Ligand source activities (1 row/activity)
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
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Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
|
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
9868867 | 187228 | None | 0 | Mouse | Functional | pEC50 | = | 8.7 | 8.7 | - | 1 | Agonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation countingAgonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation counting |
ChEMBL | 460 | 12 | 4 | 5 | 3.3 | O=C(O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1OC[C@@H](O)CCc1cccc(C(F)(F)F)c1 | 10.1016/j.bmc.2008.11.070 | ||
CHEMBL491667 | 187228 | None | 0 | Mouse | Functional | pEC50 | = | 8.7 | 8.7 | - | 1 | Agonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation countingAgonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation counting |
ChEMBL | 460 | 12 | 4 | 5 | 3.3 | O=C(O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1OC[C@@H](O)CCc1cccc(C(F)(F)F)c1 | 10.1016/j.bmc.2008.11.070 | ||
1894 | 957 | None | 35 | Human | Functional | pEC50 | = | 8 | 8.0 | 229 | 5 | Functional activity in RAT-1cells, transiently-transfected with human FP-receptor (% of control ligand, fluprostenol=100%)Functional activity in RAT-1cells, transiently-transfected with human FP-receptor (% of control ligand, fluprostenol=100%) |
ChEMBL | 424 | 11 | 4 | 5 | 3.2 | OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O | 10.1016/s0960-894x(00)00273-0 | ||
5311053 | 957 | None | 35 | Human | Functional | pEC50 | = | 8 | 8.0 | 229 | 5 | Functional activity in RAT-1cells, transiently-transfected with human FP-receptor (% of control ligand, fluprostenol=100%)Functional activity in RAT-1cells, transiently-transfected with human FP-receptor (% of control ligand, fluprostenol=100%) |
ChEMBL | 424 | 11 | 4 | 5 | 3.2 | OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O | 10.1016/s0960-894x(00)00273-0 | ||
CHEMBL37853 | 957 | None | 35 | Human | Functional | pEC50 | = | 8 | 8.0 | 229 | 5 | Functional activity in RAT-1cells, transiently-transfected with human FP-receptor (% of control ligand, fluprostenol=100%)Functional activity in RAT-1cells, transiently-transfected with human FP-receptor (% of control ligand, fluprostenol=100%) |
ChEMBL | 424 | 11 | 4 | 5 | 3.2 | OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O | 10.1016/s0960-894x(00)00273-0 | ||
DB11507 | 957 | None | 35 | Human | Functional | pEC50 | = | 8 | 8.0 | 229 | 5 | Functional activity in RAT-1cells, transiently-transfected with human FP-receptor (% of control ligand, fluprostenol=100%)Functional activity in RAT-1cells, transiently-transfected with human FP-receptor (% of control ligand, fluprostenol=100%) |
ChEMBL | 424 | 11 | 4 | 5 | 3.2 | OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O | 10.1016/s0960-894x(00)00273-0 | ||
134157766 | 154139 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | -1 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 390 | 8 | 3 | 5 | 2.6 | O=C(O)CC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 | 10.1021/acsmedchemlett.6b00415 | ||
CHEMBL3984438 | 154139 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | -1 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 390 | 8 | 3 | 5 | 2.6 | O=C(O)CC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 | 10.1021/acsmedchemlett.6b00415 | ||
134149776 | 148591 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | 43 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 390 | 8 | 3 | 5 | 2.6 | O=C(O)CC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 | 10.1021/acsmedchemlett.6b00415 | ||
CHEMBL3938300 | 148591 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | 43 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 390 | 8 | 3 | 5 | 2.6 | O=C(O)CC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 | 10.1021/acsmedchemlett.6b00415 | ||
134151657 | 153203 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | 1 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 418 | 10 | 3 | 5 | 3.4 | O=C(O)CCCC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 | 10.1021/acsmedchemlett.6b00415 | ||
CHEMBL3976382 | 153203 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | 1 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 418 | 10 | 3 | 5 | 3.4 | O=C(O)CCCC[C@@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)OC1 | 10.1021/acsmedchemlett.6b00415 | ||
1959 | 659 | None | 34 | Human | Functional | pEC50 | = | 7.9 | 7.9 | 1737 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 388 | 11 | 4 | 4 | 3.1 | OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O | 10.1021/acsmedchemlett.6b00415 | ||
5283081 | 659 | None | 34 | Human | Functional | pEC50 | = | 7.9 | 7.9 | 1737 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 388 | 11 | 4 | 4 | 3.1 | OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O | 10.1021/acsmedchemlett.6b00415 | ||
CHEMBL3914661 | 659 | None | 34 | Human | Functional | pEC50 | = | 7.9 | 7.9 | 1737 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 388 | 11 | 4 | 4 | 3.1 | OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O | 10.1021/acsmedchemlett.6b00415 | ||
1884 | 3083 | None | 40 | Mouse | Functional | pEC50 | = | 7.9 | 7.9 | -2 | 9 | Agonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPRAgonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPR |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/j.bmcl.2012.12.058 | ||
5280363 | 3083 | None | 40 | Mouse | Functional | pEC50 | = | 7.9 | 7.9 | -2 | 9 | Agonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPRAgonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPR |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/j.bmcl.2012.12.058 | ||
912 | 3083 | None | 40 | Mouse | Functional | pEC50 | = | 7.9 | 7.9 | -2 | 9 | Agonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPRAgonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPR |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/j.bmcl.2012.12.058 | ||
CHEMBL815 | 3083 | None | 40 | Mouse | Functional | pEC50 | = | 7.9 | 7.9 | -2 | 9 | Agonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPRAgonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPR |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/j.bmcl.2012.12.058 | ||
DB12789 | 3083 | None | 40 | Mouse | Functional | pEC50 | = | 7.9 | 7.9 | -2 | 9 | Agonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPRAgonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPR |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/j.bmcl.2012.12.058 | ||
13174090 | 152219 | None | 9 | Human | Functional | pEC50 | = | 7.8 | 7.8 | -17 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 388 | 11 | 3 | 5 | 2.8 | O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)COc1ccccc1 | 10.1021/acsmedchemlett.6b00415 | ||
CHEMBL3967903 | 152219 | None | 9 | Human | Functional | pEC50 | = | 7.8 | 7.8 | -17 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 388 | 11 | 3 | 5 | 2.8 | O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)COc1ccccc1 | 10.1021/acsmedchemlett.6b00415 | ||
14429703 | 142459 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -5248 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 467 | 12 | 4 | 7 | 1.5 | CS(=O)(=O)NC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)COc1ccccc1 | 10.1021/acsmedchemlett.6b00415 | ||
CHEMBL3889508 | 142459 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -5248 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 467 | 12 | 4 | 7 | 1.5 | CS(=O)(=O)NC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)COc1ccccc1 | 10.1021/acsmedchemlett.6b00415 | ||
44393462 | 66868 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 458 | 12 | 3 | 5 | 4.0 | O=C(O)CCCC/C=C\C[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@@H](O)COc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2004.06.037 | ||
CHEMBL186192 | 66868 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 458 | 12 | 3 | 5 | 4.0 | O=C(O)CCCC/C=C\C[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@@H](O)COc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2004.06.037 | ||
44393438 | 66185 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 424 | 12 | 3 | 5 | 3.6 | O=C(O)CCCC/C=C\C[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@H](O)COc1cccc(Cl)c1 | 10.1016/j.bmcl.2004.06.037 | ||
CHEMBL184264 | 66185 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 424 | 12 | 3 | 5 | 3.6 | O=C(O)CCCC/C=C\C[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@H](O)COc1cccc(Cl)c1 | 10.1016/j.bmcl.2004.06.037 | ||
71552665 | 87111 | None | 0 | Mouse | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPRAgonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPR |
ChEMBL | 450 | 9 | 4 | 8 | 0.9 | NS(=O)(=O)c1ccc(-n2cc([C@H]3[C@H](O)C[C@H](O)[C@@H]3C/C=C\CCCC(=O)O)nn2)cc1 | 10.1016/j.bmcl.2012.12.058 | ||
CHEMBL2326219 | 87111 | None | 0 | Mouse | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPRAgonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPR |
ChEMBL | 450 | 9 | 4 | 8 | 0.9 | NS(=O)(=O)c1ccc(-n2cc([C@H]3[C@H](O)C[C@H](O)[C@@H]3C/C=C\CCCC(=O)O)nn2)cc1 | 10.1016/j.bmcl.2012.12.058 | ||
6438324 | 66712 | None | 0 | Human | Functional | pEC50 | = | 8.6 | 8.6 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 500 | 12 | 3 | 6 | 4.4 | CC(C)OC(=O)CCC/C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/C(O)COc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2004.06.037 | ||
CHEMBL185484 | 66712 | None | 0 | Human | Functional | pEC50 | = | 8.6 | 8.6 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 500 | 12 | 3 | 6 | 4.4 | CC(C)OC(=O)CCC/C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/C(O)COc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2004.06.037 | ||
68749474 | 146321 | None | 0 | Human | Functional | pEC50 | = | 7.7 | 7.7 | -1 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 390 | 8 | 3 | 5 | 2.8 | O=C(O)CC[C@H]1CCC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 | 10.1021/acsmedchemlett.6b00415 | ||
CHEMBL3920347 | 146321 | None | 0 | Human | Functional | pEC50 | = | 7.7 | 7.7 | -1 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assayAgonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay |
ChEMBL | 390 | 8 | 3 | 5 | 2.8 | O=C(O)CC[C@H]1CCC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 | 10.1021/acsmedchemlett.6b00415 | ||
44393448 | 65601 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 424 | 12 | 3 | 5 | 3.6 | O=C(O)CC/C=C\CCC[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@@H](O)COc1cccc(Cl)c1 | 10.1016/j.bmcl.2004.06.037 | ||
CHEMBL183193 | 65601 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 424 | 12 | 3 | 5 | 3.6 | O=C(O)CC/C=C\CCC[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@@H](O)COc1cccc(Cl)c1 | 10.1016/j.bmcl.2004.06.037 | ||
44393474 | 123059 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 340 | 12 | 3 | 4 | 3.1 | CCCCC[C@H](O)/C=C/[C@H]1OC[C@H](O)[C@@H]1C/C=C\CCCC(=O)O | 10.1016/j.bmcl.2004.06.037 | ||
CHEMBL360869 | 123059 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 340 | 12 | 3 | 4 | 3.1 | CCCCC[C@H](O)/C=C/[C@H]1OC[C@H](O)[C@@H]1C/C=C\CCCC(=O)O | 10.1016/j.bmcl.2004.06.037 | ||
1884 | 3083 | None | 40 | Mouse | Functional | pEC50 | = | 7.6 | 7.6 | -2 | 9 | Agonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation countingAgonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation counting |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/j.bmc.2008.11.070 | ||
5280363 | 3083 | None | 40 | Mouse | Functional | pEC50 | = | 7.6 | 7.6 | -2 | 9 | Agonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation countingAgonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation counting |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/j.bmc.2008.11.070 | ||
912 | 3083 | None | 40 | Mouse | Functional | pEC50 | = | 7.6 | 7.6 | -2 | 9 | Agonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation countingAgonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation counting |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/j.bmc.2008.11.070 | ||
CHEMBL815 | 3083 | None | 40 | Mouse | Functional | pEC50 | = | 7.6 | 7.6 | -2 | 9 | Agonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation countingAgonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation counting |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/j.bmc.2008.11.070 | ||
DB12789 | 3083 | None | 40 | Mouse | Functional | pEC50 | = | 7.6 | 7.6 | -2 | 9 | Agonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation countingAgonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation counting |
ChEMBL | 354 | 12 | 4 | 4 | 3.0 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O | 10.1016/j.bmc.2008.11.070 | ||
1884 | 3083 | None | 40 | Human | Functional | pEC50 | = | 7.6 | 7.6 | -2 | 9 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast 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 | 10.1016/j.bmcl.2004.06.037 | ||
5280363 | 3083 | None | 40 | Human | Functional | pEC50 | = | 7.6 | 7.6 | -2 | 9 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast 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 | 10.1016/j.bmcl.2004.06.037 | ||
912 | 3083 | None | 40 | Human | Functional | pEC50 | = | 7.6 | 7.6 | -2 | 9 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast 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 | 10.1016/j.bmcl.2004.06.037 | ||
CHEMBL815 | 3083 | None | 40 | Human | Functional | pEC50 | = | 7.6 | 7.6 | -2 | 9 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast 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 | 10.1016/j.bmcl.2004.06.037 | ||
DB12789 | 3083 | None | 40 | Human | Functional | pEC50 | = | 7.6 | 7.6 | -2 | 9 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast 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 | 10.1016/j.bmcl.2004.06.037 | ||
44393451 | 168353 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 424 | 12 | 3 | 5 | 3.6 | O=C(O)CC/C=C\CCC[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@H](O)COc1cccc(Cl)c1 | 10.1016/j.bmcl.2004.06.037 | ||
CHEMBL433752 | 168353 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cellsEfficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells |
ChEMBL | 424 | 12 | 3 | 5 | 3.6 | O=C(O)CC/C=C\CCC[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@H](O)COc1cccc(Cl)c1 | 10.1016/j.bmcl.2004.06.037 |
Showing 1 to 50 of 293 entries
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
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Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
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Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
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Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
68749980 | 189170 | None | 0 | Human | Binding | pEC50 | = | 7.7 | 7.7 | - | 0 | Agonist activity at FP receptor (unknown origin)Agonist activity at FP receptor (unknown origin) |
ChEMBL | 440 | 9 | 3 | 5 | 3.3 | O=C(O)CCC[C@H]1CC[C@@H]2[C@@H](/C=C/[C@@H](O)COc3cc(F)ccc3F)[C@H](O)C[C@@H]2OC1 | 10.1016/j.ejmech.2021.113842 | ||
CHEMBL5095395 | 189170 | None | 0 | Human | Binding | pEC50 | = | 7.7 | 7.7 | - | 0 | Agonist activity at FP receptor (unknown origin)Agonist activity at FP receptor (unknown origin) |
ChEMBL | 440 | 9 | 3 | 5 | 3.3 | O=C(O)CCC[C@H]1CC[C@@H]2[C@@H](/C=C/[C@@H](O)COc3cc(F)ccc3F)[C@H](O)C[C@@H]2OC1 | 10.1016/j.ejmech.2021.113842 | ||
50902259 | 2939 | None | 1 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 1 | Agonist activity at FP receptor (unknown origin)Agonist activity at FP receptor (unknown origin) |
ChEMBL | 482 | 10 | 2 | 6 | 4.2 | CC(OC(=O)CCC[C@H]1CC[C@H]2[C@@H](OC1)C[C@H]([C@@H]2/C=C/[C@H](COc1cc(F)ccc1F)O)O)C | 10.1016/j.ejmech.2021.113842 | ||
9875 | 2939 | None | 1 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 1 | Agonist activity at FP receptor (unknown origin)Agonist activity at FP receptor (unknown origin) |
ChEMBL | 482 | 10 | 2 | 6 | 4.2 | CC(OC(=O)CCC[C@H]1CC[C@H]2[C@@H](OC1)C[C@H]([C@@H]2/C=C/[C@H](COc1cc(F)ccc1F)O)O)C | 10.1016/j.ejmech.2021.113842 | ||
CHEMBL4297633 | 2939 | None | 1 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 1 | Agonist activity at FP receptor (unknown origin)Agonist activity at FP receptor (unknown origin) |
ChEMBL | 482 | 10 | 2 | 6 | 4.2 | CC(OC(=O)CCC[C@H]1CC[C@H]2[C@@H](OC1)C[C@H]([C@@H]2/C=C/[C@H](COc1cc(F)ccc1F)O)O)C | 10.1016/j.ejmech.2021.113842 | ||
DB12043 | 2939 | None | 1 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 1 | Agonist activity at FP receptor (unknown origin)Agonist activity at FP receptor (unknown origin) |
ChEMBL | 482 | 10 | 2 | 6 | 4.2 | CC(OC(=O)CCC[C@H]1CC[C@H]2[C@@H](OC1)C[C@H]([C@@H]2/C=C/[C@H](COc1cc(F)ccc1F)O)O)C | 10.1016/j.ejmech.2021.113842 | ||
1955 | 16 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Displacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cellsDisplacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cells |
ChEMBL | 428 | 13 | 4 | 5 | 3.6 | O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(00)00273-0 | ||
5311240 | 16 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Displacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cellsDisplacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cells |
ChEMBL | 428 | 13 | 4 | 5 | 3.6 | O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(00)00273-0 | ||
CHEMBL36041 | 16 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Displacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cellsDisplacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cells |
ChEMBL | 428 | 13 | 4 | 5 | 3.6 | O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O | 10.1016/s0960-894x(00)00273-0 | ||
1894 | 957 | None | 35 | Human | Binding | pIC50 | = | 9 | 9.0 | 1 | 5 | Displacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cellsDisplacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cells |
ChEMBL | 424 | 11 | 4 | 5 | 3.2 | OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O | 10.1016/s0960-894x(00)00273-0 | ||
5311053 | 957 | None | 35 | Human | Binding | pIC50 | = | 9 | 9.0 | 1 | 5 | Displacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cellsDisplacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cells |
ChEMBL | 424 | 11 | 4 | 5 | 3.2 | OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O | 10.1016/s0960-894x(00)00273-0 | ||
CHEMBL37853 | 957 | None | 35 | Human | Binding | pIC50 | = | 9 | 9.0 | 1 | 5 | Displacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cellsDisplacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cells |
ChEMBL | 424 | 11 | 4 | 5 | 3.2 | OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O | 10.1016/s0960-894x(00)00273-0 | ||
DB11507 | 957 | None | 35 | Human | Binding | pIC50 | = | 9 | 9.0 | 1 | 5 | Displacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cellsDisplacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cells |
ChEMBL | 424 | 11 | 4 | 5 | 3.2 | OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O | 10.1016/s0960-894x(00)00273-0 | ||
9825293 | 100109 | None | 8 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Displacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cellsDisplacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cells |
ChEMBL | 456 | 11 | 4 | 4 | 4.1 | O=C(O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCc1cccc(C(F)(F)F)c1 | 10.1016/s0960-894x(00)00273-0 | ||
CHEMBL287080 | 100109 | None | 8 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Displacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cellsDisplacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cells |
ChEMBL | 456 | 11 | 4 | 4 | 4.1 | O=C(O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCc1cccc(C(F)(F)F)c1 | 10.1016/s0960-894x(00)00273-0 | ||
44354547 | 116643 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | In vitro binding at FP human prostaglandin receptor using [3H]- PGF-2 alpha as radioligandIn vitro binding at FP human prostaglandin receptor using [3H]- PGF-2 alpha as radioligand |
ChEMBL | 390 | 12 | 5 | 4 | 2.7 | CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C[C@H](O)[C@@H]1C/C=C\CCCP(=O)(O)O | 10.1021/jm010264b | ||
CHEMBL336543 | 116643 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | In vitro binding at FP human prostaglandin receptor using [3H]- PGF-2 alpha as radioligandIn vitro binding at FP human prostaglandin receptor using [3H]- PGF-2 alpha as radioligand |
ChEMBL | 390 | 12 | 5 | 4 | 2.7 | CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C[C@H](O)[C@@H]1C/C=C\CCCP(=O)(O)O | 10.1021/jm010264b | ||
44571206 | 184095 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Binding affinity to human FP receptor by radioligand binding assayBinding affinity to human FP receptor by radioligand binding assay |
ChEMBL | 574 | 6 | 1 | 5 | 6.4 | CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc3ccccc3c1)C(=O)C2 | 10.1016/j.bmcl.2008.12.027 | ||
CHEMBL481813 | 184095 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Binding affinity to human FP receptor by radioligand binding assayBinding affinity to human FP receptor by radioligand binding assay |
ChEMBL | 574 | 6 | 1 | 5 | 6.4 | CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)=C1N(Cc1ccc3ccccc3c1)C(=O)C2 | 10.1016/j.bmcl.2008.12.027 | ||
10047541 | 132578 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Affinity for human Prostanoid FP receptor expressed in COS-7 cellsAffinity for human Prostanoid FP receptor expressed in COS-7 cells |
ChEMBL | 416 | 13 | 4 | 6 | 3.8 | O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccs1 | 10.1021/jm990542v | ||
CHEMBL369797 | 132578 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Affinity for human Prostanoid FP receptor expressed in COS-7 cellsAffinity for human Prostanoid FP receptor expressed in COS-7 cells |
ChEMBL | 416 | 13 | 4 | 6 | 3.8 | O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccs1 | 10.1021/jm990542v | ||
11283 | 586 | None | 11 | Rat | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | Antagonist activity at rat FPR stably expressed in CHO cells assessed as inhibition of PGF2alpha-induced calcium flux preincubated for 10 mins followed by PGF2alpha stimulation and measured for 120 secs by fluo-8 AM dye based fluorescence assayAntagonist activity at rat FPR stably expressed in CHO cells assessed as inhibition of PGF2alpha-induced calcium flux preincubated for 10 mins followed by PGF2alpha stimulation and measured for 120 secs by fluo-8 AM dye based fluorescence assay |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.1021/acs.jmedchem.0c00834 | ||
146368333 | 586 | None | 11 | Rat | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | Antagonist activity at rat FPR stably expressed in CHO cells assessed as inhibition of PGF2alpha-induced calcium flux preincubated for 10 mins followed by PGF2alpha stimulation and measured for 120 secs by fluo-8 AM dye based fluorescence assayAntagonist activity at rat FPR stably expressed in CHO cells assessed as inhibition of PGF2alpha-induced calcium flux preincubated for 10 mins followed by PGF2alpha stimulation and measured for 120 secs by fluo-8 AM dye based fluorescence assay |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.1021/acs.jmedchem.0c00834 | ||
CHEMBL4643852 | 586 | None | 11 | Rat | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | Antagonist activity at rat FPR stably expressed in CHO cells assessed as inhibition of PGF2alpha-induced calcium flux preincubated for 10 mins followed by PGF2alpha stimulation and measured for 120 secs by fluo-8 AM dye based fluorescence assayAntagonist activity at rat FPR stably expressed in CHO cells assessed as inhibition of PGF2alpha-induced calcium flux preincubated for 10 mins followed by PGF2alpha stimulation and measured for 120 secs by fluo-8 AM dye based fluorescence assay |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.1021/acs.jmedchem.0c00834 | ||
11283 | 586 | None | 11 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | Bayer inhouse assay (human)Bayer inhouse assay (human) |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.6019/CHEMBL4630901 | ||
146368333 | 586 | None | 11 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | Bayer inhouse assay (human)Bayer inhouse assay (human) |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.6019/CHEMBL4630901 | ||
CHEMBL4643852 | 586 | None | 11 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | Bayer inhouse assay (human)Bayer inhouse assay (human) |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.6019/CHEMBL4630901 | ||
11283 | 586 | None | 11 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | Bayer inhouse assay (rat)Bayer inhouse assay (rat) |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.6019/CHEMBL4630901 | ||
146368333 | 586 | None | 11 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | Bayer inhouse assay (rat)Bayer inhouse assay (rat) |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.6019/CHEMBL4630901 | ||
CHEMBL4643852 | 586 | None | 11 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | Bayer inhouse assay (rat)Bayer inhouse assay (rat) |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.6019/CHEMBL4630901 | ||
44322535 | 209080 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in ovine luteal cells (OLC)Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in ovine luteal cells (OLC) |
ChEMBL | 447 | 12 | 5 | 7 | 3.2 | [N-]=[N+]=Nc1cc(O)cc(OC[C@H](O)/C=C/[C@H]2[C@H](O)C[C@H](O)[C@@H]2C/C=C\CCCC(=O)O)c1 | 10.1021/jm00121a046 | ||
CHEMBL89096 | 209080 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in ovine luteal cells (OLC)Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in ovine luteal cells (OLC) |
ChEMBL | 447 | 12 | 5 | 7 | 3.2 | [N-]=[N+]=Nc1cc(O)cc(OC[C@H](O)/C=C/[C@H]2[C@H](O)C[C@H](O)[C@@H]2C/C=C\CCCC(=O)O)c1 | 10.1021/jm00121a046 | ||
102305175 | 24898 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | In vitro binding at FP human prostaglandin receptor using [3H]PGF-2 alpha as radioligandIn vitro binding at FP human prostaglandin receptor using [3H]PGF-2 alpha as radioligand |
ChEMBL | 374 | 12 | 4 | 4 | 3.0 | CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C[C@H](O)[C@@H]1C/C=C\CCC[PH](=O)O | 10.1021/jm010264b | ||
CHEMBL134546 | 24898 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | In vitro binding at FP human prostaglandin receptor using [3H]PGF-2 alpha as radioligandIn vitro binding at FP human prostaglandin receptor using [3H]PGF-2 alpha as radioligand |
ChEMBL | 374 | 12 | 4 | 4 | 3.0 | CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C[C@H](O)[C@@H]1C/C=C\CCC[PH](=O)O | 10.1021/jm010264b | ||
15486805 | 166148 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Affinity for human Prostanoid FP receptor expressed in COS-7 cellsAffinity for human Prostanoid FP receptor expressed in COS-7 cells |
ChEMBL | 394 | 13 | 4 | 5 | 3.0 | O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)COc1ccccc1 | 10.1021/jm990542v | ||
CHEMBL425681 | 166148 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Affinity for human Prostanoid FP receptor expressed in COS-7 cellsAffinity for human Prostanoid FP receptor expressed in COS-7 cells |
ChEMBL | 394 | 13 | 4 | 5 | 3.0 | O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)COc1ccccc1 | 10.1021/jm990542v | ||
11283 | 586 | None | 11 | Mouse | Binding | pIC50 | = | 7.9 | 7.9 | - | 1 | Antagonist activity at FPR in mouse NIH3T3 cells assessed as inhibition of PGF2alpha-induced cytokine induced neutrophil attracting chemokine production measured after 24 hrs by Bio-Rad assayAntagonist activity at FPR in mouse NIH3T3 cells assessed as inhibition of PGF2alpha-induced cytokine induced neutrophil attracting chemokine production measured after 24 hrs by Bio-Rad assay |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.1021/acs.jmedchem.0c00834 | ||
146368333 | 586 | None | 11 | Mouse | Binding | pIC50 | = | 7.9 | 7.9 | - | 1 | Antagonist activity at FPR in mouse NIH3T3 cells assessed as inhibition of PGF2alpha-induced cytokine induced neutrophil attracting chemokine production measured after 24 hrs by Bio-Rad assayAntagonist activity at FPR in mouse NIH3T3 cells assessed as inhibition of PGF2alpha-induced cytokine induced neutrophil attracting chemokine production measured after 24 hrs by Bio-Rad assay |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.1021/acs.jmedchem.0c00834 | ||
CHEMBL4643852 | 586 | None | 11 | Mouse | Binding | pIC50 | = | 7.9 | 7.9 | - | 1 | Antagonist activity at FPR in mouse NIH3T3 cells assessed as inhibition of PGF2alpha-induced cytokine induced neutrophil attracting chemokine production measured after 24 hrs by Bio-Rad assayAntagonist activity at FPR in mouse NIH3T3 cells assessed as inhibition of PGF2alpha-induced cytokine induced neutrophil attracting chemokine production measured after 24 hrs by Bio-Rad assay |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.1021/acs.jmedchem.0c00834 | ||
11283 | 586 | None | 11 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 1 | Functional cellular assay: cytokine-induced neutrophil-attracting chemokine (KC) inhibitionFunctional cellular assay: cytokine-induced neutrophil-attracting chemokine (KC) inhibition |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.6019/CHEMBL4630901 | ||
146368333 | 586 | None | 11 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 1 | Functional cellular assay: cytokine-induced neutrophil-attracting chemokine (KC) inhibitionFunctional cellular assay: cytokine-induced neutrophil-attracting chemokine (KC) inhibition |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.6019/CHEMBL4630901 | ||
CHEMBL4643852 | 586 | None | 11 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 1 | Functional cellular assay: cytokine-induced neutrophil-attracting chemokine (KC) inhibitionFunctional cellular assay: cytokine-induced neutrophil-attracting chemokine (KC) inhibition |
ChEMBL | 543 | 8 | 2 | 4 | 5.9 | OC(=O)CC[C@H](c1ccccc1Cl)CNC(=O)c1c(C)c(nc2c1cc(Br)cc2)N1CCCC1 | 10.6019/CHEMBL4630901 | ||
CHEMBL4642079 | 216506 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 1 | Bayer inhouse assay (human)Bayer inhouse assay (human) |
ChEMBL | None | None | None | Cc1c(N2CCNCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | 10.6019/CHEMBL4630901 | ||||
1884 | 3083 | None | 40 | Bovine | Binding | pIC50 | = | 6.9 | 6.9 | -14 | 22 | Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM)Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM) |
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/jm00121a046 | ||
5280363 | 3083 | None | 40 | Bovine | Binding | pIC50 | = | 6.9 | 6.9 | -14 | 22 | Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM)Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM) |
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/jm00121a046 | ||
912 | 3083 | None | 40 | Bovine | Binding | pIC50 | = | 6.9 | 6.9 | -14 | 22 | Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM)Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM) |
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/jm00121a046 | ||
CHEMBL815 | 3083 | None | 40 | Bovine | Binding | pIC50 | = | 6.9 | 6.9 | -14 | 22 | Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM)Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM) |
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/jm00121a046 | ||
DB12789 | 3083 | None | 40 | Bovine | Binding | pIC50 | = | 6.9 | 6.9 | -14 | 22 | Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM)Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM) |
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/jm00121a046 | ||
162671048 | 182913 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Displacement of [3H]PGF2alpha from full-length recombinant human FP receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]PGF2alpha from full-length recombinant human FP receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method |
ChEMBL | 451 | 5 | 1 | 4 | 5.4 | Cc1c(-c2cccs2)nc2ccc(Br)cc2c1C(=O)NCCc1cccnc1 | 10.1021/acs.jmedchem.0c00834 | ||
CHEMBL4790821 | 182913 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Displacement of [3H]PGF2alpha from full-length recombinant human FP receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]PGF2alpha from full-length recombinant human FP receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method |
ChEMBL | 451 | 5 | 1 | 4 | 5.4 | Cc1c(-c2cccs2)nc2ccc(Br)cc2c1C(=O)NCCc1cccnc1 | 10.1021/acs.jmedchem.0c00834 |
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