Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 49783414 | 17684 | None | 0 | Human | Functional | pEC50 | = | 9.8 | 9.8 | - | 1 | Agonist activity at 5HT4 receptor expressed in HEK293/L9 cells by cAMP assayAgonist activity at 5HT4 receptor expressed in HEK293/L9 cells by cAMP assay |
ChEMBL | 320 | 7 | 1 | 5 | 2.9 | CCCCN1CCC(COC(=O)c2ccc(N)cc2OC)CC1 | 10.1021/jm100668r | ||
| CHEMBL1258451 | 17684 | None | 0 | Human | Functional | pEC50 | = | 9.8 | 9.8 | - | 1 | Agonist activity at 5HT4 receptor expressed in HEK293/L9 cells by cAMP assayAgonist activity at 5HT4 receptor expressed in HEK293/L9 cells by cAMP assay |
ChEMBL | 320 | 7 | 1 | 5 | 2.9 | CCCCN1CCC(COC(=O)c2ccc(N)cc2OC)CC1 | 10.1021/jm100668r | ||
| 53354764 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.7 | 9.7 | 1 | 2 | Partial agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assayPartial agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 9059 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.7 | 9.7 | 1 | 2 | Partial agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assayPartial agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| CHEMBL2152922 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.7 | 9.7 | 1 | 2 | Partial agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assayPartial agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| DB12675 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.7 | 9.7 | 1 | 2 | Partial agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assayPartial agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 53354764 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.6 | 9.6 | 1 | 2 | Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 9059 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.6 | 9.6 | 1 | 2 | Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| CHEMBL2152922 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.6 | 9.6 | 1 | 2 | Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| DB12675 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.6 | 9.6 | 1 | 2 | Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 53354764 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 1 | 2 | Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 9059 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 1 | 2 | Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| CHEMBL2152922 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 1 | 2 | Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| DB12675 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 1 | 2 | Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 11166796 | 82708 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 1 | 2 | Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 448 | 5 | 2 | 7 | 2.3 | CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 | 10.1021/jm300953p | ||
| CHEMBL2179583 | 82708 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 1 | 2 | Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 448 | 5 | 2 | 7 | 2.3 | CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 | 10.1021/jm300953p | ||
| 11504722 | 76449 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulation |
ChEMBL | 532 | 8 | 2 | 8 | 1.3 | CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)c2ccccc21 | 10.1016/j.bmcl.2012.05.034 | ||
| CHEMBL2059588 | 76449 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulation |
ChEMBL | 532 | 8 | 2 | 8 | 1.3 | CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)c2ccccc21 | 10.1016/j.bmcl.2012.05.034 | ||
| 44224237 | 194902 | None | 5 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulation |
ChEMBL | 559 | 8 | 2 | 8 | 1.2 | CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 | 10.1016/j.bmcl.2012.05.034 | ||
| CHEMBL538635 | 194902 | None | 5 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulation |
ChEMBL | 559 | 8 | 2 | 8 | 1.2 | CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 | 10.1016/j.bmcl.2012.05.034 | ||
| 44224237 | 194902 | None | 5 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay |
ChEMBL | 559 | 8 | 2 | 8 | 1.2 | CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 | 10.1021/jm900881j | ||
| CHEMBL538635 | 194902 | None | 5 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay |
ChEMBL | 559 | 8 | 2 | 8 | 1.2 | CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 | 10.1021/jm900881j | ||
| 44248189 91900499 | 195128 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay |
ChEMBL | 549 | 12 | 2 | 6 | 4.2 | CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCC[C@@H]2C(N)=O)cc2ccccc21 | 10.1021/jm900881j | ||
| CHEMBL539713 | 195128 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay |
ChEMBL | 549 | 12 | 2 | 6 | 4.2 | CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCC[C@@H]2C(N)=O)cc2ccccc21 | 10.1021/jm900881j | ||
| 71712463 | 91424 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation |
ChEMBL | 465 | 9 | 3 | 6 | 1.4 | CC(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN(C)S(C)(=O)=O)CC3)cccc2[nH]1 | 10.1016/j.bmcl.2013.05.018 | ||
| CHEMBL2402900 | 91424 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation |
ChEMBL | 465 | 9 | 3 | 6 | 1.4 | CC(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN(C)S(C)(=O)=O)CC3)cccc2[nH]1 | 10.1016/j.bmcl.2013.05.018 | ||
| 53357011 | 82705 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay |
ChEMBL | 446 | 7 | 2 | 8 | 2.8 | O[C@@H]1CC[C@@H](Oc2cccc3onc(OCC4CCN(CC5(O)CCOCC5)CC4)c23)C1 | 10.1021/jm300953p | ||
| CHEMBL2179580 | 82705 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay |
ChEMBL | 446 | 7 | 2 | 8 | 2.8 | O[C@@H]1CC[C@@H](Oc2cccc3onc(OCC4CCN(CC5(O)CCOCC5)CC4)c23)C1 | 10.1021/jm300953p | ||
| 53354764 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 1 | 2 | Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 9059 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 1 | 2 | Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| CHEMBL2152922 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 1 | 2 | Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| DB12675 | 3064 | None | 36 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 1 | 2 | Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 11350913 | 136882 | None | 2 | Human | Functional | pEC50 | = | 9.3 | 9.3 | - | 1 | Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assayAgonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay |
ChEMBL | 430 | 5 | 2 | 7 | 2.2 | CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2ccccc21 | 10.1016/j.ejmech.2015.08.051 | ||
| CHEMBL3741376 | 136882 | None | 2 | Human | Functional | pEC50 | = | 9.3 | 9.3 | - | 1 | Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assayAgonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay |
ChEMBL | 430 | 5 | 2 | 7 | 2.2 | CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2ccccc21 | 10.1016/j.ejmech.2015.08.051 | ||
| 11961293 | 3769 | None | 21 | Human | Functional | pEC50 | = | 9.3 | 9.3 | - | 1 | Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation |
ChEMBL | 455 | 6 | 2 | 5 | 3.6 | COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C | 10.1016/j.bmcl.2013.05.018 | ||
| 8426 | 3769 | None | 21 | Human | Functional | pEC50 | = | 9.3 | 9.3 | - | 1 | Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation |
ChEMBL | 455 | 6 | 2 | 5 | 3.6 | COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C | 10.1016/j.bmcl.2013.05.018 | ||
| CHEMBL2402904 | 3769 | None | 21 | Human | Functional | pEC50 | = | 9.3 | 9.3 | - | 1 | Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation |
ChEMBL | 455 | 6 | 2 | 5 | 3.6 | COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C | 10.1016/j.bmcl.2013.05.018 | ||
| DB12725 | 3769 | None | 21 | Human | Functional | pEC50 | = | 9.3 | 9.3 | - | 1 | Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation |
ChEMBL | 455 | 6 | 2 | 5 | 3.6 | COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C | 10.1016/j.bmcl.2013.05.018 | ||
| 53354764 | 3064 | None | 36 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 2 | Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 9059 | 3064 | None | 36 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 2 | Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| CHEMBL2152922 | 3064 | None | 36 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 2 | Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| DB12675 | 3064 | None | 36 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 2 | Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 53354764 | 3064 | None | 36 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 2 | Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 9059 | 3064 | None | 36 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 2 | Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| CHEMBL2152922 | 3064 | None | 36 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 2 | Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| DB12675 | 3064 | None | 36 | Rat | Functional | pEC50 | = | 9.2 | 9.2 | -1 | 2 | Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/jm300953p | ||
| 11842633 | 3981 | None | 22 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at 5HT4c receptor expressed in cells at 100-fold physiological level assessed as cAMP accumulationAgonist activity at 5HT4c receptor expressed in cells at 100-fold physiological level assessed as cAMP accumulation |
ChEMBL | 504 | 8 | 2 | 7 | 1.6 | O[C@@H](CN(S(=O)(=O)C)C)CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)c1cc2ccccc2n(c1=O)C(C)C | 10.1016/j.bmcl.2012.08.051 | ||
| 8425 | 3981 | None | 22 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at 5HT4c receptor expressed in cells at 100-fold physiological level assessed as cAMP accumulationAgonist activity at 5HT4c receptor expressed in cells at 100-fold physiological level assessed as cAMP accumulation |
ChEMBL | 504 | 8 | 2 | 7 | 1.6 | O[C@@H](CN(S(=O)(=O)C)C)CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)c1cc2ccccc2n(c1=O)C(C)C | 10.1016/j.bmcl.2012.08.051 | ||
| CHEMBL2087337 | 3981 | None | 22 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at 5HT4c receptor expressed in cells at 100-fold physiological level assessed as cAMP accumulationAgonist activity at 5HT4c receptor expressed in cells at 100-fold physiological level assessed as cAMP accumulation |
ChEMBL | 504 | 8 | 2 | 7 | 1.6 | O[C@@H](CN(S(=O)(=O)C)C)CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)c1cc2ccccc2n(c1=O)C(C)C | 10.1016/j.bmcl.2012.08.051 | ||
| 70686434 | 76444 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulation |
ChEMBL | 560 | 10 | 3 | 8 | 2.0 | CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCC(CNS(C)(=O)=O)CC2)c2ccccc21 | 10.1016/j.bmcl.2012.05.034 | ||
Showing 1 to 50 of 862 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 145973928 | 164664 | None | 0 | Human | Binding | pEC50 | = | 10 | 10.0 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 398 | 6 | 1 | 5 | 3.3 | CC(C)c1cc2cccc(C(=O)NCC3CCN(CC4CCOCC4)CC3)n2n1 | 10.1021/acs.jmedchem.8b00457 | ||
| CHEMBL4215329 | 164664 | None | 0 | Human | Binding | pEC50 | = | 10 | 10.0 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 398 | 6 | 1 | 5 | 3.3 | CC(C)c1cc2cccc(C(=O)NCC3CCN(CC4CCOCC4)CC3)n2n1 | 10.1021/acs.jmedchem.8b00457 | ||
| 53354764 | 3064 | None | 36 | Human | Binding | pEC50 | = | 9.6 | 9.6 | 1 | 2 | Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin) |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.8b00457 | ||
| 9059 | 3064 | None | 36 | Human | Binding | pEC50 | = | 9.6 | 9.6 | 1 | 2 | Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin) |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.8b00457 | ||
| CHEMBL2152922 | 3064 | None | 36 | Human | Binding | pEC50 | = | 9.6 | 9.6 | 1 | 2 | Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin) |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.8b00457 | ||
| DB12675 | 3064 | None | 36 | Human | Binding | pEC50 | = | 9.6 | 9.6 | 1 | 2 | Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin) |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.8b00457 | ||
| 145975193 | 163966 | None | 0 | Human | Binding | pEC50 | = | 9.5 | 9.5 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 372 | 8 | 1 | 5 | 2.9 | COCCCN1CCC(CNC(=O)c2cccc3cc(C(C)C)nn23)CC1 | 10.1021/acs.jmedchem.8b00457 | ||
| CHEMBL4206847 | 163966 | None | 0 | Human | Binding | pEC50 | = | 9.5 | 9.5 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 372 | 8 | 1 | 5 | 2.9 | COCCCN1CCC(CNC(=O)c2cccc3cc(C(C)C)nn23)CC1 | 10.1021/acs.jmedchem.8b00457 | ||
| 145973097 | 164813 | None | 0 | Human | Binding | pEC50 | = | 9.5 | 9.5 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 412 | 6 | 2 | 5 | 3.6 | CC(C)c1cn2cccc(C(=O)NCC3CCN(CC4(O)CCCCC4)CC3)c2n1 | 10.1021/acs.jmedchem.8b00457 | ||
| CHEMBL4217381 | 164813 | None | 0 | Human | Binding | pEC50 | = | 9.5 | 9.5 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 412 | 6 | 2 | 5 | 3.6 | CC(C)c1cn2cccc(C(=O)NCC3CCN(CC4(O)CCCCC4)CC3)c2n1 | 10.1021/acs.jmedchem.8b00457 | ||
| 145965246 | 164316 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 414 | 6 | 2 | 6 | 2.4 | CC(C)c1cn2cccc(C(=O)NCC3CCN(CC4(O)CCOCC4)CC3)c2n1 | 10.1021/acs.jmedchem.8b00457 | ||
| CHEMBL4211044 | 164316 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 414 | 6 | 2 | 6 | 2.4 | CC(C)c1cn2cccc(C(=O)NCC3CCN(CC4(O)CCOCC4)CC3)c2n1 | 10.1021/acs.jmedchem.8b00457 | ||
| 77105903 | 164095 | None | 0 | Human | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 398 | 6 | 1 | 5 | 3.3 | CC(C)c1cn2cccc(C(=O)NCC3CCN(CC4CCOCC4)CC3)c2n1 | 10.1021/acs.jmedchem.8b00457 | ||
| CHEMBL4208302 | 164095 | None | 0 | Human | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 398 | 6 | 1 | 5 | 3.3 | CC(C)c1cn2cccc(C(=O)NCC3CCN(CC4CCOCC4)CC3)c2n1 | 10.1021/acs.jmedchem.8b00457 | ||
| 145967487 | 164495 | None | 0 | Human | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 455 | 6 | 1 | 6 | 3.4 | COC(=O)N1CCC(CN2CCC(CNC(=O)c3cccn4cc(C(C)C)nc34)CC2)CC1 | 10.1021/acs.jmedchem.8b00457 | ||
| CHEMBL4213334 | 164495 | None | 0 | Human | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 455 | 6 | 1 | 6 | 3.4 | COC(=O)N1CCC(CN2CCC(CNC(=O)c3cccn4cc(C(C)C)nc34)CC2)CC1 | 10.1021/acs.jmedchem.8b00457 | ||
| 145972577 | 164712 | None | 0 | Human | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 372 | 6 | 2 | 5 | 2.7 | CC(C)c1cn2cccc(C(=O)NCC3CCN(CC(C)(C)O)CC3)c2n1 | 10.1021/acs.jmedchem.8b00457 | ||
| CHEMBL4216003 | 164712 | None | 0 | Human | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 372 | 6 | 2 | 5 | 2.7 | CC(C)c1cn2cccc(C(=O)NCC3CCN(CC(C)(C)O)CC3)c2n1 | 10.1021/acs.jmedchem.8b00457 | ||
| 11350913 | 136882 | None | 2 | Human | Binding | pEC50 | = | 8.9 | 8.9 | - | 0 | Agonist activity at 5-HT4D receptor (unknown origin)Agonist activity at 5-HT4D receptor (unknown origin) |
ChEMBL | 430 | 5 | 2 | 7 | 2.2 | CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2ccccc21 | 10.1016/j.ejmech.2015.08.051 | ||
| CHEMBL3741376 | 136882 | None | 2 | Human | Binding | pEC50 | = | 8.9 | 8.9 | - | 0 | Agonist activity at 5-HT4D receptor (unknown origin)Agonist activity at 5-HT4D receptor (unknown origin) |
ChEMBL | 430 | 5 | 2 | 7 | 2.2 | CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2ccccc21 | 10.1016/j.ejmech.2015.08.051 | ||
| 53354764 | 3064 | None | 36 | Human | Binding | pEC50 | = | 8.9 | 8.9 | 1 | 2 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.1c00703 | ||
| 9059 | 3064 | None | 36 | Human | Binding | pEC50 | = | 8.9 | 8.9 | 1 | 2 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.1c00703 | ||
| CHEMBL2152922 | 3064 | None | 36 | Human | Binding | pEC50 | = | 8.9 | 8.9 | 1 | 2 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.1c00703 | ||
| DB12675 | 3064 | None | 36 | Human | Binding | pEC50 | = | 8.9 | 8.9 | 1 | 2 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.1c00703 | ||
| 53354764 | 3064 | None | 36 | Human | Binding | pEC50 | = | 8.8 | 8.8 | 1 | 2 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.8b00457 | ||
| 9059 | 3064 | None | 36 | Human | Binding | pEC50 | = | 8.8 | 8.8 | 1 | 2 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.8b00457 | ||
| CHEMBL2152922 | 3064 | None | 36 | Human | Binding | pEC50 | = | 8.8 | 8.8 | 1 | 2 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.8b00457 | ||
| DB12675 | 3064 | None | 36 | Human | Binding | pEC50 | = | 8.8 | 8.8 | 1 | 2 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 432 | 7 | 1 | 8 | 2.6 | OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 | 10.1021/acs.jmedchem.8b00457 | ||
| 145975035 | 163626 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 372 | 8 | 1 | 5 | 2.9 | COCCCN1CCC(CNC(=O)c2cccn3cc(C(C)C)nc23)CC1 | 10.1021/acs.jmedchem.8b00457 | ||
| CHEMBL4202791 | 163626 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 372 | 8 | 1 | 5 | 2.9 | COCCCN1CCC(CNC(=O)c2cccn3cc(C(C)C)nc23)CC1 | 10.1021/acs.jmedchem.8b00457 | ||
| 145966407 | 164310 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 382 | 5 | 1 | 5 | 2.5 | CC(C)c1nc(C(=O)NCC2C3CN(C4CCOCC4)CC23)n2ccccc12 | 10.1021/acs.jmedchem.8b00457 | ||
| CHEMBL4210983 | 164310 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay |
ChEMBL | 382 | 5 | 1 | 5 | 2.5 | CC(C)c1nc(C(=O)NCC2C3CN(C4CCOCC4)CC23)n2ccccc12 | 10.1021/acs.jmedchem.8b00457 | ||
| 171347354 | 194732 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 386 | 6 | 2 | 5 | 2.9 | CC(C)n1nc(C(=O)NC2CCN(CC(C)(C)C(=O)O)CC2)c2ccccc21 | 10.1021/acs.jmedchem.1c00703 | ||
| CHEMBL5283568 | 194732 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 386 | 6 | 2 | 5 | 2.9 | CC(C)n1nc(C(=O)NC2CCN(CC(C)(C)C(=O)O)CC2)c2ccccc21 | 10.1021/acs.jmedchem.1c00703 | ||
| CHEMBL5315410 | 194732 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 386 | 6 | 2 | 5 | 2.9 | CC(C)n1nc(C(=O)NC2CCN(CC(C)(C)C(=O)O)CC2)c2ccccc21 | 10.1021/acs.jmedchem.1c00703 | ||
| 171344909 | 194765 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 370 | 4 | 1 | 5 | 3.0 | CC(C)n1nc(C(=O)NC2CCN(C3CCOCC3)CC2)c2ccccc21 | 10.1021/acs.jmedchem.1c00703 | ||
| CHEMBL5275962 | 194765 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 370 | 4 | 1 | 5 | 3.0 | CC(C)n1nc(C(=O)NC2CCN(C3CCOCC3)CC2)c2ccccc21 | 10.1021/acs.jmedchem.1c00703 | ||
| CHEMBL5315855 | 194765 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 370 | 4 | 1 | 5 | 3.0 | CC(C)n1nc(C(=O)NC2CCN(C3CCOCC3)CC2)c2ccccc21 | 10.1021/acs.jmedchem.1c00703 | ||
| 68592173 | 137928 | None | 0 | Rat | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contractionAgonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contraction |
ChEMBL | 494 | 6 | 2 | 6 | 3.0 | COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)C(C)(C)C)CC2)C[C@H]1OC | 10.1016/j.ejmech.2015.12.006 | ||
| CHEMBL3759944 | 137928 | None | 0 | Rat | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contractionAgonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contraction |
ChEMBL | 494 | 6 | 2 | 6 | 3.0 | COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)C(C)(C)C)CC2)C[C@H]1OC | 10.1016/j.ejmech.2015.12.006 | ||
| 5311047 | 207221 | None | 22 | Rat | Binding | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contractionAgonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contraction |
ChEMBL | 465 | 9 | 2 | 6 | 3.4 | COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCOc2ccc(F)cc2)C[C@H]1OC | 10.1016/j.ejmech.2015.12.006 | ||
| CHEMBL74656 | 207221 | None | 22 | Rat | Binding | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contractionAgonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contraction |
ChEMBL | 465 | 9 | 2 | 6 | 3.4 | COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCOc2ccc(F)cc2)C[C@H]1OC | 10.1016/j.ejmech.2015.12.006 | ||
| 67922794 | 137807 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Agonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contractionAgonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contraction |
ChEMBL | 452 | 7 | 2 | 6 | 2.2 | COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCCCC2)C[C@H]1OC | 10.1016/j.ejmech.2015.12.006 | ||
| CHEMBL3758945 | 137807 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Agonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contractionAgonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contraction |
ChEMBL | 452 | 7 | 2 | 6 | 2.2 | COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCCCC2)C[C@H]1OC | 10.1016/j.ejmech.2015.12.006 | ||
| 171348105 | 194738 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 409 | 5 | 0 | 7 | 4.3 | CC(C)n1nc(-c2nc(C3CCN(CC4CCOCC4)CC3)no2)c2ccccc21 | 10.1021/acs.jmedchem.1c00703 | ||
| CHEMBL5287697 | 194738 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 409 | 5 | 0 | 7 | 4.3 | CC(C)n1nc(-c2nc(C3CCN(CC4CCOCC4)CC3)no2)c2ccccc21 | 10.1021/acs.jmedchem.1c00703 | ||
| CHEMBL5315464 | 194738 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 409 | 5 | 0 | 7 | 4.3 | CC(C)n1nc(-c2nc(C3CCN(CC4CCOCC4)CC3)no2)c2ccccc21 | 10.1021/acs.jmedchem.1c00703 | ||
| 171348479 | 194751 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 409 | 7 | 0 | 7 | 4.4 | COCCCN1C2CCC1CC(c1nnc(-c3nn(C(C)C)c4ccccc34)o1)C2 | 10.1021/acs.jmedchem.1c00703 | ||
| CHEMBL5267721 | 194751 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 409 | 7 | 0 | 7 | 4.4 | COCCCN1C2CCC1CC(c1nnc(-c3nn(C(C)C)c4ccccc34)o1)C2 | 10.1021/acs.jmedchem.1c00703 | ||
| CHEMBL5315690 | 194751 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayPartial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay |
ChEMBL | 409 | 7 | 0 | 7 | 4.4 | COCCCN1C2CCC1CC(c1nnc(-c3nn(C(C)C)c4ccccc34)o1)C2 | 10.1021/acs.jmedchem.1c00703 | ||
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