
ChEMBL 467 4 2 3 5.7 O=C(O)c1ccc(C2(NC(=O)c3cccc4c3Oc3cc(C(F)(F)F)ccc3CC4)CC2)cc1 10.1016/j.bmcl.2011.08.102
CHEMBL1910023 67871 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay
ChEMBL 467 4 2 3 5.7 O=C(O)c1ccc(C2(NC(=O)c3cccc4c3Oc3cc(C(F)(F)F)ccc3CC4)CC2)cc1 10.1016/j.bmcl.2011.08.102
172442059 195161 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 389 5 2 4 4.2 O=C(O)c1cccc(NC(=O)c2c3ccccc3nn2Cc2cccc(F)c2)c1 10.1021/acs.jmedchem.2c02058
CHEMBL5397734 195161 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 389 5 2 4 4.2 O=C(O)c1cccc(NC(=O)c2c3ccccc3nn2Cc2cccc(F)c2)c1 10.1021/acs.jmedchem.2c02058
172438908 195240 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 389 5 2 4 4.2 O=C(O)c1cccc(NC(=O)c2c3ccccc3nn2Cc2ccc(F)cc2)c1 10.1021/acs.jmedchem.2c02058
CHEMBL5399302 195240 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 389 5 2 4 4.2 O=C(O)c1cccc(NC(=O)c2c3ccccc3nn2Cc2ccc(F)cc2)c1 10.1021/acs.jmedchem.2c02058
172445147 195431 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2nn(Cc3cccc(C(F)(F)F)c3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5403528 195431 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2nn(Cc3cccc(C(F)(F)F)c3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
172446527 195518 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 403 6 2 4 3.9 O=C(O)c1ccc(CNC(=O)c2nn(Cc3cccc(F)c3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5405242 195518 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 403 6 2 4 3.9 O=C(O)c1ccc(CNC(=O)c2nn(Cc3cccc(F)c3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
172453558 195636 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 403 6 2 4 3.9 O=C(O)c1ccc(CNC(=O)c2nn(Cc3ccc(F)cc3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5407788 195636 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 403 6 2 4 3.9 O=C(O)c1ccc(CNC(=O)c2nn(Cc3ccc(F)cc3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
172452658 195850 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 385 6 2 4 3.7 O=C(O)c1ccc(CNC(=O)c2nn(Cc3ccccc3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5411952 195850 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 385 6 2 4 3.7 O=C(O)c1ccc(CNC(=O)c2nn(Cc3ccccc3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
172453340 195988 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 415 7 2 5 3.7 COc1ccc(Cn2nc(C(=O)NCc3ccc(C(=O)O)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5414713 195988 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 415 7 2 5 3.7 COc1ccc(Cn2nc(C(=O)NCc3ccc(C(=O)O)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.2c02058
172466331 196547 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 419 6 2 4 4.4 O=C(O)c1ccc(CNC(=O)c2nn(Cc3cccc(Cl)c3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5426457 196547 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 419 6 2 4 4.4 O=C(O)c1ccc(CNC(=O)c2nn(Cc3cccc(Cl)c3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
172464025 196601 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 469 7 2 5 4.6 O=C(O)c1ccc(CNC(=O)c2nn(Cc3ccc(OC(F)(F)F)cc3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5427584 196601 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 469 7 2 5 4.6 O=C(O)c1ccc(CNC(=O)c2nn(Cc3ccc(OC(F)(F)F)cc3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
172469255 197006 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 419 6 2 4 4.4 O=C(O)c1ccc(CNC(=O)c2nn(Cc3ccc(Cl)cc3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5436556 197006 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 419 6 2 4 4.4 O=C(O)c1ccc(CNC(=O)c2nn(Cc3ccc(Cl)cc3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
172469762 197039 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 415 7 2 5 3.7 COc1cccc(Cn2nc(C(=O)NCc3ccc(C(=O)O)cc3)c3ccccc32)c1 10.1021/acs.jmedchem.2c02058
CHEMBL5437320 197039 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 415 7 2 5 3.7 COc1cccc(Cn2nc(C(=O)NCc3ccc(C(=O)O)cc3)c3ccccc32)c1 10.1021/acs.jmedchem.2c02058
172468746 197068 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2nn(Cc3ccc(C(F)(F)F)cc3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5438025 197068 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2nn(Cc3ccc(C(F)(F)F)cc3)c3ccccc23)cc1 10.1021/acs.jmedchem.2c02058
58905368 156465 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 399 6 2 3 4.9 O=C(O)c1ccc(CNC(=O)c2cc(Cl)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4066230 156465 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 399 6 2 3 4.9 O=C(O)c1ccc(CNC(=O)c2cc(Cl)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
56944705 129281 None 39 Mouse Functional pIC50 = 7 7.0 -11 3
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL3670685 129281 None 39 Mouse Functional pIC50 = 7 7.0 -11 3
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
25019434 57711 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 673 12 2 8 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(OC)cccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669005 57711 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 673 12 2 8 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(OC)cccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
24952929 2554 None 35 Human Functional pIC50 = 8.0 8.0 - 1
Activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseActivity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
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 2554 None 35 Human Functional pIC50 = 8.0 8.0 - 1
Activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseActivity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
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 2554 None 35 Human Functional pIC50 = 8.0 8.0 - 1
Activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseActivity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
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
172464219 196752 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 433 6 2 4 4.9 C[C@H](NC(=O)c1c2ccccc2nn1Cc1ccc(Cl)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5431483 196752 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 433 6 2 4 4.9 C[C@H](NC(=O)c1c2ccccc2nn1Cc1ccc(Cl)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
71186338 145873 None 0 Human Functional pIC50 = 8.0 8.0 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 482 6 2 3 4.8 O=C(O)c1ccc(C2(NC(=O)C3CC(F)(F)CCN3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
CHEMBL3916857 145873 None 0 Human Functional pIC50 = 8.0 8.0 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 482 6 2 3 4.8 O=C(O)c1ccc(C2(NC(=O)C3CC(F)(F)CCN3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
118174952 136909 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 396 4 2 3 5.5 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2ccccc2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3741642 136909 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 396 4 2 3 5.5 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2ccccc2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
71186249 150476 None 0 Human Functional pIC50 = 7.9 7.9 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 458 6 2 3 4.4 O=C(O)c1ccc(C2(NC(=O)C3CC4CC4CN3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
CHEMBL3953493 150476 None 0 Human Functional pIC50 = 7.9 7.9 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 458 6 2 3 4.4 O=C(O)c1ccc(C2(NC(=O)C3CC4CC4CN3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
11677589 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2016.03.041
11677589.0 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2016.03.041
5858 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2016.03.041
CHEMBL3039498 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2016.03.041
DB12836 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2016.03.041
11677589 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.11.023
11677589.0 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.11.023
5858 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.11.023
CHEMBL3039498 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.11.023
DB12836 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.11.023
11677589 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
11677589.0 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
5858 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
CHEMBL3039498 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
DB12836 1859 None 51 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
24765671 6959 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 466 6 2 3 5.9 C[C@H](NC(=O)c1cccc2ccn(Cc3cccc(C(F)(F)F)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1084551 6959 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 466 6 2 3 5.9 C[C@H](NC(=O)c1cccc2ccn(Cc3cccc(C(F)(F)F)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
76284214 175891 None 0 Mouse Functional pIC50 = 7.0 7.0 -8 2
Antagonist activity at mouse EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at mouse EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 409 5 1 4 5.9 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4584103 175891 None 0 Mouse Functional pIC50 = 7.0 7.0 -8 2
Antagonist activity at mouse EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at mouse EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 409 5 1 4 5.9 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
53322911 57126 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 456 6 2 3 5.7 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(C)(C)C)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645147 57126 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 456 6 2 3 5.7 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(C)(C)C)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
155555513 174556 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human EP4 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 EP4 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 500 7 2 6 4.3 C[C@H](NC(=O)c1c(C2=CCOCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4553892 174556 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human EP4 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 EP4 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 500 7 2 6 4.3 C[C@H](NC(=O)c1c(C2=CCOCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
155552440 174160 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human EP4 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 EP4 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 486 9 2 7 4.2 COc1ccc(Cn2nnc(-c3ccccc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)cc1OC 10.1021/acs.jmedchem.9b01269
CHEMBL4544033 174160 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human EP4 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 EP4 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 486 9 2 7 4.2 COc1ccc(Cn2nnc(-c3ccccc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)cc1OC 10.1021/acs.jmedchem.9b01269
72695136 131403 None 2 Rat Functional pIC50 = 7.9 7.9 2 2
Antagonist activity against rat EP4 assessed as inhibition of PGE2-stimulated production of cAMPAntagonist activity against rat EP4 assessed as inhibition of PGE2-stimulated production of cAMP
ChEMBL 383 4 3 5 2.9 Cc1ccc(N2CCC(O)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
CHEMBL3686863 131403 None 2 Rat Functional pIC50 = 7.9 7.9 2 2
Antagonist activity against rat EP4 assessed as inhibition of PGE2-stimulated production of cAMPAntagonist activity against rat EP4 assessed as inhibition of PGE2-stimulated production of cAMP
ChEMBL 383 4 3 5 2.9 Cc1ccc(N2CCC(O)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
24952577 203017 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 399 6 2 3 5.2 C[C@H](NC(=O)c1cscc1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
CHEMBL599051 203017 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 399 6 2 3 5.2 C[C@H](NC(=O)c1cscc1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
172466489 196690 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 415 7 2 5 3.7 COc1cccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)c1 10.1021/acs.jmedchem.2c02058
CHEMBL5430051 196690 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 415 7 2 5 3.7 COc1cccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)c1 10.1021/acs.jmedchem.2c02058
156073551 192114 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 461 5 2 5 4.4 COc1cccc(C#Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)c1 10.1021/acs.jmedchem.2c00448
CHEMBL5201557 192114 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 461 5 2 5 4.4 COc1cccc(C#Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)c1 10.1021/acs.jmedchem.2c00448
76284214 175891 None 0 Human Functional pIC50 = 7.9 7.9 8 2
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 409 5 1 4 5.9 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4584103 175891 None 0 Human Functional pIC50 = 7.9 7.9 8 2
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 409 5 1 4 5.9 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
141730914 174992 None 0 Human Functional pIC50 = 7.9 7.9 2 2
Antagonist activity at human EP4 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 EP4 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 500 7 2 6 5.3 C[C@H](NC(=O)c1c(-c2ccsc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4564092 174992 None 0 Human Functional pIC50 = 7.9 7.9 2 2
Antagonist activity at human EP4 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 EP4 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 500 7 2 6 5.3 C[C@H](NC(=O)c1c(-c2ccsc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
137646517 157918 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4083413 157918 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
1351369 136918 None 8 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 352 3 1 2 5.8 Cc1cccc(C)c1NC(=O)c1cc(-c2ccccc2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3741710 136918 None 8 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 352 3 1 2 5.8 Cc1cccc(C)c1NC(=O)c1cc(-c2ccccc2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
11524454 946 None 36 Human Functional pIC50 = 7.9 7.9 52 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2011.08.102
5857 946 None 36 Human Functional pIC50 = 7.9 7.9 52 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2011.08.102
CHEMBL591666 946 None 36 Human Functional pIC50 = 7.9 7.9 52 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2011.08.102
172467164 196583 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 433 6 2 4 4.9 C[C@H](NC(=O)c1c2ccccc2nn1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5427264 196583 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 433 6 2 4 4.9 C[C@H](NC(=O)c1c2ccccc2nn1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
172462045 196868 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5433721 196868 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.2c02058
156073552 192590 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 453 7 2 4 4.9 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1COCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5208903 192590 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 453 7 2 4 4.9 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1COCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
155555000 174437 None 0 Human Functional pIC50 = 7.9 7.9 15 2
Antagonist activity at human EP4 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 EP4 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 450 7 2 5 4.0 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NCC1CCC(C(=O)O)CC1 10.1021/acs.jmedchem.9b01269
CHEMBL4550862 174437 None 0 Human Functional pIC50 = 7.9 7.9 15 2
Antagonist activity at human EP4 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 EP4 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 450 7 2 5 4.0 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NCC1CCC(C(=O)O)CC1 10.1021/acs.jmedchem.9b01269
155554096 175547 None 0 Human Functional pIC50 = 7.9 7.9 2 2
Antagonist activity at human EP4 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 EP4 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 470 7 2 5 4.5 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NC1(c2ccc(C(=O)O)cc2)CC1 10.1021/acs.jmedchem.9b01269
CHEMBL4576681 175547 None 0 Human Functional pIC50 = 7.9 7.9 2 2
Antagonist activity at human EP4 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 EP4 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 470 7 2 5 4.5 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NC1(c2ccc(C(=O)O)cc2)CC1 10.1021/acs.jmedchem.9b01269
155524726 171071 None 0 Mouse Functional pIC50 = 6.9 6.9 -12 2
Antagonist activity at mouse EP4 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 mouse EP4 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 444 7 2 5 4.0 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NCc1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4455965 171071 None 0 Mouse Functional pIC50 = 6.9 6.9 -12 2
Antagonist activity at mouse EP4 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 mouse EP4 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 444 7 2 5 4.0 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NCc1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
141730916 169894 None 0 Mouse Functional pIC50 = 6.9 6.9 -42 2
Antagonist activity at mouse EP4 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 mouse EP4 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 474 9 2 6 4.4 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4439228 169894 None 0 Mouse Functional pIC50 = 6.9 6.9 -42 2
Antagonist activity at mouse EP4 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 mouse EP4 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 474 9 2 6 4.4 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
76283442 176045 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 412 6 1 5 4.6 CCn1c2ccccc2c2cc(-c3nc4cc(C(N)=O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4587734 176045 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 412 6 1 5 4.6 CCn1c2ccccc2c2cc(-c3nc4cc(C(N)=O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
141730900 171217 None 0 Mouse Functional pIC50 = 6.9 6.9 -104 2
Antagonist activity at mouse EP4 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 mouse EP4 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 524 9 2 6 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1CCOc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4457944 171217 None 0 Mouse Functional pIC50 = 6.9 6.9 -104 2
Antagonist activity at mouse EP4 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 mouse EP4 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 524 9 2 6 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1CCOc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
58905363 159677 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 431 6 2 5 4.8 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cncc(Cl)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4102924 159677 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 431 6 2 5 4.8 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cncc(Cl)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
86707350 139525 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 397 5 3 5 3.2 Cc1ccc(N2CCCC(CO)C2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
CHEMBL3793928 139525 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 397 5 3 5 3.2 Cc1ccc(N2CCCC(CO)C2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
89914445 122660 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 410 9 2 4 3.9 CC[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600787 122660 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 410 9 2 4 3.9 CC[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601950 122660 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 410 9 2 4 3.9 CC[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
76281723 172597 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 586 8 1 7 6.3 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)NS(=O)(=O)c5cccc(Cl)c5)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4483339 172597 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 586 8 1 7 6.3 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)NS(=O)(=O)c5cccc(Cl)c5)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
155555737 174555 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 413 6 1 5 5.2 CCn1c2ccccc2c2cc(-c3nc4ccc(C(=O)O)cc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4553842 174555 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 413 6 1 5 5.2 CCn1c2ccccc2c2cc(-c3nc4ccc(C(=O)O)cc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
58905345 158985 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 398 6 2 4 4.3 C[C@H](NC(=O)c1cc(F)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4095293 158985 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 398 6 2 4 4.3 C[C@H](NC(=O)c1cc(F)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
155519679 170526 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4 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 EP4 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 462 7 2 5 4.5 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1ccc(F)c(F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4448318 170526 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4 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 EP4 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 462 7 2 5 4.5 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1ccc(F)c(F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
155542414 173248 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 519 8 1 7 4.0 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)NS(=O)(=O)N(C)C)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4521321 173248 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 519 8 1 7 4.0 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)NS(=O)(=O)N(C)C)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
172468000 196534 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 457 5 2 4 4.5 O=C(NC1CC2(C1)CC(C(=O)O)C2)c1c2ccccc2nn1Cc1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5426152 196534 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 457 5 2 4 4.5 O=C(NC1CC2(C1)CC(C(=O)O)C2)c1c2ccccc2nn1Cc1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.2c02058
72695027 106322 None 0 Rat Functional pIC50 = 7.8 7.8 2 3
Antagonist activity at rat EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at rat EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
CHEMBL3115074 106322 None 0 Rat Functional pIC50 = 7.8 7.8 2 3
Antagonist activity at rat EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at rat EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
CHEMBL3138992 106322 None 0 Rat Functional pIC50 = 7.8 7.8 2 3
Antagonist activity at rat EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at rat EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
71186604 149388 None 0 Human Functional pIC50 = 7.8 7.8 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 482 6 2 3 4.8 O=C(O)c1ccc(C2(NC(=O)C3CC(F)(F)CCN3Cc3cccc(C(F)(F)F)c3)CC2)cc1 nan
CHEMBL3944767 149388 None 0 Human Functional pIC50 = 7.8 7.8 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 482 6 2 3 4.8 O=C(O)c1ccc(C2(NC(=O)C3CC(F)(F)CCN3Cc3cccc(C(F)(F)F)c3)CC2)cc1 nan
12783 578 None 26 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 441 6 1 5 5.8 O=C(O)C1=CC=C2N(CCOC)C(C3=CC=C4N(CC)C=5C=CC(=CC5C4=C3)C)=NC2=C1C 10.1021/acs.jmedchem.8b01862
90202558 578 None 26 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 441 6 1 5 5.8 O=C(O)C1=CC=C2N(CCOC)C(C3=CC=C4N(CC)C=5C=CC(=CC5C4=C3)C)=NC2=C1C 10.1021/acs.jmedchem.8b01862
CHEMBL4526403 578 None 26 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 441 6 1 5 5.8 O=C(O)C1=CC=C2N(CCOC)C(C3=CC=C4N(CC)C=5C=CC(=CC5C4=C3)C)=NC2=C1C 10.1021/acs.jmedchem.8b01862
56944705 129281 None 39 Human Functional pIC50 = 7.8 7.8 11 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced CRE-mediated gene transcription preincubated with compound followed by PGE2 stimulation and measured after 12 hrs by firefly luciferase assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced CRE-mediated gene transcription preincubated with compound followed by PGE2 stimulation and measured after 12 hrs by firefly luciferase assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL3670685 129281 None 39 Human Functional pIC50 = 7.8 7.8 11 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced CRE-mediated gene transcription preincubated with compound followed by PGE2 stimulation and measured after 12 hrs by firefly luciferase assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced CRE-mediated gene transcription preincubated with compound followed by PGE2 stimulation and measured after 12 hrs by firefly luciferase assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
138670556 190410 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 449 4 2 4 4.5 C[C@H](NC(=O)c1c(C#Cc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5175990 190410 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 449 4 2 4 4.5 C[C@H](NC(=O)c1c(C#Cc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
155559561 174953 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 447 6 1 5 5.8 CCn1c2ccccc2c2cc(-c3nc4c(Cl)c(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4563081 174953 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 447 6 1 5 5.8 CCn1c2ccccc2c2cc(-c3nc4c(Cl)c(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
76284215 173232 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 427 7 1 5 5.6 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CCCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4520842 173232 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 427 7 1 5 5.6 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CCCOC)ccc21 10.1021/acs.jmedchem.8b01862
71502472 160510 None 0 Human Functional pIC50 = 7.8 7.8 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 444 6 2 3 4.2 O=C(O)c1ccc(C2(NC(=O)[C@H]3C[C@H]4C[C@H]4N3Cc3cccc(C(F)(F)F)c3)CC2)cc1 nan
CHEMBL4111368 160510 None 0 Human Functional pIC50 = 7.8 7.8 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 444 6 2 3 4.2 O=C(O)c1ccc(C2(NC(=O)[C@H]3C[C@H]4C[C@H]4N3Cc3cccc(C(F)(F)F)c3)CC2)cc1 nan
172440250 194939 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 421 6 2 4 4.0 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(F)c(F)c2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5393749 194939 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 421 6 2 4 4.0 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(F)c(F)c2)cc1 10.1021/acs.jmedchem.2c02058
146014480 173818 None 18 Mouse Functional pIC50 = 7.8 7.8 -4 2
Antagonist activity at mouse EP4 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 mouse EP4 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 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4535971 173818 None 18 Mouse Functional pIC50 = 7.8 7.8 -4 2
Antagonist activity at mouse EP4 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 mouse EP4 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 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
11577792 159412 None 20 Human Functional pIC50 = 7.8 7.8 309 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4099851 159412 None 20 Human Functional pIC50 = 7.8 7.8 309 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
86707347 139529 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 397 5 3 5 3.2 Cc1ccc(N2CCCC(CO)C2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
CHEMBL3793956 139529 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 397 5 3 5 3.2 Cc1ccc(N2CCCC(CO)C2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
141730908 174217 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4 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 EP4 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 500 7 2 5 5.6 C[C@H](NC(=O)c1c(C2CCCCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4545487 174217 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4 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 EP4 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 500 7 2 5 5.6 C[C@H](NC(=O)c1c(C2CCCCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
25019185 57715 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 643 11 2 7 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669009 57715 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 643 11 2 7 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
76283951 173163 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 369 3 1 4 5.1 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3C)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4519444 173163 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 369 3 1 4 5.1 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3C)ccc21 10.1021/acs.jmedchem.8b01862
172467044 196938 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 403 6 2 4 3.9 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2cccc(F)c2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5435216 196938 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 403 6 2 4 3.9 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2cccc(F)c2)cc1 10.1021/acs.jmedchem.2c02058
155546443 173652 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 495 6 1 5 6.5 CCn1c2ccc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)cc2c2cc(C(F)(F)F)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4531968 173652 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 495 6 1 5 6.5 CCn1c2ccc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)cc2c2cc(C(F)(F)F)ccc21 10.1021/acs.jmedchem.8b01862
137641524 158182 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 415 6 2 5 4.3 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cncc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4086496 158182 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 415 6 2 5 4.3 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cncc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
137633712 156359 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 480 7 2 5 5.6 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(OC(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4065050 156359 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 480 7 2 5 5.6 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(OC(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
76281455 174304 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 439 7 1 5 5.6 COCCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4548032 174304 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 439 7 1 5 5.6 COCCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
89914844 122662 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 382 8 2 4 2.9 O=C(O)c1ccc(CNC(=O)[C@H]2CCCCN2CCOc2ccccc2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600786 122662 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 382 8 2 4 2.9 O=C(O)c1ccc(CNC(=O)[C@H]2CCCCN2CCOc2ccccc2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601983 122662 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 382 8 2 4 2.9 O=C(O)c1ccc(CNC(=O)[C@H]2CCCCN2CCOc2ccccc2)cc1 10.1016/j.bmcl.2015.05.091
56944705 129281 None 39 Human Functional pIC50 = 7.7 7.7 11 3
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by GloSensor cAMP assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by GloSensor cAMP assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL3670685 129281 None 39 Human Functional pIC50 = 7.7 7.7 11 3
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by GloSensor cAMP assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by GloSensor cAMP assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
146014480 173818 None 18 Human Functional pIC50 = 7.7 7.7 4 2
Inhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP AssayInhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP Assay
ChEMBL 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4535971 173818 None 18 Human Functional pIC50 = 7.7 7.7 4 2
Inhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP AssayInhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP Assay
ChEMBL 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
56944705 129281 None 39 Mouse Functional pIC50 = 6.7 6.7 -11 3
Antagonist activity at mouse EP4 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 mouse EP4 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 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL3670685 129281 None 39 Mouse Functional pIC50 = 6.7 6.7 -11 3
Antagonist activity at mouse EP4 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 mouse EP4 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 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
155563161 175424 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human EP4 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 EP4 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 498 7 2 5 5.5 C[C@H](NC(=O)c1c(C2=CCCCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4573602 175424 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human EP4 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 EP4 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 498 7 2 5 5.5 C[C@H](NC(=O)c1c(C2=CCCCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
156073546 192340 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 482 7 1 5 4.7 CON(C)C(=O)c1ccc([C@H](C)NC(=O)c2c(Cc3ccc(F)cc3)sc3c2CCOC3)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5205100 192340 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 482 7 1 5 4.7 CON(C)C(=O)c1ccc([C@H](C)NC(=O)c2c(Cc3ccc(F)cc3)sc3c2CCOC3)cc1 10.1021/acs.jmedchem.2c00448
172440736 195536 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 429 7 2 5 4.3 COc1cccc(Cn2nc3ccccc3c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1 10.1021/acs.jmedchem.2c02058
CHEMBL5405516 195536 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 429 7 2 5 4.3 COc1cccc(Cn2nc3ccccc3c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1 10.1021/acs.jmedchem.2c02058
138672156 191685 None 0 Human Functional pIC50 = 7.7 7.7 2 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 453 7 2 4 4.9 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5195058 191685 None 0 Human Functional pIC50 = 7.7 7.7 2 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 453 7 2 4 4.9 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
86707344 139416 None 1 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 383 4 3 5 2.9 Cc1ccc(N2CCC(O)CC2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
CHEMBL3792709 139416 None 1 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 383 4 3 5 2.9 Cc1ccc(N2CCC(O)CC2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
138670958 190780 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 437 7 2 3 5.4 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5181722 190780 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 437 7 2 3 5.4 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
155521594 170823 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human EP4 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 EP4 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 486 6 2 5 4.6 C[C@H](NC(=O)c1c(C(F)(F)F)nnn1Cc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4452087 170823 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human EP4 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 EP4 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 486 6 2 5 4.6 C[C@H](NC(=O)c1c(C(F)(F)F)nnn1Cc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
172468550 196605 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 469 7 2 5 4.6 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(OC(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5427672 196605 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 469 7 2 5 4.6 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(OC(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
172467662 196632 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 471 6 2 4 4.9 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2F)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5428393 196632 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 471 6 2 4 4.9 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2F)cc1 10.1021/acs.jmedchem.2c02058
171361355 196742 None 1 Human Functional pIC50 = 8.7 8.7 -1 3
Antagonist activity at human EP4 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of PGE2 induced intracellular calcium flux preincubated for 20 mins followed by PGE2 stimulation and measured immediately by microplate reader analysisAntagonist activity at human EP4 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of PGE2 induced intracellular calcium flux preincubated for 20 mins followed by PGE2 stimulation and measured immediately by microplate reader analysis
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5431224 196742 None 1 Human Functional pIC50 = 8.7 8.7 -1 3
Antagonist activity at human EP4 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of PGE2 induced intracellular calcium flux preincubated for 20 mins followed by PGE2 stimulation and measured immediately by microplate reader analysisAntagonist activity at human EP4 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of PGE2 induced intracellular calcium flux preincubated for 20 mins followed by PGE2 stimulation and measured immediately by microplate reader analysis
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
138671692 192362 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 451 7 2 5 4.6 COc1ccc(Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5205440 192362 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 451 7 2 5 4.6 COc1ccc(Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)cc1 10.1021/acs.jmedchem.2c00448
138670951 192537 None 0 Human Functional pIC50 = 8.7 8.7 162 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 489 6 2 4 5.6 C[C@H](NC(=O)c1c(Cc2ccc(C(F)(F)F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5208220 192537 None 0 Human Functional pIC50 = 8.7 8.7 162 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 489 6 2 4 5.6 C[C@H](NC(=O)c1c(Cc2ccc(C(F)(F)F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
172451440 195672 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 433 7 2 5 3.9 COc1ccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1F 10.1021/acs.jmedchem.2c02058
CHEMBL5408721 195672 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 433 7 2 5 3.9 COc1ccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1F 10.1021/acs.jmedchem.2c02058
172463002 196997 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 427 7 2 4 4.8 CC(C)c1ccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5436396 196997 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 427 7 2 4 4.8 CC(C)c1ccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1 10.1021/acs.jmedchem.2c02058
23660841 57116 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 468 6 2 3 5.5 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645137 57116 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 468 6 2 3 5.5 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
53323050 57134 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 486 6 2 3 5.6 C[C@H](NC(=O)c1cc(F)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645155 57134 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 486 6 2 3 5.6 C[C@H](NC(=O)c1cc(F)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
53325182 57132 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 502 6 2 3 6.1 C[C@H](NC(=O)c1cc(Cl)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645153 57132 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 502 6 2 3 6.1 C[C@H](NC(=O)c1cc(Cl)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
24952928 202881 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 497 6 2 5 5.6 Cc1sc(C)c(C(=O)NC2(c3ccc(-c4nn[nH]n4)cc3)CC2)c1Cc1ccc(C(F)(F)F)cc1 10.1021/jm901771h
CHEMBL598198 202881 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 497 6 2 5 5.6 Cc1sc(C)c(C(=O)NC2(c3ccc(-c4nn[nH]n4)cc3)CC2)c1Cc1ccc(C(F)(F)F)cc1 10.1021/jm901771h
118190908 137489 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 389 5 3 3 4.7 Cc1ccc(-c2cccc(CO)c2)cc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
CHEMBL3753274 137489 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 389 5 3 3 4.7 Cc1ccc(-c2cccc(CO)c2)cc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
91810751 137592 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
CHEMBL3754085 137592 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
91810751 137592 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
CHEMBL3754085 137592 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
53316600 56903 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor in HEK293 cells by cell-based functional assayAntagonist activity at human EP4 receptor in HEK293 cells by cell-based functional assay
ChEMBL 500 8 1 4 5.8 COc1ccccc1CC(=O)NCCc1ccc(-c2c(C(=O)N(C)C)sc3c(C)cc(C)cc23)cc1 10.1016/j.bmcl.2010.11.118
CHEMBL1644016 56903 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor in HEK293 cells by cell-based functional assayAntagonist activity at human EP4 receptor in HEK293 cells by cell-based functional assay
ChEMBL 500 8 1 4 5.8 COc1ccccc1CC(=O)NCCc1ccc(-c2c(C(=O)N(C)C)sc3c(C)cc(C)cc23)cc1 10.1016/j.bmcl.2010.11.118
58306787 196284 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 419 6 2 4 4.4 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5420529 196284 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 419 6 2 4 4.4 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.2c02058
118191104 136760 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 425 5 3 3 5.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.12.057
CHEMBL3740223 136760 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 425 5 3 3 5.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.12.057
118191104 136760 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 425 5 3 3 5.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3740223 136760 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 425 5 3 3 5.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
24952929 2554 None 35 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
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 2554 None 35 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
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 2554 None 35 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
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
24952929 2554 None 35 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
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/acs.jmedchem.2c00448
4041 2554 None 35 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
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/acs.jmedchem.2c00448
CHEMBL597997 2554 None 35 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
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/acs.jmedchem.2c00448
168286339 191794 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 507 6 2 4 6.0 C[C@H](NC(=O)c1c(Cc2cc(F)c(Cl)cc2Cl)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5196679 191794 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 507 6 2 4 6.0 C[C@H](NC(=O)c1c(Cc2cc(F)c(Cl)cc2Cl)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
12017 1103 None 0 Human Functional pIC50 = 8.6 8.6 5 2
Antagonist activity at human EP4 receptor expressed in CHO cells coexpressing tTA-dependent luciferase reporter and beta arrestin 2-TEV assessed as reduction in beta-arrestin recruitment preincubated for 30 mins followed by PEG2 addition and measured after 12 hrs by Tango assayAntagonist activity at human EP4 receptor expressed in CHO cells coexpressing tTA-dependent luciferase reporter and beta arrestin 2-TEV assessed as reduction in beta-arrestin recruitment preincubated for 30 mins followed by PEG2 addition and measured after 12 hrs by Tango assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
138670561 1103 None 0 Human Functional pIC50 = 8.6 8.6 5 2
Antagonist activity at human EP4 receptor expressed in CHO cells coexpressing tTA-dependent luciferase reporter and beta arrestin 2-TEV assessed as reduction in beta-arrestin recruitment preincubated for 30 mins followed by PEG2 addition and measured after 12 hrs by Tango assayAntagonist activity at human EP4 receptor expressed in CHO cells coexpressing tTA-dependent luciferase reporter and beta arrestin 2-TEV assessed as reduction in beta-arrestin recruitment preincubated for 30 mins followed by PEG2 addition and measured after 12 hrs by Tango assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
CHEMBL5186525 1103 None 0 Human Functional pIC50 = 8.6 8.6 5 2
Antagonist activity at human EP4 receptor expressed in CHO cells coexpressing tTA-dependent luciferase reporter and beta arrestin 2-TEV assessed as reduction in beta-arrestin recruitment preincubated for 30 mins followed by PEG2 addition and measured after 12 hrs by Tango assayAntagonist activity at human EP4 receptor expressed in CHO cells coexpressing tTA-dependent luciferase reporter and beta arrestin 2-TEV assessed as reduction in beta-arrestin recruitment preincubated for 30 mins followed by PEG2 addition and measured after 12 hrs by Tango assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
168297548 192332 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 463 7 2 4 5.7 CC(C)c1ccc(Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5204873 192332 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 463 7 2 4 5.7 CC(C)c1ccc(Cc2sc3c(c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)CCOC3)cc1 10.1021/acs.jmedchem.2c00448
46890659 6961 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 466 6 2 3 5.9 C[C@H](NC(=O)c1cccc2ccn(Cc3ccc(C(F)(F)F)cc3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1084553 6961 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 466 6 2 3 5.9 C[C@H](NC(=O)c1cccc2ccn(Cc3ccc(C(F)(F)F)cc3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
23660504 57118 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 484 7 2 4 5.3 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(OC(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645139 57118 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 484 7 2 4 5.3 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(OC(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
138671623 191327 None 0 Mouse Functional pIC50 = 8.6 8.6 -1 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 489 6 2 4 5.6 C[C@H](NC(=O)c1c(Cc2cccc(C(F)(F)F)c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5189703 191327 None 0 Mouse Functional pIC50 = 8.6 8.6 -1 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 489 6 2 4 5.6 C[C@H](NC(=O)c1c(Cc2cccc(C(F)(F)F)c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
89914526 122664 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 414 8 2 4 3.6 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600884 122664 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 414 8 2 4 3.6 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601985 122664 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 414 8 2 4 3.6 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
24952929 2554 None 35 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
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 2554 None 35 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
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 2554 None 35 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
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
57392712 67870 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay
ChEMBL 455 4 2 3 5.8 C[C@H](NC(=O)c1cccc2c1Oc1cc(C(F)(F)F)ccc1CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.08.102
CHEMBL1910022 67870 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay
ChEMBL 455 4 2 3 5.8 C[C@H](NC(=O)c1cccc2c1Oc1cc(C(F)(F)F)ccc1CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.08.102
138670944 190739 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 465 7 2 3 6.1 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCCCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5181142 190739 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 465 7 2 3 6.1 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCCCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
71186498 160295 None 0 Human Functional pIC50 = 7.7 7.7 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 444 6 2 3 4.2 O=C(O)c1ccc(C2(NC(=O)[C@H]3C[C@H]4C[C@H]4N3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
CHEMBL4109532 160295 None 0 Human Functional pIC50 = 7.7 7.7 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 444 6 2 3 4.2 O=C(O)c1ccc(C2(NC(=O)[C@H]3C[C@H]4C[C@H]4N3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
11502889 156151 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 430 6 2 4 5.4 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4062620 156151 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 430 6 2 4 5.4 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
172440113 195358 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 449 8 2 5 4.4 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2CCOc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5401935 195358 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 449 8 2 5 4.4 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2CCOc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.2c02058
23660505 57130 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 425 6 2 4 4.3 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(C#N)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645151 57130 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 425 6 2 4 4.3 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(C#N)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
155555000 174437 None 0 Mouse Functional pIC50 = 6.7 6.7 -15 2
Antagonist activity at mouse EP4 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 mouse EP4 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 450 7 2 5 4.0 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NCC1CCC(C(=O)O)CC1 10.1021/acs.jmedchem.9b01269
CHEMBL4550862 174437 None 0 Mouse Functional pIC50 = 6.7 6.7 -15 2
Antagonist activity at mouse EP4 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 mouse EP4 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 450 7 2 5 4.0 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NCC1CCC(C(=O)O)CC1 10.1021/acs.jmedchem.9b01269
71186236 146402 None 6 Human Functional pIC50 = 7.7 7.7 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 472 6 2 3 5.0 O=C(O)c1ccc(C2(NC(=O)C3CC4(CCN3Cc3ccc(C(F)(F)F)cc3)CC4)CC2)cc1 nan
71186236.0 146402 None 6 Human Functional pIC50 = 7.7 7.7 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 472 6 2 3 5.0 O=C(O)c1ccc(C2(NC(=O)C3CC4(CCN3Cc3ccc(C(F)(F)F)cc3)CC4)CC2)cc1 nan
CHEMBL3920982 146402 None 6 Human Functional pIC50 = 7.7 7.7 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 472 6 2 3 5.0 O=C(O)c1ccc(C2(NC(=O)C3CC4(CCN3Cc3ccc(C(F)(F)F)cc3)CC4)CC2)cc1 nan
90202708 174449 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 423 6 1 4 6.3 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CCC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4551140 174449 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 423 6 1 4 6.3 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CCC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
155561196 175785 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 449 6 1 6 4.7 CCn1c2ccccc2c2cc(-c3nc4cc(S(=O)(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4581855 175785 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 449 6 1 6 4.7 CCn1c2ccccc2c2cc(-c3nc4cc(S(=O)(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
155521209 170676 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human EP4 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 EP4 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 486 6 2 5 4.6 C[C@H](NC(=O)c1c(C(F)(F)F)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4450391 170676 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human EP4 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 EP4 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 486 6 2 5 4.6 C[C@H](NC(=O)c1c(C(F)(F)F)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
167092434 196254 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 481 6 3 4 6.1 C[C@@H](NC(=O)c1c(Nc2cccc(C(F)(F)F)c2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
CHEMBL5419747 196254 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 481 6 3 4 6.1 C[C@@H](NC(=O)c1c(Nc2cccc(C(F)(F)F)c2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
155550848 175225 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human EP4 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 EP4 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 494 7 2 5 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4569593 175225 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human EP4 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 EP4 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 494 7 2 5 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
71186604 149388 None 0 Human Functional pIC50 = 7.6 7.6 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 482 6 2 3 4.8 O=C(O)c1ccc(C2(NC(=O)C3CC(F)(F)CCN3Cc3cccc(C(F)(F)F)c3)CC2)cc1 nan
CHEMBL3944767 149388 None 0 Human Functional pIC50 = 7.6 7.6 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 482 6 2 3 4.8 O=C(O)c1ccc(C2(NC(=O)C3CC(F)(F)CCN3Cc3cccc(C(F)(F)F)c3)CC2)cc1 nan
76281721 176029 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 490 7 1 7 4.2 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)NS(C)(=O)=O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4587481 176029 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 490 7 1 7 4.2 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)NS(C)(=O)=O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
155549272 173937 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human EP4 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 EP4 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 436 6 2 5 3.7 C[C@H](NC(=O)c1c(C(F)(F)F)nnn1Cc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4538786 173937 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human EP4 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 EP4 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 436 6 2 5 3.7 C[C@H](NC(=O)c1c(C(F)(F)F)nnn1Cc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
172464828 196908 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 417 7 2 4 3.9 O=C(O)c1ccc(CCNC(=O)c2c3ccccc3nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5434593 196908 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 417 7 2 4 3.9 O=C(O)c1ccc(CCNC(=O)c2c3ccccc3nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c02058
12017 1103 None 0 Mouse Functional pIC50 = 7.6 7.6 -5 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
138670561 1103 None 0 Mouse Functional pIC50 = 7.6 7.6 -5 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
CHEMBL5186525 1103 None 0 Mouse Functional pIC50 = 7.6 7.6 -5 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
90202404 174084 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 427 6 1 5 5.5 CCn1c2ccccc2c2cc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4541894 174084 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 427 6 1 5 5.5 CCn1c2ccccc2c2cc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
56944705 129281 None 39 Human Functional pIC50 = 7.6 7.6 11 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL3670685 129281 None 39 Human Functional pIC50 = 7.6 7.6 11 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
11683088 159070 None 0 Human Functional pIC50 = 7.6 7.6 275 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4096216 159070 None 0 Human Functional pIC50 = 7.6 7.6 275 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
58905349 156369 None 0 Human Functional pIC50 = 6.6 6.6 12 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 400 6 2 4 4.3 O=C(O)c1ccc(CNC(=O)c2cc(Cl)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4065183 156369 None 0 Human Functional pIC50 = 6.6 6.6 12 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 400 6 2 4 4.3 O=C(O)c1ccc(CNC(=O)c2cc(Cl)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
90202707 173431 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 449 6 1 4 6.7 O=C(O)c1ccc2c(c1)nc(-c1ccc3c(c1)c1ccccc1n3CC1CCC1)n2CC1CC1 10.1021/acs.jmedchem.8b01862
CHEMBL4526568 173431 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 449 6 1 4 6.7 O=C(O)c1ccc2c(c1)nc(-c1ccc3c(c1)c1ccccc1n3CC1CCC1)n2CC1CC1 10.1021/acs.jmedchem.8b01862
53318618 57125 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 401 6 2 4 3.8 C[C@H](NC(=O)c1cccc2c1N(Cc1cccnc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645146 57125 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 401 6 2 4 3.8 C[C@H](NC(=O)c1cccc2c1N(Cc1cccnc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
156073539 191435 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 511 5 2 5 5.6 COc1ccc2cc(C#Cc3sc4c(c3C(=O)N[C@@H](C)c3ccc(C(=O)O)cc3)CCOC4)ccc2c1 10.1021/acs.jmedchem.2c00448
CHEMBL5191478 191435 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 511 5 2 5 5.6 COc1ccc2cc(C#Cc3sc4c(c3C(=O)N[C@@H](C)c3ccc(C(=O)O)cc3)CCOC4)ccc2c1 10.1021/acs.jmedchem.2c00448
141730914 174992 None 0 Mouse Functional pIC50 = 7.6 7.6 -2 2
Antagonist activity at mouse EP4 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 mouse EP4 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 500 7 2 6 5.3 C[C@H](NC(=O)c1c(-c2ccsc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4564092 174992 None 0 Mouse Functional pIC50 = 7.6 7.6 -2 2
Antagonist activity at mouse EP4 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 mouse EP4 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 500 7 2 6 5.3 C[C@H](NC(=O)c1c(-c2ccsc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
138671622 190594 None 0 Human Functional pIC50 = 7.6 7.6 1 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 451 7 2 3 5.7 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5179032 190594 None 0 Human Functional pIC50 = 7.6 7.6 1 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 451 7 2 3 5.7 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
155522808 170936 None 0 Human Functional pIC50 = 7.6 7.6 14 2
Antagonist activity at human EP4 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 EP4 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 484 7 2 5 5.1 C[C@H](NC(=O)c1c(C2=CCCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4453648 170936 None 0 Human Functional pIC50 = 7.6 7.6 14 2
Antagonist activity at human EP4 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 EP4 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 484 7 2 5 5.1 C[C@H](NC(=O)c1c(C2=CCCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
155533165 171942 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human EP4 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 EP4 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 466 8 2 6 3.7 C[C@H](NC(=O)c1c(C(F)(F)F)nnn1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4468734 171942 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human EP4 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 EP4 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 466 8 2 6 3.7 C[C@H](NC(=O)c1c(C(F)(F)F)nnn1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
71186336 160284 None 0 Human Functional pIC50 = 7.6 7.6 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 482 6 2 3 4.8 O=C(O)c1ccc(C2(NC(=O)[C@H]3CC(F)(F)CCN3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
CHEMBL4109410 160284 None 0 Human Functional pIC50 = 7.6 7.6 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 482 6 2 3 4.8 O=C(O)c1ccc(C2(NC(=O)[C@H]3CC(F)(F)CCN3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
76281993 176280 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 422 5 1 4 5.6 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)NC)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4593176 176280 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 422 5 1 4 5.6 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)NC)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
138671622 190594 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 451 7 2 3 5.7 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5179032 190594 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 451 7 2 3 5.7 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCCC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
71186475 151753 None 0 Human Functional pIC50 = 7.5 7.5 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 460 6 2 3 5.0 C[C@H](NC(=O)C1CC2(CCN1Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 nan
CHEMBL3963981 151753 None 0 Human Functional pIC50 = 7.5 7.5 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 460 6 2 3 5.0 C[C@H](NC(=O)C1CC2(CCN1Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 nan
155515639 170092 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4 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 EP4 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 474 8 2 6 4.3 COc1ccc(Cn2nnc(-c3ccccc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)cc1F 10.1021/acs.jmedchem.9b01269
CHEMBL4442135 170092 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4 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 EP4 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 474 8 2 6 4.3 COc1ccc(Cn2nnc(-c3ccccc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)cc1F 10.1021/acs.jmedchem.9b01269
137643633 158268 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 380 6 2 4 4.0 Cc1cnc(Oc2ccc(F)cc2)c(C(=O)NCc2ccc(C(=O)O)cc2)c1 10.1016/j.bmcl.2017.01.067
CHEMBL4087592 158268 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 380 6 2 4 4.0 Cc1cnc(Oc2ccc(F)cc2)c(C(=O)NCc2ccc(C(=O)O)cc2)c1 10.1016/j.bmcl.2017.01.067
25018911 57714 None 7 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2015.12.057
CHEMBL1669008 57714 None 7 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2015.12.057
53326475 57133 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 536 6 2 3 6.5 C[C@H](NC(=O)c1cc(C(F)(F)F)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645154 57133 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 536 6 2 3 6.5 C[C@H](NC(=O)c1cc(C(F)(F)F)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
118174968 136705 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 426 5 3 4 5.0 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3739779 136705 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 426 5 3 4 5.0 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
141730916 169894 None 0 Human Functional pIC50 = 8.5 8.5 42 2
Antagonist activity at human EP4 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 EP4 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 474 9 2 6 4.4 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4439228 169894 None 0 Human Functional pIC50 = 8.5 8.5 42 2
Antagonist activity at human EP4 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 EP4 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 474 9 2 6 4.4 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
138670968 191743 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 455 6 2 4 5.3 C[C@H](NC(=O)c1c(Cc2cccc(Cl)c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5195791 191743 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 455 6 2 4 5.3 C[C@H](NC(=O)c1c(Cc2cccc(Cl)c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
46890616 7088 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 450 6 2 3 5.7 C[C@H](NC(=O)c1cc(F)cc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1085041 7088 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 450 6 2 3 5.7 C[C@H](NC(=O)c1cc(F)cc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
138671595 190512 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 475 6 2 4 5.1 O=C(O)c1ccc(CNC(=O)c2c(Cc3cccc(C(F)(F)F)c3)sc3c2CCOC3)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5177678 190512 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 475 6 2 4 5.1 O=C(O)c1ccc(CNC(=O)c2c(Cc3cccc(C(F)(F)F)c3)sc3c2CCOC3)cc1 10.1021/acs.jmedchem.2c00448
138671612 190796 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 451 6 2 4 4.7 O=C(O)c1ccc(C2(NC(=O)c3c(Cc4ccc(F)cc4)sc4c3CCOC4)CC2)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5181946 190796 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 451 6 2 4 4.7 O=C(O)c1ccc(C2(NC(=O)c3c(Cc4ccc(F)cc4)sc4c3CCOC4)CC2)cc1 10.1021/acs.jmedchem.2c00448
118191080 136950 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 395 4 2 2 6.1 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2ccccc2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3742015 136950 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 395 4 2 2 6.1 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2ccccc2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
23661015 57131 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 492 6 2 5 4.9 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(-c2nn[nH]n2)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645152 57131 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 492 6 2 5 4.9 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(-c2nn[nH]n2)cc1 10.1016/j.bmcl.2010.10.106
24952580 203018 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 467 6 2 3 6.5 C[C@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
CHEMBL599052 203018 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 467 6 2 3 6.5 C[C@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
118175009 136772 None 0 Human Functional pIC50 = 8.4 8.4 125 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.12.057
CHEMBL3740325 136772 None 0 Human Functional pIC50 = 8.4 8.4 125 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.12.057
118175009 136772 None 0 Human Functional pIC50 = 8.4 8.4 125 2
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3740325 136772 None 0 Human Functional pIC50 = 8.4 8.4 125 2
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
172439276 195400 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 437 6 2 4 4.5 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(F)c(Cl)c2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5402938 195400 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 437 6 2 4 4.5 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(F)c(Cl)c2)cc1 10.1021/acs.jmedchem.2c02058
138671633 191610 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 431 6 2 4 4.2 O=C(NCC1CCC(C(=O)O)CC1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
CHEMBL5193793 191610 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 431 6 2 4 4.2 O=C(NCC1CCC(C(=O)O)CC1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
11575201 157514 None 0 Human Functional pIC50 = 7.5 7.5 100 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 413 6 2 3 5.5 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4078648 157514 None 0 Human Functional pIC50 = 7.5 7.5 100 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 413 6 2 3 5.5 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
137633794 156546 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 609 9 2 7 5.7 O=C(NCc1ccc(C(=O)NS(=O)(=O)c2cccc(Cl)c2)cc1)c1cccc(OCc2nc3cc(F)ccc3s2)c1 10.1016/j.bmcl.2017.01.067
CHEMBL4067234 156546 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 609 9 2 7 5.7 O=C(NCc1ccc(C(=O)NS(=O)(=O)c2cccc(Cl)c2)cc1)c1cccc(OCc2nc3cc(F)ccc3s2)c1 10.1016/j.bmcl.2017.01.067
172458649 196456 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at EP4 receptor (unknown origin) by GloSensor cAMP assayAntagonist activity at EP4 receptor (unknown origin) by GloSensor cAMP assay
ChEMBL 389 5 2 4 4.2 O=C(O)c1ccc(NC(=O)c2c3ccccc3nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5424332 196456 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at EP4 receptor (unknown origin) by GloSensor cAMP assayAntagonist activity at EP4 receptor (unknown origin) by GloSensor cAMP assay
ChEMBL 389 5 2 4 4.2 O=C(O)c1ccc(NC(=O)c2c3ccccc3nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c02058
155568276 176205 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 431 4 1 4 6.5 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3-c3ccccc3)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4591445 176205 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 431 4 1 4 6.5 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3-c3ccccc3)ccc21 10.1021/acs.jmedchem.8b01862
156073545 191612 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 552 7 2 5 6.2 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCN(C(=O)OC(C)(C)C)C2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5193807 191612 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 552 7 2 5 6.2 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCN(C(=O)OC(C)(C)C)C2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
58905388 158758 None 0 Human Functional pIC50 = 6.5 6.5 1 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 383 6 2 3 4.4 O=C(O)c1ccc(CNC(=O)c2cc(F)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4092846 158758 None 0 Human Functional pIC50 = 6.5 6.5 1 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 383 6 2 3 4.4 O=C(O)c1ccc(CNC(=O)c2cc(F)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
141730897 176220 None 0 Human Functional pIC50 = 7.5 7.5 2 3
Antagonist activity at human EP4 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 EP4 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 176220 None 0 Human Functional pIC50 = 7.5 7.5 2 3
Antagonist activity at human EP4 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 EP4 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
71186600 167722 None 0 Human Functional pIC50 = 7.5 7.5 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 446 6 2 3 4.6 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
CHEMBL4111996 167722 None 0 Human Functional pIC50 = 7.5 7.5 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 446 6 2 3 4.6 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
CHEMBL4301416 167722 None 0 Human Functional pIC50 = 7.5 7.5 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 446 6 2 3 4.6 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
138671611 191251 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 504 7 3 5 5.6 C[C@H](NC(=O)c1c(NCc2ccc(C(F)(F)F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5188328 191251 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 504 7 3 5 5.6 C[C@H](NC(=O)c1c(NCc2ccc(C(F)(F)F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
155554096 175547 None 0 Mouse Functional pIC50 = 7.5 7.5 -2 2
Antagonist activity at mouse EP4 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 mouse EP4 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 470 7 2 5 4.5 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NC1(c2ccc(C(=O)O)cc2)CC1 10.1021/acs.jmedchem.9b01269
CHEMBL4576681 175547 None 0 Mouse Functional pIC50 = 7.5 7.5 -2 2
Antagonist activity at mouse EP4 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 mouse EP4 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 470 7 2 5 4.5 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)NC1(c2ccc(C(=O)O)cc2)CC1 10.1021/acs.jmedchem.9b01269
76282475 175304 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 435 6 1 4 6.3 O=C(O)c1ccc2c(c1)nc(-c1ccc3c(c1)c1ccccc1n3CC1CC1)n2CC1CC1 10.1021/acs.jmedchem.8b01862
CHEMBL4571025 175304 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 435 6 1 4 6.3 O=C(O)c1ccc2c(c1)nc(-c1ccc3c(c1)c1ccccc1n3CC1CC1)n2CC1CC1 10.1021/acs.jmedchem.8b01862
155516871 170227 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human EP4 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 EP4 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 444 7 2 5 4.3 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4443888 170227 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human EP4 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 EP4 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 444 7 2 5 4.3 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
138670951 192537 None 0 Mouse Functional pIC50 = 6.5 6.5 -162 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 489 6 2 4 5.6 C[C@H](NC(=O)c1c(Cc2ccc(C(F)(F)F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5208220 192537 None 0 Mouse Functional pIC50 = 6.5 6.5 -162 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 489 6 2 4 5.6 C[C@H](NC(=O)c1c(Cc2ccc(C(F)(F)F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
57399661 67873 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay
ChEMBL 467 4 2 3 5.7 O=C(O)c1ccc(C2(NC(=O)c3cccc4c3Oc3ccc(C(F)(F)F)cc3CC4)CC2)cc1 10.1016/j.bmcl.2011.08.102
CHEMBL1910025 67873 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay
ChEMBL 467 4 2 3 5.7 O=C(O)c1ccc(C2(NC(=O)c3cccc4c3Oc3ccc(C(F)(F)F)cc3CC4)CC2)cc1 10.1016/j.bmcl.2011.08.102
76282476 174692 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 395 4 1 4 5.5 Cn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4556932 174692 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 395 4 1 4 5.5 Cn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
90202545 173624 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 431 6 1 5 5.3 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)c(F)cc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4530975 173624 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 431 6 1 5 5.3 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)c(F)cc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
58905312 157128 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 426 7 2 5 4.7 COc1cccc(Oc2ncc(Cl)cc2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1 10.1016/j.bmcl.2017.01.067
CHEMBL4073631 157128 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 426 7 2 5 4.7 COc1cccc(Oc2ncc(Cl)cc2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1 10.1016/j.bmcl.2017.01.067
89914863 122663 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 421 8 2 5 3.4 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(C#N)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600883 122663 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 421 8 2 5 3.4 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(C#N)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601984 122663 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 421 8 2 5 3.4 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(C#N)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
11618662 158914 None 0 Human Functional pIC50 = 7.4 7.4 151 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 421 6 2 5 4.6 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(C#N)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4094572 158914 None 0 Human Functional pIC50 = 7.4 7.4 151 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 421 6 2 5 4.6 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(C#N)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
138670964 192216 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 481 7 2 4 5.7 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CC(C)(C)OC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5203156 192216 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 481 7 2 4 5.7 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CC(C)(C)OC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
171361355 196742 None 1 Rat Functional pIC50 = 7.4 7.4 -22 3
Antagonist activity at rat EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at rat EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5431224 196742 None 1 Rat Functional pIC50 = 7.4 7.4 -22 3
Antagonist activity at rat EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at rat EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
156073536 191796 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 481 6 2 4 5.1 O=C(NCC1CCC(C(=O)O)CC1)c1c(Cc2cccc(C(F)(F)F)c2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
CHEMBL5196717 191796 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 481 6 2 4 5.1 O=C(NCC1CCC(C(=O)O)CC1)c1c(Cc2cccc(C(F)(F)F)c2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
155520059 173345 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 511 7 1 6 6.4 CCn1c2ccc(OC(F)(F)F)cc2c2cc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4524507 173345 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 511 7 1 6 6.4 CCn1c2ccc(OC(F)(F)F)cc2c2cc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
137648241 158076 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 436 7 2 5 4.6 O=C(O)c1ccc(CNC(=O)c2cccc(OCc3nc4cc(F)ccc4s3)c2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4085097 158076 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 436 7 2 5 4.6 O=C(O)c1ccc(CNC(=O)c2cccc(OCc3nc4cc(F)ccc4s3)c2)cc1 10.1016/j.bmcl.2017.01.067
11524454 946 None 36 Human Functional pIC50 = 7.4 7.4 52 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
5857 946 None 36 Human Functional pIC50 = 7.4 7.4 52 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
CHEMBL591666 946 None 36 Human Functional pIC50 = 7.4 7.4 52 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
86707352 139524 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 397 4 3 5 3.3 Cc1ccc(N2CCC(C)(O)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
CHEMBL3793924 139524 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 397 4 3 5 3.3 Cc1ccc(N2CCC(C)(O)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
71186491 143313 None 0 Human Functional pIC50 = 8.4 8.4 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 472 6 2 3 5.0 O=C(O)c1ccc(C2(NC(=O)C3CC4(CCN3Cc3cccc(C(F)(F)F)c3)CC4)CC2)cc1 nan
CHEMBL3896466 143313 None 0 Human Functional pIC50 = 8.4 8.4 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 472 6 2 3 5.0 O=C(O)c1ccc(C2(NC(=O)C3CC4(CCN3Cc3cccc(C(F)(F)F)c3)CC4)CC2)cc1 nan
171361355 196742 None 1 Human Functional pIC50 = 8.4 8.4 -1 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced CRE-mediated gene transcription preincubated with compound followed by PGE2 stimulation and measured after 12 hrs by firefly luciferase assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced CRE-mediated gene transcription preincubated with compound followed by PGE2 stimulation and measured after 12 hrs by firefly luciferase assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5431224 196742 None 1 Human Functional pIC50 = 8.4 8.4 -1 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced CRE-mediated gene transcription preincubated with compound followed by PGE2 stimulation and measured after 12 hrs by firefly luciferase assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced CRE-mediated gene transcription preincubated with compound followed by PGE2 stimulation and measured after 12 hrs by firefly luciferase assay
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
172452597 195774 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 399 6 2 4 4.0 Cc1ccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5410514 195774 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 399 6 2 4 4.0 Cc1ccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1 10.1021/acs.jmedchem.2c02058
129161002 173236 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 441 6 1 5 5.8 CCn1c2ccc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)cc2c2cccc(C)c21 10.1021/acs.jmedchem.8b01862
CHEMBL4520937 173236 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 441 6 1 5 5.8 CCn1c2ccc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)cc2c2cccc(C)c21 10.1021/acs.jmedchem.8b01862
168355579 196173 None 6 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 481 6 3 4 6.1 C[C@H](NC(=O)c1c(Nc2cccc(C(F)(F)F)c2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
CHEMBL5418164 196173 None 6 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 481 6 3 4 6.1 C[C@H](NC(=O)c1c(Nc2cccc(C(F)(F)F)c2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
12017 1103 None 0 Human Functional pIC50 = 8.4 8.4 5 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
138670561 1103 None 0 Human Functional pIC50 = 8.4 8.4 5 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
CHEMBL5186525 1103 None 0 Human Functional pIC50 = 8.4 8.4 5 2
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
172451670 195906 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 483 7 2 5 5.2 C[C@H](NC(=O)c1c2ccccc2nn1Cc1ccc(OC(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5413066 195906 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 483 7 2 5 5.2 C[C@H](NC(=O)c1c2ccccc2nn1Cc1ccc(OC(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
90202587 174331 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 431 6 1 5 5.3 CCn1c2ccccc2c2cc(-c3nc4c(F)c(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4548693 174331 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 431 6 1 5 5.3 CCn1c2ccccc2c2cc(-c3nc4c(F)c(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
172466722 196548 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 415 7 2 5 3.7 COc1ccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5426459 196548 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 415 7 2 5 3.7 COc1ccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1 10.1021/acs.jmedchem.2c02058
90202660 173014 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 461 6 1 5 6.1 CCn1c2ccc(Cl)cc2c2cc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4516303 173014 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 461 6 1 5 6.1 CCn1c2ccc(Cl)cc2c2cc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
118175029 137468 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 393 5 3 3 4.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)ccc1F 10.1016/j.bmcl.2015.12.057
CHEMBL3753133 137468 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 1 hr by HTRF assay
ChEMBL 393 5 3 3 4.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)ccc1F 10.1016/j.bmcl.2015.12.057
24952927 203688 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(C(F)(F)F)cc1 10.1021/jm901771h
CHEMBL603690 203688 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(C(F)(F)F)cc1 10.1021/jm901771h
138670563 190450 None 6 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 439 6 2 4 4.7 C[C@H](NC(=O)c1c(Cc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5176688 190450 None 6 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 439 6 2 4 4.7 C[C@H](NC(=O)c1c(Cc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
56944705 129281 None 39 Human Functional pIC50 = 8.4 8.4 11 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced beta-arrestin recruitment preincubated with compound for 20 mins followed by PGE2 stimulation and measured after 12 hrs by Tango assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced beta-arrestin recruitment preincubated with compound for 20 mins followed by PGE2 stimulation and measured after 12 hrs by Tango assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL3670685 129281 None 39 Human Functional pIC50 = 8.4 8.4 11 3
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced beta-arrestin recruitment preincubated with compound for 20 mins followed by PGE2 stimulation and measured after 12 hrs by Tango assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced beta-arrestin recruitment preincubated with compound for 20 mins followed by PGE2 stimulation and measured after 12 hrs by Tango assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
155554217 174311 None 0 Human Functional pIC50 = 8.3 8.3 9 2
Antagonist activity at human EP4 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 EP4 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 514 7 2 6 5.6 Cc1ccc(-c2nnn(Cc3ccc(C(F)(F)F)cc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)s1 10.1021/acs.jmedchem.9b01269
CHEMBL4548291 174311 None 0 Human Functional pIC50 = 8.3 8.3 9 2
Antagonist activity at human EP4 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 EP4 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 514 7 2 6 5.6 Cc1ccc(-c2nnn(Cc3ccc(C(F)(F)F)cc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)s1 10.1021/acs.jmedchem.9b01269
24953625 203989 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(C(F)(F)F)c1 10.1021/jm901771h
CHEMBL605330 203989 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(C(F)(F)F)c1 10.1021/jm901771h
74762651 172588 None 0 Human Functional pIC50 = 8.3 8.3 17 2
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 413 6 1 5 5.2 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4483026 172588 None 0 Human Functional pIC50 = 8.3 8.3 17 2
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 413 6 1 5 5.2 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
23660845 57128 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 546 6 2 3 6.2 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(F)(F)F)cc1Br)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645149 57128 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 546 6 2 3 6.2 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(F)(F)F)cc1Br)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
58905340 158888 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 442 7 2 5 5.4 CSc1cccc(Oc2ncc(Cl)cc2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1 10.1016/j.bmcl.2017.01.067
CHEMBL4094257 158888 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 442 7 2 5 5.4 CSc1cccc(Oc2ncc(Cl)cc2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1 10.1016/j.bmcl.2017.01.067
155522808 170936 None 0 Mouse Functional pIC50 = 6.4 6.4 -14 2
Antagonist activity at mouse EP4 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 mouse EP4 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 484 7 2 5 5.1 C[C@H](NC(=O)c1c(C2=CCCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4453648 170936 None 0 Mouse Functional pIC50 = 6.4 6.4 -14 2
Antagonist activity at mouse EP4 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 mouse EP4 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 484 7 2 5 5.1 C[C@H](NC(=O)c1c(C2=CCCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
11718930 158974 None 1 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 429 6 2 3 6.0 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4095176 158974 None 1 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 429 6 2 3 6.0 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
57401413 67872 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay
ChEMBL 455 4 2 3 5.8 C[C@H](NC(=O)c1cccc2c1Oc1ccc(C(F)(F)F)cc1CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.08.102
CHEMBL1910024 67872 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay
ChEMBL 455 4 2 3 5.8 C[C@H](NC(=O)c1cccc2c1Oc1ccc(C(F)(F)F)cc1CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.08.102
71204738 152213 None 0 Human Functional pIC50 = 7.4 7.4 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 446 6 2 3 4.6 C[C@H](NC(=O)[C@H]1CCC2CC2N1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 nan
CHEMBL3967868 152213 None 0 Human Functional pIC50 = 7.4 7.4 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 446 6 2 3 4.6 C[C@H](NC(=O)[C@H]1CCC2CC2N1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 nan
155554217 174311 None 0 Mouse Functional pIC50 = 7.4 7.4 -9 2
Antagonist activity at mouse EP4 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 mouse EP4 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 514 7 2 6 5.6 Cc1ccc(-c2nnn(Cc3ccc(C(F)(F)F)cc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)s1 10.1021/acs.jmedchem.9b01269
CHEMBL4548291 174311 None 0 Mouse Functional pIC50 = 7.4 7.4 -9 2
Antagonist activity at mouse EP4 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 mouse EP4 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 514 7 2 6 5.6 Cc1ccc(-c2nnn(Cc3ccc(C(F)(F)F)cc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)s1 10.1021/acs.jmedchem.9b01269
25019183 57718 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 647 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669012 57718 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 647 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
71502439 160169 None 0 Human Functional pIC50 = 7.4 7.4 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 458 6 2 3 4.6 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCC4CC4N3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
CHEMBL4108479 160169 None 0 Human Functional pIC50 = 7.4 7.4 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 458 6 2 3 4.6 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCC4CC4N3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 nan
90202554 175690 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 453 6 1 7 4.8 CCn1c2ccccc2c2cc(-c3nc4cc(-c5n[nH]c(=O)o5)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4579666 175690 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 453 6 1 7 4.8 CCn1c2ccccc2c2cc(-c3nc4cc(-c5n[nH]c(=O)o5)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
172467840 196976 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 447 6 3 4 5.8 C[C@H](NC(=O)c1c(Nc2cccc(Cl)c2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
CHEMBL5435929 196976 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 447 6 3 4 5.8 C[C@H](NC(=O)c1c(Nc2cccc(Cl)c2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
141730923 169971 None 0 Human Functional pIC50 = 7.3 7.3 1 2
Antagonist activity at human EP4 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 EP4 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 484 7 2 6 4.8 C[C@H](NC(=O)c1c(-c2ccoc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4440382 169971 None 0 Human Functional pIC50 = 7.3 7.3 1 2
Antagonist activity at human EP4 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 EP4 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 484 7 2 6 4.8 C[C@H](NC(=O)c1c(-c2ccoc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
172468536 196587 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 493 6 3 4 6.1 Cn1c(C(=O)NC2(c3ccc(C(=O)O)cc3)CC2)c(Nc2cccc(C(F)(F)F)c2)c2ccccc21 10.1021/acsmedchemlett.2c00495
CHEMBL5427309 196587 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 493 6 3 4 6.1 Cn1c(C(=O)NC2(c3ccc(C(=O)O)cc3)CC2)c(Nc2cccc(C(F)(F)F)c2)c2ccccc21 10.1021/acsmedchemlett.2c00495
141730904 175479 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4 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 EP4 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 524 9 2 6 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1CCOc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4574900 175479 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4 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 EP4 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 524 9 2 6 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1CCOc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
172459261 196252 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 417 6 2 4 4.4 C[C@H](NC(=O)c1c2ccccc2nn1Cc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5419736 196252 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 417 6 2 4 4.4 C[C@H](NC(=O)c1c2ccccc2nn1Cc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
12017 1103 None 0 Human Functional pIC50 = 8.3 8.3 5 2
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by GloSensor cAMP assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by GloSensor cAMP assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
138670561 1103 None 0 Human Functional pIC50 = 8.3 8.3 5 2
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by GloSensor cAMP assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by GloSensor cAMP assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
CHEMBL5186525 1103 None 0 Human Functional pIC50 = 8.3 8.3 5 2
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by GloSensor cAMP assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by GloSensor cAMP assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
138670961 192165 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 439 6 2 4 4.7 C[C@H](NC(=O)c1c(Cc2cccc(F)c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5202462 192165 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 439 6 2 4 4.7 C[C@H](NC(=O)c1c(Cc2cccc(F)c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
118191085 136938 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 426 5 3 4 5.0 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3741902 136938 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 426 5 3 4 5.0 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
90202434 173459 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 461 6 1 5 6.1 CCn1c2ccc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)cc2c2cccc(Cl)c21 10.1021/acs.jmedchem.8b01862
CHEMBL4527180 173459 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 461 6 1 5 6.1 CCn1c2ccc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)cc2c2cccc(Cl)c21 10.1021/acs.jmedchem.8b01862
146014480 173818 None 18 Human Functional pIC50 = 8.3 8.3 4 2
Inhibition of human EP4 transfected in human HEK293 cells co transfected with CRE-luciferase assessed as reduction in PGE2-induced luciferase expression incubated for 24 hrs by luciferase reporter gene AssayInhibition of human EP4 transfected in human HEK293 cells co transfected with CRE-luciferase assessed as reduction in PGE2-induced luciferase expression incubated for 24 hrs by luciferase reporter gene Assay
ChEMBL 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4535971 173818 None 18 Human Functional pIC50 = 8.3 8.3 4 2
Inhibition of human EP4 transfected in human HEK293 cells co transfected with CRE-luciferase assessed as reduction in PGE2-induced luciferase expression incubated for 24 hrs by luciferase reporter gene AssayInhibition of human EP4 transfected in human HEK293 cells co transfected with CRE-luciferase assessed as reduction in PGE2-induced luciferase expression incubated for 24 hrs by luciferase reporter gene Assay
ChEMBL 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
24953628 203059 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(Cl)cc1 10.1021/jm901771h
CHEMBL599262 203059 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(Cl)cc1 10.1021/jm901771h
172446661 194973 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 467 6 2 4 5.3 C[C@H](NC(=O)c1c2ccccc2nn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5394316 194973 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 467 6 2 4 5.3 C[C@H](NC(=O)c1c2ccccc2nn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
89914524 122661 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 408 8 2 4 3.4 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3CCOc3ccccc3)CC2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600788 122661 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 408 8 2 4 3.4 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3CCOc3ccccc3)CC2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601973 122661 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 408 8 2 4 3.4 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3CCOc3ccccc3)CC2)cc1 10.1016/j.bmcl.2015.05.091
72695136 131403 None 2 Human Functional pIC50 = 8.3 8.3 -2 2
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 383 4 3 5 2.9 Cc1ccc(N2CCC(O)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
CHEMBL3686863 131403 None 2 Human Functional pIC50 = 8.3 8.3 -2 2
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 383 4 3 5 2.9 Cc1ccc(N2CCC(O)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
72695027 106322 None 0 Human Functional pIC50 = 8.3 8.3 -2 3
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3115074 106322 None 0 Human Functional pIC50 = 8.3 8.3 -2 3
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3138992 106322 None 0 Human Functional pIC50 = 8.3 8.3 -2 3
Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMPAntagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scintillation proximity assay in presence of [125I]-cAMP
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
118191081 136661 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 395 4 2 2 6.1 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2ccccc2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3739435 136661 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationAntagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation
ChEMBL 395 4 2 2 6.1 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2ccccc2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
172450528 195803 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 471 6 2 4 4.9 O=C(O)c1ccc(CNC(=O)c2c3ccc(F)cc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5411028 195803 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 471 6 2 4 4.9 O=C(O)c1ccc(CNC(=O)c2c3ccc(F)cc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
53323904 57127 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 414 6 2 3 4.7 Cc1ccc(CN2CCc3cccc(C(=O)N[C@@H](C)c4ccc(C(=O)O)cc4)c32)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645148 57127 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 414 6 2 3 4.7 Cc1ccc(CN2CCc3cccc(C(=O)N[C@@H](C)c4ccc(C(=O)O)cc4)c32)cc1 10.1016/j.bmcl.2010.10.106
24765672 7091 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 432 6 2 3 5.5 C[C@H](NC(=O)c1cccc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1085081 7091 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 432 6 2 3 5.5 C[C@H](NC(=O)c1cccc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
71502474 154630 None 0 Human Functional pIC50 = 7.3 7.3 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 420 6 2 3 4.2 C[C@H](NC(=O)[C@H]1CCCN1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 nan
CHEMBL3894772 154630 None 0 Human Functional pIC50 = 7.3 7.3 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 420 6 2 3 4.2 C[C@H](NC(=O)[C@H]1CCCN1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 nan
CHEMBL3990930 154630 None 0 Human Functional pIC50 = 7.3 7.3 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 420 6 2 3 4.2 C[C@H](NC(=O)[C@H]1CCCN1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 nan
138672156 191685 None 0 Mouse Functional pIC50 = 7.3 7.3 -2 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 453 7 2 4 4.9 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5195058 191685 None 0 Mouse Functional pIC50 = 7.3 7.3 -2 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 453 7 2 4 4.9 C[C@H](NC(=O)c1c(CCc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
90202594 175955 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 425 5 1 5 5.3 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CCO3)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4585611 175955 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 425 5 1 5 5.3 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CCO3)ccc21 10.1021/acs.jmedchem.8b01862
155541822 173177 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4 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 EP4 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 458 7 2 5 4.4 C[C@H](NC(=O)c1c(C2CC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4519666 173177 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4 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 EP4 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 458 7 2 5 4.4 C[C@H](NC(=O)c1c(C2CC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
155556156 174606 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 441 6 1 5 5.8 CCn1c2ccc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)cc2c2c(C)cccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4554923 174606 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 441 6 1 5 5.8 CCn1c2ccc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)cc2c2c(C)cccc21 10.1021/acs.jmedchem.8b01862
172464304 196869 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 481 6 3 4 6.1 C[C@H](NC(=O)c1c(Nc2ccc(C(F)(F)F)cc2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
CHEMBL5433739 196869 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 481 6 3 4 6.1 C[C@H](NC(=O)c1c(Nc2ccc(C(F)(F)F)cc2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
172466349 196596 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 458 7 3 6 5.0 C[C@H](NC(=O)c1c(Nc2cccc([N+](=O)[O-])c2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
CHEMBL5427471 196596 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 458 7 3 6 5.0 C[C@H](NC(=O)c1c(Nc2cccc([N+](=O)[O-])c2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
141730923 169971 None 0 Mouse Functional pIC50 = 7.2 7.2 -1 2
Antagonist activity at mouse EP4 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 mouse EP4 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 484 7 2 6 4.8 C[C@H](NC(=O)c1c(-c2ccoc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4440382 169971 None 0 Mouse Functional pIC50 = 7.2 7.2 -1 2
Antagonist activity at mouse EP4 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 mouse EP4 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 484 7 2 6 4.8 C[C@H](NC(=O)c1c(-c2ccoc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
155560334 175170 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 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 EP4 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 512 7 2 5 5.3 C[C@H](NC(=O)c1c(-c2ccc(F)cc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4568156 175170 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 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 EP4 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 512 7 2 5 5.3 C[C@H](NC(=O)c1c(-c2ccc(F)cc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
58905358 159685 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 384 6 2 4 3.8 O=C(O)c1ccc(CNC(=O)c2cc(F)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4103046 159685 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 384 6 2 4 3.8 O=C(O)c1ccc(CNC(=O)c2cc(F)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
172455873 196329 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 483 7 2 5 4.7 COc1ccc2c(C(=O)NCc3ccc(C(=O)O)cc3)n(Cc3ccc(C(F)(F)F)cc3)nc2c1 10.1021/acs.jmedchem.2c02058
CHEMBL5421486 196329 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 483 7 2 5 4.7 COc1ccc2c(C(=O)NCc3ccc(C(=O)O)cc3)n(Cc3ccc(C(F)(F)F)cc3)nc2c1 10.1021/acs.jmedchem.2c02058
24765672 7091 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 432 6 2 3 5.5 C[C@H](NC(=O)c1cccc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1085081 7091 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 432 6 2 3 5.5 C[C@H](NC(=O)c1cccc2ccn(Cc3cccc(Cl)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
146014480 173818 None 18 Human Functional pIC50 = 8.2 8.2 4 2
Antagonist activity at human EP4 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 EP4 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 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4535971 173818 None 18 Human Functional pIC50 = 8.2 8.2 4 2
Antagonist activity at human EP4 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 EP4 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 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
136216100 175791 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 453 6 1 7 4.8 CCn1c2ccccc2c2cc(-c3nc4cc(-c5noc(=O)[nH]5)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4581918 175791 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 453 6 1 7 4.8 CCn1c2ccccc2c2cc(-c3nc4cc(-c5noc(=O)[nH]5)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
53317328 57115 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 418 6 2 3 4.6 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645136 57115 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 418 6 2 3 4.6 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
172452269 196065 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 449 7 2 5 4.4 COc1ccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1Cl 10.1021/acs.jmedchem.2c02058
CHEMBL5416297 196065 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 449 7 2 5 4.4 COc1ccc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1Cl 10.1021/acs.jmedchem.2c02058
168271481 190721 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 539 7 2 5 6.2 C[C@H](NC(=O)c1c(Cc2ccc(OC(F)(F)F)c(Cl)c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5180884 190721 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 539 7 2 5 6.2 C[C@H](NC(=O)c1c(Cc2ccc(OC(F)(F)F)c(Cl)c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
76284477 172931 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 437 6 1 7 4.7 CCn1c2ccccc2c2cc(-c3nc4cc(-c5nnn[nH]5)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4514122 172931 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 437 6 1 7 4.7 CCn1c2ccccc2c2cc(-c3nc4cc(-c5nnn[nH]5)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
72695027 106322 None 0 Human Functional pIC50 = 8.2 8.2 -2 3
Antagonist activity at human EP4 receptor expressed in recombinant HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human EP4 receptor expressed in recombinant HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
CHEMBL3115074 106322 None 0 Human Functional pIC50 = 8.2 8.2 -2 3
Antagonist activity at human EP4 receptor expressed in recombinant HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human EP4 receptor expressed in recombinant HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
CHEMBL3138992 106322 None 0 Human Functional pIC50 = 8.2 8.2 -2 3
Antagonist activity at human EP4 receptor expressed in recombinant HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human EP4 receptor expressed in recombinant HEK293 cells assessed as inhibition of PGE2-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
172440877 195024 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 419 6 2 4 4.4 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5395138 195024 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 419 6 2 4 4.4 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.2c02058
172439206 195373 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 479 6 2 4 5.2 O=C(O)c1ccc(C2(NC(=O)c3c4ccccc4nn3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5402258 195373 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 479 6 2 4 5.2 O=C(O)c1ccc(C2(NC(=O)c3c4ccccc4nn3Cc3ccc(C(F)(F)F)cc3)CC2)cc1 10.1021/acs.jmedchem.2c02058
172461314 196721 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 427 6 3 4 5.4 Cc1cccc(Nc2c(C(=O)N[C@@H](C)c3ccc(C(=O)O)cc3)n(C)c3ccccc23)c1 10.1021/acsmedchemlett.2c00495
CHEMBL5430749 196721 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 427 6 3 4 5.4 Cc1cccc(Nc2c(C(=O)N[C@@H](C)c3ccc(C(=O)O)cc3)n(C)c3ccccc23)c1 10.1021/acsmedchemlett.2c00495
137640686 157153 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 464 6 2 4 5.7 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4074035 157153 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 464 6 2 4 5.7 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
137637160 156303 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccccc1F)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4064393 156303 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccccc1F)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
90202748 174731 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 427 6 1 5 5.5 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)c(C)cc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4557909 174731 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 427 6 1 5 5.5 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)c(C)cc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
53323098 57719 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(C)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669013 57719 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(C)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
90202705 173544 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 423 6 1 4 6.3 CCCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4529022 173544 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 423 6 1 4 6.3 CCCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CC3)ccc21 10.1021/acs.jmedchem.8b01862
156073541 192004 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 448 4 3 5 3.1 C[C@H](NC(=O)c1c(C#Cc2ccc(=O)[nH]c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5199895 192004 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 448 4 3 5 3.1 C[C@H](NC(=O)c1c(C#Cc2ccc(=O)[nH]c2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
155516014 170147 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4 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 EP4 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 426 7 2 5 4.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4442888 170147 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4 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 EP4 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 426 7 2 5 4.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
168269127 190091 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 479 8 2 3 6.4 CCC1CCc2c(sc(CCc3ccc(F)cc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)C1 10.1021/acs.jmedchem.2c00448
CHEMBL5170985 190091 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 479 8 2 3 6.4 CCC1CCc2c(sc(CCc3ccc(F)cc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)C1 10.1021/acs.jmedchem.2c00448
155531552 171783 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 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 EP4 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 486 7 2 5 5.2 C[C@H](NC(=O)c1c(C2CCCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4466382 171783 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 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 EP4 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 486 7 2 5 5.2 C[C@H](NC(=O)c1c(C2CCCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
155548433 173857 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 461 6 1 5 6.1 CCn1c2ccc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)cc2c2c(Cl)cccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4536877 173857 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 461 6 1 5 6.1 CCn1c2ccc(-c3nc4c(C)c(C(=O)O)ccc4n3CCOC)cc2c2c(Cl)cccc21 10.1021/acs.jmedchem.8b01862
138671611 191251 None 0 Mouse Functional pIC50 = 7.2 7.2 -1 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 504 7 3 5 5.6 C[C@H](NC(=O)c1c(NCc2ccc(C(F)(F)F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5188328 191251 None 0 Mouse Functional pIC50 = 7.2 7.2 -1 2
Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 504 7 3 5 5.6 C[C@H](NC(=O)c1c(NCc2ccc(C(F)(F)F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
172460302 196145 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 385 6 2 4 3.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccccc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5417603 196145 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 385 6 2 4 3.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccccc2)cc1 10.1021/acs.jmedchem.2c02058
155559165 174900 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 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 EP4 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 460 8 2 5 4.5 CCCc1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4562090 174900 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 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 EP4 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 460 8 2 5 4.5 CCCc1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
172448105 195969 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 483 8 2 5 4.8 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2CCOc2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5414398 195969 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 483 8 2 5 4.8 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2CCOc2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.2c02058
172449151 195615 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 467 6 2 4 5.3 C[C@@H](NC(=O)c1c2ccccc2nn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5407123 195615 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 467 6 2 4 5.3 C[C@@H](NC(=O)c1c2ccccc2nn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c02058
90202290 173591 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 439 5 1 5 5.7 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CCCO3)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4530347 173591 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 439 5 1 5 5.7 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CC3CCCO3)ccc21 10.1021/acs.jmedchem.8b01862
172463977 196569 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 403 6 2 4 3.9 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5426943 196569 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 403 6 2 4 3.9 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c02058
172443755 195030 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 429 7 2 5 4.3 COc1ccc(Cn2nc3ccccc3c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5395204 195030 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 429 7 2 5 4.3 COc1ccc(Cn2nc3ccccc3c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)cc1 10.1021/acs.jmedchem.2c02058
23660675 57119 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 425 6 2 4 4.3 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C#N)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645140 57119 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 425 6 2 4 4.3 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C#N)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
56944705 129281 None 39 Human Functional pIC50 = 8.1 8.1 11 3
Antagonist activity at human EP4 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 EP4 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 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL3670685 129281 None 39 Human Functional pIC50 = 8.1 8.1 11 3
Antagonist activity at human EP4 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 EP4 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 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
56944705 129281 None 39 Human Functional pIC50 = 8.1 8.1 11 3
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL3670685 129281 None 39 Human Functional pIC50 = 8.1 8.1 11 3
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
172462765 196678 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 451 7 2 5 4.0 COc1c(F)cc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1F 10.1021/acs.jmedchem.2c02058
CHEMBL5429723 196678 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 451 7 2 5 4.0 COc1c(F)cc(Cn2nc3ccccc3c2C(=O)NCc2ccc(C(=O)O)cc2)cc1F 10.1021/acs.jmedchem.2c02058
141730897 176220 None 0 Mouse Functional pIC50 = 7.2 7.2 -2 3
Antagonist activity at mouse EP4 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 mouse EP4 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 176220 None 0 Mouse Functional pIC50 = 7.2 7.2 -2 3
Antagonist activity at mouse EP4 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 mouse EP4 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
53325181 57129 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 443 7 3 4 3.5 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(C(N)=O)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645150 57129 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 443 7 3 4 3.5 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(C(N)=O)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
23661017 57124 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 443 7 3 4 3.5 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(N)=O)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645145 57124 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 443 7 3 4 3.5 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(N)=O)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
76283950 175235 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 397 4 1 4 6.1 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3C(C)C)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4569727 175235 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 397 4 1 4 6.1 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3C(C)C)ccc21 10.1021/acs.jmedchem.8b01862
156073547 191392 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 453 6 3 5 3.6 C[C@H](NC(=O)c1c(Cc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)NN)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5190720 191392 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 453 6 3 5 3.6 C[C@H](NC(=O)c1c(Cc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)NN)cc1 10.1021/acs.jmedchem.2c00448
172451066 195815 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 391 6 2 4 4.2 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2CC2CCCCC2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5411223 195815 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 391 6 2 4 4.2 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2CC2CCCCC2)cc1 10.1021/acs.jmedchem.2c02058
155568436 176116 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human EP4 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 EP4 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 472 7 2 5 4.8 C[C@H](NC(=O)c1c(C2CCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4589657 176116 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human EP4 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 EP4 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 472 7 2 5 4.8 C[C@H](NC(=O)c1c(C2CCC2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
155544290 173480 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 447 6 1 5 5.8 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)c(Cl)cc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4527730 173480 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 447 6 1 5 5.8 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)c(Cl)cc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
25019694 57732 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 641 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(C)cccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669026 57732 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 641 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(C)cccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25018911 57714 None 7 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669008 57714 None 7 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 releaseAntagonist activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
138670564 192325 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 439 6 2 4 4.7 C[C@@H](NC(=O)c1c(Cc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5204798 192325 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 439 6 2 4 4.7 C[C@@H](NC(=O)c1c(Cc2ccc(F)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
172451441 195673 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 433 8 2 5 3.9 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2CCOc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5408723 195673 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 433 8 2 5 3.9 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2CCOc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c02058
71186415 147572 None 0 Human Functional pIC50 = 8.1 8.1 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 462 6 2 3 5.3 C[C@H](NC(=O)C1CC(C)(C)CCN1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 nan
CHEMBL3930412 147572 None 0 Human Functional pIC50 = 8.1 8.1 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 462 6 2 3 5.3 C[C@H](NC(=O)C1CC(C)(C)CCN1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 nan
53317329 57123 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 512 6 2 3 5.9 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(Cl)cc1Br)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645144 57123 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 512 6 2 3 5.9 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(Cl)cc1Br)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
155529786 171561 None 0 Human Functional pIC50 = 8.1 8.1 107 2
Antagonist activity at human EP4 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 EP4 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 494 7 2 5 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4463343 171561 None 0 Human Functional pIC50 = 8.1 8.1 107 2
Antagonist activity at human EP4 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 EP4 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 494 7 2 5 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
24953286 203841 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(Cl)c1 10.1021/jm901771h
CHEMBL604546 203841 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(Cl)c1 10.1021/jm901771h
172465410 196573 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 431 6 3 4 5.3 C[C@H](NC(=O)c1c(Nc2cccc(F)c2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
CHEMBL5426990 196573 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay
ChEMBL 431 6 3 4 5.3 C[C@H](NC(=O)c1c(Nc2cccc(F)c2)c2ccccc2n1C)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
74762651 172588 None 0 Mouse Functional pIC50 = 7.1 7.1 -17 2
Antagonist activity at mouse EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at mouse EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 413 6 1 5 5.2 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4483026 172588 None 0 Mouse Functional pIC50 = 7.1 7.1 -17 2
Antagonist activity at mouse EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at mouse EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 413 6 1 5 5.2 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CCOC)ccc21 10.1021/acs.jmedchem.8b01862
76281184 174806 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 426 6 1 5 5.1 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CCN(C)C)ccc21 10.1021/acs.jmedchem.8b01862
CHEMBL4559616 174806 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assayAntagonist activity at human EP4R assessed as inhibition of agonist-induced cAMP production by fluorescent cAMP tracer cAMP-d2 based FRET assay
ChEMBL 426 6 1 5 5.1 CCn1c2ccccc2c2cc(-c3nc4cc(C(=O)O)ccc4n3CCN(C)C)ccc21 10.1021/acs.jmedchem.8b01862
86707358 139533 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 383 5 3 5 2.8 Cc1ccc(N2CCC(CO)C2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
CHEMBL3793994 139533 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 383 5 3 5 2.8 Cc1ccc(N2CCC(CO)C2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
86707355 139442 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 397 4 3 5 3.3 Cc1ccc(N2CCC(C)(O)CC2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
CHEMBL3792999 139442 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 397 4 3 5 3.3 Cc1ccc(N2CCC(C)(O)CC2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
71204672 144699 None 0 Human Functional pIC50 = 8.1 8.1 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 470 6 2 3 4.9 C[C@H](NC(=O)[C@H]1CC(F)(F)CCN1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 nan
CHEMBL3907863 144699 None 0 Human Functional pIC50 = 8.1 8.1 - 1
cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.cAMPFunctional Assay: The assay is based on the competition between endogenous cAMP and exogenously added biotinylated cAMP. The capture of cAMP is achieved by using a specific antibody conjugated to Donor beads.Cell membranes prepared as described above, were resuspended in 1 ml stimulation buffer (HBSS 1x+BSA 0.1%+IBMX 0.5 mM+HEPES 5 mM+MgCl2 10 mM+GTP 1 nM+GDP 10 uM+ATP 100 uM - pH 7.4). Cell membranes were dispensed into white 384-well microplates at final concentration of 1 ug/well and used for the determination of cAMP with the alphascreen cAMP functional assay (EnVision-PerkinElmer). Cell membrane/anti-cAMP Acceptor beads mix (5 ul) and a mixture of analysed compounds (dissolved in 100% DMSO to a final maximal concentration of 0.01% DMSO)/PGE2 (5 ul) were incubated at room temperature (22-23° C.) for 30 min in the dark. The Biotinylated-cAMP and donor beads (15 ul) were dispensed into each well to start the competition reaction.
ChEMBL 470 6 2 3 4.9 C[C@H](NC(=O)[C@H]1CC(F)(F)CCN1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 nan
155528854 171491 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human EP4 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 EP4 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 8 2 6 4.2 COc1ccc(Cn2nnc(-c3ccccc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4462095 171491 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human EP4 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 EP4 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 8 2 6 4.2 COc1ccc(Cn2nnc(-c3ccccc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)cc1 10.1021/acs.jmedchem.9b01269
168292957 192174 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 477 6 2 4 5.9 C[C@H](NC(=O)c1c(Cc2ccc(C(C)(C)C)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
CHEMBL5202597 192174 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assayAntagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay
ChEMBL 477 6 2 4 5.9 C[C@H](NC(=O)c1c(Cc2ccc(C(C)(C)C)cc2)sc2c1CCOC2)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.2c00448
25003075 6840 None 21 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at prostanoid EP4 receptor in human whole blood assessed as inhibition of TNF-alpha-induced IP-10 release in presence EP4 agonist L-000902688Antagonist activity at prostanoid EP4 receptor in human whole blood assessed as inhibition of TNF-alpha-induced IP-10 release in presence EP4 agonist L-000902688
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 6840 None 21 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at prostanoid EP4 receptor in human whole blood assessed as inhibition of TNF-alpha-induced IP-10 release in presence EP4 agonist L-000902688Antagonist activity at prostanoid EP4 receptor in human whole blood assessed as inhibition of TNF-alpha-induced IP-10 release in presence EP4 agonist L-000902688
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
172442260 195327 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 487 6 2 4 5.4 O=C(O)c1ccc(CNC(=O)c2c3ccc(Cl)cc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5401228 195327 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assayAntagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay
ChEMBL 487 6 2 4 5.4 O=C(O)c1ccc(CNC(=O)c2c3ccc(Cl)cc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
155529786 171561 None 0 Mouse Functional pIC50 = 6.0 6.0 -107 2
Antagonist activity at mouse EP4 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 mouse EP4 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 494 7 2 5 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4463343 171561 None 0 Mouse Functional pIC50 = 6.0 6.0 -107 2
Antagonist activity at mouse EP4 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 mouse EP4 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 494 7 2 5 5.2 C[C@H](NC(=O)c1c(-c2ccccc2)nnn1Cc1ccc(C(F)(F)F)cc1)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
137661981 159624 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 430 6 2 4 5.4 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccccc1Cl)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4102314 159624 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 430 6 2 4 5.4 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccccc1Cl)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
11626153 158008 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 430 6 2 4 5.4 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(Cl)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4084355 158008 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 430 6 2 4 5.4 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(Cl)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
86707359 139523 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 397 5 2 5 3.6 COC1CCN(c2ccc(C)c(C(=O)Nc3c(C)cc(C(=O)O)cc3C)n2)CC1 10.1016/j.bmcl.2016.03.041
CHEMBL3793912 139523 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assayAntagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by HTRF assay
ChEMBL 397 5 2 5 3.6 COC1CCN(c2ccc(C)c(C(=O)Nc3c(C)cc(C(=O)O)cc3C)n2)CC1 10.1016/j.bmcl.2016.03.041
155524501 171066 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human EP4 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 EP4 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 8 2 6 4.2 COc1cccc(Cn2nnc(-c3ccccc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1 10.1021/acs.jmedchem.9b01269
CHEMBL4455816 171066 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human EP4 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 EP4 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 8 2 6 4.2 COc1cccc(Cn2nnc(-c3ccccc3)c2C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1 10.1021/acs.jmedchem.9b01269
11577792 159412 None 20 Mouse Functional pKd = 9 9.0 - 2
Antagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4099851 159412 None 20 Mouse Functional pKd = 9 9.0 - 2
Antagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
11577792 159412 None 20 Human Functional pKd = 9.0 9.0 309 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4099851 159412 None 20 Human Functional pKd = 9.0 9.0 309 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
11575201 157514 None 0 Human Functional pKd = 8.9 8.9 100 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 413 6 2 3 5.5 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4078648 157514 None 0 Human Functional pKd = 8.9 8.9 100 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 413 6 2 3 5.5 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
11524454 946 None 36 Human Functional pKd = 8.8 8.8 52 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
5857 946 None 36 Human Functional pKd = 8.8 8.8 52 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
CHEMBL591666 946 None 36 Human Functional pKd = 8.8 8.8 52 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
11683088 159070 None 0 Human Functional pKd = 8.6 8.6 275 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4096216 159070 None 0 Human Functional pKd = 8.6 8.6 275 2
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
11577792 159412 None 20 Rat Functional pKd = 8.3 8.3 - 2
Antagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4099851 159412 None 20 Rat Functional pKd = 8.3 8.3 - 2
Antagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
11677589 1859 None 51 Human Functional pKd = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
11677589.0 1859 None 51 Human Functional pKd = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
5858 1859 None 51 Human Functional pKd = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
CHEMBL3039498 1859 None 51 Human Functional pKd = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
DB12836 1859 None 51 Human Functional pKd = 8.3 8.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
146014480 173818 None 18 Human Functional pKd = 8.3 8.3 4 2
Inhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP AssayInhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP Assay
ChEMBL 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4535971 173818 None 18 Human Functional pKd = 8.3 8.3 4 2
Inhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP AssayInhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP Assay
ChEMBL 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
11677589 1859 None 51 Rat Functional pKd = 8.2 8.2 - 1
Antagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
11677589.0 1859 None 51 Rat Functional pKd = 8.2 8.2 - 1
Antagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
5858 1859 None 51 Rat Functional pKd = 8.2 8.2 - 1
Antagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
CHEMBL3039498 1859 None 51 Rat Functional pKd = 8.2 8.2 - 1
Antagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
DB12836 1859 None 51 Rat Functional pKd = 8.2 8.2 - 1
Antagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at rat recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
12017 1103 None 0 Human Functional pKd = 8.2 8.2 5 2
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by Schild plot based GloSensor cAMP assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by Schild plot based GloSensor cAMP assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
138670561 1103 None 0 Human Functional pKd = 8.2 8.2 5 2
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by Schild plot based GloSensor cAMP assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by Schild plot based GloSensor cAMP assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
CHEMBL5186525 1103 None 0 Human Functional pKd = 8.2 8.2 5 2
Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by Schild plot based GloSensor cAMP assayAntagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by Schild plot based GloSensor cAMP assay
ChEMBL 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 10.1021/acs.jmedchem.2c00448
11677589 1859 None 51 Mouse Functional pKd = 8.1 8.1 - 1
Antagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
11677589.0 1859 None 51 Mouse Functional pKd = 8.1 8.1 - 1
Antagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
5858 1859 None 51 Mouse Functional pKd = 8.1 8.1 - 1
Antagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
CHEMBL3039498 1859 None 51 Mouse Functional pKd = 8.1 8.1 - 1
Antagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
DB12836 1859 None 51 Mouse Functional pKd = 8.1 8.1 - 1
Antagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assayAntagonist activity at mouse recombinant EP4 receptor assessed as inhibition of PGE2-induced cAMP level by cell based assay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2017.01.067
53323098 57719 None 0 Human Functional pKi = 10.0 10.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(C)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669013 57719 None 0 Human Functional pKi = 10.0 10.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(C)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019183 57718 None 0 Human Functional pKi = 9.8 9.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 647 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669012 57718 None 0 Human Functional pKi = 9.8 9.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 647 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53325765 57723 None 0 Human Functional pKi = 9.8 9.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 579 11 1 6 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ncccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669017 57723 None 0 Human Functional pKi = 9.8 9.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 579 11 1 6 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ncccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019185 57715 None 0 Human Functional pKi = 9.8 9.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 643 11 2 7 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669009 57715 None 0 Human Functional pKi = 9.8 9.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 643 11 2 7 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53325764 57722 None 0 Human Functional pKi = 9.7 9.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 622 12 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4cc(C(=O)O)ccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669016 57722 None 0 Human Functional pKi = 9.7 9.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 622 12 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4cc(C(=O)O)ccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53323099 57724 None 0 Human Functional pKi = 9.7 9.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 578 11 1 5 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669018 57724 None 0 Human Functional pKi = 9.7 9.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 578 11 1 5 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019184 57716 None 0 Human Functional pKi = 9.6 9.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669010 57716 None 0 Human Functional pKi = 9.6 9.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25018911 57714 None 7 Human Functional pKi = 9.5 9.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669008 57714 None 7 Human Functional pKi = 9.5 9.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53319154 57721 None 0 Human Functional pKi = 9.5 9.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 582 10 1 4 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669015 57721 None 0 Human Functional pKi = 9.5 9.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 582 10 1 4 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53325767 57729 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 552 11 1 5 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CCNC(=O)Cc3ccccc3OC)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669023 57729 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 552 11 1 5 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CCNC(=O)Cc3ccccc3OC)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019434 57711 None 0 Human Functional pKi = 9.5 9.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 673 12 2 8 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(OC)cccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669005 57711 None 0 Human Functional pKi = 9.5 9.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 673 12 2 8 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(OC)cccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53325585 57720 None 0 Human Functional pKi = 9.5 9.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 616 10 1 4 7.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccc(Cl)cc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669014 57720 None 0 Human Functional pKi = 9.5 9.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 616 10 1 4 7.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccc(Cl)cc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25016088 57712 None 0 Human Functional pKi = 9.4 9.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 681 10 2 6 6.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C(F)(F)F)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669006 57712 None 0 Human Functional pKi = 9.4 9.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 681 10 2 6 6.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C(F)(F)F)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019695 57731 None 0 Human Functional pKi = 9.4 9.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4cccc(Cl)c4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669025 57731 None 0 Human Functional pKi = 9.4 9.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4cccc(Cl)c4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019694 57732 None 0 Human Functional pKi = 9.4 9.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 641 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(C)cccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669026 57732 None 0 Human Functional pKi = 9.4 9.4 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 641 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(C)cccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
24944538 57717 None 0 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 756 10 2 7 7.0 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccccc3Cl)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669011 57717 None 0 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 756 10 2 7 7.0 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccccc3Cl)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
25019696 57730 None 0 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 631 10 2 6 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669024 57730 None 0 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 631 10 2 6 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019433 57710 None 0 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 691 10 2 6 6.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Br)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669004 57710 None 0 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 691 10 2 6 6.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Br)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019435 57713 None 0 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 663 10 2 6 7.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc5ccccc5c4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669007 57713 None 0 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 663 10 2 6 7.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc5ccccc5c4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53325585 57720 None 0 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 616 10 1 4 7.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccc(Cl)cc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669014 57720 None 0 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 616 10 1 4 7.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccc(Cl)cc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019697 57708 None 0 Human Functional pKi = 9.2 9.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 697 11 2 7 6.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(OC(F)(F)F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669002 57708 None 0 Human Functional pKi = 9.2 9.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 697 11 2 7 6.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(OC(F)(F)F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53321772 57725 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 567 11 1 6 5.8 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CC(C)NC(=O)Cc3ccccc3OC)cc1C)C2=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669019 57725 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 567 11 1 6 5.8 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CC(C)NC(=O)Cc3ccccc3OC)cc1C)C2=O 10.1016/j.bmcl.2010.12.014
53323099 57724 None 0 Human Functional pKi = 9.2 9.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 578 11 1 5 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669018 57724 None 0 Human Functional pKi = 9.2 9.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 578 11 1 5 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53324453 57728 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 596 11 1 5 6.4 COc1ccccc1CC(=O)NCCc1ccc(N2Cc3c(c(OC(F)F)c4ccccc4c3OC(F)F)C2=O)c(C)c1 10.1016/j.bmcl.2010.12.014
CHEMBL1669022 57728 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 596 11 1 5 6.4 COc1ccccc1CC(=O)NCCc1ccc(N2Cc3c(c(OC(F)F)c4ccccc4c3OC(F)F)C2=O)c(C)c1 10.1016/j.bmcl.2010.12.014
53317842 57726 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 553 11 1 6 5.4 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CCNC(=O)Cc3ccccc3OC)cc1C)C2=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669020 57726 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 553 11 1 6 5.4 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CCNC(=O)Cc3ccccc3OC)cc1C)C2=O 10.1016/j.bmcl.2010.12.014
25015836 57709 None 0 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 772 10 2 7 7.5 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccc4ccccc4c3)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669003 57709 None 0 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 772 10 2 7 7.5 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccc4ccccc4c3)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
53319154 57721 None 0 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 582 10 1 4 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669015 57721 None 0 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 582 10 1 4 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53321772 57725 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 567 11 1 6 5.8 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CC(C)NC(=O)Cc3ccccc3OC)cc1C)C2=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669019 57725 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 567 11 1 6 5.8 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CC(C)NC(=O)Cc3ccccc3OC)cc1C)C2=O 10.1016/j.bmcl.2010.12.014
53325765 57723 None 0 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 579 11 1 6 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ncccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669017 57723 None 0 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 579 11 1 6 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ncccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019434 57711 None 0 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 673 12 2 8 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(OC)cccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669005 57711 None 0 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 673 12 2 8 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(OC)cccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019694 57732 None 0 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 641 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(C)cccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669026 57732 None 0 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 641 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(C)cccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53323098 57719 None 0 Human Functional pKi = 8 8.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(C)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669013 57719 None 0 Human Functional pKi = 8 8.0 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(C)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
10402929 57560 None 0 Human Functional pKi = 5 5.0 - 0
Antagonistic activity at Prostanoid EP4 receptor in human was determinedAntagonistic activity at Prostanoid EP4 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 57560 None 0 Human Functional pKi = 5 5.0 - 0
Antagonistic activity at Prostanoid EP4 receptor in human was determinedAntagonistic activity at Prostanoid EP4 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
53325766 57727 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 660 11 1 5 7.1 COc1ccccc1CC(=O)NCCc1ccc(N2Cc3c(c(OCC(F)(F)F)c4ccccc4c3OCC(F)(F)F)C2=O)c(C)c1 10.1016/j.bmcl.2010.12.014
CHEMBL1669021 57727 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 660 11 1 5 7.1 COc1ccccc1CC(=O)NCCc1ccc(N2Cc3c(c(OCC(F)(F)F)c4ccccc4c3OCC(F)(F)F)C2=O)c(C)c1 10.1016/j.bmcl.2010.12.014
24944538 57717 None 0 Human Functional pKi = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 756 10 2 7 7.0 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccccc3Cl)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669011 57717 None 0 Human Functional pKi = 7.9 7.9 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 756 10 2 7 7.0 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccccc3Cl)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
25019183 57718 None 0 Human Functional pKi = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 647 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669012 57718 None 0 Human Functional pKi = 8.6 8.6 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 647 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53317842 57726 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 553 11 1 6 5.4 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CCNC(=O)Cc3ccccc3OC)cc1C)C2=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669020 57726 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 553 11 1 6 5.4 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CCNC(=O)Cc3ccccc3OC)cc1C)C2=O 10.1016/j.bmcl.2010.12.014
53325767 57729 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 552 11 1 5 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CCNC(=O)Cc3ccccc3OC)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669023 57729 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 552 11 1 5 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CCNC(=O)Cc3ccccc3OC)cc1C)C2 10.1016/j.bmcl.2010.12.014
25015836 57709 None 0 Human Functional pKi = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 772 10 2 7 7.5 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccc4ccccc4c3)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669003 57709 None 0 Human Functional pKi = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 772 10 2 7 7.5 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccc4ccccc4c3)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
25019696 57730 None 0 Human Functional pKi = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 631 10 2 6 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669024 57730 None 0 Human Functional pKi = 7.7 7.7 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 631 10 2 6 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019185 57715 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 643 11 2 7 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669009 57715 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 643 11 2 7 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019184 57716 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669010 57716 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25018911 57714 None 7 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669008 57714 None 7 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
9817405 165498 None 5 Human Functional pKi = 5.5 5.5 - 0
Antagonistic activity at Prostanoid EP4 receptor in human was determinedAntagonistic activity at Prostanoid EP4 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 165498 None 5 Human Functional pKi = 5.5 5.5 - 0
Antagonistic activity at Prostanoid EP4 receptor in human was determinedAntagonistic activity at Prostanoid EP4 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
53325766 57727 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 660 11 1 5 7.1 COc1ccccc1CC(=O)NCCc1ccc(N2Cc3c(c(OCC(F)(F)F)c4ccccc4c3OCC(F)(F)F)C2=O)c(C)c1 10.1016/j.bmcl.2010.12.014
CHEMBL1669021 57727 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assayAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay
ChEMBL 660 11 1 5 7.1 COc1ccccc1CC(=O)NCCc1ccc(N2Cc3c(c(OCC(F)(F)F)c4ccccc4c3OCC(F)(F)F)C2=O)c(C)c1 10.1016/j.bmcl.2010.12.014
10483360 201684 None 28 Human Functional pKi = 4.4 4.4 - 4
Inhibition of EP4 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP productionInhibition of EP4 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP production
ChEMBL 580 12 3 6 5.8 CCCCNC(=O)c1ccc(Oc2ccc(CC(=O)O)cc2OC)c(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1 10.1016/j.bmcl.2009.09.052
CHEMBL589973 201684 None 28 Human Functional pKi = 4.4 4.4 - 4
Inhibition of EP4 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP productionInhibition of EP4 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP production
ChEMBL 580 12 3 6 5.8 CCCCNC(=O)c1ccc(Oc2ccc(CC(=O)O)cc2OC)c(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1 10.1016/j.bmcl.2009.09.052
25019697 57708 None 0 Human Functional pKi = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 697 11 2 7 6.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(OC(F)(F)F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669002 57708 None 0 Human Functional pKi = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 697 11 2 7 6.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(OC(F)(F)F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53325764 57722 None 0 Human Functional pKi = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 622 12 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4cc(C(=O)O)ccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669016 57722 None 0 Human Functional pKi = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 622 12 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4cc(C(=O)O)ccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019435 57713 None 0 Human Functional pKi = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 663 10 2 6 7.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc5ccccc5c4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669007 57713 None 0 Human Functional pKi = 8.2 8.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 663 10 2 6 7.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc5ccccc5c4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
10095268 86190 None 0 Human Functional pKi = 5.2 5.2 -3162 3
Inhibition of human EP4 recombinant receptor expressed in CHO cells by cAMP mobilisation assayInhibition of human EP4 recombinant receptor expressed in CHO cells by cAMP 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 86190 None 0 Human Functional pKi = 5.2 5.2 -3162 3
Inhibition of human EP4 recombinant receptor expressed in CHO cells by cAMP mobilisation assayInhibition of human EP4 recombinant receptor expressed in CHO cells by cAMP 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
25019695 57731 None 0 Human Functional pKi = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4cccc(Cl)c4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669025 57731 None 0 Human Functional pKi = 7.2 7.2 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4cccc(Cl)c4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019433 57710 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 691 10 2 6 6.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Br)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669004 57710 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 691 10 2 6 6.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Br)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53324453 57728 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 596 11 1 5 6.4 COc1ccccc1CC(=O)NCCc1ccc(N2Cc3c(c(OC(F)F)c4ccccc4c3OC(F)F)C2=O)c(C)c1 10.1016/j.bmcl.2010.12.014
CHEMBL1669022 57728 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 596 11 1 5 6.4 COc1ccccc1CC(=O)NCCc1ccc(N2Cc3c(c(OC(F)F)c4ccccc4c3OC(F)F)C2=O)c(C)c1 10.1016/j.bmcl.2010.12.014
25016088 57712 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 681 10 2 6 6.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C(F)(F)F)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669006 57712 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serumAntagonist activity at human EP4 receptor expressed in HEK293 cells assessed as PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
ChEMBL 681 10 2 6 6.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C(F)(F)F)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
2720 3854 None 49 Human Functional pEC50 = 8.2 8.2 -60 5
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 3854 None 49 Human Functional pEC50 = 8.2 8.2 -60 5
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 3854 None 49 Human Functional pEC50 = 8.2 8.2 -60 5
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
6918140.0 3854 None 49 Human Functional pEC50 = 8.2 8.2 -60 5
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 3854 None 49 Human Functional pEC50 = 8.2 8.2 -60 5
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 3854 None 49 Human Functional pEC50 = 8.2 8.2 -60 5
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
138 3081 None 57 Human Functional pEC50 = 8.1 8.1 1 10
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 3081 None 57 Human Functional pEC50 = 8.1 8.1 1 10
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
149351.0 3081 None 57 Human Functional pEC50 = 8.1 8.1 1 10
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 3081 None 57 Human Functional pEC50 = 8.1 8.1 1 10
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 3081 None 57 Human Functional pEC50 = 8.1 8.1 1 10
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
5280723.0 3081 None 57 Human Functional pEC50 = 8.1 8.1 1 10
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 3081 None 57 Human Functional pEC50 = 8.1 8.1 1 10
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 3081 None 57 Human Functional pEC50 = 8.1 8.1 1 10
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
1883 3082 None 47 Human Functional pEC50 = 6.1 6.1 -1 12
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 19584306
1916 3082 None 47 Human Functional pEC50 = 6.1 6.1 -1 12
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 19584306
5280360 3082 None 47 Human Functional pEC50 = 6.1 6.1 -1 12
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 19584306
5280360.0 3082 None 47 Human Functional pEC50 = 6.1 6.1 -1 12
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 19584306
913 3082 None 47 Human Functional pEC50 = 6.1 6.1 -1 12
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 19584306
CHEMBL548 3082 None 47 Human Functional pEC50 = 6.1 6.1 -1 12
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 19584306
DB00917 3082 None 47 Human Functional pEC50 = 6.1 6.1 -1 12
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 19584306
1884 3083 None 40 Human Functional pEC50 = 6.1 6.1 -45 9
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 19584306
5280363 3083 None 40 Human Functional pEC50 = 6.1 6.1 -45 9
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 19584306
912 3083 None 40 Human Functional pEC50 = 6.1 6.1 -45 9
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 19584306
CHEMBL815 3083 None 40 Human Functional pEC50 = 6.1 6.1 -45 9
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 19584306
DB12789 3083 None 40 Human Functional pEC50 = 6.1 6.1 -45 9
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 19584306
1895 2007 None 0 Human Functional pEC50 = 6.4 6.4 -630 2
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 2007 None 0 Human Functional pEC50 = 6.4 6.4 -630 2
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 2007 None 0 Human Functional pEC50 = 6.4 6.4 -630 2
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 2007 None 0 Human Functional pEC50 = 6.4 6.4 -630 2
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
2720 3854 None 49 Human Functional pEC50 = 6.7 6.7 -60 5
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 3854 None 49 Human Functional pEC50 = 6.7 6.7 -60 5
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 3854 None 49 Human Functional pEC50 = 6.7 6.7 -60 5
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
6918140.0 3854 None 49 Human Functional pEC50 = 6.7 6.7 -60 5
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 3854 None 49 Human Functional pEC50 = 6.7 6.7 -60 5
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 3854 None 49 Human Functional pEC50 = 6.7 6.7 -60 5
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
1933 2943 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 18516068
1933 2943 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 21323896
5311230 2943 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 18516068
5311230 2943 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 21323896
1913 2464 None 0 Human Functional pEC50 = 7.8 7.8 -32 2
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 19584306
5311223 2464 None 0 Human Functional pEC50 = 7.8 7.8 -32 2
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 19584306
1881 3079 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 19584306
1891 3079 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 19584306
448457 3079 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 19584306
CHEMBL1235252 3079 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 19584306
DB02056 3079 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 19584306
4039 1186 None 0 Human Functional pEC50 = 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 468 10 1 5 3.4 O[C@@H](Cc1cccc(c1)C(F)(F)F)CC[C@H]1CCC(=O)N1CCCc1ccc(s1)C(=O)[O-] 19445930
73755071 1186 None 0 Human Functional pEC50 = 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 468 10 1 5 3.4 O[C@@H](Cc1cccc(c1)C(F)(F)F)CC[C@H]1CCC(=O)N1CCCc1ccc(s1)C(=O)[O-] 19445930
11316084 2264 None 0 Human Functional pEC50 = 9.2 9.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 419 11 2 5 3.0 O=C1CC[C@@H](N1CCCCCCc1nnn[nH]1)/C=C/[C@H](C(c1ccccc1)(F)F)O 18516068
11316084 2264 None 0 Human Functional pEC50 = 9.2 9.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 419 11 2 5 3.0 O=C1CC[C@@H](N1CCCCCCc1nnn[nH]1)/C=C/[C@H](C(c1ccccc1)(F)F)O 19584306
3357 2264 None 0 Human Functional pEC50 = 9.2 9.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 419 11 2 5 3.0 O=C1CC[C@@H](N1CCCCCCc1nnn[nH]1)/C=C/[C@H](C(c1ccccc1)(F)F)O 18516068
3357 2264 None 0 Human Functional pEC50 = 9.2 9.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 419 11 2 5 3.0 O=C1CC[C@@H](N1CCCCCCc1nnn[nH]1)/C=C/[C@H](C(c1ccccc1)(F)F)O 19584306
CHEMBL1956373 2264 None 0 Human Functional pEC50 = 9.2 9.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 419 11 2 5 3.0 O=C1CC[C@@H](N1CCCCCCc1nnn[nH]1)/C=C/[C@H](C(c1ccccc1)(F)F)O 18516068
CHEMBL1956373 2264 None 0 Human Functional pEC50 = 9.2 9.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 419 11 2 5 3.0 O=C1CC[C@@H](N1CCCCCCc1nnn[nH]1)/C=C/[C@H](C(c1ccccc1)(F)F)O 19584306
1925 7 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 19584306
5283055 7 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 19584306
CHEMBL3246389 7 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 19584306
138 3081 None 57 Human Functional pEC50 = 9.5 9.5 1 10
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 19584306
149351 3081 None 57 Human Functional pEC50 = 9.5 9.5 1 10
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 19584306
149351.0 3081 None 57 Human Functional pEC50 = 9.5 9.5 1 10
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 19584306
1882 3081 None 57 Human Functional pEC50 = 9.5 9.5 1 10
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 19584306
5280723 3081 None 57 Human Functional pEC50 = 9.5 9.5 1 10
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 19584306
5280723.0 3081 None 57 Human Functional pEC50 = 9.5 9.5 1 10
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 19584306
CHEMBL495 3081 None 57 Human Functional pEC50 = 9.5 9.5 1 10
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 19584306
DB00770 3081 None 57 Human Functional pEC50 = 9.5 9.5 1 10
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 19584306
1883 3082 None 47 Rat Functional pIC50 = 8.1 8.1 -1 12
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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 3082 None 47 Rat Functional pIC50 = 8.1 8.1 -1 12
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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 3082 None 47 Rat Functional pIC50 = 8.1 8.1 -1 12
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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
5280360.0 3082 None 47 Rat Functional pIC50 = 8.1 8.1 -1 12
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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 3082 None 47 Rat Functional pIC50 = 8.1 8.1 -1 12
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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 3082 None 47 Rat Functional pIC50 = 8.1 8.1 -1 12
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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 3082 None 47 Rat Functional pIC50 = 8.1 8.1 -1 12
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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
12017 1103 None 0 Human Functional pIC50 = 8.3 8.3 5 2
Measuring antagonism of PGE2-mediated calcium flux in HEK293 cells transiently expressing hEP4, using Promega's proprietary GloSensor cAMP assay systemMeasuring antagonism of PGE2-mediated calcium flux in HEK293 cells transiently expressing hEP4, using Promega's proprietary GloSensor cAMP assay system
Guide to Pharmacology 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 35640059
138670561 1103 None 0 Human Functional pIC50 = 8.3 8.3 5 2
Measuring antagonism of PGE2-mediated calcium flux in HEK293 cells transiently expressing hEP4, using Promega's proprietary GloSensor cAMP assay systemMeasuring antagonism of PGE2-mediated calcium flux in HEK293 cells transiently expressing hEP4, using Promega's proprietary GloSensor cAMP assay system
Guide to Pharmacology 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 35640059
CHEMBL5186525 1103 None 0 Human Functional pIC50 = 8.3 8.3 5 2
Measuring antagonism of PGE2-mediated calcium flux in HEK293 cells transiently expressing hEP4, using Promega's proprietary GloSensor cAMP assay systemMeasuring antagonism of PGE2-mediated calcium flux in HEK293 cells transiently expressing hEP4, using Promega's proprietary GloSensor cAMP assay system
Guide to Pharmacology 425 6 2 4 4.2 O=C(NCc1ccc(C(=O)O)cc1)c1c(Cc2ccc(F)cc2)sc2c1CCOC2 35640059
5860 3801 None 0 Rat Functional pIC50 = 5.5 5.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 23152113
4040 1579 None 0 Human Functional pIC50 = 7.2 7.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 489 5 0 4 5.6 CCN1C(=O)N2C(=C[C@@H](c3c(C2)cc(OC)cc3OC)C)C21CCN(CC2)Cc1cc(C)cc(c1)C 20423341
42596951 1579 None 0 Human Functional pIC50 = 7.2 7.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 489 5 0 4 5.6 CCN1C(=O)N2C(=C[C@@H](c3c(C2)cc(OC)cc3OC)C)C21CCN(CC2)Cc1cc(C)cc(c1)C 20423341
12783 578 None 26 Human Functional pIC50 = 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 441 6 1 5 5.8 O=C(O)C1=CC=C2N(CCOC)C(C3=CC=C4N(CC)C=5C=CC(=CC5C4=C3)C)=NC2=C1C 30707023
90202558 578 None 26 Human Functional pIC50 = 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 441 6 1 5 5.8 O=C(O)C1=CC=C2N(CCOC)C(C3=CC=C4N(CC)C=5C=CC(=CC5C4=C3)C)=NC2=C1C 30707023
CHEMBL4526403 578 None 26 Human Functional pIC50 = 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 441 6 1 5 5.8 O=C(O)C1=CC=C2N(CCOC)C(C3=CC=C4N(CC)C=5C=CC(=CC5C4=C3)C)=NC2=C1C 30707023
4039 1186 None 0 Human Functional pIC50 = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 468 10 1 5 3.4 O[C@@H](Cc1cccc(c1)C(F)(F)F)CC[C@H]1CCC(=O)N1CCCc1ccc(s1)C(=O)[O-] 19445930
73755071 1186 None 0 Human Functional pIC50 = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 468 10 1 5 3.4 O[C@@H](Cc1cccc(c1)C(F)(F)F)CC[C@H]1CCC(=O)N1CCCc1ccc(s1)C(=O)[O-] 19445930
10603 3792 None 0 Human Functional pKB = 5.3 5.3 -537 3
UnclassifiedUnclassified
Guide to Pharmacology 400 6 3 5 4.0 Cc1cc(Nc2ncc(cn2)C(=O)NCCc2c(C)[nH]c3c2cccc3)nc(c1)C 31904232
145996528 3792 None 0 Human Functional pKB = 5.3 5.3 -537 3
UnclassifiedUnclassified
Guide to Pharmacology 400 6 3 5 4.0 Cc1cc(Nc2ncc(cn2)C(=O)NCCc2c(C)[nH]c3c2cccc3)nc(c1)C 31904232
CHEMBL4552900 3792 None 0 Human Functional pKB = 5.3 5.3 -537 3
UnclassifiedUnclassified
Guide to Pharmacology 400 6 3 5 4.0 Cc1cc(Nc2ncc(cn2)C(=O)NCCc2c(C)[nH]c3c2cccc3)nc(c1)C 31904232
1987175 3794 None 27 Human Functional pKB = 5.4 5.4 -33 5
UnclassifiedUnclassified
Guide to Pharmacology 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 23914286
9283 3794 None 27 Human Functional pKB = 5.4 5.4 -33 5
UnclassifiedUnclassified
Guide to Pharmacology 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 23914286
CHEMBL1372836 3794 None 27 Human Functional pKB = 5.4 5.4 -33 5
UnclassifiedUnclassified
Guide to Pharmacology 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 23914286




Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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72950260 151248 None 0 Human Binding pEC50 = 11 11.0 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 437 14 2 3 4.6 O=C(O)CCCCCCN1C(=O)C(F)(F)C[C@@H]1/C=C/[C@@H](O)CCCCc1ccccc1 nan
CHEMBL3959605 151248 None 0 Human Binding pEC50 = 11 11.0 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 437 14 2 3 4.6 O=C(O)CCCCCCN1C(=O)C(F)(F)C[C@@H]1/C=C/[C@@H](O)CCCCc1ccccc1 nan
72950425 143137 None 0 Human Binding pEC50 = 10.5 10.5 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3895047 143137 None 0 Human Binding pEC50 = 10.5 10.5 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
12521 2197 None 0 Human Binding pEC50 = 10.4 10.4 -1 4
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
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 nan
72722131 2197 None 0 Human Binding pEC50 = 10.4 10.4 -1 4
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
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 nan
CHEMBL3918816 2197 None 0 Human Binding pEC50 = 10.4 10.4 -1 4
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
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 nan
5283086 205768 None 20 Human Binding pEC50 = 10.3 10.3 21 5
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
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 nan
CHEMBL64804 205768 None 20 Human Binding pEC50 = 10.3 10.3 21 5
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
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 nan
72950089 150679 None 0 Human Binding pEC50 = 10.2 10.2 1621 3
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3955128 150679 None 0 Human Binding pEC50 = 10.2 10.2 1621 3
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
72949200 153866 None 0 Human Binding pEC50 = 10.2 10.2 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 385 11 2 3 3.2 CC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3982139 153866 None 0 Human Binding pEC50 = 10.2 10.2 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 385 11 2 3 3.2 CC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
72948663 145822 None 0 Human Binding pEC50 = 10.2 10.2 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3916499 145822 None 0 Human Binding pEC50 = 10.2 10.2 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
72950929 146670 None 0 Human Binding pEC50 = 10.1 10.1 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3923027 146670 None 0 Human Binding pEC50 = 10.1 10.1 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
9807398 151387 None 0 Human Binding pEC50 = 10 10.0 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 542 12 3 7 5.3 CC1(C)C(=O)[C@H](SCCCSCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
CHEMBL3960625 151387 None 0 Human Binding pEC50 = 10 10.0 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 542 12 3 7 5.3 CC1(C)C(=O)[C@H](SCCCSCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
72948294 150045 None 0 Human Binding pEC50 = 10.0 10.0 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 439 9 2 4 4.0 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3949856 150045 None 0 Human Binding pEC50 = 10.0 10.0 - 1
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 439 9 2 4 4.0 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
10339756 143172 None 0 Human Binding pEC50 = 9.7 9.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 143172 None 0 Human Binding pEC50 = 9.7 9.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
10479215 146549 None 0 Human Binding pEC50 = 9.5 9.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 146549 None 0 Human Binding pEC50 = 9.5 9.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
10006340 150730 None 0 Human Binding pEC50 = 9.5 9.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 504 11 3 5 5.8 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
CHEMBL3955476 150730 None 0 Human Binding pEC50 = 9.5 9.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 504 11 3 5 5.8 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
10046549 151824 None 0 Human Binding pEC50 = 9.4 9.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 151824 None 0 Human Binding pEC50 = 9.4 9.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
11362836 137383 None 0 Human Binding pEC50 = 5.9 5.9 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137383 None 0 Human Binding pEC50 = 5.9 5.9 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
10369368 153526 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 518 11 2 6 5.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
CHEMBL3979233 153526 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 518 11 2 6 5.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
10409554 149609 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 11 3 4 3.9 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O nan
CHEMBL3946494 149609 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 11 3 4 3.9 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O nan
11294085 137339 None 0 Human Binding pEC50 = 6.7 6.7 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137339 None 0 Human Binding pEC50 = 6.7 6.7 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
66857670 137488 None 0 Human Binding pEC50 = 6.6 6.6 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137488 None 0 Human Binding pEC50 = 6.6 6.6 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
10369368 153526 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 518 11 2 6 5.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
CHEMBL3979233 153526 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 518 11 2 6 5.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
127037150 137647 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137647 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
11961366 150560 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 556 12 2 8 5.4 COC(=O)CSCCCS[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
CHEMBL3954286 150560 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 556 12 2 8 5.4 COC(=O)CSCCCS[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
10432730 147357 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 147357 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
10029056 150086 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 502 9 3 5 5.3 CC1(C)C(=O)[C@H](CC#CCCCC(=O)O)[C@@H](/C=C\C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
CHEMBL3950189 150086 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 502 9 3 5 5.3 CC1(C)C(=O)[C@H](CC#CCCCC(=O)O)[C@@H](/C=C\C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
59554824 137562 None 0 Human Binding pEC50 = 6.5 6.5 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137562 None 0 Human Binding pEC50 = 6.5 6.5 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
10479215 146549 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 146549 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
59554827 137380 None 0 Human Binding pEC50 = 8.4 8.4 - 0
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137380 None 0 Human Binding pEC50 = 8.4 8.4 - 0
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
66858111 137538 None 0 Human Binding pEC50 = 6.3 6.3 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137538 None 0 Human Binding pEC50 = 6.3 6.3 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
66857738 137387 None 0 Human Binding pEC50 = 5.3 5.3 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137387 None 0 Human Binding pEC50 = 5.3 5.3 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
10023570 153425 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 153425 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
118689427 151941 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, 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; 10N 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 PGF2a (5 nM) were performed in a 100 μl 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 harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, 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; 10N 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 PGF2a (5 nM) were performed in a 100 μl 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 harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
CHEMBL3965497 151941 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, 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; 10N 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 PGF2a (5 nM) were performed in a 100 μl 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 harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, 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; 10N 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 PGF2a (5 nM) were performed in a 100 μl 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 harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
10409554 149609 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 11 3 4 3.9 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O nan
CHEMBL3946494 149609 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 11 3 4 3.9 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O nan
10045223 152056 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 152056 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
10029056 150086 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 502 9 3 5 5.3 CC1(C)C(=O)[C@H](CC#CCCCC(=O)O)[C@@H](/C=C\C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
CHEMBL3950189 150086 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 502 9 3 5 5.3 CC1(C)C(=O)[C@H](CC#CCCCC(=O)O)[C@@H](/C=C\C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
11328569 137555 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137555 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
59554822 137481 None 0 Human Binding pEC50 = 7.1 7.1 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137481 None 0 Human Binding pEC50 = 7.1 7.1 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
127026652 137569 None 0 Human Binding pEC50 = 6.1 6.1 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137569 None 0 Human Binding pEC50 = 6.1 6.1 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
11156167 137607 None 0 Human Binding pEC50 = 5.1 5.1 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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 137607 None 0 Human Binding pEC50 = 5.1 5.1 - 1
Agonist activity at human EP4 receptorAgonist activity at human EP4 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
72950929 146670 None 0 Human Binding pIC50 = 9.7 9.7 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3923027 146670 None 0 Human Binding pIC50 = 9.7 9.7 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
72948663 145822 None 0 Human Binding pIC50 = 9.6 9.6 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3916499 145822 None 0 Human Binding pIC50 = 9.6 9.6 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
72950425 143137 None 0 Human Binding pIC50 = 9.5 9.5 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3895047 143137 None 0 Human Binding pIC50 = 9.5 9.5 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
5283086 205768 None 20 Human Binding pIC50 = 9.4 9.4 21 5
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
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 nan
CHEMBL64804 205768 None 20 Human Binding pIC50 = 9.4 9.4 21 5
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
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 nan
146014480 173818 None 18 Human Binding pIC50 = 9.4 9.4 - 1
Inhibition of human EP4 transfected in human HEK293 cells co transfected with SmBit-beta-arrestin. assessed as reduction in PGE2 induced-beta-arrestin recruitment by NanoBiT beta-arrestin recruitment assayInhibition of human EP4 transfected in human HEK293 cells co transfected with SmBit-beta-arrestin. assessed as reduction in PGE2 induced-beta-arrestin recruitment by NanoBiT beta-arrestin recruitment assay
ChEMBL 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
CHEMBL4535971 173818 None 18 Human Binding pIC50 = 9.4 9.4 - 1
Inhibition of human EP4 transfected in human HEK293 cells co transfected with SmBit-beta-arrestin. assessed as reduction in PGE2 induced-beta-arrestin recruitment by NanoBiT beta-arrestin recruitment assayInhibition of human EP4 transfected in human HEK293 cells co transfected with SmBit-beta-arrestin. assessed as reduction in PGE2 induced-beta-arrestin recruitment by NanoBiT beta-arrestin recruitment assay
ChEMBL 458 7 2 5 4.6 C/C=C/c1nnn(Cc2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 10.1021/acs.jmedchem.9b01269
1883 3082 None 47 Human Binding pIC50 = 9.4 9.4 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
1916 3082 None 47 Human Binding pIC50 = 9.4 9.4 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
5280360 3082 None 47 Human Binding pIC50 = 9.4 9.4 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
5280360.0 3082 None 47 Human Binding pIC50 = 9.4 9.4 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
913 3082 None 47 Human Binding pIC50 = 9.4 9.4 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
CHEMBL548 3082 None 47 Human Binding pIC50 = 9.4 9.4 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
DB00917 3082 None 47 Human Binding pIC50 = 9.4 9.4 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
1883 3082 None 47 Human Binding pIC50 = 9.3 9.3 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by 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 10.1016/j.bmc.2016.11.014
1916 3082 None 47 Human Binding pIC50 = 9.3 9.3 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by 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 10.1016/j.bmc.2016.11.014
5280360 3082 None 47 Human Binding pIC50 = 9.3 9.3 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by 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 10.1016/j.bmc.2016.11.014
5280360.0 3082 None 47 Human Binding pIC50 = 9.3 9.3 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by 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 10.1016/j.bmc.2016.11.014
913 3082 None 47 Human Binding pIC50 = 9.3 9.3 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by 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 10.1016/j.bmc.2016.11.014
CHEMBL548 3082 None 47 Human Binding pIC50 = 9.3 9.3 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by 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 10.1016/j.bmc.2016.11.014
DB00917 3082 None 47 Human Binding pIC50 = 9.3 9.3 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by 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 10.1016/j.bmc.2016.11.014
72950089 150679 None 0 Human Binding pIC50 = 9.2 9.2 1621 3
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3955128 150679 None 0 Human Binding pIC50 = 9.2 9.2 1621 3
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
1883 3082 None 47 Human Binding pIC50 = 9.2 9.2 -1 24
Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cellsInhibitory activity against human EP4 receptor expressed in HEK293 ebna 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/s0960-894x(03)00042-8
1916 3082 None 47 Human Binding pIC50 = 9.2 9.2 -1 24
Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cellsInhibitory activity against human EP4 receptor expressed in HEK293 ebna 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/s0960-894x(03)00042-8
5280360 3082 None 47 Human Binding pIC50 = 9.2 9.2 -1 24
Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cellsInhibitory activity against human EP4 receptor expressed in HEK293 ebna 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/s0960-894x(03)00042-8
5280360.0 3082 None 47 Human Binding pIC50 = 9.2 9.2 -1 24
Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cellsInhibitory activity against human EP4 receptor expressed in HEK293 ebna 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/s0960-894x(03)00042-8
913 3082 None 47 Human Binding pIC50 = 9.2 9.2 -1 24
Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cellsInhibitory activity against human EP4 receptor expressed in HEK293 ebna 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/s0960-894x(03)00042-8
CHEMBL548 3082 None 47 Human Binding pIC50 = 9.2 9.2 -1 24
Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cellsInhibitory activity against human EP4 receptor expressed in HEK293 ebna 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/s0960-894x(03)00042-8
DB00917 3082 None 47 Human Binding pIC50 = 9.2 9.2 -1 24
Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cellsInhibitory activity against human EP4 receptor expressed in HEK293 ebna 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/s0960-894x(03)00042-8
72948479 153122 None 0 Human Binding pIC50 = 9.1 9.1 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3975743 153122 None 0 Human Binding pIC50 = 9.1 9.1 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
44409738 139693 None 0 Rat Binding pIC50 = 9.0 9.0 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL379746 139693 None 0 Rat Binding pIC50 = 9.0 9.0 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmcl.2006.01.018
1883 3082 None 47 Human Binding pIC50 = 9.0 9.0 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
1916 3082 None 47 Human Binding pIC50 = 9.0 9.0 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
5280360 3082 None 47 Human Binding pIC50 = 9.0 9.0 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
5280360.0 3082 None 47 Human Binding pIC50 = 9.0 9.0 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
913 3082 None 47 Human Binding pIC50 = 9.0 9.0 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
CHEMBL548 3082 None 47 Human Binding pIC50 = 9.0 9.0 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
DB00917 3082 None 47 Human Binding pIC50 = 9.0 9.0 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
72949200 153866 None 0 Human Binding pIC50 = 8.9 8.9 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 385 11 2 3 3.2 CC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3982139 153866 None 0 Human Binding pIC50 = 8.9 8.9 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 385 11 2 3 3.2 CC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
12521 2197 None 0 Human Binding pIC50 = 8.9 8.9 -1 4
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
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 nan
72722131 2197 None 0 Human Binding pIC50 = 8.9 8.9 -1 4
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
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 nan
CHEMBL3918816 2197 None 0 Human Binding pIC50 = 8.9 8.9 -1 4
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
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 nan
5859 3767 None 24 Human Binding pIC50 = 8.9 8.9 - 1
Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cellsInhibitory activity against human EP4 receptor expressed in HEK293 ebna cells
ChEMBL 383 11 2 5 2.5 O[C@@H](Cc1ccccc1)/C=C/[C@H]1CCC(=O)N1CCCCCCc1nnn[nH]1 10.1016/s0960-894x(03)00042-8
9864831 3767 None 24 Human Binding pIC50 = 8.9 8.9 - 1
Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cellsInhibitory activity against human EP4 receptor expressed in HEK293 ebna cells
ChEMBL 383 11 2 5 2.5 O[C@@H](Cc1ccccc1)/C=C/[C@H]1CCC(=O)N1CCCCCCc1nnn[nH]1 10.1016/s0960-894x(03)00042-8
CHEMBL275667 3767 None 24 Human Binding pIC50 = 8.9 8.9 - 1
Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cellsInhibitory activity against human EP4 receptor expressed in HEK293 ebna cells
ChEMBL 383 11 2 5 2.5 O[C@@H](Cc1ccccc1)/C=C/[C@H]1CCC(=O)N1CCCCCCc1nnn[nH]1 10.1016/s0960-894x(03)00042-8
53323098 57719 None 0 Human Binding pIC50 = 8.8 8.8 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(C)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669013 57719 None 0 Human Binding pIC50 = 8.8 8.8 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(C)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
11524454 946 None 36 Human Binding pIC50 = 8 8.0 - 1
Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cellsDisplacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2011.08.102
5857 946 None 36 Human Binding pIC50 = 8 8.0 - 1
Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cellsDisplacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2011.08.102
CHEMBL591666 946 None 36 Human Binding pIC50 = 8 8.0 - 1
Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cellsDisplacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2011.08.102
53325585 57720 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 616 10 1 4 7.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccc(Cl)cc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669014 57720 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 616 10 1 4 7.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccc(Cl)cc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
10029056 150086 None 0 Human Binding pIC50 = 7 7.0 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 502 9 3 5 5.3 CC1(C)C(=O)[C@H](CC#CCCCC(=O)O)[C@@H](/C=C\C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
CHEMBL3950189 150086 None 0 Human Binding pIC50 = 7 7.0 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 502 9 3 5 5.3 CC1(C)C(=O)[C@H](CC#CCCCC(=O)O)[C@@H](/C=C\C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
786859 110764 None 6 Human Binding pIC50 = 6 6.0 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 308 5 1 3 4.5 Cc1oc(C(=O)O)cc1COc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2014.02.068
CHEMBL3260419 110764 None 6 Human Binding pIC50 = 6 6.0 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 308 5 1 3 4.5 Cc1oc(C(=O)O)cc1COc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2014.02.068
1144137 110767 None 3 Human Binding pIC50 = 6 6.0 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 452 7 3 5 3.9 CC(=O)c1ccc(NS(=O)(=O)c2cc(C(=O)Nc3ccc(C(=O)O)cc3)ccc2C)cc1 10.1016/j.bmcl.2014.02.068
CHEMBL3260422 110767 None 3 Human Binding pIC50 = 6 6.0 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 452 7 3 5 3.9 CC(=O)c1ccc(NS(=O)(=O)c2cc(C(=O)Nc3ccc(C(=O)O)cc3)ccc2C)cc1 10.1016/j.bmcl.2014.02.068
90656152 110769 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 308 5 1 3 4.5 Cc1oc(C(=O)O)cc1COc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2014.02.068
CHEMBL3260426 110769 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 308 5 1 3 4.5 Cc1oc(C(=O)O)cc1COc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2014.02.068
44564990 192759 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of radioligand from EP4 receptorDisplacement of radioligand from EP4 receptor
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 192759 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of radioligand from EP4 receptorDisplacement of radioligand from EP4 receptor
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
10096272 146691 None 0 Human Binding pIC50 = 5 5.0 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 470 10 2 6 4.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1cc2ccccc2s1 nan
CHEMBL3923193 146691 None 0 Human Binding pIC50 = 5 5.0 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 470 10 2 6 4.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1cc2ccccc2s1 nan
44627395 199328 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP4 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 199328 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP4 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
25015836 57709 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 772 10 2 7 7.5 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccc4ccccc4c3)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669003 57709 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 772 10 2 7 7.5 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccc4ccccc4c3)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
58905358 159685 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 384 6 2 4 3.8 O=C(O)c1ccc(CNC(=O)c2cc(F)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4103046 159685 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 384 6 2 4 3.8 O=C(O)c1ccc(CNC(=O)c2cc(F)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4448899 216397 None 46 Human Binding pIC50 = 6.0 6.0 - 2
Selectivity interaction (Eurofins-Panlabs radioligand binding assay ) EUB0000307b PTGER4Selectivity interaction (Eurofins-Panlabs radioligand binding assay ) EUB0000307b PTGER4
ChEMBL None None None Cc1c(NC(=O)c2cc(C(N)=O)nc3cc(F)ccc23)c(C(F)(F)F)nn1Cc1ccc(C#N)cc1 10.6019/CHEMBL5212743
86707361 139444 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 403 4 2 4 4.2 Cc1ccc(N2CCC(F)(F)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
CHEMBL3793002 139444 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 403 4 2 4 4.2 Cc1ccc(N2CCC(F)(F)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
90656151 110765 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 363 4 1 5 5.0 CC(C)c1c(C(=O)O)cnn1-c1nc(-c2ccc3ccccc3c2)cs1 10.1016/j.bmcl.2014.02.068
CHEMBL3260420 110765 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 363 4 1 5 5.0 CC(C)c1c(C(=O)O)cnn1-c1nc(-c2ccc3ccccc3c2)cs1 10.1016/j.bmcl.2014.02.068
44409902 74772 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 377 12 3 4 3.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(O)c1 10.1016/j.bmcl.2006.01.018
CHEMBL203076 74772 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 377 12 3 4 3.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(O)c1 10.1016/j.bmcl.2006.01.018
89914863 122663 None 0 Human Binding pIC50 = 5.9 5.9 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 421 8 2 5 3.4 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(C#N)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600883 122663 None 0 Human Binding pIC50 = 5.9 5.9 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 421 8 2 5 3.4 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(C#N)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601984 122663 None 0 Human Binding pIC50 = 5.9 5.9 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 421 8 2 5 3.4 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(C#N)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
89914526 122664 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 414 8 2 4 3.6 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600884 122664 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 414 8 2 4 3.6 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601985 122664 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 414 8 2 4 3.6 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
118191094 137441 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 444 5 3 4 4.8 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1nc(-c2cccc(CO)c2)ccc1C(F)(F)F 10.1016/j.bmcl.2015.12.057
CHEMBL3752948 137441 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 444 5 3 4 4.8 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1nc(-c2cccc(CO)c2)ccc1C(F)(F)F 10.1016/j.bmcl.2015.12.057
72695136 131403 None 2 Human Binding pIC50 = 6.9 6.9 - 1
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 383 4 3 5 2.9 Cc1ccc(N2CCC(O)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
CHEMBL3686863 131403 None 2 Human Binding pIC50 = 6.9 6.9 - 1
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 383 4 3 5 2.9 Cc1ccc(N2CCC(O)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
72695027 106322 None 0 Human Binding pIC50 = 6.9 6.9 28 2
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of PGE2 inhibitory effect on LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS/PGE2 addition measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of PGE2 inhibitory effect on LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS/PGE2 addition measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
CHEMBL3115074 106322 None 0 Human Binding pIC50 = 6.9 6.9 28 2
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of PGE2 inhibitory effect on LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS/PGE2 addition measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of PGE2 inhibitory effect on LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS/PGE2 addition measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
CHEMBL3138992 106322 None 0 Human Binding pIC50 = 6.9 6.9 28 2
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of PGE2 inhibitory effect on LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS/PGE2 addition measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of PGE2 inhibitory effect on LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS/PGE2 addition measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
58905388 158758 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 383 6 2 3 4.4 O=C(O)c1ccc(CNC(=O)c2cc(F)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4092846 158758 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 383 6 2 3 4.4 O=C(O)c1ccc(CNC(=O)c2cc(F)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
44157014 192726 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of radioligand from EP4 receptorDisplacement of radioligand from EP4 receptor
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 192726 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of radioligand from EP4 receptorDisplacement of radioligand from EP4 receptor
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
72695027 106322 None 0 Human Binding pIC50 = 6.9 6.9 28 2
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3115074 106322 None 0 Human Binding pIC50 = 6.9 6.9 28 2
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3138992 106322 None 0 Human Binding pIC50 = 6.9 6.9 28 2
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
11165865 77303 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 413 10 2 3 3.8 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL208080 77303 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 413 10 2 3 3.8 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.01.018
11618662 158914 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 421 6 2 5 4.6 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(C#N)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4094572 158914 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 421 6 2 5 4.6 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(C#N)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
56944705 129281 None 39 Human Binding pIC50 = 7.9 7.9 - 1
Antagonist activity at EP4 receptor (unknown origin)Antagonist activity at EP4 receptor (unknown origin)
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
CHEMBL3670685 129281 None 39 Human Binding pIC50 = 7.9 7.9 - 1
Antagonist activity at EP4 receptor (unknown origin)Antagonist activity at EP4 receptor (unknown origin)
ChEMBL 483 7 2 5 5.4 C[C@H](NC(=O)c1c(C(F)F)nn(C)c1Oc1cccc(C(F)(F)F)c1)c1ccc(C(=O)O)cc1 10.1021/acsmedchemlett.2c00495
44564892 180628 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of radioligand from EP4 receptorDisplacement of radioligand from EP4 receptor
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 180628 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of radioligand from EP4 receptorDisplacement of radioligand from EP4 receptor
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
11955357 148716 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [3H]PGE2 from from human EP4 receptor expressed in HEK293 cells membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP4 receptor expressed in HEK293 cells membranes incubated for 60 mins
ChEMBL 378 8 1 3 4.8 COC(=O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl nan
CHEMBL3939358 148716 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [3H]PGE2 from from human EP4 receptor expressed in HEK293 cells membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP4 receptor expressed in HEK293 cells membranes incubated for 60 mins
ChEMBL 378 8 1 3 4.8 COC(=O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl nan
118191077 136887 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 425 5 3 3 5.6 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3741430 136887 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 425 5 3 3 5.6 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
25018911 57714 None 7 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669008 57714 None 7 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019184 57716 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669010 57716 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
44409693 166193 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 429 11 2 4 4.3 CCc1ccc(CC(O)CC[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL425950 166193 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 429 11 2 4 4.3 CCc1ccc(CC(O)CC[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)cc1 10.1016/j.bmcl.2006.01.018
10319627 154376 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 10 2 5 3.6 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1ccccc1 nan
CHEMBL3986534 154376 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 10 2 5 3.6 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1ccccc1 nan
86707344 139416 None 1 Human Binding pIC50 = 5.8 5.8 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 383 4 3 5 2.9 Cc1ccc(N2CCC(O)CC2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
CHEMBL3792709 139416 None 1 Human Binding pIC50 = 5.8 5.8 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 383 4 3 5 2.9 Cc1ccc(N2CCC(O)CC2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
86707347 139529 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 397 5 3 5 3.2 Cc1ccc(N2CCCC(CO)C2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
CHEMBL3793956 139529 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 397 5 3 5 3.2 Cc1ccc(N2CCCC(CO)C2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
44564804 176805 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of radioligand from EP4 receptorDisplacement of radioligand from EP4 receptor
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 176805 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of radioligand from EP4 receptorDisplacement of radioligand from EP4 receptor
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
46885690 8458 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity to human EP4 receptor by radioligand displacement assayBinding affinity to human EP4 receptor by radioligand displacement assay
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 8458 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity to human EP4 receptor by radioligand displacement assayBinding affinity to human EP4 receptor by radioligand displacement assay
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
11677589 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2016.03.041
11677589.0 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2016.03.041
5858 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2016.03.041
CHEMBL3039498 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2016.03.041
DB12836 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2016.03.041
11677589 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.11.023
11677589.0 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.11.023
5858 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.11.023
CHEMBL3039498 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.11.023
DB12836 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.11.023
10007859 166584 None 0 Human Binding pIC50 = 6.8 6.8 - 2
Inhibition of EP4 receptorInhibition of EP4 receptor
ChEMBL 554 7 2 4 6.7 CC(=O)Nc1cc(C(=O)O)cc(-n2c(C)ccc2-c2cc(Br)ccc2OCc2ccc(F)cc2F)c1 10.1016/j.bmcl.2006.10.078
CHEMBL427844 166584 None 0 Human Binding pIC50 = 6.8 6.8 - 2
Inhibition of EP4 receptorInhibition of EP4 receptor
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 86190 None 0 Human Binding pIC50 = 4.8 4.8 -7079 4
Binding affinity to human EP4 receptor expressed in CHO cellsBinding affinity to human EP4 receptor expressed in CHO cells
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 86190 None 0 Human Binding pIC50 = 4.8 4.8 -7079 4
Binding affinity to human EP4 receptor expressed in CHO cellsBinding affinity to human EP4 receptor expressed in CHO cells
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
53323099 57724 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 578 11 1 5 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669018 57724 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 578 11 1 5 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
11677589 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.12.057
11677589.0 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.12.057
5858 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.12.057
CHEMBL3039498 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.12.057
DB12836 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.12.057
44409739 139747 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2-c2ccccc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL379785 139747 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2-c2ccccc2)s1 10.1016/j.bmcl.2006.01.018
11677589 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
11677589.0 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
5858 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
CHEMBL3039498 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
DB12836 1859 None 51 Human Binding pIC50 = 5.8 5.8 -3 4
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
44409917 139337 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(F)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL378968 139337 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(F)c2)s1 10.1016/j.bmcl.2006.01.018
53323098 57719 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(C)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669013 57719 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(C)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
78319379 137564 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 389 5 3 3 4.7 Cc1ccc(-c2cccc(CO)c2)cc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2015.12.057
CHEMBL3753860 137564 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 389 5 3 3 4.7 Cc1ccc(-c2cccc(CO)c2)cc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2015.12.057
122180295 121709 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 422 3 1 4 5.3 O=c1cc(CN2CCOc3c(Cl)cc(-c4csc5ccccc45)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586359 121709 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 422 3 1 4 5.3 O=c1cc(CN2CCOc3c(Cl)cc(-c4csc5ccccc45)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
58905313 157064 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 412 7 2 4 4.7 CCC(NC(=O)c1cc(F)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4072974 157064 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 412 7 2 4 4.7 CCC(NC(=O)c1cc(F)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
46879894 6183 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity to human EP4 receptor by radioligand displacement assayBinding affinity to human EP4 receptor by radioligand displacement assay
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 6183 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity to human EP4 receptor by radioligand displacement assayBinding affinity to human EP4 receptor by radioligand displacement assay
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
25019694 57732 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 641 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(C)cccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669026 57732 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 641 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(C)cccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
118174952 136909 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 396 4 2 3 5.5 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2ccccc2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3741642 136909 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 396 4 2 3 5.5 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2ccccc2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
9934368 139008 None 11 Human Binding pIC50 = 8.7 8.7 - 1
Agonist activity at human EP4 receptor expressed in CHO cells co-transfected with CRE-beta-lactamase reporter gene assessed as increase in intracellular cAMP measured after 3 hrs by TR FRET based assayAgonist activity at human EP4 receptor expressed in CHO cells co-transfected with CRE-beta-lactamase reporter gene assessed as increase in intracellular cAMP measured after 3 hrs by TR FRET based assay
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.ejmech.2021.113842
CHEMBL378376 139008 None 11 Human Binding pIC50 = 8.7 8.7 - 1
Agonist activity at human EP4 receptor expressed in CHO cells co-transfected with CRE-beta-lactamase reporter gene assessed as increase in intracellular cAMP measured after 3 hrs by TR FRET based assayAgonist activity at human EP4 receptor expressed in CHO cells co-transfected with CRE-beta-lactamase reporter gene assessed as increase in intracellular cAMP measured after 3 hrs by TR FRET based assay
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.ejmech.2021.113842
171347889 193838 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Agonist activity at human EP4 receptor expressed in CHO cells co-transfected with CRE-beta-lactamase reporter gene assessed as increase in intracellular cAMP measured after 3 hrs by TR FRET based assayAgonist activity at human EP4 receptor expressed in CHO cells co-transfected with CRE-beta-lactamase reporter gene assessed as increase in intracellular cAMP measured after 3 hrs by TR FRET based assay
ChEMBL 509 12 1 4 6.3 CC(C)CC(=O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.ejmech.2021.113842
CHEMBL5272661 193838 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Agonist activity at human EP4 receptor expressed in CHO cells co-transfected with CRE-beta-lactamase reporter gene assessed as increase in intracellular cAMP measured after 3 hrs by TR FRET based assayAgonist activity at human EP4 receptor expressed in CHO cells co-transfected with CRE-beta-lactamase reporter gene assessed as increase in intracellular cAMP measured after 3 hrs by TR FRET based assay
ChEMBL 509 12 1 4 6.3 CC(C)CC(=O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.ejmech.2021.113842
57392712 67870 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cellsDisplacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells
ChEMBL 455 4 2 3 5.8 C[C@H](NC(=O)c1cccc2c1Oc1cc(C(F)(F)F)ccc1CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.08.102
CHEMBL1910022 67870 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cellsDisplacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells
ChEMBL 455 4 2 3 5.8 C[C@H](NC(=O)c1cccc2c1Oc1cc(C(F)(F)F)ccc1CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.08.102
25019695 57731 None 0 Human Binding pIC50 = 8.7 8.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4cccc(Cl)c4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669025 57731 None 0 Human Binding pIC50 = 8.7 8.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4cccc(Cl)c4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53325585 57720 None 0 Human Binding pIC50 = 8.7 8.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 616 10 1 4 7.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccc(Cl)cc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669014 57720 None 0 Human Binding pIC50 = 8.7 8.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 616 10 1 4 7.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccc(Cl)cc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
1883 3082 None 47 Rat Binding pIC50 = 8.7 8.7 1 24
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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.2009.01.059
1916 3082 None 47 Rat Binding pIC50 = 8.7 8.7 1 24
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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.2009.01.059
5280360 3082 None 47 Rat Binding pIC50 = 8.7 8.7 1 24
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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.2009.01.059
5280360.0 3082 None 47 Rat Binding pIC50 = 8.7 8.7 1 24
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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.2009.01.059
913 3082 None 47 Rat Binding pIC50 = 8.7 8.7 1 24
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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.2009.01.059
CHEMBL548 3082 None 47 Rat Binding pIC50 = 8.7 8.7 1 24
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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.2009.01.059
DB00917 3082 None 47 Rat Binding pIC50 = 8.7 8.7 1 24
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 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.2009.01.059
25019433 57710 None 0 Human Binding pIC50 = 8.7 8.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 691 10 2 6 6.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Br)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669004 57710 None 0 Human Binding pIC50 = 8.7 8.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 691 10 2 6 6.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Br)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
11577792 159412 None 20 Human Binding pIC50 = 8.6 8.6 -1 5
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4099851 159412 None 20 Human Binding pIC50 = 8.6 8.6 -1 5
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
25019183 57718 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 647 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669012 57718 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 647 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
72949915 143420 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 451 14 2 3 4.8 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3897335 143420 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 451 14 2 3 4.8 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
25019435 57713 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 663 10 2 6 7.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc5ccccc5c4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669007 57713 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 663 10 2 6 7.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc5ccccc5c4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
10479215 146549 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 146549 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
10006340 150730 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 504 11 3 5 5.8 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
CHEMBL3955476 150730 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 504 11 3 5 5.8 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
10029056 150086 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 502 9 3 5 5.3 CC1(C)C(=O)[C@H](CC#CCCCC(=O)O)[C@@H](/C=C\C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
CHEMBL3950189 150086 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 502 9 3 5 5.3 CC1(C)C(=O)[C@H](CC#CCCCC(=O)O)[C@@H](/C=C\C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
10006340 150730 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 504 11 3 5 5.8 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
CHEMBL3955476 150730 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 504 11 3 5 5.8 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
122180297 121712 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 437 3 1 4 4.9 C[C@@H]1COc2c(Cl)cc(-n3ccc4cc(F)ccc43)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586362 121712 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 437 3 1 4 4.9 C[C@@H]1COc2c(Cl)cc(-n3ccc4cc(F)ccc43)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
89914844 122662 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 382 8 2 4 2.9 O=C(O)c1ccc(CNC(=O)[C@H]2CCCCN2CCOc2ccccc2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600786 122662 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 382 8 2 4 2.9 O=C(O)c1ccc(CNC(=O)[C@H]2CCCCN2CCOc2ccccc2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601983 122662 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 382 8 2 4 2.9 O=C(O)c1ccc(CNC(=O)[C@H]2CCCCN2CCOc2ccccc2)cc1 10.1016/j.bmcl.2015.05.091
44564571 186921 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of radioligand from EP4 receptorDisplacement of radioligand from EP4 receptor
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 186921 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of radioligand from EP4 receptorDisplacement of radioligand from EP4 receptor
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
44570712 183184 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity to human EP4 receptor by radioligand binding assayBinding affinity to human EP4 receptor by radioligand binding assay
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 183184 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity to human EP4 receptor by radioligand binding assayBinding affinity to human EP4 receptor by radioligand binding assay
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
44570668 184123 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity to human EP4 receptor by radioligand binding assayBinding affinity to human EP4 receptor by radioligand binding assay
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 184123 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity to human EP4 receptor by radioligand binding assayBinding affinity to human EP4 receptor by radioligand binding assay
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
44409733 140971 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 401 10 2 4 3.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL382029 140971 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 401 10 2 4 3.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2)s1 10.1016/j.bmcl.2006.01.018
10113454 177606 None 0 Rat Binding pIC50 = 7.7 7.7 - 3
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
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.2006.01.018
CHEMBL46395 177606 None 0 Rat Binding pIC50 = 7.7 7.7 - 3
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
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.2006.01.018
25019434 57711 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 673 12 2 8 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(OC)cccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669005 57711 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 673 12 2 8 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(OC)cccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
58905368 156465 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 399 6 2 3 4.9 O=C(O)c1ccc(CNC(=O)c2cc(Cl)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4066230 156465 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 399 6 2 3 4.9 O=C(O)c1ccc(CNC(=O)c2cc(Cl)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
44409743 141386 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 419 15 2 4 3.6 COCCc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
CHEMBL383339 141386 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 419 15 2 4 3.6 COCCc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
10096272 146691 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 470 10 2 6 4.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1cc2ccccc2s1 nan
CHEMBL3923193 146691 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 470 10 2 6 4.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1cc2ccccc2s1 nan
22394738 75440 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 395 12 2 3 4.1 O=C(O)CCCCCCN1C(=O)CCC1CCC(O)Cc1cccc(Cl)c1 10.1016/j.bmcl.2006.01.018
CHEMBL204058 75440 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 395 12 2 3 4.1 O=C(O)CCCCCCN1C(=O)CCC1CCC(O)Cc1cccc(Cl)c1 10.1016/j.bmcl.2006.01.018
25019433 57710 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 691 10 2 6 6.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Br)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669004 57710 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 691 10 2 6 6.6 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Br)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
11260304 140803 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 487 12 2 4 5.5 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL381755 140803 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 487 12 2 4 5.5 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(Oc3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.018
25019185 57715 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 643 11 2 7 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669009 57715 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 643 11 2 7 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53325765 57723 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 579 11 1 6 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ncccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669017 57723 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 579 11 1 6 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ncccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
46885691 8459 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity to human EP4 receptor by radioligand displacement assayBinding affinity to human EP4 receptor by radioligand displacement assay
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 8459 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity to human EP4 receptor by radioligand displacement assayBinding affinity to human EP4 receptor by radioligand displacement assay
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
10369368 153526 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 518 11 2 6 5.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
CHEMBL3979233 153526 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 518 11 2 6 5.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
89914445 122660 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 410 9 2 4 3.9 CC[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600787 122660 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 410 9 2 4 3.9 CC[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601950 122660 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 410 9 2 4 3.9 CC[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
10432730 147357 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 147357 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
16664733 154917 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Inhibition of human recombinant EP4 receptor expressed in 293EBNA cellsInhibition of human recombinant EP4 receptor expressed in 293EBNA cells
ChEMBL 483 9 3 5 4.3 CC(=O)Nc1cccc(-c2ccc(Cc3ocnc3C(=O)N[C@@H](Cc3ccccc3)C(=O)O)cc2)c1 10.1016/j.bmcl.2006.12.025
CHEMBL400404 154917 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Inhibition of human recombinant EP4 receptor expressed in 293EBNA cellsInhibition of human recombinant EP4 receptor expressed in 293EBNA cells
ChEMBL 483 9 3 5 4.3 CC(=O)Nc1cccc(-c2ccc(Cc3ocnc3C(=O)N[C@@H](Cc3ccccc3)C(=O)O)cc2)c1 10.1016/j.bmcl.2006.12.025
118175009 136772 None 0 Human Binding pIC50 = 6.6 6.6 812 2
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.12.057
CHEMBL3740325 136772 None 0 Human Binding pIC50 = 6.6 6.6 812 2
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.12.057
118175009 136772 None 0 Human Binding pIC50 = 6.6 6.6 812 2
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3740325 136772 None 0 Human Binding pIC50 = 6.6 6.6 812 2
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
10436601 152641 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 516 9 2 6 5.3 COC(=O)CCCC#CC[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C\C(O)CCc1sc2ccccc2c1Cl nan
CHEMBL3971666 152641 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 516 9 2 6 5.3 COC(=O)CCCC#CC[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C\C(O)CCc1sc2ccccc2c1Cl nan
16048029 197960 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 receptor expressed in HEK293 cells
ChEMBL 369 10 1 3 3.8 CC(C)(C)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL553468 197960 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 receptor expressed in HEK293 cells
ChEMBL 369 10 1 3 3.8 CC(C)(C)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11326896 166381 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 395 10 2 3 3.7 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2ccccc2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL427035 166381 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 395 10 2 3 3.7 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2ccccc2)cc1 10.1016/j.bmcl.2006.01.018
9885481 197839 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 receptor expressed in HEK293 cells
ChEMBL 365 16 2 4 3.0 CCCCCC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
CHEMBL551951 197839 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of rat EP4 receptor expressed in HEK293 cellsInhibition of rat EP4 receptor expressed in HEK293 cells
ChEMBL 365 16 2 4 3.0 CCCCCC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
10434119 150526 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 454 8 3 5 4.2 CC1(C)C(=O)[C@H](CC#CCCCC(=O)O)[C@@H](/C=C/C(O)Cc2cc3ccccc3s2)[C@@H]1O nan
CHEMBL3954031 150526 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 454 8 3 5 4.2 CC1(C)C(=O)[C@H](CC#CCCCC(=O)O)[C@@H](/C=C/C(O)Cc2cc3ccccc3s2)[C@@H]1O nan
775693 46505 None 21 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 305 4 2 2 3.7 O=C(Cc1cccc2ccccc12)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2014.02.068
CHEMBL1537470 46505 None 21 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 305 4 2 2 3.7 O=C(Cc1cccc2ccccc12)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2014.02.068
57399661 67873 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cellsDisplacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells
ChEMBL 467 4 2 3 5.7 O=C(O)c1ccc(C2(NC(=O)c3cccc4c3Oc3ccc(C(F)(F)F)cc3CC4)CC2)cc1 10.1016/j.bmcl.2011.08.102
CHEMBL1910025 67873 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cellsDisplacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells
ChEMBL 467 4 2 3 5.7 O=C(O)c1ccc(C2(NC(=O)c3cccc4c3Oc3ccc(C(F)(F)F)cc3CC4)CC2)cc1 10.1016/j.bmcl.2011.08.102
10369368 153526 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 518 11 2 6 5.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
CHEMBL3979233 153526 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 518 11 2 6 5.9 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
71458060 79117 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 375 13 2 3 3.8 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)CCc1ccccc1 10.1016/j.bmcl.2006.01.018
CHEMBL2113220 79117 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 375 13 2 3 3.8 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)CCc1ccccc1 10.1016/j.bmcl.2006.01.018
11486771 170497 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 413 10 2 3 3.8 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL444798 170497 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 413 10 2 3 3.8 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.01.018
25016088 57712 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 681 10 2 6 6.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C(F)(F)F)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669006 57712 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 681 10 2 6 6.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C(F)(F)F)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019695 57731 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4cccc(Cl)c4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669025 57731 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4cccc(Cl)c4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
58905345 158985 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 398 6 2 4 4.3 C[C@H](NC(=O)c1cc(F)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4095293 158985 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 398 6 2 4 4.3 C[C@H](NC(=O)c1cc(F)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
86707350 139525 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 397 5 3 5 3.2 Cc1ccc(N2CCCC(CO)C2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
CHEMBL3793928 139525 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 397 5 3 5 3.2 Cc1ccc(N2CCCC(CO)C2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
9807398 151387 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 542 12 3 7 5.3 CC1(C)C(=O)[C@H](SCCCSCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
CHEMBL3960625 151387 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 542 12 3 7 5.3 CC1(C)C(=O)[C@H](SCCCSCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
89914445 122660 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 410 9 2 4 3.9 CC[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600787 122660 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 410 9 2 4 3.9 CC[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601950 122660 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 410 9 2 4 3.9 CC[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
25018911 57714 None 7 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669008 57714 None 7 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
24944538 57717 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 756 10 2 7 7.0 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccccc3Cl)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669011 57717 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 756 10 2 7 7.0 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccccc3Cl)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
25019694 57732 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 641 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(C)cccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669026 57732 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 641 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(C)cccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019434 57711 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 673 12 2 8 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(OC)cccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669005 57711 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 673 12 2 8 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(OC)cccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25016088 57712 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 681 10 2 6 6.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C(F)(F)F)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669006 57712 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 681 10 2 6 6.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C(F)(F)F)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019184 57716 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669010 57716 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 627 10 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4C)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
72948294 150045 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 439 9 2 4 4.0 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3949856 150045 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 439 9 2 4 4.0 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
25019185 57715 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 643 11 2 7 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669009 57715 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 643 11 2 7 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53325764 57722 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 622 12 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4cc(C(=O)O)ccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669016 57722 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 622 12 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4cc(C(=O)O)ccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
1883 3082 None 47 Human Binding pIC50 = 8.4 8.4 -1 24
Displacement of radiolabeled PGE2 from human prostanoid EP4 receptorDisplacement of radiolabeled PGE2 from human prostanoid EP4 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/jm8007618
1916 3082 None 47 Human Binding pIC50 = 8.4 8.4 -1 24
Displacement of radiolabeled PGE2 from human prostanoid EP4 receptorDisplacement of radiolabeled PGE2 from human prostanoid EP4 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/jm8007618
5280360 3082 None 47 Human Binding pIC50 = 8.4 8.4 -1 24
Displacement of radiolabeled PGE2 from human prostanoid EP4 receptorDisplacement of radiolabeled PGE2 from human prostanoid EP4 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/jm8007618
5280360.0 3082 None 47 Human Binding pIC50 = 8.4 8.4 -1 24
Displacement of radiolabeled PGE2 from human prostanoid EP4 receptorDisplacement of radiolabeled PGE2 from human prostanoid EP4 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/jm8007618
913 3082 None 47 Human Binding pIC50 = 8.4 8.4 -1 24
Displacement of radiolabeled PGE2 from human prostanoid EP4 receptorDisplacement of radiolabeled PGE2 from human prostanoid EP4 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/jm8007618
CHEMBL548 3082 None 47 Human Binding pIC50 = 8.4 8.4 -1 24
Displacement of radiolabeled PGE2 from human prostanoid EP4 receptorDisplacement of radiolabeled PGE2 from human prostanoid EP4 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/jm8007618
DB00917 3082 None 47 Human Binding pIC50 = 8.4 8.4 -1 24
Displacement of radiolabeled PGE2 from human prostanoid EP4 receptorDisplacement of radiolabeled PGE2 from human prostanoid EP4 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/jm8007618
11961366 150560 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 556 12 2 8 5.4 COC(=O)CSCCCS[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
CHEMBL3954286 150560 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 556 12 2 8 5.4 COC(=O)CSCCCS[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
56927669 121710 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 121710 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
122180296 121711 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 436 3 1 4 5.7 C[C@@H]1COc2c(Cl)cc(-c3csc4ccccc34)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586361 121711 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 436 3 1 4 5.7 C[C@@H]1COc2c(Cl)cc(-c3csc4ccccc34)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
10479215 146549 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 146549 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
118191085 136938 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 426 5 3 4 5.0 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3741902 136938 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 426 5 3 4 5.0 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
122180289 121704 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 406 3 0 4 6.0 Clc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586353 121704 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 406 3 0 4 6.0 Clc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
25019183 57718 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 647 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669012 57718 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 647 10 2 6 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
44409712 77369 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 437 13 2 3 5.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2006.01.018
CHEMBL208399 77369 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 437 13 2 3 5.1 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2006.01.018
53319154 57721 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 582 10 1 4 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669015 57721 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 582 10 1 4 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
30897313 121663 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 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 121663 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP4 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
86707352 139524 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 397 4 3 5 3.3 Cc1ccc(N2CCC(C)(O)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
CHEMBL3793924 139524 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 397 4 3 5 3.3 Cc1ccc(N2CCC(C)(O)CC2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2016.03.041
44627515 199293 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP4 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 199293 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP4 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
25019435 57713 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 663 10 2 6 7.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc5ccccc5c4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669007 57713 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 663 10 2 6 7.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc5ccccc5c4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
58905349 156369 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 400 6 2 4 4.3 O=C(O)c1ccc(CNC(=O)c2cc(Cl)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4065183 156369 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 400 6 2 4 4.3 O=C(O)c1ccc(CNC(=O)c2cc(Cl)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
25019697 57708 None 0 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 697 11 2 7 6.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(OC(F)(F)F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669002 57708 None 0 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 697 11 2 7 6.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(OC(F)(F)F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
44190762 176985 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of prostanoid EP4 receptorInhibition of prostanoid EP4 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 176985 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of prostanoid EP4 receptorInhibition of prostanoid EP4 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
91810751 137592 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
CHEMBL3754085 137592 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassayAntagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2016.03.041
91810751 137592 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
CHEMBL3754085 137592 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
44409923 166098 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 386 12 2 4 3.3 N#Cc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
CHEMBL425409 166098 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 386 12 2 4 3.3 N#Cc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
57396195 67871 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cellsDisplacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells
ChEMBL 467 4 2 3 5.7 O=C(O)c1ccc(C2(NC(=O)c3cccc4c3Oc3cc(C(F)(F)F)ccc3CC4)CC2)cc1 10.1016/j.bmcl.2011.08.102
CHEMBL1910023 67871 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cellsDisplacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells
ChEMBL 467 4 2 3 5.7 O=C(O)c1ccc(C2(NC(=O)c3cccc4c3Oc3cc(C(F)(F)F)ccc3CC4)CC2)cc1 10.1016/j.bmcl.2011.08.102
10046549 151824 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 151824 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
53323099 57724 None 0 Human Binding pIC50 = 8.3 8.3 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 578 11 1 5 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669018 57724 None 0 Human Binding pIC50 = 8.3 8.3 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 578 11 1 5 6.5 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
25019696 57730 None 0 Human Binding pIC50 = 8.3 8.3 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 631 10 2 6 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669024 57730 None 0 Human Binding pIC50 = 8.3 8.3 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 631 10 2 6 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
53325765 57723 None 0 Human Binding pIC50 = 8.3 8.3 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 579 11 1 6 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ncccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669017 57723 None 0 Human Binding pIC50 = 8.3 8.3 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 579 11 1 6 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ncccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
72950260 151248 None 0 Human Binding pIC50 = 8.3 8.3 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 437 14 2 3 4.6 O=C(O)CCCCCCN1C(=O)C(F)(F)C[C@@H]1/C=C/[C@@H](O)CCCCc1ccccc1 nan
CHEMBL3959605 151248 None 0 Human Binding pIC50 = 8.3 8.3 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 437 14 2 3 4.6 O=C(O)CCCCCCN1C(=O)C(F)(F)C[C@@H]1/C=C/[C@@H](O)CCCCc1ccccc1 nan
10045223 152056 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 152056 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
10023570 153425 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 153425 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
10323691 143315 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 499 12 4 6 3.8 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)NCCO)[C@@H](/C=C/C(O)Cc2cc3ccccc3s2)[C@@H]1O nan
CHEMBL3896491 143315 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 499 12 4 6 3.8 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)NCCO)[C@@H](/C=C/C(O)Cc2cc3ccccc3s2)[C@@H]1O nan
11339406 141421 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 429 10 2 3 4.3 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL383515 141421 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 429 10 2 3 4.3 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2006.01.018
1884 3083 None 40 Human Binding pIC50 = 5.4 5.4 -15 22
Affinity for Prostanoid EP4 receptor expressed in CHO cellsAffinity for Prostanoid EP4 receptor expressed in CHO cells
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 3083 None 40 Human Binding pIC50 = 5.4 5.4 -15 22
Affinity for Prostanoid EP4 receptor expressed in CHO cellsAffinity for Prostanoid EP4 receptor expressed in CHO cells
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 3083 None 40 Human Binding pIC50 = 5.4 5.4 -15 22
Affinity for Prostanoid EP4 receptor expressed in CHO cellsAffinity for Prostanoid EP4 receptor expressed in CHO cells
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 3083 None 40 Human Binding pIC50 = 5.4 5.4 -15 22
Affinity for Prostanoid EP4 receptor expressed in CHO cellsAffinity for Prostanoid EP4 receptor expressed in CHO cells
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 3083 None 40 Human Binding pIC50 = 5.4 5.4 -15 22
Affinity for Prostanoid EP4 receptor expressed in CHO cellsAffinity for Prostanoid EP4 receptor expressed in CHO cells
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
1884 3083 None 40 Human Binding pIC50 = 5.4 5.4 -15 22
In vitro binding at EP4 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP4 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 3083 None 40 Human Binding pIC50 = 5.4 5.4 -15 22
In vitro binding at EP4 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP4 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 3083 None 40 Human Binding pIC50 = 5.4 5.4 -15 22
In vitro binding at EP4 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP4 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 3083 None 40 Human Binding pIC50 = 5.4 5.4 -15 22
In vitro binding at EP4 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP4 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 3083 None 40 Human Binding pIC50 = 5.4 5.4 -15 22
In vitro binding at EP4 human prostaglandin receptor using [3H]PGE-2 as radioligandIn vitro binding at EP4 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
9807398 151387 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 542 12 3 7 5.3 CC1(C)C(=O)[C@H](SCCCSCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
CHEMBL3960625 151387 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 542 12 3 7 5.3 CC1(C)C(=O)[C@H](SCCCSCC(=O)O)[C@@H](/C=C/C(O)CCc2sc3ccccc3c2Cl)[C@@H]1O nan
10319627 154376 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 10 2 5 3.6 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1ccccc1 nan
CHEMBL3986534 154376 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 10 2 5 3.6 COC(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1ccccc1 nan
3756926 110766 None 6 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 357 2 1 4 4.1 O=C(O)c1ccc2c(c1)C(=O)N(c1ccc3c(c1)oc1ccccc13)C2=O 10.1016/j.bmcl.2014.02.068
CHEMBL3260421 110766 None 6 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 357 2 1 4 4.1 O=C(O)c1ccc2c(c1)C(=O)N(c1ccc3c(c1)oc1ccccc13)C2=O 10.1016/j.bmcl.2014.02.068
2883793 110768 None 5 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 322 4 1 4 4.8 Cc1oc(C(=O)O)cc1COc1ccc2oc3ccccc3c2c1 10.1016/j.bmcl.2014.02.068
CHEMBL3260423 110768 None 5 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 322 4 1 4 4.8 Cc1oc(C(=O)O)cc1COc1ccc2oc3ccccc3c2c1 10.1016/j.bmcl.2014.02.068
11351910 77372 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 471 11 2 3 5.4 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL208411 77372 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 471 11 2 3 5.4 O=C(O)c1ccc(CCCN2C(=O)CCC2CCC(O)Cc2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmcl.2006.01.018
118190924 137529 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 393 5 3 3 4.6 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)ccc1F 10.1016/j.bmcl.2015.12.057
CHEMBL3753567 137529 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 393 5 3 3 4.6 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)ccc1F 10.1016/j.bmcl.2015.12.057
9983881 144936 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 511 12 2 5 5.5 CCN(CC)C(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1cc2ccccc2s1 nan
CHEMBL3909714 144936 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 511 12 2 5 5.5 CCN(CC)C(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1cc2ccccc2s1 nan
24944538 57717 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 756 10 2 7 7.0 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccccc3Cl)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669011 57717 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 756 10 2 7 7.0 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccccc3Cl)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
11502889 156151 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 430 6 2 4 5.4 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4062620 156151 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 430 6 2 4 5.4 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
10339756 143172 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 143172 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
44409910 140996 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 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 140996 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 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
9981458 143820 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 455 10 3 5 4.2 CC1(C)C(=O)[C@H](C/C=C\CCCC(N)=O)[C@@H](/C=C/C(O)Cc2cc3ccccc3s2)[C@@H]1O nan
CHEMBL3900651 143820 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 455 10 3 5 4.2 CC1(C)C(=O)[C@H](C/C=C\CCCC(N)=O)[C@@H](/C=C/C(O)Cc2cc3ccccc3s2)[C@@H]1O nan
118174968 136705 None 0 Human Binding pIC50 = 6.3 6.3 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 426 5 3 4 5.0 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3739779 136705 None 0 Human Binding pIC50 = 6.3 6.3 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 426 5 3 4 5.0 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2cccc(CO)c2)nc2ccccc12 10.1016/j.bmcl.2015.11.023
10275911 76782 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 453 14 2 4 5.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CCC(O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2006.01.018
CHEMBL206774 76782 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 453 14 2 4 5.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CCC(O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2006.01.018
9820333 75397 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 361 12 2 3 3.4 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CCC(O)Cc1ccccc1 10.1016/j.bmcl.2006.01.018
CHEMBL203780 75397 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 361 12 2 3 3.4 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CCC(O)Cc1ccccc1 10.1016/j.bmcl.2006.01.018
58905379 156073 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 412 6 2 4 4.5 CC(C)(NC(=O)c1cc(F)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4061595 156073 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 412 6 2 4 4.5 CC(C)(NC(=O)c1cc(F)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
118191092 137560 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2015.12.057
CHEMBL3753835 137560 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 390 5 3 4 4.1 Cc1ccc(-c2cccc(CO)c2)nc1C(=O)Nc1c(C)cc(C(=O)O)cc1C 10.1016/j.bmcl.2015.12.057
118191081 136661 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 395 4 2 2 6.1 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2ccccc2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3739435 136661 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 395 4 2 2 6.1 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2ccccc2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
89914524 122661 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 408 8 2 4 3.4 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3CCOc3ccccc3)CC2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600788 122661 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 408 8 2 4 3.4 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3CCOc3ccccc3)CC2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601973 122661 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 408 8 2 4 3.4 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3CCOc3ccccc3)CC2)cc1 10.1016/j.bmcl.2015.05.091
118191093 137494 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 444 5 3 4 4.8 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1nc(-c2cccc(CO)c2)ccc1C(F)(F)F 10.1016/j.bmcl.2015.12.057
CHEMBL3753286 137494 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 444 5 3 4 4.8 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1nc(-c2cccc(CO)c2)ccc1C(F)(F)F 10.1016/j.bmcl.2015.12.057
44409717 77386 None 1 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 445 13 2 4 4.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2006.01.018
CHEMBL208510 77386 None 1 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 445 13 2 4 4.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2006.01.018
10409554 149609 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 11 3 4 3.9 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O nan
CHEMBL3946494 149609 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 11 3 4 3.9 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O nan
118190908 137489 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 389 5 3 3 4.7 Cc1ccc(-c2cccc(CO)c2)cc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
CHEMBL3753274 137489 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 389 5 3 3 4.7 Cc1ccc(-c2cccc(CO)c2)cc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
9934368 139008 None 11 Rat Binding pIC50 = 8.2 8.2 - 1
Binding affinity to rat EP4 receptorBinding affinity to rat EP4 receptor
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1021/jm9018756
CHEMBL378376 139008 None 11 Rat Binding pIC50 = 8.2 8.2 - 1
Binding affinity to rat EP4 receptorBinding affinity to rat EP4 receptor
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1021/jm9018756
9934368 139008 None 11 Rat Binding pIC50 = 8.2 8.2 - 1
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL378376 139008 None 11 Rat Binding pIC50 = 8.2 8.2 - 1
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2006.01.018
53319154 57721 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 582 10 1 4 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669015 57721 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 582 10 1 4 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4ccccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
118191104 136760 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 425 5 3 3 5.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.12.057
CHEMBL3740223 136760 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 425 5 3 3 5.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.12.057
118191104 136760 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 425 5 3 3 5.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3740223 136760 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 425 5 3 3 5.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
11524454 946 None 36 Human Binding pIC50 = 8.2 8.2 - 1
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
5857 946 None 36 Human Binding pIC50 = 8.2 8.2 - 1
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
CHEMBL591666 946 None 36 Human Binding pIC50 = 8.2 8.2 - 1
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
53325764 57722 None 0 Human Binding pIC50 = 7.2 7.2 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 622 12 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4cc(C(=O)O)ccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669016 57722 None 0 Human Binding pIC50 = 7.2 7.2 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 622 12 2 6 6.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)Cc4cc(C(=O)O)ccc4OC)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
44409742 76220 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 405 14 2 4 3.5 COCc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
CHEMBL205819 76220 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 405 14 2 4 3.5 COCc1cccc(C[C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2006.01.018
25195248 183041 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity to human EP4 receptor by radioligand binding assayBinding affinity to human EP4 receptor by radioligand binding assay
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 183041 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity to human EP4 receptor by radioligand binding assayBinding affinity to human EP4 receptor by radioligand binding assay
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
89914863 122663 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 421 8 2 5 3.4 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(C#N)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600883 122663 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 421 8 2 5 3.4 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(C#N)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601984 122663 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 421 8 2 5 3.4 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(C#N)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
118191080 136950 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 395 4 2 2 6.1 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2ccccc2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3742015 136950 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretreated for 30 mins using 3,3',5,5' tetramethylbiphenyl-4,4'-diamine substrate measured after 20 to 24 hrs by immunoassay
ChEMBL 395 4 2 2 6.1 Cc1cc(C(=O)O)cc(C)c1NC(=O)c1cc(-c2ccccc2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
57401413 67872 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cellsDisplacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells
ChEMBL 455 4 2 3 5.8 C[C@H](NC(=O)c1cccc2c1Oc1ccc(C(F)(F)F)cc1CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.08.102
CHEMBL1910024 67872 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cellsDisplacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells
ChEMBL 455 4 2 3 5.8 C[C@H](NC(=O)c1cccc2c1Oc1ccc(C(F)(F)F)cc1CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.08.102
118174960 137507 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 394 4 2 3 5.3 Cc1ccc(-c2cccc(Cl)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
CHEMBL3753372 137507 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 394 4 2 3 5.3 Cc1ccc(-c2cccc(Cl)c2)nc1C(=O)Nc1c(C)ccc(C(=O)O)c1C 10.1016/j.bmcl.2015.12.057
44570000 178755 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP4 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 178755 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP4 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
44409737 77371 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 451 10 2 4 4.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc3ccccc3c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL208410 77371 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 451 10 2 4 4.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc3ccccc3c2)s1 10.1016/j.bmcl.2006.01.018
9981458 143820 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 455 10 3 5 4.2 CC1(C)C(=O)[C@H](C/C=C\CCCC(N)=O)[C@@H](/C=C/C(O)Cc2cc3ccccc3s2)[C@@H]1O nan
CHEMBL3900651 143820 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 455 10 3 5 4.2 CC1(C)C(=O)[C@H](C/C=C\CCCC(N)=O)[C@@H](/C=C/C(O)Cc2cc3ccccc3s2)[C@@H]1O nan
72695027 106322 None 0 Human Binding pIC50 = 7.2 7.2 28 2
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3115074 106322 None 0 Human Binding pIC50 = 7.2 7.2 28 2
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3138992 106322 None 0 Human Binding pIC50 = 7.2 7.2 28 2
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
11677589 1859 None 51 Human Binding pIC50 = 6.2 6.2 -3 4
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
11677589.0 1859 None 51 Human Binding pIC50 = 6.2 6.2 -3 4
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
5858 1859 None 51 Human Binding pIC50 = 6.2 6.2 -3 4
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
CHEMBL3039498 1859 None 51 Human Binding pIC50 = 6.2 6.2 -3 4
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
DB12836 1859 None 51 Human Binding pIC50 = 6.2 6.2 -3 4
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 491 7 2 6 4.1 CCc1nc2c(n1c1ccc(cc1)CCNC(=O)NS(=O)(=O)c1ccc(cc1)C)cc(nc2C)C 10.1016/j.bmcl.2015.05.091
44409907 77078 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2ccc(F)cc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL207237 77078 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2ccc(F)cc2)s1 10.1016/j.bmcl.2006.01.018
44409920 140452 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 463 10 2 3 4.7 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL380839 140452 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 463 10 2 3 4.7 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2006.01.018
10432730 147357 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 147357 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
89914526 122664 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 414 8 2 4 3.6 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600884 122664 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 414 8 2 4 3.6 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601985 122664 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 414 8 2 4 3.6 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
10409554 149609 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 11 3 4 3.9 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O nan
CHEMBL3946494 149609 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 414 11 3 4 3.9 CC1(C)C(=O)[C@H](C/C=C\CCCC(=O)O)[C@@H](/C=C/C(O)CCc2ccccc2)[C@@H]1O nan
118175029 137468 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 393 5 3 3 4.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)ccc1F 10.1016/j.bmcl.2015.12.057
CHEMBL3753133 137468 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 393 5 3 3 4.6 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(CO)c2)ccc1F 10.1016/j.bmcl.2015.12.057
44571354 184175 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to human EP4 receptor by radioligand binding assayBinding affinity to human EP4 receptor by radioligand binding assay
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 184175 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to human EP4 receptor by radioligand binding assayBinding affinity to human EP4 receptor by radioligand binding assay
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
10046549 151824 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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 151824 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 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
89914524 122661 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 408 8 2 4 3.4 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3CCOc3ccccc3)CC2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600788 122661 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 408 8 2 4 3.4 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3CCOc3ccccc3)CC2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601973 122661 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 408 8 2 4 3.4 O=C(O)c1ccc(C2(NC(=O)[C@H]3CCCCN3CCOc3ccccc3)CC2)cc1 10.1016/j.bmcl.2015.05.091
44570666 183376 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to human EP4 receptor by radioligand binding assayBinding affinity to human EP4 receptor by radioligand binding assay
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 183376 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to human EP4 receptor by radioligand binding assayBinding affinity to human EP4 receptor by radioligand binding assay
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
25018911 57714 None 7 Human Binding pIC50 = 7.1 7.1 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2015.12.057
CHEMBL1669008 57714 None 7 Human Binding pIC50 = 7.1 7.1 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassayAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mins followed by addition of PGE2 measured after 20 to 24 hrs by immunoassay
ChEMBL 681 10 2 6 7.2 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4c(Cl)cccc4Cl)CC3)cc1C)C2 10.1016/j.bmcl.2015.12.057
25019697 57708 None 0 Human Binding pIC50 = 8.1 8.1 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 697 11 2 7 6.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(OC(F)(F)F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669002 57708 None 0 Human Binding pIC50 = 8.1 8.1 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 697 11 2 7 6.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(OC(F)(F)F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
11575201 157514 None 0 Human Binding pIC50 = 8.1 8.1 - 1
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 413 6 2 3 5.5 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4078648 157514 None 0 Human Binding pIC50 = 8.1 8.1 - 1
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 413 6 2 3 5.5 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
25015836 57709 None 0 Human Binding pIC50 = 8.1 8.1 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 772 10 2 7 7.5 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccc4ccccc4c3)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
CHEMBL1669003 57709 None 0 Human Binding pIC50 = 8.1 8.1 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting
ChEMBL 772 10 2 7 7.5 Cc1cc(CC2(NC(=O)NS(=O)(=O)c3ccc4ccccc4c3)CC2)ccc1N1Cc2c(c(OCC(F)(F)F)c3cccnc3c2OCC(F)(F)F)C1=O 10.1016/j.bmcl.2010.12.014
44409918 166068 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc(Cl)cc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL425243 166068 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
Binding affinity to rat EP4 receptor expressed in HEK293 cellsBinding affinity to rat EP4 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc(Cl)cc2)s1 10.1016/j.bmcl.2006.01.018
25019696 57730 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 631 10 2 6 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
CHEMBL1669024 57730 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells by scintillation counting in presence of 10% human serum
ChEMBL 631 10 2 6 6.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CC3(NC(=O)NS(=O)(=O)c4ccc(F)cc4)CC3)cc1C)C2 10.1016/j.bmcl.2010.12.014
11296282 1409 None 31 Human Binding pIC50 = 5.1 5.1 - 1
Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
5822 1409 None 31 Human Binding pIC50 = 5.1 5.1 - 1
Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
CHEMBL565591 1409 None 31 Human Binding pIC50 = 5.1 5.1 - 1
Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP4 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
44626877 201458 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP4 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 201458 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP4 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
9983881 144936 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 511 12 2 5 5.5 CCN(CC)C(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1cc2ccccc2s1 nan
CHEMBL3909714 144936 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 511 12 2 5 5.5 CCN(CC)C(=O)CCC/C=C\C[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)Cc1cc2ccccc2s1 nan
46885735 8370 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to human EP4 receptor by radioligand displacement assayBinding affinity to human EP4 receptor by radioligand displacement assay
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 8370 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to human EP4 receptor by radioligand displacement assayBinding affinity to human EP4 receptor by radioligand displacement assay
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
89914844 122662 None 0 Human Binding pIC50 = 6.1 6.1 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 382 8 2 4 2.9 O=C(O)c1ccc(CNC(=O)[C@H]2CCCCN2CCOc2ccccc2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3600786 122662 None 0 Human Binding pIC50 = 6.1 6.1 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 382 8 2 4 2.9 O=C(O)c1ccc(CNC(=O)[C@H]2CCCCN2CCOc2ccccc2)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3601983 122662 None 0 Human Binding pIC50 = 6.1 6.1 - 1
Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISAAntagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 30 mins followed by PGE2 addition measured after 24 hrs by ELISA
ChEMBL 382 8 2 4 2.9 O=C(O)c1ccc(CNC(=O)[C@H]2CCCCN2CCOc2ccccc2)cc1 10.1016/j.bmcl.2015.05.091
11683088 159070 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4096216 159070 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranesDisplacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
1883 3082 None 47 Human Binding pIC50 = 8 8.0 -1 24
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
1916 3082 None 47 Human Binding pIC50 = 8 8.0 -1 24
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
5280360 3082 None 47 Human Binding pIC50 = 8 8.0 -1 24
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
5280360.0 3082 None 47 Human Binding pIC50 = 8 8.0 -1 24
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
913 3082 None 47 Human Binding pIC50 = 8 8.0 -1 24
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
CHEMBL548 3082 None 47 Human Binding pIC50 = 8 8.0 -1 24
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
DB00917 3082 None 47 Human Binding pIC50 = 8 8.0 -1 24
Binding affinity to EP4 receptorBinding affinity to EP4 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
11961366 150560 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 556 12 2 8 5.4 COC(=O)CSCCCS[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
CHEMBL3954286 150560 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 556 12 2 8 5.4 COC(=O)CSCCCS[C@H]1C(=O)C(C)(C)[C@@H](O)[C@@H]1/C=C/C(O)CCc1sc2ccccc2c1Cl nan
171361355 196742 None 1 Human Binding pKd = 9.1 9.1 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells measured for 30 mins by schild plot analysisAntagonist activity at human EP4 receptor transfected in HEK293 cells measured for 30 mins by schild plot analysis
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
CHEMBL5431224 196742 None 1 Human Binding pKd = 9.1 9.1 - 1
Antagonist activity at human EP4 receptor transfected in HEK293 cells measured for 30 mins by schild plot analysisAntagonist activity at human EP4 receptor transfected in HEK293 cells measured for 30 mins by schild plot analysis
ChEMBL 453 6 2 4 4.7 O=C(O)c1ccc(CNC(=O)c2c3ccccc3nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c02058
57396660 71332 None 0 Mouse Binding pKi = 10.9 10.9 1819 2
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957437 71332 None 0 Mouse Binding pKi = 10.9 10.9 1819 2
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.02.018
57396660 71332 None 0 Mouse Binding pKi = 10.9 10.9 1819 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957437 71332 None 0 Mouse Binding pKi = 10.9 10.9 1819 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.04.008
44455046 95780 None 0 Human Binding pKi = 10.7 10.7 50118 2
Displacement of [3H]PGE4 from human EP4 receptorDisplacement of [3H]PGE4 from human EP4 receptor
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL258332 95780 None 0 Human Binding pKi = 10.7 10.7 50118 2
Displacement of [3H]PGE4 from human EP4 receptorDisplacement of [3H]PGE4 from human EP4 receptor
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
9821171 97919 None 0 Human Binding pKi = 10.3 10.3 51286 2
Displacement of [3H]PGE4 from human EP4 receptorDisplacement of [3H]PGE4 from human EP4 receptor
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL272276 97919 None 0 Human Binding pKi = 10.3 10.3 51286 2
Displacement of [3H]PGE4 from human EP4 receptorDisplacement of [3H]PGE4 from human EP4 receptor
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
72950929 146670 None 0 Human Binding pKi = 10.1 10.1 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3923027 146670 None 0 Human Binding pKi = 10.1 10.1 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
12002527 75186 None 0 Mouse Binding pKi = 10 10.0 19952 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 493 12 2 5 5.1 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2cc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036314 75186 None 0 Mouse Binding pKi = 10 10.0 19952 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 493 12 2 5 5.1 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2cc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
72948663 145822 None 0 Human Binding pKi = 10 10.0 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3916499 145822 None 0 Human Binding pKi = 10 10.0 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
1883 3082 None 47 Human Binding pKi = 10.0 10.0 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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 3082 None 47 Human Binding pKi = 10.0 10.0 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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 3082 None 47 Human Binding pKi = 10.0 10.0 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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
5280360.0 3082 None 47 Human Binding pKi = 10.0 10.0 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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 3082 None 47 Human Binding pKi = 10.0 10.0 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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 3082 None 47 Human Binding pKi = 10.0 10.0 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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 3082 None 47 Human Binding pKi = 10.0 10.0 -1 24
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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
44453566 95447 None 0 Human Binding pKi = 9.9 9.9 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 645 12 1 9 4.9 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3c(OC)cccc3C(C)=O)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
CHEMBL256873 95447 None 0 Human Binding pKi = 9.9 9.9 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 645 12 1 9 4.9 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3c(OC)cccc3C(C)=O)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
57464006 75194 None 0 Mouse Binding pKi = 9.9 9.9 17 4
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 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 75194 None 0 Mouse Binding pKi = 9.9 9.9 17 4
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 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
57893848 75195 None 0 Mouse Binding pKi = 9.9 9.9 234 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036323 75195 None 0 Mouse Binding pKi = 9.9 9.9 234 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
72950425 143137 None 0 Human Binding pKi = 9.9 9.9 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3895047 143137 None 0 Human Binding pKi = 9.9 9.9 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
5283086 205768 None 20 Human Binding pKi = 9.9 9.9 21 5
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
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 nan
CHEMBL64804 205768 None 20 Human Binding pKi = 9.9 9.9 21 5
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
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 nan
10076580 75315 None 0 Mouse Binding pKi = 9.8 9.8 158 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 563 10 2 8 5.5 Cc1cc(C)c2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2037291 75315 None 0 Mouse Binding pKi = 9.8 9.8 158 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 563 10 2 8 5.5 Cc1cc(C)c2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
58932683 75313 None 0 Mouse Binding pKi = 9.8 9.8 354 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2037289 75313 None 0 Mouse Binding pKi = 9.8 9.8 354 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
1883 3082 None 47 Human Binding pKi = 9.8 9.8 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
1916 3082 None 47 Human Binding pKi = 9.8 9.8 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
5280360 3082 None 47 Human Binding pKi = 9.8 9.8 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
5280360.0 3082 None 47 Human Binding pKi = 9.8 9.8 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
913 3082 None 47 Human Binding pKi = 9.8 9.8 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
CHEMBL548 3082 None 47 Human Binding pKi = 9.8 9.8 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
DB00917 3082 None 47 Human Binding pKi = 9.8 9.8 -1 24
Binding affinity to human prostanoid EP4 receptor by radioligand displacement assayBinding affinity to human prostanoid EP4 receptor by radioligand displacement assay
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.ejmech.2013.01.044
57894053 75196 None 0 Mouse Binding pKi = 9.7 9.7 79 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036324 75196 None 0 Mouse Binding pKi = 9.7 9.7 79 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
53316600 56903 None 0 Human Binding pKi = 9.7 9.7 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 500 8 1 4 5.8 COc1ccccc1CC(=O)NCCc1ccc(-c2c(C(=O)N(C)C)sc3c(C)cc(C)cc23)cc1 10.1016/j.bmcl.2010.11.118
CHEMBL1644016 56903 None 0 Human Binding pKi = 9.7 9.7 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 500 8 1 4 5.8 COc1ccccc1CC(=O)NCCc1ccc(-c2c(C(=O)N(C)C)sc3c(C)cc(C)cc23)cc1 10.1016/j.bmcl.2010.11.118
72950089 150679 None 0 Human Binding pKi = 9.7 9.7 1621 3
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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 150679 None 0 Human Binding pKi = 9.7 9.7 1621 3
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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
57894092 75184 None 0 Mouse Binding pKi = 9.7 9.7 8511 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 12 2 6 4.5 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036312 75184 None 0 Mouse Binding pKi = 9.7 9.7 8511 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 12 2 6 4.5 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
10348006 75316 None 0 Mouse Binding pKi = 9.7 9.7 338 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 569 10 2 8 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2037292 75316 None 0 Mouse Binding pKi = 9.7 9.7 338 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 569 10 2 8 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
15948558 97484 None 0 Human Binding pKi = 9.7 9.7 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 657 11 1 8 5.6 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3OC(F)(F)F)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
CHEMBL269987 97484 None 0 Human Binding pKi = 9.7 9.7 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 657 11 1 8 5.6 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3OC(F)(F)F)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
58932681 75198 None 0 Mouse Binding pKi = 9.7 9.7 100 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2036326 75198 None 0 Mouse Binding pKi = 9.7 9.7 100 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
58932678 75314 None 0 Mouse Binding pKi = 9.7 9.7 104 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
CHEMBL2037290 75314 None 0 Mouse Binding pKi = 9.7 9.7 104 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
72950089 150679 None 0 Human Binding pKi = 9.7 9.7 1621 3
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3955128 150679 None 0 Human Binding pKi = 9.7 9.7 1621 3
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
25003075 6840 None 21 Human Binding pKi = 9.6 9.6 5888 7
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 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 6840 None 21 Human Binding pKi = 9.6 9.6 5888 7
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 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
44453376 95171 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 572 10 1 6 5.3 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3)cc1C)C2 10.1016/j.bmcl.2008.01.103
CHEMBL255527 95171 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 572 10 1 6 5.3 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3)cc1C)C2 10.1016/j.bmcl.2008.01.103
10348321 75197 None 0 Mouse Binding pKi = 9.6 9.6 87 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 585 10 2 8 6.0 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036325 75197 None 0 Mouse Binding pKi = 9.6 9.6 87 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 585 10 2 8 6.0 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
15948554 83274 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 607 10 1 7 5.3 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3Cl)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
CHEMBL218699 83274 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 607 10 1 7 5.3 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3Cl)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
15947546 95245 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 617 12 1 8 5.1 CCOc1ccccc1CC(=O)NS(=O)(=O)Cc1ccc(N2Cc3c(c(OCC)c4cccnc4c3OCC)C2=O)c(C)c1 10.1016/j.bmcl.2008.01.103
CHEMBL255906 95245 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 617 12 1 8 5.1 CCOc1ccccc1CC(=O)NS(=O)(=O)Cc1ccc(N2Cc3c(c(OCC)c4cccnc4c3OCC)C2=O)c(C)c1 10.1016/j.bmcl.2008.01.103
15947337 97941 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 641 10 1 7 6.0 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3c(Cl)cccc3Cl)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
CHEMBL272363 97941 None 0 Human Binding pKi = 9.6 9.6 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 641 10 1 7 6.0 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3c(Cl)cccc3Cl)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
53317509 57120 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 476 7 2 3 6.1 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(-c3ccccc3)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645141 57120 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 476 7 2 3 6.1 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(-c3ccccc3)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
57893867 75183 None 0 Mouse Binding pKi = 9.6 9.6 12302 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 492 12 3 4 4.9 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3[nH]ccc3c2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036311 75183 None 0 Mouse Binding pKi = 9.6 9.6 12302 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 492 12 3 4 4.9 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3[nH]ccc3c2)c1 10.1016/j.bmc.2012.04.008
72948479 153122 None 0 Human Binding pKi = 9.6 9.6 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3975743 153122 None 0 Human Binding pKi = 9.6 9.6 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
18444619 110882 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 526 9 2 6 5.9 Cc1ccccc1S(=O)(=O)NC(=O)c1cc(CNc2ccc(-c3ccc(OC(F)F)cc3)cc2)c(C)o1 10.1016/j.bmcl.2014.02.068
CHEMBL3260768 110882 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 526 9 2 6 5.9 Cc1ccccc1S(=O)(=O)NC(=O)c1cc(CNc2ccc(-c3ccc(OC(F)F)cc3)cc2)c(C)o1 10.1016/j.bmcl.2014.02.068
9894720 68321 None 13 Human Binding pKi = 9.5 9.5 2 2
Inhibition of [3H]PGE-2 binding to human prostanoid EP4 receptorInhibition of [3H]PGE-2 binding to human prostanoid EP4 receptor
ChEMBL 588 9 1 5 7.7 O=C(NS(=O)(=O)Cc1ccccc1)c1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1021/jm050085k
CHEMBL191638 68321 None 13 Human Binding pKi = 9.5 9.5 2 2
Inhibition of [3H]PGE-2 binding to human prostanoid EP4 receptorInhibition of [3H]PGE-2 binding to human prostanoid EP4 receptor
ChEMBL 588 9 1 5 7.7 O=C(NS(=O)(=O)Cc1ccccc1)c1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1021/jm050085k
10120328 95150 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 558 10 1 6 5.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3)cc1)C2 10.1016/j.bmcl.2008.01.103
CHEMBL255422 95150 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 558 10 1 6 5.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3)cc1)C2 10.1016/j.bmcl.2008.01.103
25002382 7397 None 0 Human Binding pKi = 9.5 9.5 1819 2
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 512 6 2 3 6.5 O=C(O)c1ccc(C2(NC(=O)c3cc(Cl)cc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1086490 7397 None 0 Human Binding pKi = 9.5 9.5 1819 2
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 512 6 2 3 6.5 O=C(O)c1ccc(C2(NC(=O)c3cc(Cl)cc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.065
15947640 95539 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 639 12 1 8 5.3 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3OC(F)F)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
CHEMBL257255 95539 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 639 12 1 8 5.3 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3OC(F)F)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
53320541 56892 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 576 8 1 6 5.6 COc1ccccc1C1(C(=O)NS(=O)(=O)Cc2ccc(-c3c(C(=O)N(C)C)sc4c(C)cc(C)cc34)cc2)CC1 10.1016/j.bmcl.2010.11.118
CHEMBL1644006 56892 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 576 8 1 6 5.6 COc1ccccc1C1(C(=O)NS(=O)(=O)Cc2ccc(-c3c(C(=O)N(C)C)sc4c(C)cc(C)cc34)cc2)CC1 10.1016/j.bmcl.2010.11.118
23660678 57121 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 556 6 2 3 6.0 C[C@H](NC(=O)c1cccc2c1N(Cc1cc(Br)cc(Br)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645142 57121 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 556 6 2 3 6.0 C[C@H](NC(=O)c1cccc2c1N(Cc1cc(Br)cc(Br)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
23661189 57113 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 468 6 2 3 5.7 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(Cl)c(Cl)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645134 57113 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 468 6 2 3 5.7 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(Cl)c(Cl)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
25003075 6840 None 21 Human Binding pKi = 9.5 9.5 5888 7
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting in presence of 10% human serum
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 6840 None 21 Human Binding pKi = 9.5 9.5 5888 7
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting in presence of 10% human serumDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting in presence of 10% human serum
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
10481859 75193 None 0 Mouse Binding pKi = 9.5 9.5 4 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
CHEMBL2036321 75193 None 0 Mouse Binding pKi = 9.5 9.5 4 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
15948789 97966 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 631 11 1 8 5.5 COc1ccccc1CC(=O)NS(=O)(=O)Cc1ccc(N2Cc3c(c(OC(C)C)c4cccnc4c3OC(C)C)C2=O)c(C)c1 10.1016/j.bmcl.2008.01.103
CHEMBL272498 97966 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 631 11 1 8 5.5 COc1ccccc1CC(=O)NS(=O)(=O)Cc1ccc(N2Cc3c(c(OC(C)C)c4cccnc4c3OC(C)C)C2=O)c(C)c1 10.1016/j.bmcl.2008.01.103
57893891 75185 None 0 Mouse Binding pKi = 9.4 9.4 1995 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 12 2 6 5.0 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3s2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036313 75185 None 0 Mouse Binding pKi = 9.4 9.4 1995 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 12 2 6 5.0 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3s2)c1 10.1016/j.bmc.2012.04.008
10189261 95309 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 618 12 1 8 5.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)Cc3cc(OC)ccc3OC)cc1)C2 10.1016/j.bmcl.2008.01.103
CHEMBL256220 95309 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 618 12 1 8 5.0 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)Cc3cc(OC)ccc3OC)cc1)C2 10.1016/j.bmcl.2008.01.103
23660841 57116 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 468 6 2 3 5.5 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645137 57116 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 468 6 2 3 5.5 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
53323050 57134 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 486 6 2 3 5.6 C[C@H](NC(=O)c1cc(F)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645155 57134 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 486 6 2 3 5.6 C[C@H](NC(=O)c1cc(F)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
12521 2197 None 0 Human Binding pKi = 9.4 9.4 -1 4
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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 2197 None 0 Human Binding pKi = 9.4 9.4 -1 4
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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 2197 None 0 Human Binding pKi = 9.4 9.4 -1 4
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 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
44453656 95301 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 574 11 1 7 4.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)COc3ccccc3)cc1)C2 10.1016/j.bmcl.2008.01.103
CHEMBL256183 95301 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 574 11 1 7 4.8 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)COc3ccccc3)cc1)C2 10.1016/j.bmcl.2008.01.103
15947448 97706 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 711 11 1 8 5.8 COc1ccccc1CC(=O)NS(=O)(=O)Cc1ccc(N2Cc3c(c(OCC(F)(F)F)c4cccnc4c3OCC(F)(F)F)C2=O)c(C)c1 10.1016/j.bmcl.2008.01.103
CHEMBL271095 97706 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 711 11 1 8 5.8 COc1ccccc1CC(=O)NS(=O)(=O)Cc1ccc(N2Cc3c(c(OCC(F)(F)F)c4cccnc4c3OCC(F)(F)F)C2=O)c(C)c1 10.1016/j.bmcl.2008.01.103
11744126 69390 None 0 Mouse Binding pKi = 9.4 9.4 1174 2
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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 69390 None 0 Mouse Binding pKi = 9.4 9.4 1174 2
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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
46890658 6960 None 0 Human Binding pKi = 9.4 9.4 128 2
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 516 7 2 4 6.4 C[C@H](NC(=O)c1cccc2ccn(Cc3cc(Cl)cc(OC(F)(F)F)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1084552 6960 None 0 Human Binding pKi = 9.4 9.4 128 2
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 516 7 2 4 6.4 C[C@H](NC(=O)c1cccc2ccn(Cc3cc(Cl)cc(OC(F)(F)F)c3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
8541 2944 None 1 Human Binding pKi = 9.4 9.4 1 4
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
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 10.1021/acs.jmedchem.9b00336
9824353 2944 None 1 Human Binding pKi = 9.4 9.4 1 4
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
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 10.1021/acs.jmedchem.9b00336
CHEMBL292964 2944 None 1 Human Binding pKi = 9.4 9.4 1 4
Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
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 10.1021/acs.jmedchem.9b00336
53325840 56890 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 569 7 2 5 5.8 Cc1cc(C)c2sc(C(=O)N(C)C)c(-c3ccc(CCNC(=O)NS(=O)(=O)c4ccc(Cl)cc4)cc3)c2c1 10.1016/j.bmcl.2010.11.118
CHEMBL1644004 56890 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 569 7 2 5 5.8 Cc1cc(C)c2sc(C(=O)N(C)C)c(-c3ccc(CCNC(=O)NS(=O)(=O)c4ccc(Cl)cc4)cc3)c2c1 10.1016/j.bmcl.2010.11.118
10319835 69389 None 0 Mouse Binding pKi = 9.4 9.4 5011 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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 69389 None 0 Mouse Binding pKi = 9.4 9.4 5011 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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
23660680 57117 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 468 6 2 3 5.5 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(C(F)(F)F)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645138 57117 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 468 6 2 3 5.5 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(C(F)(F)F)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
53325182 57132 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 502 6 2 3 6.1 C[C@H](NC(=O)c1cc(Cl)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645153 57132 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 502 6 2 3 6.1 C[C@H](NC(=O)c1cc(Cl)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
44304436 205778 None 0 Mouse Binding pKi = 9.4 9.4 8 5
Evaluated for its competitive binding affinity towards mouse Prostanoid EP4 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP4 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 205778 None 0 Mouse Binding pKi = 9.4 9.4 8 5
Evaluated for its competitive binding affinity towards mouse Prostanoid EP4 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP4 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
53323010 56897 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 575 7 2 5 6.0 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N4CCCC4)sc4c(C)cc(C)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
CHEMBL1644010 56897 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 575 7 2 5 6.0 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N4CCCC4)sc4c(C)cc(C)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
56835070 69493 None 0 Mouse Binding pKi = 9.4 9.4 22 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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 69493 None 0 Mouse Binding pKi = 9.4 9.4 22 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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 69493 None 0 Mouse Binding pKi = 9.4 9.4 22 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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 69493 None 0 Mouse Binding pKi = 9.4 9.4 22 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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 69493 None 0 Mouse Binding pKi = 9.4 9.4 22 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 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 69493 None 0 Mouse Binding pKi = 9.4 9.4 22 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 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
53323177 56891 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 569 7 2 5 5.8 Cc1cc(C)c2sc(C(=O)N(C)C)c(-c3ccc(CCNC(=O)NS(=O)(=O)c4ccccc4Cl)cc3)c2c1 10.1016/j.bmcl.2010.11.118
CHEMBL1644005 56891 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 569 7 2 5 5.8 Cc1cc(C)c2sc(C(=O)N(C)C)c(-c3ccc(CCNC(=O)NS(=O)(=O)c4ccccc4Cl)cc3)c2c1 10.1016/j.bmcl.2010.11.118
44453545 95172 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 608 10 1 6 6.1 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)Cc3cccc4ccccc34)cc1)C2 10.1016/j.bmcl.2008.01.103
CHEMBL255529 95172 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 608 10 1 6 6.1 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)Cc3cccc4ccccc34)cc1)C2 10.1016/j.bmcl.2008.01.103
11957776 97566 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 641 10 1 7 5.7 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3C(F)(F)F)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
CHEMBL270397 97566 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 641 10 1 7 5.7 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3C(F)(F)F)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
44454021 97693 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 600 10 1 6 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)Cc3c(C)cc(C)cc3C)cc1)C2 10.1016/j.bmcl.2008.01.103
CHEMBL271070 97693 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 600 10 1 6 5.9 CCOc1c2c(c(OCC)c3ccccc13)C(=O)N(c1ccc(CS(=O)(=O)NC(=O)Cc3c(C)cc(C)cc3C)cc1)C2 10.1016/j.bmcl.2008.01.103
57893982 75190 None 0 Mouse Binding pKi = 9.4 9.4 4 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
CHEMBL2036318 75190 None 0 Mouse Binding pKi = 9.4 9.4 4 3
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
53319233 56893 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 614 7 1 5 6.9 Cc1cc(C)c2sc(C(=O)N(C)C)c(-c3ccc(CS(=O)(=O)NC(=O)C4(c5c(Cl)cccc5Cl)CC4)cc3)c2c1 10.1016/j.bmcl.2010.11.118
CHEMBL1644007 56893 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 614 7 1 5 6.9 Cc1cc(C)c2sc(C(=O)N(C)C)c(-c3ccc(CS(=O)(=O)NC(=O)C4(c5c(Cl)cccc5Cl)CC4)cc3)c2c1 10.1016/j.bmcl.2010.11.118
46890660 6660 None 0 Human Binding pKi = 9.4 9.4 478 2
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 500 6 2 3 6.6 C[C@H](NC(=O)c1cc(Cl)cc2ccn(Cc3ccc(C(F)(F)F)cc3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1083400 6660 None 0 Human Binding pKi = 9.4 9.4 478 2
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 500 6 2 3 6.6 C[C@H](NC(=O)c1cc(Cl)cc2ccn(Cc3ccc(C(F)(F)F)cc3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
23634376 57112 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 434 6 2 3 5.1 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(Cl)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645133 57112 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 434 6 2 3 5.1 C[C@H](NC(=O)c1cccc2c1N(Cc1cccc(Cl)c1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
23661014 57114 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 434 6 2 3 5.1 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(Cl)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645135 57114 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 434 6 2 3 5.1 C[C@H](NC(=O)c1cccc2c1N(Cc1ccc(Cl)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
72949200 153866 None 0 Human Binding pKi = 9.4 9.4 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 385 11 2 3 3.2 CC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3982139 153866 None 0 Human Binding pKi = 9.4 9.4 - 1
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
ChEMBL 385 11 2 3 3.2 CC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
1883 3082 None 47 Human Binding pKi = 9.4 9.4 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
1916 3082 None 47 Human Binding pKi = 9.4 9.4 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
5280360 3082 None 47 Human Binding pKi = 9.4 9.4 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
5280360.0 3082 None 47 Human Binding pKi = 9.4 9.4 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
913 3082 None 47 Human Binding pKi = 9.4 9.4 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
CHEMBL548 3082 None 47 Human Binding pKi = 9.4 9.4 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
DB00917 3082 None 47 Human Binding pKi = 9.4 9.4 -1 24
Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrsDisplacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs
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.2013.01.025
77050677 128651 None 0 Human Binding pKi = 9.4 9.4 588 2
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 385 10 2 4 3.7 CC(C)[C@@H](OCCOc1ccccc1)C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 nan
CHEMBL3667607 128651 None 0 Human Binding pKi = 9.4 9.4 588 2
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 385 10 2 4 3.7 CC(C)[C@@H](OCCOc1ccccc1)C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 nan
24178408 132180 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.
ChEMBL 555 6 2 3 6.7 C[C@H](NC(=O)c1c(Br)sc(Br)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 nan
CHEMBL3695937 132180 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.
ChEMBL 555 6 2 3 6.7 C[C@H](NC(=O)c1c(Br)sc(Br)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 nan
15948439 155386 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 591 10 1 7 4.8 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3F)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
CHEMBL402960 155386 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 591 10 1 7 4.8 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3F)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
12521 2197 None 0 Human Binding pKi = 9.3 9.3 -1 4
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
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 nan
72722131 2197 None 0 Human Binding pKi = 9.3 9.3 -1 4
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
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 nan
CHEMBL3918816 2197 None 0 Human Binding pKi = 9.3 9.3 -1 4
Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).Radioligand Binding Assay: Assay Volume and Format:200 μl in 96-well plateCell membrane homogenates (20 μg protein) are incubated for 120 min at 22° C. with 0.5 nM [3H]PGE2 in the absence or presence of the test compound in a buffer containing 10 mM MES/KOH (pH 6.0), 10 mM MgCl2 and 1 mM EDTA.Nonspecific binding is determined in the presence of 10 M PGE2.Following incubation, the samples are filtered rapidly under vacuum through glass fiber filters (GF/B, Packard) presoaked with 0.3% PEI and rinsed several times with ice-cold 50 mM Tris-HCl using a 96-sample cell harvester (Unifilter, Packard). The filters are dried then counted for radioactivity in a scintillation counter (Topcount, Packard) using a scintillation cocktail (Microscint 0, Packard).
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 nan
44304404 100635 None 0 Mouse Binding pKi = 9.3 9.3 23 4
Affinity for mouse Prostanoid EP4 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP4 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 100635 None 0 Mouse Binding pKi = 9.3 9.3 23 4
Affinity for mouse Prostanoid EP4 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP4 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
44304388 205610 None 0 Mouse Binding pKi = 9.3 9.3 3 5
Affinity for mouse Prostanoid EP4 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP4 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 205610 None 0 Mouse Binding pKi = 9.3 9.3 3 5
Affinity for mouse Prostanoid EP4 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP4 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
24952929 2554 None 35 Human Binding pKi = 9.3 9.3 1 5
Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.
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 nan
4041 2554 None 35 Human Binding pKi = 9.3 9.3 1 5
Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.
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 nan
CHEMBL597997 2554 None 35 Human Binding pKi = 9.3 9.3 1 5
Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.
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 nan
53319234 56895 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 535 7 3 5 5.1 CNC(=O)c1sc2c(C)cc(C)cc2c1-c1ccc(CCNC(=O)NS(=O)(=O)c2ccc(C)cc2)cc1 10.1016/j.bmcl.2010.11.118
CHEMBL1644009 56895 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 535 7 3 5 5.1 CNC(=O)c1sc2c(C)cc(C)cc2c1-c1ccc(CCNC(=O)NS(=O)(=O)c2ccc(C)cc2)cc1 10.1016/j.bmcl.2010.11.118
56949973 69394 None 0 Mouse Binding pKi = 9.3 9.3 1949 4
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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 69394 None 0 Mouse Binding pKi = 9.3 9.3 1949 4
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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
57396825 69495 None 0 Mouse Binding pKi = 9.3 9.3 6 4
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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 69495 None 0 Mouse Binding pKi = 9.3 9.3 6 4
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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 69495 None 0 Mouse Binding pKi = 9.3 9.3 6 4
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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 69495 None 0 Mouse Binding pKi = 9.3 9.3 6 4
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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
53320542 56899 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 557 7 2 5 5.1 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(F)cc(F)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
CHEMBL1644012 56899 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 557 7 2 5 5.1 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(F)cc(F)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
50898361 56889 None 0 Human Binding pKi = 9.3 9.3 48 4
Binding affinity to EP4 receptorBinding affinity to EP4 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 56889 None 0 Human Binding pKi = 9.3 9.3 48 4
Binding affinity to EP4 receptorBinding affinity to EP4 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
15947856 155817 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 659 12 1 9 5.2 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)C3(c4c(OC)cccc4OC)CC3)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
CHEMBL405446 155817 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 659 12 1 9 5.2 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)C3(c4c(OC)cccc4OC)CC3)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
53321855 56900 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 623 7 2 5 6.5 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(Cl)cc(C(F)(F)F)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
CHEMBL1644013 56900 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 623 7 2 5 6.5 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(Cl)cc(C(F)(F)F)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
15948788 95440 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 629 11 1 8 5.2 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)C3(c4ccccc4OC)CC3)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
CHEMBL256822 95440 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 629 11 1 8 5.2 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)C3(c4ccccc4OC)CC3)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
24952929 2554 None 35 Human Binding pKi = 9.3 9.3 1 5
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 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 2554 None 35 Human Binding pKi = 9.3 9.3 1 5
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 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 2554 None 35 Human Binding pKi = 9.3 9.3 1 5
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 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
53317905 56898 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 589 7 2 5 6.1 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(Cl)cc(Cl)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
CHEMBL1644011 56898 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 589 7 2 5 6.1 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(Cl)cc(Cl)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
24952928 202881 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.
ChEMBL 497 6 2 5 5.6 Cc1sc(C)c(C(=O)NC2(c3ccc(-c4nn[nH]n4)cc3)CC2)c1Cc1ccc(C(F)(F)F)cc1 nan
CHEMBL598198 202881 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.
ChEMBL 497 6 2 5 5.6 Cc1sc(C)c(C(=O)NC2(c3ccc(-c4nn[nH]n4)cc3)CC2)c1Cc1ccc(C(F)(F)F)cc1 nan
10112412 69490 None 0 Mouse Binding pKi = 9.2 9.2 208 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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 69490 None 0 Mouse Binding pKi = 9.2 9.2 208 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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 69490 None 0 Mouse Binding pKi = 9.2 9.2 208 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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 69490 None 0 Mouse Binding pKi = 9.2 9.2 208 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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
58824190 110881 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 532 9 1 8 5.2 Cc1noc(C)c1S(=O)(=O)NC(=O)c1cc(COc2ccc(-c3ccc(OC(F)F)cc3)cc2)c(C)o1 10.1016/j.bmcl.2014.02.068
CHEMBL3260767 110881 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in cell membranes by scintillation counting
ChEMBL 532 9 1 8 5.2 Cc1noc(C)c1S(=O)(=O)NC(=O)c1cc(COc2ccc(-c3ccc(OC(F)F)cc3)cc2)c(C)o1 10.1016/j.bmcl.2014.02.068
57894081 75180 None 0 Mouse Binding pKi = 9.2 9.2 3467 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 503 12 2 4 5.6 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036308 75180 None 0 Mouse Binding pKi = 9.2 9.2 3467 2
Displacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 503 12 2 4 5.6 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2012.04.008
46890659 6961 None 0 Human Binding pKi = 9.2 9.2 2238 2
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 466 6 2 3 5.9 C[C@H](NC(=O)c1cccc2ccn(Cc3ccc(C(F)(F)F)cc3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1084553 6961 None 0 Human Binding pKi = 9.2 9.2 2238 2
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 466 6 2 3 5.9 C[C@H](NC(=O)c1cccc2ccn(Cc3ccc(C(F)(F)F)cc3)c12)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.04.065
24952928 202881 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 497 6 2 5 5.6 Cc1sc(C)c(C(=O)NC2(c3ccc(-c4nn[nH]n4)cc3)CC2)c1Cc1ccc(C(F)(F)F)cc1 10.1021/jm901771h
CHEMBL598198 202881 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 497 6 2 5 5.6 Cc1sc(C)c(C(=O)NC2(c3ccc(-c4nn[nH]n4)cc3)CC2)c1Cc1ccc(C(F)(F)F)cc1 10.1021/jm901771h
10363310 69381 None 0 Mouse Binding pKi = 9.2 9.2 60 2
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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 69381 None 0 Mouse Binding pKi = 9.2 9.2 60 2
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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
53326475 57133 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 536 6 2 3 6.5 C[C@H](NC(=O)c1cc(C(F)(F)F)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645154 57133 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 536 6 2 3 6.5 C[C@H](NC(=O)c1cc(C(F)(F)F)cc2c1N(Cc1ccc(C(F)(F)F)cc1)CC2)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2010.10.106
11387144 133690 None 0 Human Binding pKi = 9.2 9.2 - 1
Inhibition of [3H]PGE-2 binding to human prostanoid EP4 receptorInhibition of [3H]PGE-2 binding to human prostanoid EP4 receptor
ChEMBL 540 9 1 4 8.3 O=C(NOCc1ccccc1)c1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1021/jm050085k
CHEMBL371394 133690 None 0 Human Binding pKi = 9.2 9.2 - 1
Inhibition of [3H]PGE-2 binding to human prostanoid EP4 receptorInhibition of [3H]PGE-2 binding to human prostanoid EP4 receptor
ChEMBL 540 9 1 4 8.3 O=C(NOCc1ccccc1)c1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1021/jm050085k
10000670 69391 None 0 Mouse Binding pKi = 9.2 9.2 2454 2
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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 69391 None 0 Mouse Binding pKi = 9.2 9.2 2454 2
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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
8541 2944 None 1 Mouse Binding pKi = 9.2 9.2 -1 4
Affinity for mouse Prostanoid EP4 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP4 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 2944 None 1 Mouse Binding pKi = 9.2 9.2 -1 4
Affinity for mouse Prostanoid EP4 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP4 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 2944 None 1 Mouse Binding pKi = 9.2 9.2 -1 4
Affinity for mouse Prostanoid EP4 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP4 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
13231966 101005 None 0 Mouse Binding pKi = 9.2 9.2 6 5
Affinity for mouse Prostanoid EP4 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP4 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 101005 None 0 Mouse Binding pKi = 9.2 9.2 6 5
Affinity for mouse Prostanoid EP4 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP4 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
24953627 132188 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.
ChEMBL 497 6 2 5 5.6 Cc1sc(C)c(C(=O)NC2(c3ccc(-c4nn[nH]n4)cc3)CC2)c1Cc1cccc(C(F)(F)F)c1 nan
CHEMBL3695945 132188 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.
ChEMBL 497 6 2 5 5.6 Cc1sc(C)c(C(=O)NC2(c3ccc(-c4nn[nH]n4)cc3)CC2)c1Cc1cccc(C(F)(F)F)c1 nan
11339240 84762 None 0 Human Binding pKi = 9.2 9.2 3548 2
Binding affinity to human EP4 receptorBinding affinity to human EP4 receptor
ChEMBL 423 10 2 4 3.2 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
CHEMBL222834 84762 None 0 Human Binding pKi = 9.2 9.2 3548 2
Binding affinity to human EP4 receptorBinding affinity to human EP4 receptor
ChEMBL 423 10 2 4 3.2 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
8541 2944 None 1 Mouse Binding pKi = 9.2 9.2 -1 4
Binding affinity to mouse EP4 receptor by competitive binding assayBinding affinity to mouse EP4 receptor by competitive binding assay
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 10.1021/jm9018756
9824353 2944 None 1 Mouse Binding pKi = 9.2 9.2 -1 4
Binding affinity to mouse EP4 receptor by competitive binding assayBinding affinity to mouse EP4 receptor by competitive binding assay
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 10.1021/jm9018756
CHEMBL292964 2944 None 1 Mouse Binding pKi = 9.2 9.2 -1 4
Binding affinity to mouse EP4 receptor by competitive binding assayBinding affinity to mouse EP4 receptor by competitive binding assay
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 10.1021/jm9018756
8541 2944 None 1 Mouse Binding pKi = 9.2 9.2 -1 4
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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 2944 None 1 Mouse Binding pKi = 9.2 9.2 -1 4
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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 2944 None 1 Mouse Binding pKi = 9.2 9.2 -1 4
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP4 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
24952929 2554 None 35 Rat Binding pKi = 9.2 9.2 -1 5
Displacement of [3H]PGE2 from rat EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP4 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 2554 None 35 Rat Binding pKi = 9.2 9.2 -1 5
Displacement of [3H]PGE2 from rat EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP4 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 2554 None 35 Rat Binding pKi = 9.2 9.2 -1 5
Displacement of [3H]PGE2 from rat EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP4 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
13231966 101005 None 0 Mouse Binding pKi = 9.2 9.2 6 5
Evaluated for its competitive binding affinity towards mouse Prostanoid EP4 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP4 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 101005 None 0 Mouse Binding pKi = 9.2 9.2 6 5
Evaluated for its competitive binding affinity towards mouse Prostanoid EP4 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP4 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
9886718 205621 None 0 Mouse Binding pKi = 9.2 9.2 309 4
Evaluated for its competitive binding affinity towards mouse Prostanoid EP4 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP4 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 205621 None 0 Mouse Binding pKi = 9.2 9.2 309 4
Evaluated for its competitive binding affinity towards mouse Prostanoid EP4 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP4 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
24952578 132179 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.
ChEMBL 477 6 2 3 5.9 C[C@H](NC(=O)c1csc(Br)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 nan
CHEMBL3695936 132179 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.Binding Assay: Transfected HEK 293(ebna) cells are maintained in culture, harvested and membranes are prepared by differential centrifugation, following lysis of the cells in the presence of protease inhibitors, for use in receptor binding assays. Prostanoid receptor binding assays (for DPI, DP2 (CRTH2), EPl, EP2, EP3-III, EP4, FP, IP, and TP) are performed in 10 mM MES/KOH (pH 6.0) (EPs, FP and TP) or 10 mM HEPES/KOH (pH 7.4) (DPs and IP), containing 1 mM EDTA, 2.5-30 mM divalent cation and the appropriate radioligand. Synthetic compounds are added in dimethylsulfoxide which is kept constant at 1 % (v/v) in all incubations. The reaction is initiated by addition of membrane protein. Non-specific binding is determined in the presence of 10 uM of the corresponding non-radioactive prostanoid . Incubations are conducted for 60-90 min at room temperature or 30 0C and terminated by rapid filtration. Specific binding is calculated by subtracting non specific binding from total binding.
ChEMBL 477 6 2 3 5.9 C[C@H](NC(=O)c1csc(Br)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 nan
24953285 203326 None 0 Human Binding pKi = 9.1 9.1 53 2
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 453 6 2 3 5.9 O=C(O)c1ccc(CNC(=O)c2c(Cl)sc(Cl)c2Cc2cccc(Cl)c2)cc1 10.1021/jm901771h
CHEMBL601299 203326 None 0 Human Binding pKi = 9.1 9.1 53 2
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 453 6 2 3 5.9 O=C(O)c1ccc(CNC(=O)c2c(Cl)sc(Cl)c2Cc2cccc(Cl)c2)cc1 10.1021/jm901771h
15948325 2526 None 39 Human Binding pKi = 9.1 9.1 512 6
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 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 2526 None 39 Human Binding pKi = 9.1 9.1 512 6
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 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 2526 None 39 Human Binding pKi = 9.1 9.1 512 6
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 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
9894720 68321 None 13 Rat Binding pKi = 9.1 9.1 -2 2
Inhibition of rat prostanoid EP4 receptorInhibition of rat prostanoid EP4 receptor
ChEMBL 588 9 1 5 7.7 O=C(NS(=O)(=O)Cc1ccccc1)c1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1021/jm050085k
CHEMBL191638 68321 None 13 Rat Binding pKi = 9.1 9.1 -2 2
Inhibition of rat prostanoid EP4 receptorInhibition of rat prostanoid EP4 receptor
ChEMBL 588 9 1 5 7.7 O=C(NS(=O)(=O)Cc1ccccc1)c1cccc(C[C@@H]2CCCC=C2c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1021/jm050085k
24953624 203647 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 Cc1sc(C)c(C(=O)NC2(c3ccc(C(=O)O)cc3)CC2)c1Cc1cccc(C(F)(F)F)c1 10.1021/jm901771h
CHEMBL603462 203647 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP4 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 Cc1sc(C)c(C(=O)NC2(c3ccc(C(=O)O)cc3)CC2)c1Cc1cccc(C(F)(F)F)c1 10.1021/jm901771h
15948329 155497 None 1 Human Binding pKi = 9.1 9.1 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 573 10 1 7 4.7 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
CHEMBL403630 155497 None 1 Human Binding pKi = 9.1 9.1 - 1
Binding affinity to human EP4 receptor expressed in HEK293 cellsBinding affinity to human EP4 receptor expressed in HEK293 cells
ChEMBL 573 10 1 7 4.7 CCOc1c2c(c(OCC)c3ncccc13)CN(c1ccc(CS(=O)(=O)NC(=O)Cc3ccccc3)cc1C)C2=O 10.1016/j.bmcl.2008.01.103
53320543 56901 None 0 Human Binding pKi = 9.1 9.1 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 549 7 2 5 5.4 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(C)ccc(C)c34)cc2)cc1 10.1016/j.bmcl.2010.11.118
CHEMBL1644014 56901 None 0 Human Binding pKi = 9.1 9.1 - 1
Binding affinity to EP4 receptorBinding affinity to EP4 receptor
ChEMBL 549 7 2 5 5.4 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(C)ccc(C)c34)cc2)cc1 10.1016/j.bmcl.2010.11.118
57398586 69498 None 0 Mouse Binding pKi = 9.1 9.1 53 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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 69498 None 0 Mouse Binding pKi = 9.1 9.1 53 3
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP4 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
53323904 57127 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 414 6 2 3 4.7 Cc1ccc(CN2CCc3cccc(C(=O)N[C@@H](C)c4ccc(C(=O)O)cc4)c32)cc1 10.1016/j.bmcl.2010.10.106
CHEMBL1645148 57127 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP4 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 414 6 2 3 4.7 Cc1ccc(CN2CCc3cccc(C(=O)N[C@@H](C)c4ccc(C(=O)O)cc4)c32)cc1 10.1016/j.bmcl.2010.10.106
1883 3082 None 47 Human Binding pKi = 9.1 9.1 -1 24
Binding affinity at human prostaglandin EP4 receptorBinding affinity at human prostaglandin EP4 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.2007.09.074
1916 3082 None 47 Human Binding pKi = 9.1 9.1 -1 24
Binding affinity at human prostaglandin EP4 receptorBinding affinity at human prostaglandin EP4 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.2007.09.074
5280360 3082 None 47 Human Binding pKi = 9.1 9.1 -1 24
Binding affinity at human prostaglandin EP4 receptorBinding affinity at human prostaglandin EP4 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.2007.09.074
5280360.0 3082 None 47 Human Binding pKi = 9.1 9.1 -1 24
Binding affinity at human prostaglandin EP4 receptorB