Ligand source activities (1 row/activity)





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49783414 24449 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
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 24449 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
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 9838 34 None 1 2 Human 9.7 pEC50 = 9.7 Functional
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 9838 34 None 1 2 Human 9.7 pEC50 = 9.7 Functional
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 9838 34 None 1 2 Human 9.7 pEC50 = 9.7 Functional
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 9838 34 None 1 2 Human 9.7 pEC50 = 9.7 Functional
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 9838 34 None 1 2 Human 9.6 pEC50 = 9.6 Functional
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 9838 34 None 1 2 Human 9.6 pEC50 = 9.6 Functional
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 9838 34 None 1 2 Human 9.6 pEC50 = 9.6 Functional
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 9838 34 None 1 2 Human 9.6 pEC50 = 9.6 Functional
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 9838 34 None 1 2 Human 9.4 pEC50 = 9.4 Functional
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 9838 34 None 1 2 Human 9.4 pEC50 = 9.4 Functional
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 9838 34 None 1 2 Human 9.4 pEC50 = 9.4 Functional
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 9838 34 None 1 2 Human 9.4 pEC50 = 9.4 Functional
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 89451 0 None 1 2 Human 9.4 pEC50 = 9.4 Functional
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 89451 0 None 1 2 Human 9.4 pEC50 = 9.4 Functional
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 83197 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 83197 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 201569 8 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 201569 8 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 201569 8 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 201569 8 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 201625 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 201625 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 98165 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 98165 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 89448 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 89448 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 9838 34 None 1 2 Human 9.3 pEC50 = 9.3 Functional
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 9838 34 None 1 2 Human 9.3 pEC50 = 9.3 Functional
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 9838 34 None 1 2 Human 9.3 pEC50 = 9.3 Functional
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 9838 34 None 1 2 Human 9.3 pEC50 = 9.3 Functional
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 143573 2 None - 1 Human 9.3 pEC50 = 9.3 Functional
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 143573 2 None - 1 Human 9.3 pEC50 = 9.3 Functional
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 10541 19 None 5 2 Human 9.3 pEC50 = 9.3 Functional
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 10541 19 None 5 2 Human 9.3 pEC50 = 9.3 Functional
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 10541 19 None 5 2 Human 9.3 pEC50 = 9.3 Functional
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 10541 19 None 5 2 Human 9.3 pEC50 = 9.3 Functional
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 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
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 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
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 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
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 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
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 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
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 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
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 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
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 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
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 10753 21 None 7 2 Human 9.2 pEC50 = 9.2 Functional
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 10753 21 None 7 2 Human 9.2 pEC50 = 9.2 Functional
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 10753 21 None 7 2 Human 9.2 pEC50 = 9.2 Functional
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 83192 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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
CHEMBL2059583 83192 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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
44248922 201679 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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 627 14 2 7 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCC(CNS(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL540981 201679 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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 627 14 2 7 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCC(CNS(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44248319 202274 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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 615 16 1 7 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN(C)CCCN(C)S(C)(=O)=O)cc2ccccc21 10.1021/jm900881j
CHEMBL553404 202274 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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 615 16 1 7 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN(C)CCCN(C)S(C)(=O)=O)cc2ccccc21 10.1021/jm900881j
44247953 202597 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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 581 12 2 5 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
CHEMBL558163 202597 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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 581 12 2 5 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
71714541 98156 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 520 9 3 7 1.1 CC(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402891 98156 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 520 9 3 7 1.1 CC(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
71714542 98157 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 518 9 3 7 0.8 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]c(C5CC5)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402892 98157 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 518 9 3 7 0.8 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]c(C5CC5)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
53354764 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4L 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 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4L 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 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4L 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 9838 34 None -1 2 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4L 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
70694780 83191 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 509 12 1 6 5.0 COC[C@@H]1CCCN1CCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
CHEMBL2059582 83191 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 509 12 1 6 5.0 COC[C@@H]1CCCN1CCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
11606227 83194 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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)N3CC(O)CN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059585 83194 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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)N3CC(O)CN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
11627949 83196 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
CHEMBL2059587 83196 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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
44248921 202025 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 520 11 1 5 5.7 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL551013 202025 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 520 11 1 5 5.7 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
44248186 202240 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 567 15 3 5 6.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
CHEMBL552484 202240 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 567 15 3 5 6.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
11519716 202275 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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)N3CC(O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL553405 202275 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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)N3CC(O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44248321 202360 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 541 8 1 6 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCN(c3ccccc3)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL555222 202360 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 541 8 1 6 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCN(c3ccccc3)CC2)cc2ccccc21 10.1021/jm900881j
71714544 98159 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 542 9 3 7 1.1 CC(F)(F)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402894 98159 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 542 9 3 7 1.1 CC(F)(F)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
71712327 98162 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 490 8 2 6 1.7 CC(C)c1nc2c(C(=O)NCC3CCN(CCN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402897 98162 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 490 8 2 6 1.7 CC(C)c1nc2c(C(=O)NCC3CCN(CCN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
71451950 89450 8 None 1 2 Human 9.1 pEC50 = 9.1 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None 1 2 Human 9.1 pEC50 = 9.1 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
71450132 89452 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 358 8 0 5 4.7 CCCCN1CCC(COc2noc3cccc(OC4CCC4)c23)CC1 10.1021/jm300953p
CHEMBL2179584 89452 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 358 8 0 5 4.7 CCCCN1CCC(COc2noc3cccc(OC4CCC4)c23)CC1 10.1021/jm300953p
71451950 89450 8 None 1 2 Human 9.1 pEC50 = 9.1 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None 1 2 Human 9.1 pEC50 = 9.1 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
11166796 89451 0 None 1 2 Human 9.1 pEC50 = 9.1 Functional
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 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 89451 0 None 1 2 Human 9.1 pEC50 = 9.1 Functional
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 448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
11166796 89451 0 None -1 2 Rat 9.1 pEC50 = 9.1 Functional
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 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 89451 0 None -1 2 Rat 9.1 pEC50 = 9.1 Functional
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 448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
11166796 89451 0 None -1 2 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4L 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 89451 0 None -1 2 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4L 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
53357029 89457 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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 418 8 1 7 3.5 CC(C)COc1cccc2onc(OCC3CCN(CC4(O)CCOCC4)CC3)c12 10.1021/jm300953p
CHEMBL2179589 89457 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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 418 8 1 7 3.5 CC(C)COc1cccc2onc(OCC3CCN(CC4(O)CCOCC4)CC3)c12 10.1021/jm300953p
11166796 89451 0 None 1 2 Human 9.0 pEC50 = 9.0 Functional
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 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 89451 0 None 1 2 Human 9.0 pEC50 = 9.0 Functional
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 448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
135409453 10545 41 None 3 36 Human 9.0 pEC50 = 9 Functional
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 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
226 10545 41 None 3 36 Human 9.0 pEC50 = 9 Functional
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 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
CHEMBL76370 10545 41 None 3 36 Human 9.0 pEC50 = 9 Functional
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 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
44248435 202359 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 623 15 2 5 7.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
CHEMBL555210 202359 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 623 15 2 5 7.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
44248680 202361 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 571 10 2 7 3.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCC(CNS(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL555223 202361 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 571 10 2 7 3.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCC(CNS(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44248313 91900492 202643 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 492 9 1 5 5.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL558719 202643 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 492 9 1 5 5.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
71714540 98155 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 506 9 3 7 0.5 CCc1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402890 98155 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 506 9 3 7 0.5 CCc1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
66810955 98168 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 475 7 2 5 2.8 CC(C)c1nc2c(C(=O)NCC3CCN(CC4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402903 98168 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 475 7 2 5 2.8 CC(C)c1nc2c(C(=O)NCC3CCN(CC4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
71462650 89454 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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 372 9 0 5 4.9 CCCCN1CCC(COc2noc3cccc(OCC4CCC4)c23)CC1 10.1021/jm300953p
CHEMBL2179586 89454 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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 372 9 0 5 4.9 CCCCN1CCC(COc2noc3cccc(OCC4CCC4)c23)CC1 10.1021/jm300953p
71451950 89450 8 None -1 2 Rat 8.9 pEC50 = 8.9 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None -1 2 Rat 8.9 pEC50 = 8.9 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
11166796 89451 0 None 1 2 Human 8.9 pEC50 = 8.9 Functional
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 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 89451 0 None 1 2 Human 8.9 pEC50 = 8.9 Functional
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 448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
71451951 89453 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 372 8 0 5 5.0 CCCCN1CCC(COc2noc3cccc(OC4CCCC4)c23)CC1 10.1021/jm300953p
CHEMBL2179585 89453 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 372 8 0 5 5.0 CCCCN1CCC(COc2noc3cccc(OC4CCCC4)c23)CC1 10.1021/jm300953p
71462651 89455 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 360 9 0 5 4.8 CCCCN1CCC(COc2noc3cccc(OCC(C)C)c23)CC1 10.1021/jm300953p
CHEMBL2179587 89455 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 360 9 0 5 4.8 CCCCN1CCC(COc2noc3cccc(OCC(C)C)c23)CC1 10.1021/jm300953p
71451950 89450 8 None 1 2 Human 8.9 pEC50 = 8.9 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None 1 2 Human 8.9 pEC50 = 8.9 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
44247820 91900493 201578 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 534 12 1 5 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL538706 201578 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 534 12 1 5 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
44247951 91900497 201691 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 539 9 2 5 5.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
CHEMBL541223 201691 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 539 9 2 5 5.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
44248923 201715 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
CHEMBL541968 201715 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
44247822 91900495 202294 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 571 10 1 7 3.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL553685 202294 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 571 10 1 7 3.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44248184 202941 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 525 12 3 5 5.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
CHEMBL561278 202941 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 525 12 3 5 5.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
71451950 89450 8 None 1 2 Human 8.9 pEC50 = 8.9 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None 1 2 Human 8.9 pEC50 = 8.9 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
53354764 9838 34 None 1 2 Human 8.9 pEC50 = 8.9 Functional
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 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1016/j.ejmech.2015.08.051
9059 9838 34 None 1 2 Human 8.9 pEC50 = 8.9 Functional
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 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1016/j.ejmech.2015.08.051
CHEMBL2152922 9838 34 None 1 2 Human 8.9 pEC50 = 8.9 Functional
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 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1016/j.ejmech.2015.08.051
DB12675 9838 34 None 1 2 Human 8.9 pEC50 = 8.9 Functional
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 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1016/j.ejmech.2015.08.051
155565664 182382 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Partial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assayPartial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assay
ChEMBL 432 8 2 6 4.5 COc1ccc(CN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1O 10.1016/j.ejmech.2019.111596
CHEMBL4580044 182382 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Partial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assayPartial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assay
ChEMBL 432 8 2 6 4.5 COc1ccc(CN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1O 10.1016/j.ejmech.2019.111596
11493559 80188 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 324 4 1 5 2.6 COc1cc(N)c(Cl)cc1C(=O)OC[C@@H]1CCN2CCC[C@@H]12 10.1021/jm0509501
CHEMBL201621 80188 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 324 4 1 5 2.6 COc1cc(N)c(Cl)cc1C(=O)OC[C@@H]1CCN2CCC[C@@H]12 10.1021/jm0509501
11961293 10541 19 None 5 2 Human 8.8 pEC50 = 8.8 Functional
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 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 10.1016/j.ejmech.2015.08.051
8426 10541 19 None 5 2 Human 8.8 pEC50 = 8.8 Functional
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 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 10.1016/j.ejmech.2015.08.051
CHEMBL2402904 10541 19 None 5 2 Human 8.8 pEC50 = 8.8 Functional
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 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 10.1016/j.ejmech.2015.08.051
DB12725 10541 19 None 5 2 Human 8.8 pEC50 = 8.8 Functional
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 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 10.1016/j.ejmech.2015.08.051
71451950 89450 8 None -1 2 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None -1 2 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assayAgonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
70688535 83193 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 586 13 2 7 4.2 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCC(CNS(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059584 83193 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 586 13 2 7 4.2 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCC(CNS(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
44248076 201823 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 543 8 1 7 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL549449 201823 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 543 8 1 7 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
71712466 98016 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 439 6 2 4 3.4 CC(=O)N1CCC(CN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2401750 98016 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 439 6 2 4 3.4 CC(=O)N1CCC(CN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
71712325 98160 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 554 9 3 7 1.6 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]c(-c5ccccc5)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402895 98160 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 554 9 3 7 1.6 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]c(-c5ccccc5)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
71712328 98163 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 470 7 2 6 2.5 COC(=O)N1CCN(CCN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402898 98163 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 470 7 2 6 2.5 COC(=O)N1CCN(CCN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
71712465 98167 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 429 8 3 5 2.0 CC(=O)N(C)CC(O)CN1CCC(CNC(=O)c2cccc3[nH]c(C(C)C)nc23)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402902 98167 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 429 8 3 5 2.0 CC(=O)N(C)CC(O)CN1CCC(CNC(=O)c2cccc3[nH]c(C(C)C)nc23)CC1 10.1016/j.bmcl.2013.05.018
11166796 89451 0 None -1 2 Rat 8.8 pEC50 = 8.8 Functional
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 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 89451 0 None -1 2 Rat 8.8 pEC50 = 8.8 Functional
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 448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
71462652 89458 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 434 8 2 8 2.6 CC(C)(O)COc1cccc2onc(OCC3CCN(CC4(O)CCOCC4)CC3)c12 10.1021/jm300953p
CHEMBL2179590 89458 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 434 8 2 8 2.6 CC(C)(O)COc1cccc2onc(OCC3CCN(CC4(O)CCOCC4)CC3)c12 10.1021/jm300953p
9952994 113747 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 366 6 1 5 3.5 CCCCN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCC3)CC1 10.1016/0960-894X(96)00002-9
CHEMBL315071 113747 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 366 6 1 5 3.5 CCCCN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCC3)CC1 10.1016/0960-894X(96)00002-9
53357016 89449 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 1 8 3.0 OC1(CN2CCC(COc3noc4cccc(OC5CCOCC5)c34)CC2)CCOCC1 10.1021/jm300953p
CHEMBL2179581 89449 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 1 8 3.0 OC1(CN2CCC(COc3noc4cccc(OC5CCOCC5)c34)CC2)CCOCC1 10.1021/jm300953p
70682173 83186 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 453 7 2 6 3.2 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCCCC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059577 83186 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 453 7 2 6 3.2 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCCCC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
44248439 202971 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 464 7 1 5 4.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL561398 202971 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 464 7 1 5 4.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
135409453 10545 41 None 3 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulation
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
226 10545 41 None 3 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulation
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
CHEMBL76370 10545 41 None 3 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulation
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
44224237 201569 8 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level 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 201569 8 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level 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
71712464 98166 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 445 8 3 6 2.2 COC(=O)N(C)CC(O)CN1CCC(CNC(=O)c2cccc3[nH]c(C(C)C)nc23)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402901 98166 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 445 8 3 6 2.2 COC(=O)N(C)CC(O)CN1CCC(CNC(=O)c2cccc3[nH]c(C(C)C)nc23)CC1 10.1016/j.bmcl.2013.05.018
44224237 201569 8 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
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.2012.08.051
CHEMBL538635 201569 8 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
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.2012.08.051
15295138 57836 0 None - 1 Guinea pig 8.0 pEC50 = 8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
CHEMBL157880 57836 0 None - 1 Guinea pig 8.0 pEC50 = 8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
19081984 212733 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 336 7 1 4 3.8 C=CCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80413-3
CHEMBL84398 212733 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 336 7 1 4 3.8 C=CCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80413-3
49783210 24411 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 440 7 1 6 3.9 CCCCN1CCC(COC(=O)c2cc(Br)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258338 24411 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 440 7 1 6 3.9 CCCCN1CCC(COC(=O)c2cc(Br)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
5 6927 72 None -13 27 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contractionAgonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contraction
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.05.034
5202 6927 72 None -13 27 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contractionAgonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contraction
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.05.034
CHEMBL39 6927 72 None -13 27 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contractionAgonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contraction
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.05.034
DB08839 6927 72 None -13 27 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contractionAgonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contraction
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2012.05.034
11225102 83199 3 None -1 2 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contractionAgonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contraction
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.05.034
CHEMBL2059590 83199 3 None -1 2 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contractionAgonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contraction
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.05.034
10837280 91900491 202601 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 450 6 1 5 3.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL558259 202601 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 450 6 1 5 3.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
44248317 202678 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 12 1 7 2.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN(C)CCCN(C)S(C)(=O)=O)cc2ccccc21 10.1021/jm900881j
CHEMBL559050 202678 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 12 1 7 2.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN(C)CCCN(C)S(C)(=O)=O)cc2ccccc21 10.1021/jm900881j
11225102 83199 3 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulation
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.05.034
CHEMBL2059590 83199 3 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulationAgonist activity at human 5HT4C receptor expressed in a cell line expressing receptor at 10 fold physiological-level assessed as cAMP accumulation
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.05.034
127039167 143599 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 398 6 1 5 3.3 CC(C)c1nc(C(=O)NCC2CCN(CC3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741608 143599 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 398 6 1 5 3.3 CC(C)c1nc(C(=O)NCC2CCN(CC3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
71712611 98152 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 478 8 3 7 -0.1 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]cnc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402887 98152 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 478 8 3 7 -0.1 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]cnc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
11225102 83199 3 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.08.051
CHEMBL2059590 83199 3 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.08.051
70684790 84282 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 484 7 2 7 2.4 COC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
CHEMBL2087333 84282 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 484 7 2 7 2.4 COC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
11432106 84284 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 504 8 2 7 1.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)S(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087335 84284 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 504 8 2 7 1.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)S(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
71462777 89740 0 None - 1 Human 8.0 pEC50 = 8 Functional
Inverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activationInverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activation
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181171 89740 0 None - 1 Human 8.0 pEC50 = 8 Functional
Inverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activationInverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activation
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3ncccc23)CC1 10.1021/jm300943r
130946 209537 2 None - 1 Rat 8.0 pEC50 = 8 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 328 2 1 5 2.0 CCn1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1016/S0960-894X(01)81243-9
CHEMBL62023 209537 2 None - 1 Rat 8.0 pEC50 = 8 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 328 2 1 5 2.0 CCn1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1016/S0960-894X(01)81243-9
5 6927 72 None -138 27 Human 7.0 pEC50 = 7 Functional
Activity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assayActivity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1038/nature05991
5202 6927 72 None -138 27 Human 7.0 pEC50 = 7 Functional
Activity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assayActivity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1038/nature05991
CHEMBL39 6927 72 None -138 27 Human 7.0 pEC50 = 7 Functional
Activity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assayActivity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1038/nature05991
DB08839 6927 72 None -138 27 Human 7.0 pEC50 = 7 Functional
Activity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assayActivity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1038/nature05991
44249186 202095 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 327 4 2 4 2.3 CC(C)n1c(=O)c(C(=O)NCC2CCNCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL551535 202095 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 327 4 2 4 2.3 CC(C)n1c(=O)c(C(=O)NCC2CCNCC2)cc2ccccc21 10.1021/jm900881j
15231247 91900477 202431 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 309 3 3 4 1.9 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C[C@@H]2CC[C@H](C1)N2 10.1021/jm900881j
CHEMBL556438 202431 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 309 3 3 4 1.9 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C[C@@H]2CC[C@H](C1)N2 10.1021/jm900881j
44249053 203280 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 394 6 2 5 2.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2CCCCC2)CC1 10.1021/jm900881j
CHEMBL563445 203280 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 394 6 2 5 2.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2CCCCC2)CC1 10.1021/jm900881j
10545215 195761 0 None - 1 Guinea pig 7.0 pEC50 = 7 Functional
concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum.concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum.
ChEMBL 341 5 2 5 3.4 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCCCC1 10.1021/jm960853v
CHEMBL50852 195761 0 None - 1 Guinea pig 7.0 pEC50 = 7 Functional
concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum.concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum.
ChEMBL 341 5 2 5 3.4 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCCCC1 10.1021/jm960853v
44247949 201893 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 475 12 3 6 3.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCS(=O)(=O)O)CC1 10.1021/jm900881j
CHEMBL549998 201893 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 475 12 3 6 3.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCS(=O)(=O)O)CC1 10.1021/jm900881j
127037817 143386 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 382 5 1 5 2.5 CC(C)c1nc(C(=O)NC2C3CN(CC4CCOCC4)CC32)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3739689 143386 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 382 5 1 5 2.5 CC(C)c1nc(C(=O)NC2C3CN(CC4CCOCC4)CC32)c2ccccn12 10.1016/j.ejmech.2015.08.051
127041480 143405 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 384 5 1 5 3.1 CC(C)c1nc(C(=O)NCC2CCN(C3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3739862 143405 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 384 5 1 5 3.1 CC(C)c1nc(C(=O)NCC2CCN(C3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
44323264 213891 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 322 2 1 5 2.1 Nc1c(Cl)cc(C(=O)O[C@@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL92100 213891 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 322 2 1 5 2.1 Nc1c(Cl)cc(C(=O)O[C@@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
44281492 125650 2 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 298 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OC1CCN(C)CC1 10.1016/S0960-894X(01)80508-4
CHEMBL34224 125650 2 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 298 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OC1CCN(C)CC1 10.1016/S0960-894X(01)80508-4
10757374 169871 0 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
CHEMBL41769 169871 0 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
10757374 169871 0 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1021/jm960320m
CHEMBL41769 169871 0 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1021/jm960320m
10018558 57525 0 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 314 5 1 6 1.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCOCC1 10.1021/jm960320m
CHEMBL157631 57525 0 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 314 5 1 6 1.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCOCC1 10.1021/jm960320m
5 6927 72 None -138 27 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801327q
5202 6927 72 None -138 27 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801327q
CHEMBL39 6927 72 None -138 27 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801327q
DB08839 6927 72 None -138 27 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801327q
3037881 106521 1 None - 1 Rat 7.9 pEC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 355 1 1 4 2.8 Nc1c(Cl)cc2c3c(cccc13)C(=O)N([C@@H]1CN3CCC1CC3)C2=O 10.1016/S0960-894X(00)80352-2
CHEMBL28499 106521 1 None - 1 Rat 7.9 pEC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 355 1 1 4 2.8 Nc1c(Cl)cc2c3c(cccc13)C(=O)N([C@@H]1CN3CCC1CC3)C2=O 10.1016/S0960-894X(00)80352-2
19081885 212123 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 338 7 1 4 4.0 CCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80413-3
CHEMBL79637 212123 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 338 7 1 4 4.0 CCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80413-3
257 10266 13 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1021/jm100668r
5311423 10266 13 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1021/jm100668r
CHEMBL114112 10266 13 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1021/jm100668r
11842633 10753 21 None -7 2 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contractionAgonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contraction
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 10753 21 None -7 2 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contractionAgonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contraction
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 10753 21 None -7 2 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contractionAgonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contraction
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
70684288 83195 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 558 11 1 7 3.5 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059586 83195 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 558 11 1 7 3.5 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
44248793 91900478 202402 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 339 3 2 4 2.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)cc2ccccc21 10.1021/jm900881j
CHEMBL556235 202402 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 339 3 2 4 2.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)cc2ccccc21 10.1021/jm900881j
44248068 202664 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 515 10 2 7 1.9 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
CHEMBL558924 202664 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 515 10 2 7 1.9 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
44247817 91900489 202754 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 489 9 2 6 3.4 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
CHEMBL559746 202754 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 489 9 2 6 3.4 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
67276147 84274 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 468 7 2 6 2.1 CC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
CHEMBL2087325 84274 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 468 7 2 6 2.1 CC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
70695322 84277 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 469 7 4 6 1.6 CNC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
CHEMBL2087328 84277 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 469 7 4 6 1.6 CNC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
131725 207216 3 None 3 2 Rat 7.9 pEC50 = 7.9 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 342 2 1 5 2.6 CC(C)n1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1016/S0960-894X(01)81243-9
CHEMBL59834 207216 3 None 3 2 Rat 7.9 pEC50 = 7.9 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 342 2 1 5 2.6 CC(C)n1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1016/S0960-894X(01)81243-9
44626295 204553 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
ChEMBL 531 8 3 7 3.8 COc1cccc([C@]2(O)CCCC[C@H]2CN2CC[C@@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@@H](OC)C2)c1 10.1016/j.bmcl.2009.08.016
CHEMBL571799 204553 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
ChEMBL 531 8 3 7 3.8 COc1cccc([C@]2(O)CCCC[C@H]2CN2CC[C@@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@@H](OC)C2)c1 10.1016/j.bmcl.2009.08.016
44461665 111325 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 325 6 2 4 2.5 COc1cc(N)c(Cl)cc1C(=O)NCCCN1CCCCC1 10.1016/S0960-894X(01)80413-3
CHEMBL310451 111325 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 325 6 2 4 2.5 COc1cc(N)c(Cl)cc1C(=O)NCCCN1CCCCC1 10.1016/S0960-894X(01)80413-3
9882676 212539 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 296 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCNCC1 10.1016/S0960-894X(01)80413-3
CHEMBL82833 212539 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 296 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCNCC1 10.1016/S0960-894X(01)80413-3
11496400 18580 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 338 4 2 3 2.3 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CC[N@@+]2(C)CCC[C@@H]12 10.1021/jm0509501
CHEMBL1181946 18580 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 338 4 2 3 2.3 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CC[N@@+]2(C)CCC[C@@H]12 10.1021/jm0509501
CHEMBL199866 18580 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 338 4 2 3 2.3 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CC[N@@+]2(C)CCC[C@@H]12 10.1021/jm0509501
10690483 56074 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 369 6 2 6 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(C)=O)CC1 10.1021/jm960320m
CHEMBL156348 56074 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 369 6 2 6 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(C)=O)CC1 10.1021/jm960320m
127039820 143556 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 366 6 1 4 3.2 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC4CCC4)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741224 143556 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 366 6 1 4 3.2 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC4CCC4)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
127039507 143648 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 360 5 1 4 3.4 CC(C)c1nc(C(=O)NC2CCN(CC(C)(C)F)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3742086 143648 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 360 5 1 4 3.4 CC(C)c1nc(C(=O)NC2CCN(CC(C)(C)F)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
127041780 143455 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 416 6 1 5 3.4 CC(C)c1nc(C(=O)NCC2(F)CCN(CC3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3740278 143455 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 416 6 1 5 3.4 CC(C)c1nc(C(=O)NCC2(F)CCN(CC3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
44323269 18844 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
CHEMBL1183709 18844 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
CHEMBL314198 18844 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
9905514 126460 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(O)CC1 10.1021/jm960320m
CHEMBL347235 126460 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(O)CC1 10.1021/jm960320m
49783209 24381 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 24381 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
127042086 143496 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 400 5 2 6 2.2 CC(C)c1nc(C(=O)NC2CCN(CC3(O)CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3740708 143496 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 400 5 2 6 2.2 CC(C)c1nc(C(=O)NC2CCN(CC3(O)CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
127042083 143661 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 344 6 1 5 2.3 COCCN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
CHEMBL3742190 143661 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 344 6 1 5 2.3 COCCN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
10381762 56077 0 None - 1 Guinea pig 7.8 pEC50 = 7.8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 326 5 1 5 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(C)C1 10.1021/jm960320m
CHEMBL156349 56077 0 None - 1 Guinea pig 7.8 pEC50 = 7.8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 326 5 1 5 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(C)C1 10.1021/jm960320m
127041784 143623 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 354 5 1 4 3.5 CC(C)c1nc(C(=O)NC2CCN(CC3CCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741826 143623 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 354 5 1 4 3.5 CC(C)c1nc(C(=O)NC2CCN(CC3CCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
19081860 212478 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 324 6 1 4 3.6 CCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80413-3
CHEMBL82360 212478 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 324 6 1 4 3.6 CCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80413-3
49783212 24448 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 387 7 1 7 3.0 CCCCN1CCC(COC(=O)c2cc(C#N)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258450 24448 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 387 7 1 7 3.0 CCCCN1CCC(COC(=O)c2cc(C#N)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
44249316 91900479 202131 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 328 2 2 5 2.2 CC(C)n1c(=O)n(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1021/jm900881j
CHEMBL551820 202131 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 328 2 2 5 2.2 CC(C)n1c(=O)n(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1021/jm900881j
44247811 202250 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 369 8 3 5 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCO)CC1 10.1021/jm900881j
CHEMBL552693 202250 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 369 8 3 5 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCO)CC1 10.1021/jm900881j
44247813 202371 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 411 11 3 5 3.5 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCO)CC1 10.1021/jm900881j
CHEMBL555447 202371 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 411 11 3 5 3.5 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCO)CC1 10.1021/jm900881j
44248072 202454 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 483 9 3 5 3.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
CHEMBL556595 202454 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 483 9 3 5 3.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
44249057 91900485 202878 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 467 11 2 5 4.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCO)cc2ccccc21 10.1021/jm900881j
CHEMBL560876 202878 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 467 11 2 5 4.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCO)cc2ccccc21 10.1021/jm900881j
44249188 202891 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 316 3 2 5 1.9 CC(C)n1c(=O)n(C(=O)NCC2CCNCC2)c2ccccc21 10.1021/jm900881j
CHEMBL560940 202891 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 316 3 2 5 1.9 CC(C)n1c(=O)n(C(=O)NCC2CCNCC2)c2ccccc21 10.1021/jm900881j
10828800 106965 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
CHEMBL288199 106965 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
10828800 106965 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1021/jm960320m
CHEMBL288199 106965 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1021/jm960320m
44249311 202105 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 313 3 2 4 2.1 CC(C)n1c(=O)c(C(=O)NC2CCNCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL551614 202105 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 313 3 2 4 2.1 CC(C)n1c(=O)c(C(=O)NC2CCNCC2)cc2ccccc21 10.1021/jm900881j
44247945 202849 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 391 6 3 6 1.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCS(=O)(=O)O)CC1 10.1021/jm900881j
CHEMBL560597 202849 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 391 6 3 6 1.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCS(=O)(=O)O)CC1 10.1021/jm900881j
132337 10316 15 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm0509501
238 10316 15 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm0509501
CHEMBL34291 10316 15 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm0509501
44308599 210479 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 349 5 2 4 2.4 COc1cc(N)c(Cl)cc1C(=O)NCCC12CC3CN(CC3C1)C2 10.1016/S0960-894X(97)00408-3
CHEMBL67554 210479 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 349 5 2 4 2.4 COc1cc(N)c(Cl)cc1C(=O)NCCC12CC3CN(CC3C1)C2 10.1016/S0960-894X(97)00408-3
9819593 105580 3 None 3 2 Guinea pig 6.8 pEC50 = 6.8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 10.1021/jm960320m
CHEMBL27846 105580 3 None 3 2 Guinea pig 6.8 pEC50 = 6.8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 10.1021/jm960320m
10548275 55285 0 None - 1 Guinea pig 7.8 pEC50 = 7.8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 307 5 1 4 2.1 COc1cc(N)c(Cl)cc1C(=O)OCC[n+]1ccccc1 10.1021/jm960320m
CHEMBL155631 55285 0 None - 1 Guinea pig 7.8 pEC50 = 7.8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 307 5 1 4 2.1 COc1cc(N)c(Cl)cc1C(=O)OCC[n+]1ccccc1 10.1021/jm960320m
54677674 119586 4 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5HT4e receptor expressed in African green monkey COS7 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at recombinant human 5HT4e receptor expressed in African green monkey COS7 cells assessed as cAMP level after 30 mins by HTRF assay
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1016/j.ejmech.2015.08.051
CHEMBL3291085 119586 4 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5HT4e receptor expressed in African green monkey COS7 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at recombinant human 5HT4e receptor expressed in African green monkey COS7 cells assessed as cAMP level after 30 mins by HTRF assay
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1016/j.ejmech.2015.08.051
CHEMBL3306918 119586 4 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5HT4e receptor expressed in African green monkey COS7 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at recombinant human 5HT4e receptor expressed in African green monkey COS7 cells assessed as cAMP level after 30 mins by HTRF assay
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1016/j.ejmech.2015.08.051
5 6927 72 None -29 27 Rat 7.8 pEC50 = 7.8 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(96)00002-9
5202 6927 72 None -29 27 Rat 7.8 pEC50 = 7.8 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(96)00002-9
CHEMBL39 6927 72 None -29 27 Rat 7.8 pEC50 = 7.8 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(96)00002-9
DB08839 6927 72 None -29 27 Rat 7.8 pEC50 = 7.8 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(96)00002-9
42618248 193807 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 479 8 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)Cc2ccccc2Cl)CC1 10.1021/jm801327q
CHEMBL490852 193807 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 479 8 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)Cc2ccccc2Cl)CC1 10.1021/jm801327q
127039821 143412 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 352 5 1 4 2.9 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(C4CCC4)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3739931 143412 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 352 5 1 4 2.9 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(C4CCC4)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
127039374 143597 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 372 6 1 4 3.1 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC(C)(C)F)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741595 143597 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 372 6 1 4 3.1 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC(C)(C)F)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
127039822 143511 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 340 5 1 4 2.8 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(C(C)C)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3740844 143511 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 340 5 1 4 2.8 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(C(C)C)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
9905225 213723 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 321 2 2 4 1.7 Nc1c(Cl)cc(C(=O)N[C@@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL91147 213723 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 321 2 2 4 1.7 Nc1c(Cl)cc(C(=O)N[C@@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
10802184 60932 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 272 5 1 5 1.6 COc1cc(N)c(Cl)cc1C(=O)OCCN(C)C 10.1021/jm960320m
CHEMBL160705 60932 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 272 5 1 5 1.6 COc1cc(N)c(Cl)cc1C(=O)OCCN(C)C 10.1021/jm960320m
10570203 56326 0 None - 1 Guinea pig 7.7 pEC50 = 7.7 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 355 6 2 6 1.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(N)=O)CC1 10.1021/jm960320m
CHEMBL156554 56326 0 None - 1 Guinea pig 7.7 pEC50 = 7.7 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 355 6 2 6 1.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(N)=O)CC1 10.1021/jm960320m
9927789 118279 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 337 5 2 4 2.5 Nc1c(Cl)cc(C(=O)NCCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL327798 118279 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 337 5 2 4 2.5 Nc1c(Cl)cc(C(=O)NCCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
127037820 143630 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 398 8 1 5 3.0 COCC(C)(C)CN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2015.08.051
CHEMBL3741918 143630 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 398 8 1 5 3.0 COCC(C)(C)CN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2015.08.051
235 9342 42 None -5 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80413-3
5311299 9342 42 None -5 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80413-3
CHEMBL286136 9342 42 None -5 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80413-3
132337 10316 15 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1016/S0960-894X(01)80413-3
238 10316 15 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1016/S0960-894X(01)80413-3
CHEMBL34291 10316 15 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1016/S0960-894X(01)80413-3
49783211 24412 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 488 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(I)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258339 24412 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 488 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(I)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
5311047 211542 33 None 1 2 Human 7.7 pEC50 = 7.7 Functional
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 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.bmcl.2012.05.034
CHEMBL74656 211542 33 None 1 2 Human 7.7 pEC50 = 7.7 Functional
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 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.bmcl.2012.05.034
44248312 91900490 201909 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 531 12 2 6 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
CHEMBL550122 201909 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 531 12 2 6 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
44248066 201965 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 473 7 2 7 0.7 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
CHEMBL550530 201965 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 473 7 2 7 0.7 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
70691118 84276 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 469 7 3 6 1.7 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)C(N)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087327 84276 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 469 7 3 6 1.7 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)C(N)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
70686943 84280 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 497 7 2 6 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)C(=O)N(C)C)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087331 84280 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 497 7 2 6 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)C(=O)N(C)C)cc2ccccc21 10.1016/j.bmcl.2012.08.051
1782 9296 84 None -93 13 Rat 5.7 pEC50 = 5.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(96)00002-9
241 9296 84 None -93 13 Rat 5.7 pEC50 = 5.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(96)00002-9
4168 9296 84 None -93 13 Rat 5.7 pEC50 = 5.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(96)00002-9
CHEMBL86 9296 84 None -93 13 Rat 5.7 pEC50 = 5.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(96)00002-9
DB01233 9296 84 None -93 13 Rat 5.7 pEC50 = 5.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(96)00002-9
11493794 79805 0 None 26 2 Rat 6.7 pEC50 = 6.7 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 337 5 2 4 2.5 CCOc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN2CCC[C@@H]12 10.1021/jm0509501
CHEMBL201019 79805 0 None 26 2 Rat 6.7 pEC50 = 6.7 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 337 5 2 4 2.5 CCOc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN2CCC[C@@H]12 10.1021/jm0509501
132164 213427 12 None - 1 Rat 6.7 pEC50 = 6.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 321 2 2 4 1.7 Nc1c(Cl)cc(C(=O)N[C@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL89259 213427 12 None - 1 Rat 6.7 pEC50 = 6.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 321 2 2 4 1.7 Nc1c(Cl)cc(C(=O)N[C@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
127039508 143607 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 402 5 1 5 3.2 CC(C)c1nc(C(=O)NC2CCN(CC3(F)CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741703 143607 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 402 5 1 5 3.2 CC(C)c1nc(C(=O)NC2CCN(CC3(F)CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
10493462 209266 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 286 3 2 4 2.1 CC(C)n1nc(C(=O)NC2CCNCC2)c2ccccc21 10.1021/jm900881j
CHEMBL61130 209266 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 286 3 2 4 2.1 CC(C)n1nc(C(=O)NC2CCNCC2)c2ccccc21 10.1021/jm900881j
19081864 111731 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Compound was tested against 5-HT4 receptor through agonism of 5-HT mediated relaxation of rat, carbachol contracted esophageal muscularis mucosaeCompound was tested against 5-HT4 receptor through agonism of 5-HT mediated relaxation of rat, carbachol contracted esophageal muscularis mucosae
ChEMBL 352 9 1 4 4.6 CCCOc1cc(N)c(Cl)cc1C(=O)CCCCN1CCCCC1 10.1016/S0960-894X(01)80414-5
CHEMBL311325 111731 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Compound was tested against 5-HT4 receptor through agonism of 5-HT mediated relaxation of rat, carbachol contracted esophageal muscularis mucosaeCompound was tested against 5-HT4 receptor through agonism of 5-HT mediated relaxation of rat, carbachol contracted esophageal muscularis mucosae
ChEMBL 352 9 1 4 4.6 CCCOc1cc(N)c(Cl)cc1C(=O)CCCCN1CCCCC1 10.1016/S0960-894X(01)80414-5
183782 10171 20 None 3 3 Human 8.7 pEC50 = 8.7 Functional
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 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2015.08.051
237 10171 20 None 3 3 Human 8.7 pEC50 = 8.7 Functional
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 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2015.08.051
CHEMBL85251 10171 20 None 3 3 Human 8.7 pEC50 = 8.7 Functional
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 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2015.08.051
44213662 213376 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 324 4 1 5 2.5 Nc1c(Cl)cc(C(=O)OCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL88973 213376 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 324 4 1 5 2.5 Nc1c(Cl)cc(C(=O)OCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
71451950 89450 8 None -1 2 Rat 8.7 pEC50 = 8.7 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None -1 2 Rat 8.7 pEC50 = 8.7 Functional
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 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
235 9342 42 None -5 4 Human 8.6 pEC50 = 8.6 Functional
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 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/j.ejmech.2015.08.051
5311299 9342 42 None -5 4 Human 8.6 pEC50 = 8.6 Functional
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 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/j.ejmech.2015.08.051
CHEMBL286136 9342 42 None -5 4 Human 8.6 pEC50 = 8.6 Functional
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 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/j.ejmech.2015.08.051
133076 10172 6 None -1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 417 9 2 6 2.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CCNS(=O)(=O)C)Cl 10.1016/S0960-894X(01)80413-3
3230 10172 6 None -1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 417 9 2 6 2.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CCNS(=O)(=O)C)Cl 10.1016/S0960-894X(01)80413-3
CHEMBL83899 10172 6 None -1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 417 9 2 6 2.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CCNS(=O)(=O)C)Cl 10.1016/S0960-894X(01)80413-3
70696825 83187 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 479 10 1 5 5.4 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCCCC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059578 83187 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 479 10 1 5 5.4 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCCCC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
11677434 83190 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 483 9 2 7 2.8 COC[C@@H]1CCCN1CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
CHEMBL2059581 83190 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 483 9 2 7 2.8 COC[C@@H]1CCCN1CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
11225102 83199 3 None 1 2 Human 8.6 pEC50 = 8.6 Functional
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 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.05.034
CHEMBL2059590 83199 3 None 1 2 Human 8.6 pEC50 = 8.6 Functional
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 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.05.034
44248191 201678 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 537 8 1 7 3.5 CCOC(=O)N1CCN(CCCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cc4ccccc4n(C(C)C)c2=O)C3)CC1 10.1021/jm900881j
CHEMBL540980 201678 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 537 8 1 7 3.5 CCOC(=O)N1CCN(CCCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cc4ccccc4n(C(C)C)c2=O)C3)CC1 10.1021/jm900881j
44248195 201861 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 466 7 1 6 3.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCOCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL549650 201861 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 466 7 1 6 3.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCOCC2)cc2ccccc21 10.1021/jm900881j
44248679 202378 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 599 12 1 7 3.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL555693 202378 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 599 12 1 7 3.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44248315 202700 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 522 11 1 6 4.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCOCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL559322 202700 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 522 11 1 6 4.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCOCC2)cc2ccccc21 10.1021/jm900881j
135409453 10545 41 None 3 36 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2013.05.018
226 10545 41 None 3 36 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2013.05.018
CHEMBL76370 10545 41 None 3 36 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2013.05.018
135409453 10545 41 None 3 36 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.08.051
226 10545 41 None 3 36 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.08.051
CHEMBL76370 10545 41 None 3 36 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.08.051
155543353 180080 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assayPartial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assay
ChEMBL 418 7 3 6 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccc(O)c(O)c2)CC1 10.1016/j.ejmech.2019.111596
CHEMBL4526049 180080 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assayPartial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assay
ChEMBL 418 7 3 6 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccc(O)c(O)c2)CC1 10.1016/j.ejmech.2019.111596
127037818 143472 2 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT4A receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assayAgonist activity at human 5-HT4A receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assay
ChEMBL 370 8 1 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2015.08.051
CHEMBL3740472 143472 2 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT4A receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assayAgonist activity at human 5-HT4A receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assay
ChEMBL 370 8 1 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2015.08.051
127037818 143472 2 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT4D receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assayAgonist activity at human 5-HT4D receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assay
ChEMBL 370 8 1 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2015.08.051
CHEMBL3740472 143472 2 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT4D receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assayAgonist activity at human 5-HT4D receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assay
ChEMBL 370 8 1 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2015.08.051
127037818 143472 2 None 1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat 5-HT4L receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assayAgonist activity at rat 5-HT4L receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assay
ChEMBL 370 8 1 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2015.08.051
CHEMBL3740472 143472 2 None 1 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat 5-HT4L receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assayAgonist activity at rat 5-HT4L receptor assessed as cAMP level after 4 hrs by luciferase reporter gene assay
ChEMBL 370 8 1 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2015.08.051
127039823 143485 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 382 5 1 5 2.5 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(C4CCOCC4)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3740612 143485 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 382 5 1 5 2.5 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(C4CCOCC4)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
10567201 191044 0 None - 1 Guinea pig 6.7 pEC50 = 6.7 Functional
concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.
ChEMBL 313 5 2 5 2.6 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCC1 10.1021/jm960853v
CHEMBL48379 191044 0 None - 1 Guinea pig 6.7 pEC50 = 6.7 Functional
concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.
ChEMBL 313 5 2 5 2.6 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCC1 10.1021/jm960853v
6604914 107160 3 None -1 2 Rat 6.7 pEC50 = 6.7 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/S0960-894X(00)80441-2
CHEMBL28992 107160 3 None -1 2 Rat 6.7 pEC50 = 6.7 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/S0960-894X(00)80441-2
9819119 210480 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 335 4 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NCC12CC3CN(CC3C1)C2 10.1016/S0960-894X(97)00408-3
CHEMBL67555 210480 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 335 4 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NCC12CC3CN(CC3C1)C2 10.1016/S0960-894X(97)00408-3
44281102 123493 0 None - 1 Guinea pig 7.7 pEC50 = 7.7 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 312 4 1 5 2.6 CCN1CCC(OC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80508-4
CHEMBL33732 123493 0 None - 1 Guinea pig 7.7 pEC50 = 7.7 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 312 4 1 5 2.6 CCN1CCC(OC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80508-4
127037818 143472 2 None -1 2 Human 7.7 pEC50 = 7.7 Functional
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 370 8 1 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2015.08.051
CHEMBL3740472 143472 2 None -1 2 Human 7.7 pEC50 = 7.7 Functional
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 370 8 1 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2015.08.051
127039819 143675 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 356 5 1 5 2.4 CC(C)c1nc(C(=O)NCC2CN(C3CCC3)CCO2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3742300 143675 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 356 5 1 5 2.4 CC(C)c1nc(C(=O)NCC2CN(C3CCC3)CCO2)c2ccccn12 10.1016/j.ejmech.2015.08.051
132337 10316 15 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Compound was tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assayCompound was tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1016/j.bmcl.2004.04.021
238 10316 15 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Compound was tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assayCompound was tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1016/j.bmcl.2004.04.021
CHEMBL34291 10316 15 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Compound was tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assayCompound was tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1016/j.bmcl.2004.04.021
132337 10316 15 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Efficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosaeEfficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm020099f
238 10316 15 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Efficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosaeEfficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm020099f
CHEMBL34291 10316 15 None -1 2 Rat 7.6 pEC50 = 7.6 Functional
Efficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosaeEfficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm020099f
127039510 143498 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 370 5 1 5 2.7 CC(C)c1nc(C(=O)NC2CCN(CC3CCOC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3740732 143498 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 370 5 1 5 2.7 CC(C)c1nc(C(=O)NC2CCN(CC3CCOC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
44248797 202491 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 353 7 2 4 3.3 CCCCCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
CHEMBL557053 202491 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 353 7 2 4 3.3 CCCCCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
44248552 91900486 202698 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 554 9 1 6 4.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
CHEMBL559317 202698 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 554 9 1 6 4.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
10574402 91900484 203251 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 425 8 2 5 3.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCO)cc2ccccc21 10.1021/jm900881j
CHEMBL563261 203251 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 425 8 2 5 3.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCO)cc2ccccc21 10.1021/jm900881j
70695323 84285 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 504 8 2 7 1.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@H](O)CN(C)S(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087336 84285 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 504 8 2 7 1.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@H](O)CN(C)S(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
71450247 89751 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activationInverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activation
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181188 89751 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activationInverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activation
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
203435 170883 3 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 311 5 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCCCC1 10.1016/S0960-894X(01)80413-3
CHEMBL420969 170883 3 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 311 5 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCCCC1 10.1016/S0960-894X(01)80413-3
71712612 98153 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 490 7 3 7 0.2 CS(=O)(=O)N1CCN(CC(O)CN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cccc4[nH]cnc24)C3)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402888 98153 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 490 7 3 7 0.2 CS(=O)(=O)N1CCN(CC(O)CN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cccc4[nH]cnc24)C3)CC1 10.1016/j.bmcl.2013.05.018
44249317 91900480 202120 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 299 3 3 3 2.2 COc1ccc2[nH]cc(C(=O)N[C@@H]3C[C@@H]4CC[C@H](C3)N4)c2c1 10.1021/jm900881j
CHEMBL551743 202120 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 299 3 3 3 2.2 COc1ccc2[nH]cc(C(=O)N[C@@H]3C[C@@H]4CC[C@H](C3)N4)c2c1 10.1021/jm900881j
243 9976 91 None -1 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.ejmech.2015.08.051
3052762 9976 91 None -1 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.ejmech.2015.08.051
3502 9976 91 None -1 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.ejmech.2015.08.051
CHEMBL117287 9976 91 None -1 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.ejmech.2015.08.051
DB06480 9976 91 None -1 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.ejmech.2015.08.051
108182 10903 22 None - 1 Guinea pig 6.6 pEC50 = 6.6 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1016/S0960-894X(01)80508-4
245 10903 22 None - 1 Guinea pig 6.6 pEC50 = 6.6 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1016/S0960-894X(01)80508-4
CHEMBL18041 10903 22 None - 1 Guinea pig 6.6 pEC50 = 6.6 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1016/S0960-894X(01)80508-4
44288600 107894 0 None -1 2 Rat 6.6 pEC50 = 6.6 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2 10.1016/S0960-894X(00)80441-2
CHEMBL295155 107894 0 None -1 2 Rat 6.6 pEC50 = 6.6 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2 10.1016/S0960-894X(00)80441-2
14403199 123388 0 None - 1 Guinea pig 7.6 pEC50 = 7.6 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 324 3 1 5 2.7 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC(C1)N2C 10.1016/S0960-894X(01)80508-4
CHEMBL33676 123388 0 None - 1 Guinea pig 7.6 pEC50 = 7.6 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 324 3 1 5 2.7 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC(C1)N2C 10.1016/S0960-894X(01)80508-4
14403199 123388 0 None - 1 Guinea pig 7.6 pEC50 = 7.6 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 324 3 1 5 2.7 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC(C1)N2C 10.1021/jm960320m
CHEMBL33676 123388 0 None - 1 Guinea pig 7.6 pEC50 = 7.6 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 324 3 1 5 2.7 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC(C1)N2C 10.1021/jm960320m
10757373 56361 0 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 310 5 1 5 2.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC=CCC1 10.1021/jm960320m
CHEMBL156579 56361 0 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 310 5 1 5 2.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC=CCC1 10.1021/jm960320m
3019427 67156 33 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
ChEMBL 313 4 3 5 1.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCNCC1OC 10.1016/j.bmcl.2009.08.016
CHEMBL1748 67156 33 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
ChEMBL 313 4 3 5 1.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCNCC1OC 10.1016/j.bmcl.2009.08.016
9973684 58248 0 None - 1 Guinea pig 8.5 pEC50 = 8.5 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 326 5 1 5 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C)CC1 10.1021/jm960320m
CHEMBL158238 58248 0 None - 1 Guinea pig 8.5 pEC50 = 8.5 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 326 5 1 5 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C)CC1 10.1021/jm960320m
44248193 201588 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 593 12 1 7 5.0 CCOC(=O)N1CCN(CCCCCCCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cc4ccccc4n(C(C)C)c2=O)C3)CC1 10.1021/jm900881j
CHEMBL538956 201588 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 593 12 1 7 5.0 CCOC(=O)N1CCN(CCCCCCCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cc4ccccc4n(C(C)C)c2=O)C3)CC1 10.1021/jm900881j
44248434 91900496 202418 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 613 13 1 7 4.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL556326 202418 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 613 13 1 7 4.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44247943 202727 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 540 12 2 6 4.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
CHEMBL559548 202727 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 540 12 2 6 4.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
44249183 203159 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 478 12 2 5 5.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2CCCCC2)CC1 10.1021/jm900881j
CHEMBL562636 203159 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 478 12 2 5 5.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2CCCCC2)CC1 10.1021/jm900881j
71714543 98158 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 534 8 3 7 1.2 CC(C)(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402893 98158 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 534 8 3 7 1.2 CC(C)(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
71712329 98164 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 454 7 2 5 2.3 CC(=O)N1CCN(CCN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402899 98164 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 454 7 2 5 2.3 CC(=O)N1CCN(CCN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
127041783 143366 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 328 4 1 4 3.1 CC(C)c1nc(C(=O)NC2CCN(C(C)C)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3739521 143366 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 328 4 1 4 3.1 CC(C)c1nc(C(=O)NC2CCN(C(C)C)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
127039509 143519 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 332 5 1 4 2.6 CC(C)c1nc(C(=O)NC2CCN(CCF)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3740908 143519 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 332 5 1 4 2.6 CC(C)c1nc(C(=O)NC2CCN(CCF)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
183782 10171 20 None 3 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/S0960-894X(01)80413-3
237 10171 20 None 3 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/S0960-894X(01)80413-3
CHEMBL85251 10171 20 None 3 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/S0960-894X(01)80413-3
11168006 83198 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 502 7 1 7 1.9 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059589 83198 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 502 7 1 7 1.9 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
44248080 91900498 202655 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 493 8 2 6 2.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCC[C@@H]2C(N)=O)cc2ccccc21 10.1021/jm900881j
CHEMBL558855 202655 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 493 8 2 6 2.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCC[C@@H]2C(N)=O)cc2ccccc21 10.1021/jm900881j
182593 10168 6 None 1 2 Guinea pig 7.5 pEC50 = 7.5 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1021/jm960320m
254 10168 6 None 1 2 Guinea pig 7.5 pEC50 = 7.5 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1021/jm960320m
CHEMBL83954 10168 6 None 1 2 Guinea pig 7.5 pEC50 = 7.5 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1021/jm960320m
10615288 193788 0 None - 1 Guinea pig 6.5 pEC50 = 6.5 Functional
concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.
ChEMBL 315 7 2 5 2.8 CCN(CC)CCOC(=O)Nc1cc(Cl)c(N)cc1OC 10.1021/jm960853v
CHEMBL49072 193788 0 None - 1 Guinea pig 6.5 pEC50 = 6.5 Functional
concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.
ChEMBL 315 7 2 5 2.8 CCN(CC)CCOC(=O)Nc1cc(Cl)c(N)cc1OC 10.1021/jm960853v
127039824 143379 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 396 6 1 5 2.8 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC4CCOCC4)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3739647 143379 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 396 6 1 5 2.8 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC4CCOCC4)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
10315431 105726 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 343 1 1 4 2.8 CN1CCC(N2C(=O)c3cccc4c(N)c(Cl)cc(c34)C2=O)CC1 10.1016/S0960-894X(00)80352-2
CHEMBL27966 105726 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 343 1 1 4 2.8 CN1CCC(N2C(=O)c3cccc4c(N)c(Cl)cc(c34)C2=O)CC1 10.1016/S0960-894X(00)80352-2
44249055 91900481 202198 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 367 4 1 4 3.3 CCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
CHEMBL552218 202198 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 367 4 1 4 3.3 CCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
10643698 202231 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 383 5 2 5 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCO)cc2ccccc21 10.1021/jm900881j
CHEMBL552420 202231 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 383 5 2 5 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCO)cc2ccccc21 10.1021/jm900881j
70682705 84278 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 483 7 3 6 1.9 CNC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
CHEMBL2087329 84278 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 483 7 3 6 1.9 CNC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
127041781 143427 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 388 8 2 6 2.1 COCCCN1CCC(O)(CNC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
CHEMBL3740030 143427 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 388 8 2 6 2.1 COCCCN1CCC(O)(CNC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
10828801 110946 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 310 6 1 4 3.4 COc1cc(N)c(Cl)cc1C(=O)CCCN1CCCCC1 10.1016/S0960-894X(01)80413-3
CHEMBL309655 110946 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 310 6 1 4 3.4 COc1cc(N)c(Cl)cc1C(=O)CCCN1CCCCC1 10.1016/S0960-894X(01)80413-3
44248794 202291 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 302 2 2 5 1.7 CC(C)n1c(=O)n(C(=O)NC2CCNCC2)c2ccccc21 10.1021/jm900881j
CHEMBL553658 202291 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 302 2 2 5 1.7 CC(C)n1c(=O)n(C(=O)NC2CCNCC2)c2ccccc21 10.1021/jm900881j
15095973 143046 0 None 12 2 Rat 6.5 pEC50 = 6.5 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN2CCC[C@H]12 10.1021/jm0509501
CHEMBL37333 143046 0 None 12 2 Rat 6.5 pEC50 = 6.5 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN2CCC[C@H]12 10.1021/jm0509501
22400452 109161 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 363 4 2 4 2.1 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC1C2CC3CC1CN3C2 10.1016/S0960-894X(97)00408-3
CHEMBL303877 109161 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 363 4 2 4 2.1 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC1C2CC3CC1CN3C2 10.1016/S0960-894X(97)00408-3
127037821 143574 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 370 6 2 5 2.1 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC(C)(C)O)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741377 143574 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 370 6 2 5 2.1 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC(C)(C)O)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
44213663 213360 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 323 4 2 4 2.1 Nc1c(Cl)cc(C(=O)NCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL88867 213360 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 323 4 2 4 2.1 Nc1c(Cl)cc(C(=O)NCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
11596009 80149 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 342 3 1 5 2.4 CC(C)n1c(=O)n(C(=O)NC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21 10.1021/jm0509501
CHEMBL201414 80149 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 342 3 1 5 2.4 CC(C)n1c(=O)n(C(=O)NC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21 10.1021/jm0509501
9861932 210355 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 321 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN3C2 10.1016/S0960-894X(97)00408-3
CHEMBL66768 210355 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 321 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN3C2 10.1016/S0960-894X(97)00408-3
44323245 113801 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 322 2 1 5 2.1 Nc1c(Cl)cc(C(=O)O[C@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL315443 113801 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 322 2 1 5 2.1 Nc1c(Cl)cc(C(=O)O[C@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
73352662 100015 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1C2CC3CN(C2)CC31 10.1016/S0960-894X(00)80441-2
CHEMBL2448137 100015 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1C2CC3CN(C2)CC31 10.1016/S0960-894X(00)80441-2
127042089 143402 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 384 5 2 5 3.0 CC(C)c1nc(C(=O)NC2CC3CCC(C2)N3CC(C)(C)O)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3739826 143402 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 384 5 2 5 3.0 CC(C)c1nc(C(=O)NC2CC3CCC(C2)N3CC(C)(C)O)c2ccccn12 10.1016/j.ejmech.2015.08.051
19081862 212173 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 310 5 1 4 3.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(C)CC1 10.1016/S0960-894X(01)80413-3
CHEMBL80015 212173 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 310 5 1 4 3.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(C)CC1 10.1016/S0960-894X(01)80413-3
9799010 212660 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 324 7 1 4 3.8 COc1cc(N)c(Cl)cc1C(=O)CCCCN1CCCCC1 10.1016/S0960-894X(01)80413-3
CHEMBL83841 212660 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 324 7 1 4 3.8 COc1cc(N)c(Cl)cc1C(=O)CCCCN1CCCCC1 10.1016/S0960-894X(01)80413-3
10757502 91929739 201904 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 312 3 2 4 2.6 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL550064 201904 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 312 3 2 4 2.6 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1016/j.bmcl.2012.05.034
10757502 91929739 201904 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 312 3 2 4 2.6 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1021/jm900881j
CHEMBL550064 201904 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 312 3 2 4 2.6 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1021/jm900881j
44247808 202158 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 395 10 2 4 4.5 CCCCCCCCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
CHEMBL551940 202158 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 395 10 2 4 4.5 CCCCCCCCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
44248187 91900482 202159 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 409 7 1 4 4.5 CCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
CHEMBL551941 202159 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 409 7 1 4 4.5 CCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
44248070 202603 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 557 13 2 7 3.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
CHEMBL558261 202603 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 557 13 2 7 3.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
44249056 91900483 203116 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 451 10 1 4 5.7 CCCCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
CHEMBL562400 203116 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 451 10 1 4 5.7 CCCCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
9799010 212660 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Compound was tested against 5-HT4 receptor through agonism of 5-HT mediated relaxation of rat, carbachol contracted esophageal muscularis mucosaeCompound was tested against 5-HT4 receptor through agonism of 5-HT mediated relaxation of rat, carbachol contracted esophageal muscularis mucosae
ChEMBL 324 7 1 4 3.8 COc1cc(N)c(Cl)cc1C(=O)CCCCN1CCCCC1 10.1016/S0960-894X(01)80414-5
CHEMBL83841 212660 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Compound was tested against 5-HT4 receptor through agonism of 5-HT mediated relaxation of rat, carbachol contracted esophageal muscularis mucosaeCompound was tested against 5-HT4 receptor through agonism of 5-HT mediated relaxation of rat, carbachol contracted esophageal muscularis mucosae
ChEMBL 324 7 1 4 3.8 COc1cc(N)c(Cl)cc1C(=O)CCCCN1CCCCC1 10.1016/S0960-894X(01)80414-5
9817713 201616 61 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 297 4 3 4 1.7 COc1cc(N)c(Cl)cc1C(=O)NCC1CCNCC1 10.1021/jm900881j
CHEMBL539652 201616 61 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 297 4 3 4 1.7 COc1cc(N)c(Cl)cc1C(=O)NCC1CCNCC1 10.1021/jm900881j
42499 201716 23 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 283 3 3 4 1.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCNCC1 10.1021/jm900881j
CHEMBL541969 201716 23 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 283 3 3 4 1.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCNCC1 10.1021/jm900881j
44247947 202112 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 433 9 3 6 2.2 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCS(=O)(=O)O)CC1 10.1021/jm900881j
CHEMBL551678 202112 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 433 9 3 6 2.2 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCS(=O)(=O)O)CC1 10.1021/jm900881j
235 9342 42 None -1 4 Guinea pig 8.4 pEC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80508-4
5311299 9342 42 None -1 4 Guinea pig 8.4 pEC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80508-4
CHEMBL286136 9342 42 None -1 4 Guinea pig 8.4 pEC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80508-4
235 9342 42 None -1 4 Guinea pig 8.4 pEC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm960320m
5311299 9342 42 None -1 4 Guinea pig 8.4 pEC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm960320m
CHEMBL286136 9342 42 None -1 4 Guinea pig 8.4 pEC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm960320m
15295138 57836 0 None - 1 Guinea pig 8.4 pEC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
CHEMBL157880 57836 0 None - 1 Guinea pig 8.4 pEC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
44582815 180007 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 621 11 3 9 3.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCN2C(=O)c3cccc4c(N)ccc(c34)C2=O)CC1 10.1021/jm801327q
CHEMBL452353 180007 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 621 11 3 9 3.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCN2C(=O)c3cccc4c(N)ccc(c34)C2=O)CC1 10.1021/jm801327q
9973683 126585 0 None - 1 Guinea pig 8.4 pEC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 326 5 1 5 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCCCC1 10.1021/jm960320m
CHEMBL348311 126585 0 None - 1 Guinea pig 8.4 pEC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 326 5 1 5 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCCCC1 10.1021/jm960320m
22708808 213842 0 None - 1 Rat 8.4 pEC50 = 8.4 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 365 6 2 4 3.1 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)c3c2OCC3)CC1 10.1016/0960-894X(96)00002-9
CHEMBL91771 213842 0 None - 1 Rat 8.4 pEC50 = 8.4 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 365 6 2 4 3.1 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)c3c2OCC3)CC1 10.1016/0960-894X(96)00002-9
155525723 177864 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assayPartial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assay
ChEMBL 515 11 3 7 4.2 COc1cc(/C=C/C(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)ccc1O 10.1016/j.ejmech.2019.111596
CHEMBL4457426 177864 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assayPartial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assay
ChEMBL 515 11 3 7 4.2 COc1cc(/C=C/C(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)ccc1O 10.1016/j.ejmech.2019.111596
127041479 143622 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 372 8 1 5 2.9 COCCCN1CCC(CNC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
CHEMBL3741821 143622 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 372 8 1 5 2.9 COCCCN1CCC(CNC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
44371317 56837 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 338 5 1 5 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1C2CCCC1CC2 10.1021/jm960320m
CHEMBL156965 56837 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 338 5 1 5 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1C2CCCC1CC2 10.1021/jm960320m
10447437 56840 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 298 5 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC1 10.1021/jm960320m
CHEMBL156970 56840 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 298 5 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC1 10.1021/jm960320m
127038726 143375 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 358 5 2 5 2.4 CC(C)c1nc(C(=O)NC2CCN(CC(C)(C)O)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3739611 143375 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 358 5 2 5 2.4 CC(C)c1nc(C(=O)NC2CCN(CC(C)(C)O)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
127042084 143617 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 358 7 1 5 2.7 COCCCN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
CHEMBL3741776 143617 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 358 7 1 5 2.7 COCCCN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
44343153 117124 0 None 1 2 Rat 7.4 pEC50 = 7.4 Functional
Efficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosaeEfficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosae
ChEMBL 356 2 1 5 3.0 CC(C)n1c(=O)n(C(=O)NC2CC3CCCC(C2)N3C)c2ccccc21 10.1021/jm020099f
CHEMBL324057 117124 0 None 1 2 Rat 7.4 pEC50 = 7.4 Functional
Efficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosaeEfficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosae
ChEMBL 356 2 1 5 3.0 CC(C)n1c(=O)n(C(=O)NC2CC3CCCC(C2)N3C)c2ccccc21 10.1021/jm020099f
22400445 210873 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 335 4 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN3C2 10.1016/S0960-894X(97)00408-3
CHEMBL70205 210873 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 335 4 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN3C2 10.1016/S0960-894X(97)00408-3
131725 207216 3 None -3 2 Guinea pig 7.4 pEC50 = 7.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 342 2 1 5 2.6 CC(C)n1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1021/jm960320m
CHEMBL59834 207216 3 None -3 2 Guinea pig 7.4 pEC50 = 7.4 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 342 2 1 5 2.6 CC(C)n1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1021/jm960320m
44281491 119251 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 312 4 1 5 2.6 CCN1CCCC(OC(=O)c2cc(Cl)c(N)cc2OC)C1 10.1016/S0960-894X(01)80508-4
CHEMBL32986 119251 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 312 4 1 5 2.6 CCN1CCCC(OC(=O)c2cc(Cl)c(N)cc2OC)C1 10.1016/S0960-894X(01)80508-4
10065690 114204 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Compound was tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assayCompound was tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay
ChEMBL 337 4 2 4 2.5 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN2CCC[C@@]12C 10.1016/j.bmcl.2004.04.021
CHEMBL318154 114204 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Compound was tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assayCompound was tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay
ChEMBL 337 4 2 4 2.5 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN2CCC[C@@]12C 10.1016/j.bmcl.2004.04.021
127042087 143586 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 386 5 1 6 2.1 CC(C)c1nc(C(=O)NCC2CN(C3CCOCC3)CCO2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741508 143586 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 386 5 1 6 2.1 CC(C)c1nc(C(=O)NCC2CN(C3CCOCC3)CCO2)c2ccccn12 10.1016/j.ejmech.2015.08.051
127038354 143413 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 386 7 1 5 3.3 COCC(C)(C)CN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
CHEMBL3739933 143413 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 386 7 1 5 3.3 COCC(C)(C)CN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
127041786 143359 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 340 5 1 4 3.1 CC(C)c1nc(C(=O)NC2CCN(CC3CC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3739470 143359 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 340 5 1 4 3.1 CC(C)c1nc(C(=O)NC2CCN(CC3CC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
127042085 143565 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 370 4 1 5 2.8 CC(C)c1nc(C(=O)NC2CCN(C3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741322 143565 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 370 4 1 5 2.8 CC(C)c1nc(C(=O)NC2CCN(C3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
5 6927 72 None -13 27 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(01)80508-4
5202 6927 72 None -13 27 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(01)80508-4
CHEMBL39 6927 72 None -13 27 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(01)80508-4
DB08839 6927 72 None -13 27 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(01)80508-4
5 6927 72 None -13 27 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960320m
5202 6927 72 None -13 27 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960320m
CHEMBL39 6927 72 None -13 27 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960320m
DB08839 6927 72 None -13 27 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960320m
15295138 57836 0 None - 1 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
CHEMBL157880 57836 0 None - 1 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
70688534 83188 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 441 8 2 6 3.0 CC(C)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
CHEMBL2059579 83188 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 441 8 2 6 3.0 CC(C)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
70696826 83189 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 467 11 1 5 5.2 CC(C)N(C)CCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
CHEMBL2059580 83189 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 467 11 1 5 5.2 CC(C)N(C)CCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
44247941 202567 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 498 9 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
CHEMBL557867 202567 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 498 9 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
44248925 203199 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 436 9 2 5 3.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2CCCCC2)CC1 10.1021/jm900881j
CHEMBL562902 203199 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 436 9 2 5 3.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2CCCCC2)CC1 10.1021/jm900881j
11842633 10753 21 None 7 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
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 10753 21 None 7 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
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 10753 21 None 7 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
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
70695321 84275 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 455 7 4 6 1.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNC(N)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087326 84275 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 455 7 4 6 1.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNC(N)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
243 9976 91 None 1 5 Human 8.3 pEC50 = 8.3 Functional
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 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.ejmech.2015.08.051
3052762 9976 91 None 1 5 Human 8.3 pEC50 = 8.3 Functional
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 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.ejmech.2015.08.051
3502 9976 91 None 1 5 Human 8.3 pEC50 = 8.3 Functional
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 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.ejmech.2015.08.051
CHEMBL117287 9976 91 None 1 5 Human 8.3 pEC50 = 8.3 Functional
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 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.ejmech.2015.08.051
DB06480 9976 91 None 1 5 Human 8.3 pEC50 = 8.3 Functional
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 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.ejmech.2015.08.051
10764565 55787 0 None - 1 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 339 5 1 4 2.7 COc1cc(N)c(Cl)cc1C(=O)OCC[N+]12CCC(CC1)CC2 10.1021/jm960320m
CHEMBL156088 55787 0 None - 1 Guinea pig 8.3 pEC50 = 8.3 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 339 5 1 4 2.7 COc1cc(N)c(Cl)cc1C(=O)OCC[N+]12CCC(CC1)CC2 10.1021/jm960320m
1782 9296 84 None -2 13 Guinea pig 8.2 pEC50 = 8.2 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960320m
241 9296 84 None -2 13 Guinea pig 8.2 pEC50 = 8.2 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960320m
4168 9296 84 None -2 13 Guinea pig 8.2 pEC50 = 8.2 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960320m
CHEMBL86 9296 84 None -2 13 Guinea pig 8.2 pEC50 = 8.2 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960320m
DB01233 9296 84 None -2 13 Guinea pig 8.2 pEC50 = 8.2 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960320m
127042670 143590 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 384 7 2 5 2.4 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC(C)(C)CO)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741548 143590 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 384 7 2 5 2.4 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC(C)(C)CO)C[C@H]23)c2ccccn12 10.1016/j.ejmech.2015.08.051
49783419 24521 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258671 24521 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
127041785 143468 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 314 4 1 4 2.7 CCN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
CHEMBL3740400 143468 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 314 4 1 4 2.7 CCN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
44248311 91900487 202409 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 596 12 1 6 5.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
CHEMBL556279 202409 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 596 12 1 6 5.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
127039505 143461 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 353 4 0 6 4.1 CC(C)c1nc(-c2nnc(C3CCN(C(C)C)CC3)o2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3740313 143461 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 353 4 0 6 4.1 CC(C)c1nc(-c2nnc(C3CCN(C(C)C)CC3)o2)c2ccccn12 10.1016/j.ejmech.2015.08.051
9819593 105580 3 None -3 2 Rat 6.3 pEC50 = 6.3 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 10.1016/S0960-894X(00)80352-2
CHEMBL27846 105580 3 None -3 2 Rat 6.3 pEC50 = 6.3 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 10.1016/S0960-894X(00)80352-2
44249179 201602 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 312 5 3 5 0.6 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCNCC1 10.1021/jm900881j
CHEMBL539212 201602 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 312 5 3 5 0.6 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCNCC1 10.1021/jm900881j
9906777 100019 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C2CC3CN(C2)CC31 10.1021/jm0509501
CHEMBL2448165 100019 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C2CC3CN(C2)CC31 10.1021/jm0509501
9885123 114992 1 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CN(C2)CC31 10.1016/S0960-894X(97)00408-3
CHEMBL319673 114992 1 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CN(C2)CC31 10.1016/S0960-894X(97)00408-3
CHEMBL558226 114992 1 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CN(C2)CC31 10.1016/S0960-894X(97)00408-3
235 9342 42 None -5 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm801327q
5311299 9342 42 None -5 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm801327q
CHEMBL286136 9342 42 None -5 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm801327q
9906777 100019 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C2CC3CN(C2)CC31 10.1016/S0960-894X(00)80441-2
CHEMBL2448165 100019 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C2CC3CN(C2)CC31 10.1016/S0960-894X(00)80441-2
127039503 143356 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 379 5 0 6 4.5 CC(C)c1nc(-c2nnc(C3CCN(CC4CCC4)CC3)o2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3739455 143356 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 379 5 0 6 4.5 CC(C)c1nc(-c2nnc(C3CCN(CC4CCC4)CC3)o2)c2ccccn12 10.1016/j.ejmech.2015.08.051
127039169 143538 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 412 6 1 5 3.7 CC(C)c1nc(C(=O)NCC2(C)CCN(CC3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741062 143538 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 412 6 1 5 3.7 CC(C)c1nc(C(=O)NCC2(C)CCN(CC3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
44288600 107894 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2 10.1016/S0960-894X(00)80441-2
CHEMBL295155 107894 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2 10.1016/S0960-894X(00)80441-2
240 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
2769 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
44279790 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
660 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
CHEMBL1729 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
CHEMBL560739 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
DB00604 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
240 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/S0960-894X(00)80441-2
2769 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/S0960-894X(00)80441-2
44279790 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/S0960-894X(00)80441-2
660 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/S0960-894X(00)80441-2
CHEMBL1729 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/S0960-894X(00)80441-2
CHEMBL560739 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/S0960-894X(00)80441-2
DB00604 7731 43 None -10 23 Rat 7.3 pEC50 = 7.3 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/S0960-894X(00)80441-2
6604914 107160 3 None -1 2 Rat 7.3 pEC50 = 7.3 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/0960-894X(96)00002-9
CHEMBL28992 107160 3 None -1 2 Rat 7.3 pEC50 = 7.3 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/0960-894X(96)00002-9
127041782 143357 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 414 6 2 6 2.4 CC(C)c1nc(C(=O)NCC2(O)CCN(CC3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3739459 143357 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 414 6 2 6 2.4 CC(C)c1nc(C(=O)NCC2(O)CCN(CC3CCOCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
54677674 119586 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1016/j.ejmech.2015.08.051
CHEMBL3291085 119586 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1016/j.ejmech.2015.08.051
CHEMBL3306918 119586 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1016/j.ejmech.2015.08.051
10449091 126743 0 None - 1 Guinea pig 8.2 pEC50 = 8.2 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 326 5 1 5 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCCC1C 10.1021/jm960320m
CHEMBL349809 126743 0 None - 1 Guinea pig 8.2 pEC50 = 8.2 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 326 5 1 5 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCCC1C 10.1021/jm960320m
71460941 89456 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 374 8 0 5 5.1 CCCCN1CCC(COc2noc3cccc(OCC(C)(C)C)c23)CC1 10.1021/jm300953p
CHEMBL2179588 89456 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 374 8 0 5 5.1 CCCCN1CCC(COc2noc3cccc(OCC(C)(C)C)c23)CC1 10.1021/jm300953p
5 6927 72 None -29 27 Rat 8.2 pEC50 = 8.2 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(00)80352-2
5202 6927 72 None -29 27 Rat 8.2 pEC50 = 8.2 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(00)80352-2
CHEMBL39 6927 72 None -29 27 Rat 8.2 pEC50 = 8.2 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(00)80352-2
DB08839 6927 72 None -29 27 Rat 8.2 pEC50 = 8.2 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(00)80352-2
135409453 10545 41 None -3 36 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contractionAgonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contraction
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
226 10545 41 None -3 36 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contractionAgonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contraction
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
CHEMBL76370 10545 41 None -3 36 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contractionAgonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contraction
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
135409453 10545 41 None -3 36 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contractionAgonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contraction
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.08.051
226 10545 41 None -3 36 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contractionAgonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contraction
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.08.051
CHEMBL76370 10545 41 None -3 36 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contractionAgonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contraction
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.08.051
44249189 91900488 202181 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 447 6 2 6 2.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
CHEMBL552075 202181 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 447 6 2 6 2.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
44248433 91900494 203520 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 529 7 1 7 1.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL565146 203520 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 529 7 1 7 1.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
67276466 84273 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 454 7 3 6 1.8 CC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
CHEMBL2087324 84273 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 454 7 3 6 1.8 CC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
10569278 194029 0 None - 1 Guinea pig 7.2 pEC50 = 7.2 Functional
concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.
ChEMBL 341 5 2 5 3.2 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCC(C)CC1 10.1021/jm960853v
CHEMBL49266 194029 0 None - 1 Guinea pig 7.2 pEC50 = 7.2 Functional
concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.concentration which gave a 50% increase in the response to electrical stimulation against 5-hydroxytryptamine 4 receptor in the guinea pig ileum. Activity expressed as percent of the maximum 5-HT response given in brackets.
ChEMBL 341 5 2 5 3.2 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCC(C)CC1 10.1021/jm960853v
6604914 107160 3 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/S0960-894X(00)80352-2
CHEMBL28992 107160 3 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/S0960-894X(00)80352-2
19081962 113636 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 380 10 1 4 5.2 CCCCCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80413-3
CHEMBL314489 113636 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 380 10 1 4 5.2 CCCCCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80413-3
20030109 203130 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 327 5 3 5 1.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCO)CC1 10.1021/jm900881j
CHEMBL562477 203130 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 327 5 3 5 1.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCO)CC1 10.1021/jm900881j
71461050 89752 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activationInverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activation
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181189 89752 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activationInverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activation
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1021/jm300943r
44374544 59927 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCC1C2 10.1016/S0960-894X(01)81243-9
CHEMBL159825 59927 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCC1C2 10.1016/S0960-894X(01)81243-9
44247815 203254 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 456 6 2 6 2.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
CHEMBL563276 203254 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 456 6 2 6 2.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
71712613 98154 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 464 7 3 7 -0.3 CS(=O)(=O)N1CCN(CC(O)CN2CCC(NC(=O)c3cccc4[nH]cnc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402889 98154 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 464 7 3 7 -0.3 CS(=O)(=O)N1CCN(CC(O)CN2CCC(NC(=O)c3cccc4[nH]cnc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
44248795 204410 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 287 4 3 3 1.9 COc1ccc2[nH]cc(C(=O)NCC3CCNCC3)c2c1 10.1021/jm900881j
CHEMBL570780 204410 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 287 4 3 3 1.9 COc1ccc2[nH]cc(C(=O)NCC3CCNCC3)c2c1 10.1021/jm900881j
127041779 143515 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 390 8 1 5 3.0 COCCCN1CCC(F)(CNC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
CHEMBL3740864 143515 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 390 8 1 5 3.0 COCCCN1CCC(F)(CNC(=O)c2nc(C(C)C)n3ccccc23)CC1 10.1016/j.ejmech.2015.08.051
132337 10316 15 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay of racemate mixtureTested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay of racemate mixture
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1016/j.bmcl.2004.04.021
238 10316 15 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay of racemate mixtureTested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay of racemate mixture
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1016/j.bmcl.2004.04.021
CHEMBL34291 10316 15 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay of racemate mixtureTested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay of racemate mixture
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1016/j.bmcl.2004.04.021
22400445 210873 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 335 4 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN3C2 10.1016/S0960-894X(97)00408-3
CHEMBL70205 210873 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 335 4 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN3C2 10.1016/S0960-894X(97)00408-3
42618252 193459 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 580 13 3 8 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm801327q
CHEMBL488325 193459 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 580 13 3 8 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm801327q
44213661 213856 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 338 5 1 5 2.9 Nc1c(Cl)cc(C(=O)OCCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL91842 213856 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 338 5 1 5 2.9 Nc1c(Cl)cc(C(=O)OCCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
10498232 58140 0 None - 1 Guinea pig 8.1 pEC50 = 8.1 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 352 5 1 5 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC2CCC(CC2)C1 10.1021/jm960320m
CHEMBL158147 58140 0 None - 1 Guinea pig 8.1 pEC50 = 8.1 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 352 5 1 5 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC2CCC(CC2)C1 10.1021/jm960320m
44248437 201615 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 597 12 1 6 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCN(c3ccccc3)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL539651 201615 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 597 12 1 6 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCN(c3ccccc3)CC2)cc2ccccc21 10.1021/jm900881j
44249315 201954 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 331 4 2 6 0.8 CC(C)n1c(=O)n(C(=O)NCCN2CCNCC2)c2ccccc21 10.1021/jm900881j
CHEMBL550459 201954 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 331 4 2 6 0.8 CC(C)n1c(=O)n(C(=O)NCCN2CCNCC2)c2ccccc21 10.1021/jm900881j
67276168 84283 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 490 8 3 7 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNS(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087334 84283 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
ChEMBL 490 8 3 7 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNS(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
9861932 210355 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 321 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN3C2 10.1016/S0960-894X(97)00408-3
CHEMBL66768 210355 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assayAgonist activity against serotonin 5-HT4 receptor in rat tunica muscularis mucosae assay
ChEMBL 321 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN3C2 10.1016/S0960-894X(97)00408-3
127039168 143658 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 388 6 3 6 1.8 CC(C)c1nc(C(=O)NCC2(O)CCN(CC(C)(C)O)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3742145 143658 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 388 6 3 6 1.8 CC(C)c1nc(C(=O)NCC2(O)CCN(CC(C)(C)O)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
127039506 143358 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3nc(C(C)C)n4ccccc34)o2)CC1 10.1016/j.ejmech.2015.08.051
CHEMBL3739467 143358 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3nc(C(C)C)n4ccccc34)o2)CC1 10.1016/j.ejmech.2015.08.051
6604914 107160 3 None 1 2 Guinea pig 7.1 pEC50 = 7.1 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1021/jm960320m
CHEMBL28992 107160 3 None 1 2 Guinea pig 7.1 pEC50 = 7.1 Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1021/jm960320m
71461049 89750 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activationInverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activation
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3c(OC)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181187 89750 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activationInverse agonist activity at human recombinant 5HT4R expressed in HEK293T cells assessed as Gs activation
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3c(OC)cccc3c3ccccc23)CC1 10.1021/jm300943r
44248310 203335 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 512 6 1 6 3.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
CHEMBL563799 203335 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 512 6 1 6 3.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
44575 204295 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 311 4 2 4 2.1 CCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
CHEMBL570074 204295 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 311 4 2 4 2.1 CCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
240 7731 43 None 1 23 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
2769 7731 43 None 1 23 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
44279790 7731 43 None 1 23 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
660 7731 43 None 1 23 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL1729 7731 43 None 1 23 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL560739 7731 43 None 1 23 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
DB00604 7731 43 None 1 23 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
5311047 211542 33 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
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.bmcl.2012.08.051
CHEMBL74656 211542 33 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMPAgonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP
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.bmcl.2012.08.051
1782 9296 84 None -1 13 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80413-3
241 9296 84 None -1 13 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80413-3
4168 9296 84 None -1 13 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80413-3
CHEMBL86 9296 84 None -1 13 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80413-3
DB01233 9296 84 None -1 13 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80413-3
1782 9296 84 None -93 13 Rat 6.1 pEC50 = 6.1 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)81243-9
241 9296 84 None -93 13 Rat 6.1 pEC50 = 6.1 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)81243-9
4168 9296 84 None -93 13 Rat 6.1 pEC50 = 6.1 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)81243-9
CHEMBL86 9296 84 None -93 13 Rat 6.1 pEC50 = 6.1 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)81243-9
DB01233 9296 84 None -93 13 Rat 6.1 pEC50 = 6.1 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)81243-9
44323244 19157 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
CHEMBL1185621 19157 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
CHEMBL423504 19157 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
127037819 143491 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 453 6 1 6 2.8 COC(=O)N1CCC(CN2C[C@H]3[C@H](CNC(=O)c4nc(C(C)C)n5ccccc45)[C@H]3C2)CC1 10.1016/j.ejmech.2015.08.051
CHEMBL3740669 143491 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 453 6 1 6 2.8 COC(=O)N1CCC(CN2C[C@H]3[C@H](CNC(=O)c4nc(C(C)C)n5ccccc45)[C@H]3C2)CC1 10.1016/j.ejmech.2015.08.051
49783207 24350 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 362 7 1 6 3.2 CCCCN1CCC(COC(=O)c2ccc(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258109 24350 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 362 7 1 6 3.2 CCCCN1CCC(COC(=O)c2ccc(NC)c3c2OCCO3)CC1 10.1021/jm100668r
127039170 143551 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 365 4 0 6 4.2 CC(C)c1nc(-c2nnc(C3CCN(C4CCC4)CC3)o2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741199 143551 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 365 4 0 6 4.2 CC(C)c1nc(-c2nnc(C3CCN(C4CCC4)CC3)o2)c2ccccn12 10.1016/j.ejmech.2015.08.051
127039504 143423 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 365 5 0 6 4.1 CC(C)c1nc(-c2nnc(C3CCN(CC4CC4)CC3)o2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3740000 143423 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 365 5 0 6 4.1 CC(C)c1nc(-c2nnc(C3CCN(CC4CC4)CC3)o2)c2ccccn12 10.1016/j.ejmech.2015.08.051
127042088 143647 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 426 5 2 6 2.7 CC(C)c1nc(C(=O)NC2CC3CCC(C2)N3CC2(O)CCOCC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3742080 143647 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 426 5 2 6 2.7 CC(C)c1nc(C(=O)NC2CC3CCC(C2)N3CC2(O)CCOCC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
42618250 176240 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 982 28 6 14 5.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCNCCCc2ccc(CCCNCCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)cc2)CC1 10.1021/jm801327q
CHEMBL442869 176240 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HTAgonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
ChEMBL 982 28 6 14 5.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCNCCCc2ccc(CCCNCCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)cc2)CC1 10.1021/jm801327q
44372468 18447 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 380 6 2 3 3.5 CCCC[N+]12CCCC(C1)C(NC(=O)c1cc(Cl)c(N)cc1OC)CC2 10.1016/S0960-894X(01)81243-9
CHEMBL1181147 18447 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 380 6 2 3 3.5 CCCC[N+]12CCCC(C1)C(NC(=O)c1cc(Cl)c(N)cc1OC)CC2 10.1016/S0960-894X(01)81243-9
CHEMBL156977 18447 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 380 6 2 3 3.5 CCCC[N+]12CCCC(C1)C(NC(=O)c1cc(Cl)c(N)cc1OC)CC2 10.1016/S0960-894X(01)81243-9
127039825 143619 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 439 5 1 6 2.6 COC(=O)N1CCC(N2C[C@H]3[C@H](CNC(=O)c4nc(C(C)C)n5ccccc45)[C@H]3C2)CC1 10.1016/j.ejmech.2015.08.051
CHEMBL3741787 143619 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 439 5 1 6 2.6 COC(=O)N1CCC(N2C[C@H]3[C@H](CNC(=O)c4nc(C(C)C)n5ccccc45)[C@H]3C2)CC1 10.1016/j.ejmech.2015.08.051
439280 126797 107 None -13 9 Rat 8.0 pEC50 = 8.0 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1016/S0960-894X(01)81243-9
6971044 126797 107 None -13 9 Rat 8.0 pEC50 = 8.0 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1016/S0960-894X(01)81243-9
CHEMBL350221 126797 107 None -13 9 Rat 8.0 pEC50 = 8.0 Functional
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosaeTested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1016/S0960-894X(01)81243-9
127041481 143611 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 354 5 1 4 3.5 CC(C)c1nc(C(=O)NCC2CCN(C3CCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
CHEMBL3741733 143611 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 354 5 1 4 3.5 CC(C)c1nc(C(=O)NCC2CCN(C3CCC3)CC2)c2ccccn12 10.1016/j.ejmech.2015.08.051
44626294 205778 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
ChEMBL 517 7 4 7 3.5 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(C[C@@H]2CCCC[C@@]2(O)c2cccc(O)c2)C[C@H]1OC 10.1016/j.bmcl.2009.08.016
CHEMBL585567 205778 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
ChEMBL 517 7 4 7 3.5 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(C[C@@H]2CCCC[C@@]2(O)c2cccc(O)c2)C[C@H]1OC 10.1016/j.bmcl.2009.08.016
6917985 100028 9 None 64 2 Rat 7.0 pEC50 = 7.0 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 323 3 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN2CCC[C@@H]1C2 10.1021/jm0509501
CHEMBL2448558 100028 9 None 64 2 Rat 7.0 pEC50 = 7.0 Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 323 3 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN2CCC[C@@H]1C2 10.1021/jm0509501
44374544 59927 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCC1C2 10.1016/S0960-894X(00)80441-2
CHEMBL159825 59927 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assayCompound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCC1C2 10.1016/S0960-894X(00)80441-2
121881 10263 27 None 281 3 Guinea pig 10.0 pIC50 = 10 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1021/jm00077a018
256 10263 27 None 281 3 Guinea pig 10.0 pIC50 = 10 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1021/jm00077a018
CHEMBL68131 10263 27 None 281 3 Guinea pig 10.0 pIC50 = 10 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1021/jm00077a018
119376 8622 48 None 61 4 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levelsAntagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm300573d
247 8622 48 None 61 4 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levelsAntagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm300573d
CHEMBL33884 8622 48 None 61 4 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levelsAntagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm300573d
10066755 122038 1 None - 1 Guinea pig 9.0 pIC50 = 9 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 354 7 1 5 3.6 CCCCN1CCC(COC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm00077a018
CHEMBL334818 122038 1 None - 1 Guinea pig 9.0 pIC50 = 9 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 354 7 1 5 3.6 CCCCN1CCC(COC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm00077a018
9998229 27367 0 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 353 7 2 4 3.2 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm00077a018
CHEMBL130809 27367 0 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 353 7 2 4 3.2 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm00077a018
10408029 23232 0 None - 1 Guinea pig 7.0 pIC50 = 7 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm960320m
CHEMBL123377 23232 0 None - 1 Guinea pig 7.0 pIC50 = 7 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm960320m
10788092 60362 0 None - 1 Guinea pig 7.0 pIC50 = 7 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 416 7 1 6 3.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)c2ccccc2)CC1 10.1021/jm960320m
CHEMBL160237 60362 0 None - 1 Guinea pig 7.0 pIC50 = 7 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 416 7 1 6 3.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)c2ccccc2)CC1 10.1021/jm960320m
10615288 193788 0 None - 1 Guinea pig 6.0 pIC50 = 6 Functional
The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.
ChEMBL 315 7 2 5 2.8 CCN(CC)CCOC(=O)Nc1cc(Cl)c(N)cc1OC 10.1021/jm960853v
CHEMBL49072 193788 0 None - 1 Guinea pig 6.0 pIC50 = 6 Functional
The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.
ChEMBL 315 7 2 5 2.8 CCN(CC)CCOC(=O)Nc1cc(Cl)c(N)cc1OC 10.1021/jm960853v
249 9343 4 None - 1 Guinea pig 8.0 pIC50 = 8.0 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
9905972 9343 4 None - 1 Guinea pig 8.0 pIC50 = 8.0 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
CHEMBL155917 9343 4 None - 1 Guinea pig 8.0 pIC50 = 8.0 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
119376 8622 48 None -61 4 Guinea pig 7.9 pIC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm960320m
247 8622 48 None -61 4 Guinea pig 7.9 pIC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm960320m
CHEMBL33884 8622 48 None -61 4 Guinea pig 7.9 pIC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm960320m
249 9343 4 None - 1 Guinea pig 7.9 pIC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
9905972 9343 4 None - 1 Guinea pig 7.9 pIC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
CHEMBL155917 9343 4 None - 1 Guinea pig 7.9 pIC50 = 7.9 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
10854687 55330 0 None - 1 Guinea pig 6.8 pIC50 = 6.8 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 340 5 1 5 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(C)(C)C1 10.1021/jm960320m
CHEMBL155682 55330 0 None - 1 Guinea pig 6.8 pIC50 = 6.8 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 340 5 1 5 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(C)(C)C1 10.1021/jm960320m
10522209 108473 0 None - 1 Guinea pig 6.8 pIC50 = 6.8 Functional
The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.
ChEMBL 355 5 2 5 3.5 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CC(C)CC(C)C1 10.1021/jm960853v
CHEMBL299408 108473 0 None - 1 Guinea pig 6.8 pIC50 = 6.8 Functional
The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.
ChEMBL 355 5 2 5 3.5 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CC(C)CC(C)C1 10.1021/jm960853v
235 9342 42 None 1 4 Rat 8.6 pIC50 = 8.6 Functional
5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80508-4
5311299 9342 42 None 1 4 Rat 8.6 pIC50 = 8.6 Functional
5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80508-4
CHEMBL286136 9342 42 None 1 4 Rat 8.6 pIC50 = 8.6 Functional
5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80508-4
44628198 89498 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levelsAntagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels
ChEMBL 443 7 1 5 4.8 Cn1cc2c(OCC3CCN(CCc4ccc(C(=O)O)cc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2179674 89498 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levelsAntagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels
ChEMBL 443 7 1 5 4.8 Cn1cc2c(OCC3CCN(CCc4ccc(C(=O)O)cc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
10447437 56840 0 None - 1 Guinea pig 6.7 pIC50 = 6.7 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 298 5 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC1 10.1021/jm960320m
CHEMBL156970 56840 0 None - 1 Guinea pig 6.7 pIC50 = 6.7 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 298 5 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC1 10.1021/jm960320m
10569278 194029 0 None - 1 Guinea pig 6.7 pIC50 = 6.7 Functional
The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.
ChEMBL 341 5 2 5 3.2 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCC(C)CC1 10.1021/jm960853v
CHEMBL49266 194029 0 None - 1 Guinea pig 6.7 pIC50 = 6.7 Functional
The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum.
ChEMBL 341 5 2 5 3.2 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCC(C)CC1 10.1021/jm960853v
10545215 195761 0 None - 1 Guinea pig 6.7 pIC50 = 6.7 Functional
The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum. 95% confidence limits are in brackets.The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum. 95% confidence limits are in brackets.
ChEMBL 341 5 2 5 3.4 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCCCC1 10.1021/jm960853v
CHEMBL50852 195761 0 None - 1 Guinea pig 6.7 pIC50 = 6.7 Functional
The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum. 95% confidence limits are in brackets.The antagonist activity was calculated as the concentration which produced a 50% reduction against 5-hydroxytryptamine 4 receptor in guinea pig ileum. 95% confidence limits are in brackets.
ChEMBL 341 5 2 5 3.4 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCCCC1 10.1021/jm960853v
258 10340 31 None 2 3 Guinea pig 6.6 pIC50 = 6.6 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm00077a018
5191 10340 31 None 2 3 Guinea pig 6.6 pIC50 = 6.6 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm00077a018
CHEMBL287045 10340 31 None 2 3 Guinea pig 6.6 pIC50 = 6.6 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm00077a018
5 6927 72 None -29 27 Rat 8.4 pIC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(01)80508-4
5202 6927 72 None -29 27 Rat 8.4 pIC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(01)80508-4
CHEMBL39 6927 72 None -29 27 Rat 8.4 pIC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(01)80508-4
DB08839 6927 72 None -29 27 Rat 8.4 pIC50 = 8.4 Functional
5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/S0960-894X(01)80508-4
10757374 169871 0 None - 1 Guinea pig 7.5 pIC50 = 7.5 Functional
5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
CHEMBL41769 169871 0 None - 1 Guinea pig 7.5 pIC50 = 7.5 Functional
5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
10757374 169871 0 None - 1 Guinea pig 7.5 pIC50 = 7.5 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1021/jm960320m
CHEMBL41769 169871 0 None - 1 Guinea pig 7.5 pIC50 = 7.5 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1021/jm960320m
44371350 126946 0 None - 1 Guinea pig 6.5 pIC50 = 6.5 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 342 5 1 6 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC(C)OC(C)C1 10.1021/jm960320m
CHEMBL351570 126946 0 None - 1 Guinea pig 6.5 pIC50 = 6.5 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 342 5 1 6 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC(C)OC(C)C1 10.1021/jm960320m
260 10641 54 None 3 9 Guinea pig 5.5 pIC50 = 5.5 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1021/jm00077a018
2775 10641 54 None 3 9 Guinea pig 5.5 pIC50 = 5.5 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1021/jm00077a018
656665 10641 54 None 3 9 Guinea pig 5.5 pIC50 = 5.5 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1021/jm00077a018
CHEMBL56564 10641 54 None 3 9 Guinea pig 5.5 pIC50 = 5.5 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1021/jm00077a018
DB11699 10641 54 None 3 9 Guinea pig 5.5 pIC50 = 5.5 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1021/jm00077a018
10828800 106965 0 None - 1 Guinea pig 6.4 pIC50 = 6.4 Functional
5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
CHEMBL288199 106965 0 None - 1 Guinea pig 6.4 pIC50 = 6.4 Functional
5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
10828800 106965 0 None - 1 Guinea pig 6.4 pIC50 = 6.4 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1021/jm960320m
CHEMBL288199 106965 0 None - 1 Guinea pig 6.4 pIC50 = 6.4 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1021/jm960320m
10020607 26510 0 None - 1 Guinea pig 7.3 pIC50 = 7.3 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 347 6 0 5 3.5 CCCCN1CCC(COC(=O)c2cccc3c2OCCCO3)CC1 10.1021/jm00077a018
CHEMBL130118 26510 0 None - 1 Guinea pig 7.3 pIC50 = 7.3 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 347 6 0 5 3.5 CCCCN1CCC(COC(=O)c2cccc3c2OCCCO3)CC1 10.1021/jm00077a018
10404587 10163 5 None - 1 Guinea pig 8.2 pIC50 = 8.2 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 333 6 0 5 3.1 CCCCN1CCC(CC1)COC(=O)c1cccc2c1OCCO2 10.1021/jm00077a018
251 10163 5 None - 1 Guinea pig 8.2 pIC50 = 8.2 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 333 6 0 5 3.1 CCCCN1CCC(CC1)COC(=O)c1cccc2c1OCCO2 10.1021/jm00077a018
CHEMBL130040 10163 5 None - 1 Guinea pig 8.2 pIC50 = 8.2 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 333 6 0 5 3.1 CCCCN1CCC(CC1)COC(=O)c1cccc2c1OCCO2 10.1021/jm00077a018
44281492 125650 2 None - 1 Guinea pig 7.2 pIC50 = 7.2 Functional
5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum
ChEMBL 298 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OC1CCN(C)CC1 10.1016/S0960-894X(01)80508-4
CHEMBL34224 125650 2 None - 1 Guinea pig 7.2 pIC50 = 7.2 Functional
5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum
ChEMBL 298 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OC1CCN(C)CC1 10.1016/S0960-894X(01)80508-4
10802184 60932 0 None - 1 Guinea pig 6.2 pIC50 = 6.2 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 272 5 1 5 1.6 COc1cc(N)c(Cl)cc1C(=O)OCCN(C)C 10.1021/jm960320m
CHEMBL160705 60932 0 None - 1 Guinea pig 6.2 pIC50 = 6.2 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 272 5 1 5 1.6 COc1cc(N)c(Cl)cc1C(=O)OCCN(C)C 10.1021/jm960320m
10041634 29600 1 None - 1 Guinea pig 7.2 pIC50 = 7.2 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 319 6 0 5 3.1 CCCCN1CCC(COC(=O)c2cccc3c2OCO3)CC1 10.1021/jm00077a018
CHEMBL132826 29600 1 None - 1 Guinea pig 7.2 pIC50 = 7.2 Functional
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
ChEMBL 319 6 0 5 3.1 CCCCN1CCC(COC(=O)c2cccc3c2OCO3)CC1 10.1021/jm00077a018
258 10340 31 None 2 3 Guinea pig 7.1 pIC50 = 7.1 Functional
5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum; Not evaluable5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum; Not evaluable
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80508-4
5191 10340 31 None 2 3 Guinea pig 7.1 pIC50 = 7.1 Functional
5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum; Not evaluable5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum; Not evaluable
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80508-4
CHEMBL287045 10340 31 None 2 3 Guinea pig 7.1 pIC50 = 7.1 Functional
5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum; Not evaluable5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum; Not evaluable
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80508-4
258 10340 31 None 2 3 Guinea pig 7.1 pIC50 = 7.1 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960320m
5191 10340 31 None 2 3 Guinea pig 7.1 pIC50 = 7.1 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960320m
CHEMBL287045 10340 31 None 2 3 Guinea pig 7.1 pIC50 = 7.1 Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960320m
19956256 122076 0 None -1 5 Human 6.1 pIC50 = 6.1 Functional
Compound was tested for agonistic activity against 5-hydroxytryptamine 4 receptor on guinea colon at a concentration 0.1 uMCompound was tested for agonistic activity against 5-hydroxytryptamine 4 receptor on guinea colon at a concentration 0.1 uM
ChEMBL 275 4 0 5 2.5 Cc1csc2c1-n1cccc1/C2=N/OCCN(C)C 10.1016/s0960-894x(00)00691-0
CHEMBL334923 122076 0 None -1 5 Human 6.1 pIC50 = 6.1 Functional
Compound was tested for agonistic activity against 5-hydroxytryptamine 4 receptor on guinea colon at a concentration 0.1 uMCompound was tested for agonistic activity against 5-hydroxytryptamine 4 receptor on guinea colon at a concentration 0.1 uM
ChEMBL 275 4 0 5 2.5 Cc1csc2c1-n1cccc1/C2=N/OCCN(C)C 10.1016/s0960-894x(00)00691-0
68490431 89503 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levelsAntagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels
ChEMBL 448 8 2 5 4.0 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(C(=O)O)cc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2179707 89503 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levelsAntagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels
ChEMBL 448 8 2 5 4.0 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(C(=O)O)cc3)CC2)c2ccccc21 10.1021/jm300573d
9800656 22322 0 None - 1 Human 9.2 pKd = 9.2 Functional
,Antagonism of stimulation of 5-hydroxytryptamine receptor on the L-type calcium current (I Ca) in isolated human atrial myocytes,Antagonism of stimulation of 5-hydroxytryptamine receptor on the L-type calcium current (I Ca) in isolated human atrial myocytes
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
CHEMBL121913 22322 0 None - 1 Human 9.2 pKd = 9.2 Functional
,Antagonism of stimulation of 5-hydroxytryptamine receptor on the L-type calcium current (I Ca) in isolated human atrial myocytes,Antagonism of stimulation of 5-hydroxytryptamine receptor on the L-type calcium current (I Ca) in isolated human atrial myocytes
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
44407083 80685 0 None - 0 Rat 8.9 pKd = 8.9 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 284 3 1 3 2.8 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1c[nH]c2ccccc12 10.1021/jm0509501
CHEMBL201946 80685 0 None - 0 Rat 8.9 pKd = 8.9 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 284 3 1 3 2.8 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1c[nH]c2ccccc12 10.1021/jm0509501
11537858 141607 0 None - 0 Rat 7.0 pKd = 7 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 327 2 1 3 2.5 CC1(C)C(=O)N(C(=O)NC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21 10.1021/jm0509501
CHEMBL371883 141607 0 None - 0 Rat 7.0 pKd = 7 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 327 2 1 3 2.5 CC1(C)C(=O)N(C(=O)NC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21 10.1021/jm0509501
11515258 81175 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 319 3 0 5 2.6 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1cc(Cl)cn2ccnc12 10.1021/jm0509501
CHEMBL202481 81175 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 319 3 0 5 2.6 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1cc(Cl)cn2ccnc12 10.1021/jm0509501
11529314 148118 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 284 3 1 4 1.5 O=C(NC[C@@H]1CCN2CCC[C@@H]12)c1cccn2ccnc12 10.1021/jm0509501
CHEMBL383554 148118 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 284 3 1 4 1.5 O=C(NC[C@@H]1CCN2CCC[C@@H]12)c1cccn2ccnc12 10.1021/jm0509501
260 10641 54 None 3 9 Guinea pig 5.7 pKd = 5.7 Functional
Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/S0960-894X(00)80170-5
2775 10641 54 None 3 9 Guinea pig 5.7 pKd = 5.7 Functional
Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/S0960-894X(00)80170-5
656665 10641 54 None 3 9 Guinea pig 5.7 pKd = 5.7 Functional
Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/S0960-894X(00)80170-5
CHEMBL56564 10641 54 None 3 9 Guinea pig 5.7 pKd = 5.7 Functional
Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/S0960-894X(00)80170-5
DB11699 10641 54 None 3 9 Guinea pig 5.7 pKd = 5.7 Functional
Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/S0960-894X(00)80170-5
11522273 148123 0 None - 0 Rat 8.6 pKd = 8.6 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 299 3 0 5 2.2 Cn1nc(C(=O)OC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21 10.1021/jm0509501
CHEMBL383577 148123 0 None - 0 Rat 8.6 pKd = 8.6 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 299 3 0 5 2.2 Cn1nc(C(=O)OC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21 10.1021/jm0509501
11580445 80739 0 None - 0 Rat 6.6 pKd = 6.6 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 312 4 1 4 2.1 CCc1nc(C(=O)NC[C@@H]2CCN3CCC[C@@H]23)c2ccccn12 10.1021/jm0509501
CHEMBL202149 80739 0 None - 0 Rat 6.6 pKd = 6.6 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 312 4 1 4 2.1 CCc1nc(C(=O)NC[C@@H]2CCN3CCC[C@@H]23)c2ccccn12 10.1021/jm0509501
11580890 80721 0 None - 0 Rat 8.5 pKd = 8.5 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 302 3 1 3 2.9 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1c[nH]c2ccc(F)cc12 10.1021/jm0509501
CHEMBL202122 80721 0 None - 0 Rat 8.5 pKd = 8.5 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 302 3 1 3 2.9 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1c[nH]c2ccc(F)cc12 10.1021/jm0509501
11508052 80612 0 None - 0 Rat 8.5 pKd = 8.5 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 285 3 1 4 2.2 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1[nH]nc2ccccc12 10.1021/jm0509501
CHEMBL201878 80612 0 None - 0 Rat 8.5 pKd = 8.5 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 285 3 1 4 2.2 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1[nH]nc2ccccc12 10.1021/jm0509501
14403147 41666 2 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.
ChEMBL 298 2 1 4 1.9 CN1C2CC(OC(=O)c3c[nH]c4ccccc34)CC1C1OC12 10.1016/S0960-894X(00)80170-5
CHEMBL143197 41666 2 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.
ChEMBL 298 2 1 4 1.9 CN1C2CC(OC(=O)c3c[nH]c4ccccc34)CC1C1OC12 10.1016/S0960-894X(00)80170-5
133999 81090 8 None - 0 Rat 8.1 pKd = 8.1 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 318 3 1 4 2.2 O=C(NC[C@@H]1CCN2CCC[C@@H]12)c1cc(Cl)cn2ccnc12 10.1021/jm0509501
CHEMBL202434 81090 8 None - 0 Rat 8.1 pKd = 8.1 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 318 3 1 4 2.2 O=C(NC[C@@H]1CCN2CCC[C@@H]12)c1cc(Cl)cn2ccnc12 10.1021/jm0509501
11508567 172748 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 314 4 1 4 2.8 COc1ccc2[nH]cc(C(=O)OC[C@@H]3CCN4CCC[C@@H]34)c2c1 10.1021/jm0509501
CHEMBL425222 172748 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 314 4 1 4 2.8 COc1ccc2[nH]cc(C(=O)OC[C@@H]3CCN4CCC[C@@H]34)c2c1 10.1021/jm0509501
11500906 142135 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 332 3 1 4 2.5 Cc1cnc2c(C(=O)NC[C@@H]3CCN4CCC[C@@H]34)cc(Cl)cn12 10.1021/jm0509501
CHEMBL372776 142135 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
ChEMBL 332 3 1 4 2.5 Cc1cnc2c(C(=O)NC[C@@H]3CCN4CCC[C@@H]34)cc(Cl)cn12 10.1021/jm0509501
119376 8622 48 None 61 4 Human 10.1 pKi = 10.1 Functional
Antagonistic activity at human 5HT4 receptor expressed in HEK293 cellsAntagonistic activity at human 5HT4 receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2010.10.011
247 8622 48 None 61 4 Human 10.1 pKi = 10.1 Functional
Antagonistic activity at human 5HT4 receptor expressed in HEK293 cellsAntagonistic activity at human 5HT4 receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2010.10.011
CHEMBL33884 8622 48 None 61 4 Human 10.1 pKi = 10.1 Functional
Antagonistic activity at human 5HT4 receptor expressed in HEK293 cellsAntagonistic activity at human 5HT4 receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2010.10.011
119376 8622 48 None 61 4 Human 9.3 pKi = 9.3 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm070552t
247 8622 48 None 61 4 Human 9.3 pKi = 9.3 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm070552t
CHEMBL33884 8622 48 None 61 4 Human 9.3 pKi = 9.3 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm070552t
53318069 63210 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonistic activity at human 5HT4 receptor expressed in HEK293 cellsAntagonistic activity at human 5HT4 receptor expressed in HEK293 cells
ChEMBL 344 7 2 4 2.9 O=C(O)CCCN1CCC(COC(=O)c2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632154 63210 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonistic activity at human 5HT4 receptor expressed in HEK293 cellsAntagonistic activity at human 5HT4 receptor expressed in HEK293 cells
ChEMBL 344 7 2 4 2.9 O=C(O)CCCN1CCC(COC(=O)c2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.10.011
53318070 63211 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity at human 5HT4 receptor expressed in HEK293 cellsAntagonistic activity at human 5HT4 receptor expressed in HEK293 cells
ChEMBL 371 8 2 4 3.0 CCOC(=O)CCCN1CCC(CNC(=O)c2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632155 63211 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity at human 5HT4 receptor expressed in HEK293 cellsAntagonistic activity at human 5HT4 receptor expressed in HEK293 cells
ChEMBL 371 8 2 4 3.0 CCOC(=O)CCCN1CCC(CNC(=O)c2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.10.011
11557207 85830 0 None - 0 Human 7.0 pKi = 7.0 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1203 39 7 18 10.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCNc2nc(NCCCCCCCCCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)nc(NCc3ccccc3)n2)CC1 10.1021/jm070552t
CHEMBL2113160 85830 0 None - 0 Human 7.0 pKi = 7.0 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1203 39 7 18 10.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCNc2nc(NCCCCCCCCCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)nc(NCc3ccccc3)n2)CC1 10.1021/jm070552t
17755141 85900 0 None - 0 Human 7.9 pKi = 7.9 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1183 28 4 16 9.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CCCc2ccc(CCCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
CHEMBL2113289 85900 0 None - 0 Human 7.9 pKi = 7.9 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1183 28 4 16 9.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CCCc2ccc(CCCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
46905984 17186 0 None - 0 Human 7.8 pKi = 7.8 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1179 30 4 14 8.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCN(CCCc2ccc(CCCN(CCCC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)C(C)(C)C)cc2)C(=O)C(C)(C)C)CC1 10.1021/jm070552t
CHEMBL1162955 17186 0 None - 0 Human 7.8 pKi = 7.8 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1179 30 4 14 8.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCN(CCCc2ccc(CCCN(CCCC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)C(C)(C)C)cc2)C(=O)C(C)(C)C)CC1 10.1021/jm070552t
44427806 150691 0 None - 0 Human 7.8 pKi = 7.8 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1151 28 4 14 8.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CCCc2cccc(CCCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)C(C)(C)C)c2)C(=O)C(C)(C)C)CC1 10.1021/jm070552t
CHEMBL390202 150691 0 None - 0 Human 7.8 pKi = 7.8 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1151 28 4 14 8.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CCCc2cccc(CCCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)C(C)(C)C)c2)C(=O)C(C)(C)C)CC1 10.1021/jm070552t
10666935 214729 0 None - 0 Human 7.8 pKi = 7.8 Functional
Tested for 5-hydroxytryptamine 4 receptor antagonist activityTested for 5-hydroxytryptamine 4 receptor antagonist activity
ChEMBL 371 5 1 6 1.7 CC(C)N1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm020099f
CHEMBL97019 214729 0 None - 0 Human 7.8 pKi = 7.8 Functional
Tested for 5-hydroxytryptamine 4 receptor antagonist activityTested for 5-hydroxytryptamine 4 receptor antagonist activity
ChEMBL 371 5 1 6 1.7 CC(C)N1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm020099f
17755040 85896 0 None - 0 Human 7.8 pKi = 7.8 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1175 22 4 16 7.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CC#Cc2ccc(C#CCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
CHEMBL2113285 85896 0 None - 0 Human 7.8 pKi = 7.8 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1175 22 4 16 7.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CC#Cc2ccc(C#CCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
17755140 85899 0 None - 0 Human 7.7 pKi = 7.7 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1155 26 4 16 7.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CN(CCCc2ccc(CCCN(CC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
CHEMBL2113288 85899 0 None - 0 Human 7.7 pKi = 7.7 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1155 26 4 16 7.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CN(CCCc2ccc(CCCN(CC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
11622025 150524 0 None - 0 Human 7.7 pKi = 7.7 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 848 23 4 12 6.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm070552t
CHEMBL390075 150524 0 None - 0 Human 7.7 pKi = 7.7 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 848 23 4 12 6.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm070552t
17756519 85901 0 None - 0 Human 7.6 pKi = 7.6 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1211 30 4 16 9.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCN(CCCc2cccc(CCCN(CCCC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)c2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
CHEMBL2113290 85901 0 None - 0 Human 7.6 pKi = 7.6 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1211 30 4 16 9.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCN(CCCc2cccc(CCCN(CCCC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)c2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
17756415 85898 0 None - 0 Human 7.6 pKi = 7.6 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1203 24 4 16 8.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCN(CC#Cc2ccc(C#CCN(CCCC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
CHEMBL2113287 85898 0 None - 0 Human 7.6 pKi = 7.6 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1203 24 4 16 8.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCN(CC#Cc2ccc(C#CCN(CCCC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
11724799 17304 0 None - 0 Rat 7.5 pKi = 7.5 Functional
Tested for potency against 5-hydroxytryptamine 4 receptor agonist in rat brainTested for potency against 5-hydroxytryptamine 4 receptor agonist in rat brain
ChEMBL 339 0 2 5 1.5 Nc1cc2c(cc1Cl)C(=O)NC1CCN(CCOCCO2)CC1 10.1021/jm020099f
CHEMBL116913 17304 0 None - 0 Rat 7.5 pKi = 7.5 Functional
Tested for potency against 5-hydroxytryptamine 4 receptor agonist in rat brainTested for potency against 5-hydroxytryptamine 4 receptor agonist in rat brain
ChEMBL 339 0 2 5 1.5 Nc1cc2c(cc1Cl)C(=O)NC1CCN(CCOCCO2)CC1 10.1021/jm020099f
17754944 85902 0 None - 0 Human 7.5 pKi = 7.5 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 955 23 3 11 8.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CCCc2ccc(CCCN(CCCC(=O)NC3CCCCC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
CHEMBL2113291 85902 0 None - 0 Human 7.5 pKi = 7.5 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 955 23 3 11 8.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CCCc2ccc(CCCN(CCCC(=O)NC3CCCCC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
53325991 63212 3 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonistic activity at human 5HT4 receptor expressed in HEK293 cellsAntagonistic activity at human 5HT4 receptor expressed in HEK293 cells
ChEMBL 343 7 3 3 2.5 O=C(O)CCCN1CCC(CNC(=O)c2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632156 63212 3 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonistic activity at human 5HT4 receptor expressed in HEK293 cellsAntagonistic activity at human 5HT4 receptor expressed in HEK293 cells
ChEMBL 343 7 3 3 2.5 O=C(O)CCCN1CCC(CNC(=O)c2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.10.011
17756414 85897 0 None - 0 Human 7.4 pKi = 7.4 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1203 24 4 16 8.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCN(CC#Cc2cccc(C#CCN(CCCC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)c2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
CHEMBL2113286 85897 0 None - 0 Human 7.4 pKi = 7.4 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1203 24 4 16 8.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCN(CC#Cc2cccc(C#CCN(CCCC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)c2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
17755039 85894 0 None - 0 Human 7.4 pKi = 7.4 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1146 20 4 16 6.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CN(CC#Cc2ccc(C#CCN(CC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
CHEMBL2113283 85894 0 None - 0 Human 7.4 pKi = 7.4 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1146 20 4 16 6.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CN(CC#Cc2ccc(C#CCN(CC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
235 9342 42 None -5 4 Human 8.3 pKi = 8.3 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm070552t
5311299 9342 42 None -5 4 Human 8.3 pKi = 8.3 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm070552t
CHEMBL286136 9342 42 None -5 4 Human 8.3 pKi = 8.3 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm070552t
11643822 164638 0 None - 0 Human 7.3 pKi = 7.3 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1158 38 6 15 8.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCN(CCCCCCCCCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC(=O)NCC2CCNCC2)CC1 10.1021/jm070552t
CHEMBL408379 164638 0 None - 0 Human 7.3 pKi = 7.3 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1158 38 6 15 8.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCN(CCCCCCCCCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC(=O)NCC2CCNCC2)CC1 10.1021/jm070552t
10666935 214729 0 None - 0 Human 8.2 pKi = 8.2 Functional
Tested for 5-hydroxytryptamine 4 receptor antagonist activityTested for 5-hydroxytryptamine 4 receptor antagonist activity
ChEMBL 371 5 1 6 1.7 CC(C)N1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm020099f
CHEMBL97019 214729 0 None - 0 Human 8.2 pKi = 8.2 Functional
Tested for 5-hydroxytryptamine 4 receptor antagonist activityTested for 5-hydroxytryptamine 4 receptor antagonist activity
ChEMBL 371 5 1 6 1.7 CC(C)N1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm020099f
11513350 150694 0 None - 0 Human 8.2 pKi = 8.2 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 778 18 4 12 4.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm070552t
CHEMBL390205 150694 0 None - 0 Human 8.2 pKi = 8.2 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 778 18 4 12 4.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm070552t
243 9976 91 None 1 5 Human 8.1 pKi = 8.1 Functional
Tested for agonist activity against 5-hydroxytryptamine 4 receptorTested for agonist activity against 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/jm020099f
3052762 9976 91 None 1 5 Human 8.1 pKi = 8.1 Functional
Tested for agonist activity against 5-hydroxytryptamine 4 receptorTested for agonist activity against 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/jm020099f
3502 9976 91 None 1 5 Human 8.1 pKi = 8.1 Functional
Tested for agonist activity against 5-hydroxytryptamine 4 receptorTested for agonist activity against 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/jm020099f
CHEMBL117287 9976 91 None 1 5 Human 8.1 pKi = 8.1 Functional
Tested for agonist activity against 5-hydroxytryptamine 4 receptorTested for agonist activity against 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/jm020099f
DB06480 9976 91 None 1 5 Human 8.1 pKi = 8.1 Functional
Tested for agonist activity against 5-hydroxytryptamine 4 receptorTested for agonist activity against 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/jm020099f
17756314 85895 0 None - 0 Human 8.1 pKi = 8.1 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1175 22 4 16 7.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CC#Cc2cccc(C#CCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)c2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
CHEMBL2113284 85895 0 None - 0 Human 8.1 pKi = 8.1 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 1175 22 4 16 7.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CC#Cc2cccc(C#CCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)c2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
11714901 141110 0 None - 0 Human 8.1 pKi = 8.1 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 904 27 4 12 7.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNC(=O)CCCCCCCCCCC(=O)NCCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm070552t
CHEMBL371718 141110 0 None - 0 Human 8.1 pKi = 8.1 Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cellsDisplacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
ChEMBL 904 27 4 12 7.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNC(=O)CCCCCCCCCCC(=O)NCCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm070552t
10688893 215166 0 None - 0 Human 7.0 pKi = 7.0 Functional
Tested for 5-hydroxytryptamine 4 receptor antagonist activityTested for 5-hydroxytryptamine 4 receptor antagonist activity
ChEMBL 345 4 1 6 1.2 CC(C)n1c(=O)n(C(=O)NCCN2CCN(C)CC2)c2ccccc21 10.1021/jm020099f
CHEMBL99591 215166 0 None - 0 Human 7.0 pKi = 7.0 Functional
Tested for 5-hydroxytryptamine 4 receptor antagonist activityTested for 5-hydroxytryptamine 4 receptor antagonist activity
ChEMBL 345 4 1 6 1.2 CC(C)n1c(=O)n(C(=O)NCCN2CCN(C)CC2)c2ccccc21 10.1021/jm020099f
1782 9296 84 None -1 13 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 9296 84 None -1 13 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 9296 84 None -1 13 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 9296 84 None -1 13 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 9296 84 None -1 13 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
243 9976 91 None -1 5 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 9976 91 None -1 5 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 9976 91 None -1 5 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 9976 91 None -1 5 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 9976 91 None -1 5 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assayAgonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
135526515 224504 0 None - 1 Guinea pig 8.1 pEC50 = 8.1 Functional
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
Drug Central 301 7 4 3 2.8 CCCCCNC(=N)NN=CC1=CNC2=C1C=C(OC)C=C2 None
133076 10172 6 None 1 2 Rat 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 9 2 6 2.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CCNS(=O)(=O)C)Cl 8903510
3230 10172 6 None 1 2 Rat 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 9 2 6 2.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CCNS(=O)(=O)C)Cl 8903510
CHEMBL83899 10172 6 None 1 2 Rat 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 9 2 6 2.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CCNS(=O)(=O)C)Cl 8903510
4223 10764 94 None -177 15 Rat 8.2 pIC50 = 8.2 Functional
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 10764 94 None -177 15 Rat 8.2 pIC50 = 8.2 Functional
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 10764 94 None -177 15 Rat 8.2 pIC50 = 8.2 Functional
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 10764 94 None -177 15 Rat 8.2 pIC50 = 8.2 Functional
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 10764 94 None -177 15 Rat 8.2 pIC50 = 8.2 Functional
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
4223 10764 94 None -177 15 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 10764 94 None -177 15 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 10764 94 None -177 15 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 10764 94 None -177 15 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 10764 94 None -177 15 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
4223 10764 94 None -177 15 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
6918314 10764 94 None -177 15 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
7427 10764 94 None -177 15 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
CHEMBL439849 10764 94 None -177 15 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
DB06684 10764 94 None -177 15 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484




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DOI

145973928 171348 0 None - 0 Human 10.0 pEC50 = 10 Binding
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 171348 0 None - 0 Human 10.0 pEC50 = 10 Binding
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 9838 34 None 1 2 Human 9.6 pEC50 = 9.6 Binding
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 9838 34 None 1 2 Human 9.6 pEC50 = 9.6 Binding
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 9838 34 None 1 2 Human 9.6 pEC50 = 9.6 Binding
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 9838 34 None 1 2 Human 9.6 pEC50 = 9.6 Binding
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 170650 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
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 170650 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
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 171497 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
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 171497 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
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 171000 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 171000 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 170779 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
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 170779 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
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 171179 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
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 171179 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
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 171396 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
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 171396 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
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 143573 2 None - 0 Human 8.9 pEC50 = 8.9 Binding
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 143573 2 None - 0 Human 8.9 pEC50 = 8.9 Binding
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 9838 34 None 1 2 Human 8.9 pEC50 = 8.9 Binding
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 9838 34 None 1 2 Human 8.9 pEC50 = 8.9 Binding
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 9838 34 None 1 2 Human 8.9 pEC50 = 8.9 Binding
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 9838 34 None 1 2 Human 8.9 pEC50 = 8.9 Binding
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 9838 34 None 1 2 Human 8.8 pEC50 = 8.8 Binding
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 9838 34 None 1 2 Human 8.8 pEC50 = 8.8 Binding
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 9838 34 None 1 2 Human 8.8 pEC50 = 8.8 Binding
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 9838 34 None 1 2 Human 8.8 pEC50 = 8.8 Binding
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 170310 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
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 170310 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
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 170994 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
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 170994 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
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
CHEMBL5283568 201400 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
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 201400 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
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
CHEMBL5275962 201432 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
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 201432 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
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 144619 0 None - 0 Rat 7.0 pEC50 = 7 Binding
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 144619 0 None - 0 Rat 7.0 pEC50 = 7 Binding
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
240 7731 43 None -4 25 Guinea pig 7.0 pEC50 = 7 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
2769 7731 43 None -4 25 Guinea pig 7.0 pEC50 = 7 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
44279790 7731 43 None -4 25 Guinea pig 7.0 pEC50 = 7 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
660 7731 43 None -4 25 Guinea pig 7.0 pEC50 = 7 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL1729 7731 43 None -4 25 Guinea pig 7.0 pEC50 = 7 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL560739 7731 43 None -4 25 Guinea pig 7.0 pEC50 = 7 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
DB00604 7731 43 None -4 25 Guinea pig 7.0 pEC50 = 7 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
5311047 211542 33 None - 2 Rat 7.0 pEC50 = 7.0 Binding
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 211542 33 None - 2 Rat 7.0 pEC50 = 7.0 Binding
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 144498 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
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 144498 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
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
CHEMBL5287697 201406 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
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 201406 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
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
CHEMBL5267721 201418 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
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 201418 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
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
145977971 170787 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
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 406 8 1 5 3.6 COCCCN1CCC(CNC(=O)c2cccn3c(Cl)c(C(C)C)nc23)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4208394 170787 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
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 406 8 1 5 3.6 COCCCN1CCC(CNC(=O)c2cccn3c(Cl)c(C(C)C)nc23)CC1 10.1021/acs.jmedchem.8b00457
10584 8245 0 None -1 2 Human 8.0 pEC50 = 8.0 Binding
Activity at 5-HT4R (unknown origin) expressed in COS7 cells assessed as increase in sAPPalpha releaseActivity at 5-HT4R (unknown origin) expressed in COS7 cells assessed as increase in sAPPalpha release
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1021/acs.jmedchem.5b00115
86582973 8245 0 None -1 2 Human 8.0 pEC50 = 8.0 Binding
Activity at 5-HT4R (unknown origin) expressed in COS7 cells assessed as increase in sAPPalpha releaseActivity at 5-HT4R (unknown origin) expressed in COS7 cells assessed as increase in sAPPalpha release
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1021/acs.jmedchem.5b00115
CHEMBL3417009 8245 0 None -1 2 Human 8.0 pEC50 = 8.0 Binding
Activity at 5-HT4R (unknown origin) expressed in COS7 cells assessed as increase in sAPPalpha releaseActivity at 5-HT4R (unknown origin) expressed in COS7 cells assessed as increase in sAPPalpha release
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1021/acs.jmedchem.5b00115
9975257 55528 1 None - 0 Human 6.0 pEC50 = 6.0 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against zacoprideTested for 5-hydroxytryptamine 4 binding affinity against zacopride
ChEMBL 351 3 2 4 3.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2C(C)CCCC2C1 10.1021/jm020099f
CHEMBL15585 55528 1 None - 0 Human 6.0 pEC50 = 6.0 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against zacoprideTested for 5-hydroxytryptamine 4 binding affinity against zacopride
ChEMBL 351 3 2 4 3.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2C(C)CCCC2C1 10.1021/jm020099f
9797313 108706 2 None - 3 Human 6.0 pEC50 = 6.0 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against zacoprideTested for 5-hydroxytryptamine 4 binding affinity against zacopride
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1021/jm020099f
CHEMBL301039 108706 2 None - 3 Human 6.0 pEC50 = 6.0 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against zacoprideTested for 5-hydroxytryptamine 4 binding affinity against zacopride
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1021/jm020099f
145975740 170766 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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 396 6 1 5 2.8 CC(C)c1cn2cccc(C(=O)NCC3C4CN(CC5CCOCC5)CC34)c2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4208144 170766 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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 396 6 1 5 2.8 CC(C)c1cn2cccc(C(=O)NCC3C4CN(CC5CCOCC5)CC34)c2n1 10.1021/acs.jmedchem.8b00457
CHEMBL5288809 201416 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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 381 6 0 6 4.9 CC(C)CCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5315677 201416 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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 381 6 0 6 4.9 CC(C)CCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5289747 201413 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
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 382 5 1 5 2.7 CC(C)n1nc(C(=O)NC2C3CN(CC4CCOCC4)CC32)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315613 201413 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
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 382 5 1 5 2.7 CC(C)n1nc(C(=O)NC2C3CN(CC4CCOCC4)CC32)c2ccccc21 10.1021/acs.jmedchem.1c00703
135409453 10545 41 None - 2 Guinea pig 7.9 pEC50 = 7.9 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2013.05.018
226 10545 41 None - 2 Guinea pig 7.9 pEC50 = 7.9 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2013.05.018
CHEMBL76370 10545 41 None - 2 Guinea pig 7.9 pEC50 = 7.9 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2013.05.018
9975257 55528 1 None - 0 Human 6.9 pEC50 = 6.9 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against renzaprideTested for 5-hydroxytryptamine 4 binding affinity against renzapride
ChEMBL 351 3 2 4 3.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2C(C)CCCC2C1 10.1021/jm020099f
CHEMBL15585 55528 1 None - 0 Human 6.9 pEC50 = 6.9 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against renzaprideTested for 5-hydroxytryptamine 4 binding affinity against renzapride
ChEMBL 351 3 2 4 3.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2C(C)CCCC2C1 10.1021/jm020099f
9797313 108706 2 None - 3 Human 6.9 pEC50 = 6.9 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against renzaprideTested for 5-hydroxytryptamine 4 binding affinity against renzapride
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1021/jm020099f
CHEMBL301039 108706 2 None - 3 Human 6.9 pEC50 = 6.9 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against renzaprideTested for 5-hydroxytryptamine 4 binding affinity against renzapride
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1021/jm020099f
CHEMBL5270858 201383 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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 365 4 0 6 4.4 CC(C)n1nc(-c2nnc(C3CCN(C4CCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315212 201383 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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 365 4 0 6 4.4 CC(C)n1nc(-c2nnc(C3CCN(C4CCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
145973946 171390 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
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 370 8 1 5 2.4 COCCCN1CC2C(CNC(=O)c3nc(C(C)C)c4ccccn34)C2C1 10.1021/acs.jmedchem.8b00457
CHEMBL4215943 171390 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
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 370 8 1 5 2.4 COCCCN1CC2C(CNC(=O)c3nc(C(C)C)c4ccccn34)C2C1 10.1021/acs.jmedchem.8b00457
145978459 170356 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
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 370 8 1 5 2.4 COCCCN1CC2C(CNC(=O)c3cccn4cc(C(C)C)nc34)C2C1 10.1021/acs.jmedchem.8b00457
CHEMBL4203277 170356 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
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 370 8 1 5 2.4 COCCCN1CC2C(CNC(=O)c3cccn4cc(C(C)C)nc34)C2C1 10.1021/acs.jmedchem.8b00457
10521792 117368 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Compound was tested for 5-hydroxytryptamine 4 binding affinityCompound was tested for 5-hydroxytryptamine 4 binding affinity
ChEMBL 349 4 2 4 2.6 Nc1c(Cl)cc(C(=O)NCCC23CCCN2CCC3)c2c1CCO2 10.1021/jm020099f
CHEMBL325494 117368 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Compound was tested for 5-hydroxytryptamine 4 binding affinityCompound was tested for 5-hydroxytryptamine 4 binding affinity
ChEMBL 349 4 2 4 2.6 Nc1c(Cl)cc(C(=O)NCCC23CCCN2CCC3)c2c1CCO2 10.1021/jm020099f
CHEMBL5286277 201410 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
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 384 5 1 5 3.2 CC(C)n1nc(C(=O)NC2CCN(CC3CCOCC3)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315498 201410 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
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 384 5 1 5 3.2 CC(C)n1nc(C(=O)NC2CCN(CC3CCOCC3)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5267237 201414 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
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 384 5 2 5 3.1 CC(C)n1nc(C(=O)NC2CC3CCC(C2)N3CC(C)(C)O)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315650 201414 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
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 384 5 2 5 3.1 CC(C)n1nc(C(=O)NC2CC3CCC(C2)N3CC(C)(C)O)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5272596 201399 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 369 6 0 7 3.5 COCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5315395 201399 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 369 6 0 7 3.5 COCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5275060 201423 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
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 400 5 2 6 2.4 CC(C)n1nc(C(=O)NC2CCN(CC3(O)CCOCC3)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315752 201423 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
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 400 5 2 6 2.4 CC(C)n1nc(C(=O)NC2CCN(CC3(O)CCOCC3)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
135409453 10545 41 None -2 2 Human 7.8 pEC50 = 7.8 Binding
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
226 10545 41 None -2 2 Human 7.8 pEC50 = 7.8 Binding
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
CHEMBL76370 10545 41 None -2 2 Human 7.8 pEC50 = 7.8 Binding
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
CHEMBL5270036 201384 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
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 311 3 1 6 3.1 CC(C)n1nc(-c2nnc(C3CCNCC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315255 201384 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
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 311 3 1 6 3.1 CC(C)n1nc(-c2nnc(C3CCNCC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5277017 201440 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 383 5 1 7 3.6 CC(C)n1nc(-c2nnc(C3CCN(CC(C)(C)O)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5316058 201440 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 383 5 1 7 3.6 CC(C)n1nc(-c2nnc(C3CCN(CC(C)(C)O)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
68593871 144542 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
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 466 7 2 6 2.4 CCC(=O)N1CCCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)C1 10.1016/j.ejmech.2015.12.006
CHEMBL3759348 144542 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
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 466 7 2 6 2.4 CCC(=O)N1CCCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)C1 10.1016/j.ejmech.2015.12.006
CHEMBL5275605 200643 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 383 7 0 7 3.9 COCCCN1CCC(c2nc(-c3nn(C(C)C)c4ccccc34)no2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5268064 201380 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 369 6 1 7 3.2 CC(C)n1nc(-c2nnc(C3CCN(CCCO)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315175 201380 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 369 6 1 7 3.2 CC(C)n1nc(-c2nnc(C3CCN(CCCO)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5286989 201146 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 379 5 0 6 4.6 CC(C)n1nc(-c2nnc(C3CCN(CC4CCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
54677674 119586 4 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.8b00457
CHEMBL3291085 119586 4 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.8b00457
CHEMBL3306918 119586 4 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.8b00457
145964870 171189 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
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 370 6 2 5 2.1 CC(C)c1cn2cccc(C(=O)NCC3C4CN(CC(C)(C)O)CC34)c2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4213441 171189 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
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 370 6 2 5 2.1 CC(C)c1cn2cccc(C(=O)NCC3C4CN(CC(C)(C)O)CC34)c2n1 10.1021/acs.jmedchem.8b00457
54677674 119586 4 None - 1 Human 7.8 pEC50 = 7.8 Binding
Partial agonist activity at human recombinant 5HT4E receptor expressed in COS7 cells assessed as cAMP accumulation by HTRF assayPartial agonist activity at human recombinant 5HT4E receptor expressed in COS7 cells assessed as cAMP accumulation by HTRF assay
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.1c00703
CHEMBL3291085 119586 4 None - 1 Human 7.8 pEC50 = 7.8 Binding
Partial agonist activity at human recombinant 5HT4E receptor expressed in COS7 cells assessed as cAMP accumulation by HTRF assayPartial agonist activity at human recombinant 5HT4E receptor expressed in COS7 cells assessed as cAMP accumulation by HTRF assay
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.1c00703
CHEMBL3306918 119586 4 None - 1 Human 7.8 pEC50 = 7.8 Binding
Partial agonist activity at human recombinant 5HT4E receptor expressed in COS7 cells assessed as cAMP accumulation by HTRF assayPartial agonist activity at human recombinant 5HT4E receptor expressed in COS7 cells assessed as cAMP accumulation by HTRF assay
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.1c00703
CHEMBL5269243 201378 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 399 7 0 7 4.6 CSCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5315148 201378 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 399 7 0 7 4.6 CSCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5283556 200995 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
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 384 7 1 5 3.4 COCCCN1C2CCC1CC(NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1021/acs.jmedchem.1c00703
CHEMBL5272676 200510 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 357 5 0 6 3.8 CC(C)n1nc(-c2nnc(C3CCN(CCF)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5278277 201436 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
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(-c2noc(C3CCN(CC4CCOCC4)CC3)n2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5316010 201436 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
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(-c2noc(C3CCN(CC4CCOCC4)CC3)n2)c2ccccc21 10.1021/acs.jmedchem.1c00703
145976249 170324 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 373 8 1 6 2.3 COCCCN1CCC(CNC(=O)c2cccn3nc(C(C)C)nc23)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4202922 170324 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 373 8 1 6 2.3 COCCCN1CCC(CNC(=O)c2cccn3nc(C(C)C)nc23)CC1 10.1021/acs.jmedchem.8b00457
145977126 170577 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 373 8 1 6 2.3 COCCCN1CCC(CNC(=O)c2cccc3nc(C(C)C)nn23)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4206020 170577 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 373 8 1 6 2.3 COCCCN1CCC(CNC(=O)c2cccc3nc(C(C)C)nn23)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL5283579 201403 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
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 351 4 0 6 4.0 CC(C)n1nc(-c2nnc(C3CCN(C4CC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315441 201403 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
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 351 4 0 6 4.0 CC(C)n1nc(-c2nnc(C3CCN(C4CC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
183782 10171 20 None -1 14 Human 8.7 pEC50 = 8.7 Binding
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 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1021/acs.jmedchem.1c00703
237 10171 20 None -1 14 Human 8.7 pEC50 = 8.7 Binding
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 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1021/acs.jmedchem.1c00703
CHEMBL85251 10171 20 None -1 14 Human 8.7 pEC50 = 8.7 Binding
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 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1021/acs.jmedchem.1c00703
11961293 10541 19 None - 1 Guinea pig 8.6 pEC50 = 8.6 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
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 10541 19 None - 1 Guinea pig 8.6 pEC50 = 8.6 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
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 10541 19 None - 1 Guinea pig 8.6 pEC50 = 8.6 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
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 10541 19 None - 1 Guinea pig 8.6 pEC50 = 8.6 Binding
Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexusInduction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
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
138376515 170567 5 None - 0 Human 7.7 pEC50 = 7.7 Binding
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 409 5 0 7 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)n2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4205936 170567 5 None - 0 Human 7.7 pEC50 = 7.7 Binding
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 409 5 0 7 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)n2n1 10.1021/acs.jmedchem.8b00457
CHEMBL5286257 201405 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
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 374 7 2 6 2.2 COCCCN1CCC(O)(NC(=O)c2nn(C(C)C)c3ccccc23)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5315460 201405 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
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 374 7 2 6 2.2 COCCCN1CCC(O)(NC(=O)c2nn(C(C)C)c3ccccc23)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5287819 201396 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
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 425 5 1 8 3.4 CC(C)n1nc(-c2nnc(C3CCN(CC4(O)CCOCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315380 201396 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
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 425 5 1 8 3.4 CC(C)n1nc(-c2nnc(C3CCN(CC4(O)CCOCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
127037818 143472 2 None - 0 Human 7.7 pEC50 = 7.7 Binding
Inhibition of 5-HT4 receptor (unknown origin)Inhibition of 5-HT4 receptor (unknown origin)
ChEMBL 370 8 1 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2019.111569
CHEMBL3740472 143472 2 None - 0 Human 7.7 pEC50 = 7.7 Binding
Inhibition of 5-HT4 receptor (unknown origin)Inhibition of 5-HT4 receptor (unknown origin)
ChEMBL 370 8 1 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1 10.1016/j.ejmech.2019.111569
CHEMBL5288438 201417 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
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 1 7 4.2 CC(C)n1nc(-c2nnc(C3CCN(CC4(O)CCCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315683 201417 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
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 1 7 4.2 CC(C)n1nc(-c2nnc(C3CCN(CC4(O)CCCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5285364 201074 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 383 7 0 7 3.9 COCCCN1CCC(c2noc(-c3nn(C(C)C)c4ccccc34)n2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5290568 201281 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 353 4 0 6 4.3 CC(C)N1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5275260 201431 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 442 6 1 5 4.1 CC(C)n1nc(C(=O)NCC2CC3CCC(C2)N3CC2(F)CCOCC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315833 201431 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 442 6 1 5 4.1 CC(C)n1nc(C(=O)NCC2CC3CCC(C2)N3CC2(F)CCOCC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5286642 201401 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 415 6 0 6 5.1 CC(C)n1nc(-c2nnc(C3CCN(CCc4ccccc4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315420 201401 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 415 6 0 6 5.1 CC(C)n1nc(-c2nnc(C3CCN(CCc4ccccc4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5290222 201444 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 400 5 2 6 2.6 CC(C)n1nc(C(=O)NC2(O)CCN(CC3CCOCC3)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5316143 201444 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 400 5 2 6 2.6 CC(C)n1nc(C(=O)NC2(O)CCN(CC3CCOCC3)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
127027397 144408 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
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 421 8 2 7 2.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2ccnc2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758199 144408 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
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 421 8 2 7 2.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2ccnc2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL5272764 201397 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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 379 5 0 6 4.5 CC(C)n1nc(-c2nnc(CC3CCN(C4CCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315381 201397 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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 379 5 0 6 4.5 CC(C)n1nc(-c2nnc(CC3CCN(C4CCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
243 9976 91 None 12 34 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.8b00457
3052762 9976 91 None 12 34 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.8b00457
3502 9976 91 None 12 34 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.8b00457
CHEMBL117287 9976 91 None 12 34 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.8b00457
DB06480 9976 91 None 12 34 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.8b00457
243 9976 91 None - 34 Rat 7.6 pEC50 = 7.6 Binding
Partial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assayPartial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.1c00703
3052762 9976 91 None - 34 Rat 7.6 pEC50 = 7.6 Binding
Partial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assayPartial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.1c00703
3502 9976 91 None - 34 Rat 7.6 pEC50 = 7.6 Binding
Partial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assayPartial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.1c00703
CHEMBL117287 9976 91 None - 34 Rat 7.6 pEC50 = 7.6 Binding
Partial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assayPartial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.1c00703
DB06480 9976 91 None - 34 Rat 7.6 pEC50 = 7.6 Binding
Partial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assayPartial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.1c00703
44288600 107894 0 None - 1 Guinea pig 6.6 pEC50 = 6.6 Binding
Effective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligandEffective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligand
ChEMBL 335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
CHEMBL295155 107894 0 None - 1 Guinea pig 6.6 pEC50 = 6.6 Binding
Effective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligandEffective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligand
ChEMBL 335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
CHEMBL5275895 201439 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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 358 5 2 5 2.6 CC(C)n1nc(C(=O)NC2CCN(CC(C)(C)O)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5316054 201439 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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 358 5 2 5 2.6 CC(C)n1nc(C(=O)NC2CCN(CC(C)(C)O)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
145974756 171536 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 416 5 1 5 3.2 CC(C)c1nn2c(C(=O)NCC3C4CN(C5CCOCC5)CC34)cccc2c1Cl 10.1021/acs.jmedchem.8b00457
CHEMBL4217842 171536 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 416 5 1 5 3.2 CC(C)c1nn2c(C(=O)NCC3C4CN(C5CCOCC5)CC34)cccc2c1Cl 10.1021/acs.jmedchem.8b00457
CHEMBL5283058 201421 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 358 7 1 5 2.8 COCCCN1CCC(NC(=O)c2nn(C(C)C)c3ccccc23)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5315718 201421 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 358 7 1 5 2.8 COCCCN1CCC(NC(=O)c2nn(C(C)C)c3ccccc23)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5281997 200917 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 353 4 0 6 4.3 CC(C)N1CCC(c2noc(-c3nn(C(C)C)c4ccccc34)n2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5274456 200596 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
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 7 1 4 4.1 CC(C)n1nc(C(=O)NC2CC3CCC(C2)N3CCCCF)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5281474 201420 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
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 439 5 1 6 2.8 COC(=O)N1CCC(N2CC3C(CNC(=O)c4nn(C(C)C)c5ccccc45)C3C2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5315714 201420 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
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 439 5 1 6 2.8 COC(=O)N1CCC(N2CC3C(CNC(=O)c4nn(C(C)C)c5ccccc45)C3C2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5276171 200666 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
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 8 1 5 2.6 COCCCN1CC2C(CNC(=O)c3nn(C(C)C)c4ccccc34)C2C1 10.1021/acs.jmedchem.1c00703
44224237 201569 8 None - 1 Human 8.4 pEC50 = 8.4 Binding
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
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 201569 8 None - 1 Human 8.4 pEC50 = 8.4 Binding
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
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
CHEMBL5270411 200411 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 330 5 1 4 2.2 CC(C)n1nc(C(=O)NC2C3CN(CCF)CC32)c2ccccc21 10.1021/acs.jmedchem.1c00703
71508291 174215 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at 5HT4A receptor (unknown origin)Partial agonist activity at 5HT4A receptor (unknown origin)
ChEMBL 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL4297327 174215 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at 5HT4A receptor (unknown origin)Partial agonist activity at 5HT4A receptor (unknown origin)
ChEMBL 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5279298 174215 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at 5HT4A receptor (unknown origin)Partial agonist activity at 5HT4A receptor (unknown origin)
ChEMBL 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
71508291 174215 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at 5HT4D receptor (unknown origin)Partial agonist activity at 5HT4D receptor (unknown origin)
ChEMBL 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL4297327 174215 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at 5HT4D receptor (unknown origin)Partial agonist activity at 5HT4D receptor (unknown origin)
ChEMBL 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5279298 174215 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at 5HT4D receptor (unknown origin)Partial agonist activity at 5HT4D receptor (unknown origin)
ChEMBL 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
71508291 174215 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at 5HT4E receptor (unknown origin)Partial agonist activity at 5HT4E receptor (unknown origin)
ChEMBL 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL4297327 174215 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at 5HT4E receptor (unknown origin)Partial agonist activity at 5HT4E receptor (unknown origin)
ChEMBL 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5279298 174215 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
Partial agonist activity at 5HT4E receptor (unknown origin)Partial agonist activity at 5HT4E receptor (unknown origin)
ChEMBL 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5275886 200653 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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 402 5 1 5 3.3 CC(C)n1nc(C(=O)NC2CCN(CC3(F)CCOCC3)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
145975076 170401 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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 340 5 1 4 2.8 CC(C)c1cn2cccc(C(=O)NCC3C4CN(C(C)C)CC34)c2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4203778 170401 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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 340 5 1 4 2.8 CC(C)c1cn2cccc(C(=O)NCC3C4CN(C(C)C)CC34)c2n1 10.1021/acs.jmedchem.8b00457
CHEMBL5291111 201300 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 374 5 1 4 3.5 CC(C)n1nc(C(=O)NC2C3CN(Cc4ccccc4)CC32)c2ccccc21 10.1021/acs.jmedchem.1c00703
145972323 171370 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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)c1cn2cccc(C(=O)NCC3C4CN(C5CCOCC5)CC34)c2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4215651 171370 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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)c1cn2cccc(C(=O)NCC3C4CN(C5CCOCC5)CC34)c2n1 10.1021/acs.jmedchem.8b00457
155554403 181411 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Inhibition of 5-HT4 receptor (unknown origin)Inhibition of 5-HT4 receptor (unknown origin)
ChEMBL 330 2 1 3 1.9 CCN1C(=O)N(C(=O)NC2CC3CCC(C2)N3C)C2C=CC=CC21 10.1016/j.ejmech.2019.111569
CHEMBL4557961 181411 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Inhibition of 5-HT4 receptor (unknown origin)Inhibition of 5-HT4 receptor (unknown origin)
ChEMBL 330 2 1 3 1.9 CCN1C(=O)N(C(=O)NC2CC3CCC(C2)N3C)C2C=CC=CC21 10.1016/j.ejmech.2019.111569
19426720 117383 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
Tested for ability to stimulate production of cAMP mediated by 5-hydroxytryptamine 4 receptor in mouse Coliculi neuronsTested for ability to stimulate production of cAMP mediated by 5-hydroxytryptamine 4 receptor in mouse Coliculi neurons
ChEMBL 342 2 1 5 2.4 CCn1c(=O)n(C(=O)NC2CC3CCCC(C2)N3C)c2ccccc21 10.1021/jm020099f
CHEMBL325603 117383 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
Tested for ability to stimulate production of cAMP mediated by 5-hydroxytryptamine 4 receptor in mouse Coliculi neuronsTested for ability to stimulate production of cAMP mediated by 5-hydroxytryptamine 4 receptor in mouse Coliculi neurons
ChEMBL 342 2 1 5 2.4 CCn1c(=O)n(C(=O)NC2CC3CCCC(C2)N3C)c2ccccc21 10.1021/jm020099f
CHEMBL5270492 201386 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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 330 5 2 5 1.8 CC(C)n1nc(C(=O)NC2CCN(CCO)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315263 201386 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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 330 5 2 5 1.8 CC(C)n1nc(C(=O)NC2CCN(CCO)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
68592299 144532 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
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 466 7 2 6 2.4 CCC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
CHEMBL3759259 144532 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
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 466 7 2 6 2.4 CCC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
CHEMBL5273433 200543 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
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 360 7 1 6 2.0 COCCCN1CCOC(NC(=O)c2nn(C(C)C)c3ccccc23)C1 10.1021/acs.jmedchem.1c00703
235 9342 42 None -5 3 Guinea pig 8.4 pEC50 = 8.4 Binding
Agonist activity at 5-HT4 receptor in guinea pig ileum assessed as increase in response to electrical stimulationAgonist activity at 5-HT4 receptor in guinea pig ileum assessed as increase in response to electrical stimulation
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/j.ejmech.2015.08.051
5311299 9342 42 None -5 3 Guinea pig 8.4 pEC50 = 8.4 Binding
Agonist activity at 5-HT4 receptor in guinea pig ileum assessed as increase in response to electrical stimulationAgonist activity at 5-HT4 receptor in guinea pig ileum assessed as increase in response to electrical stimulation
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/j.ejmech.2015.08.051
CHEMBL286136 9342 42 None -5 3 Guinea pig 8.4 pEC50 = 8.4 Binding
Agonist activity at 5-HT4 receptor in guinea pig ileum assessed as increase in response to electrical stimulationAgonist activity at 5-HT4 receptor in guinea pig ileum assessed as increase in response to electrical stimulation
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/j.ejmech.2015.08.051
CHEMBL5274204 201430 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
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 426 5 2 6 2.9 CC(C)n1nc(C(=O)NC2CC3CCC(C2)N3CC2(O)CCOCC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315832 201430 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
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 426 5 2 6 2.9 CC(C)n1nc(C(=O)NC2CC3CCC(C2)N3CC2(O)CCOCC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5289203 201415 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
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 453 6 1 6 3.0 COC(=O)N1CCC(CN2CC3C(CNC(=O)c4nn(C(C)C)c5ccccc45)C3C2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5315653 201415 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
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 453 6 1 6 3.0 COC(=O)N1CCC(CN2CC3C(CNC(=O)c4nn(C(C)C)c5ccccc45)C3C2)CC1 10.1021/acs.jmedchem.1c00703
9800656 22322 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Concentration required to produce half-maximal response against 5-hydroxytryptamine receptor on the L-type calcium current (I Ca) in isolated human atrial myocytesConcentration required to produce half-maximal response against 5-hydroxytryptamine receptor on the L-type calcium current (I Ca) in isolated human atrial myocytes
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
CHEMBL121913 22322 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Concentration required to produce half-maximal response against 5-hydroxytryptamine receptor on the L-type calcium current (I Ca) in isolated human atrial myocytesConcentration required to produce half-maximal response against 5-hydroxytryptamine receptor on the L-type calcium current (I Ca) in isolated human atrial myocytes
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
145975067 170371 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
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)c3nc(C(C)C)c4ccccn34)CC2)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4203491 170371 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
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)c3nc(C(C)C)c4ccccn34)CC2)CC1 10.1021/acs.jmedchem.8b00457
145964080 170943 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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 384 5 1 5 3.1 CC(C)c1nc(C(=O)NCC2CCN(C3CCOCC3)CC2)n2ccccc12 10.1021/acs.jmedchem.8b00457
CHEMBL4210381 170943 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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 384 5 1 5 3.1 CC(C)c1nc(C(=O)NCC2CCN(C3CCOCC3)CC2)n2ccccc12 10.1021/acs.jmedchem.8b00457
71508291 174215 12 None - 0 Human 7.4 pEC50 = 7.4 Binding
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 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL4297327 174215 12 None - 0 Human 7.4 pEC50 = 7.4 Binding
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 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5279298 174215 12 None - 0 Human 7.4 pEC50 = 7.4 Binding
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 383 7 0 7 3.9 COCCCN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5281000 201429 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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 7 1 5 3.5 COCC(C)(C)CN1CCC(NC(=O)c2nn(C(C)C)c3ccccc23)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5315826 201429 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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 7 1 5 3.5 COCC(C)(C)CN1CCC(NC(=O)c2nn(C(C)C)c3ccccc23)CC1 10.1021/acs.jmedchem.1c00703
25016328 144603 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
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 480 7 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)C(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3759860 144603 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
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 480 7 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)C(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
145977443 170716 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 342 5 1 4 3.3 CC(C)c1nc(C(=O)NCC2CCN(C(C)C)CC2)n2ccccc12 10.1021/acs.jmedchem.8b00457
CHEMBL4207586 170716 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 342 5 1 4 3.3 CC(C)c1nc(C(=O)NCC2CCN(C(C)C)CC2)n2ccccc12 10.1021/acs.jmedchem.8b00457
CHEMBL5284140 201391 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 372 6 2 5 2.8 CC(C)n1nc(C(=O)NC2CCN(CC(C)(C)CO)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315296 201391 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 372 6 2 5 2.8 CC(C)n1nc(C(=O)NC2CCN(CC(C)(C)CO)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5273457 201407 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 360 5 1 4 3.6 CC(C)n1nc(C(=O)NC2CCN(CC(C)(C)F)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315474 201407 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 360 5 1 4 3.6 CC(C)n1nc(C(=O)NC2CCN(CC(C)(C)F)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
145978825 170677 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
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 409 5 0 7 4.1 CC(C)c1nc(-c2nnc(C3CCN(CC4CCOCC4)CC3)o2)n2ccccc12 10.1021/acs.jmedchem.8b00457
CHEMBL4207136 170677 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
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 409 5 0 7 4.1 CC(C)c1nc(-c2nnc(C3CCN(CC4CCOCC4)CC3)o2)n2ccccc12 10.1021/acs.jmedchem.8b00457
CHEMBL5288891 201227 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 376 7 1 5 3.1 COCCCN1CCC(F)(NC(=O)c2nn(C(C)C)c3ccccc23)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5271080 201382 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
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 382 5 1 5 2.7 CC(C)n1nc(C(=O)NCC2C3CN(C4CCOCC4)CC23)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315204 201382 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
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 382 5 1 5 2.7 CC(C)n1nc(C(=O)NCC2C3CN(C4CCOCC4)CC23)c2ccccc21 10.1021/acs.jmedchem.1c00703
243 9976 91 None 12 34 Human 8.3 pEC50 = 8.3 Binding
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 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.8b00457
3052762 9976 91 None 12 34 Human 8.3 pEC50 = 8.3 Binding
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 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.8b00457
3502 9976 91 None 12 34 Human 8.3 pEC50 = 8.3 Binding
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 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.8b00457
CHEMBL117287 9976 91 None 12 34 Human 8.3 pEC50 = 8.3 Binding
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 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.8b00457
DB06480 9976 91 None 12 34 Human 8.3 pEC50 = 8.3 Binding
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 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.8b00457
CHEMBL5274379 200591 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
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 366 5 1 4 3.8 CC(C)n1nc(C(=O)NC2CC3CCC(C2)N3CC2CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5278851 201437 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
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 332 5 1 4 2.8 CC(C)n1nc(C(=O)NC2CCN(CCF)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5316011 201437 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
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 332 5 1 4 2.8 CC(C)n1nc(C(=O)NC2CCN(CCF)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5281078 201438 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
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 410 5 1 5 3.8 CC(C)n1nc(C(=O)NC2CC3CCC(C2)N3CC2CCOCC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5316015 201438 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
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 410 5 1 5 3.8 CC(C)n1nc(C(=O)NC2CC3CCC(C2)N3CC2CCOCC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5268956 201387 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 397 6 1 7 4.0 CC(C)n1nc(-c2nnc(C3CCN(CCC(C)(C)O)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315264 201387 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 397 6 1 7 4.0 CC(C)n1nc(-c2nnc(C3CCN(CCC(C)(C)O)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
44288600 107894 0 None - 1 Guinea pig 6.3 pEC50 = 6.3 Binding
Effective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligandEffective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligand
ChEMBL 335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
CHEMBL295155 107894 0 None - 1 Guinea pig 6.3 pEC50 = 6.3 Binding
Effective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligandEffective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligand
ChEMBL 335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
145975297 170372 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 353 4 0 6 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(C(C)C)CC4)o3)n2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4203494 170372 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 353 4 0 6 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(C(C)C)CC4)o3)n2n1 10.1021/acs.jmedchem.8b00457
9928343 110247 0 None - 1 Guinea pig 6.3 pEC50 = 6.3 Binding
Effective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligandEffective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligand
ChEMBL 349 4 2 4 2.2 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
CHEMBL3085015 110247 0 None - 1 Guinea pig 6.3 pEC50 = 6.3 Binding
Effective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligandEffective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligand
ChEMBL 349 4 2 4 2.2 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
CHEMBL5282103 201434 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
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 365 5 0 6 4.1 CC(C)n1nc(-c2nnc(CC3CCN(C4CC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315948 201434 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
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 365 5 0 6 4.1 CC(C)n1nc(-c2nnc(CC3CCN(C4CC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
54677674 119586 4 None - 1 Human 7.2 pEC50 = 7.2 Binding
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 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.8b00457
CHEMBL3291085 119586 4 None - 1 Human 7.2 pEC50 = 7.2 Binding
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 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.8b00457
CHEMBL3306918 119586 4 None - 1 Human 7.2 pEC50 = 7.2 Binding
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 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.8b00457
54677674 119586 4 None - 1 Human 7.2 pEC50 = 7.2 Binding
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 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.1c00703
CHEMBL3291085 119586 4 None - 1 Human 7.2 pEC50 = 7.2 Binding
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 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.1c00703
CHEMBL3306918 119586 4 None - 1 Human 7.2 pEC50 = 7.2 Binding
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 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1021/acs.jmedchem.1c00703
CHEMBL5278176 201425 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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 411 7 0 7 4.5 COCC(C)(C)CN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
CHEMBL5315756 201425 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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 411 7 0 7 4.5 COCC(C)(C)CN1CCC(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
145966243 171139 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 409 5 0 7 4.1 CC(C)c1cn2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)c2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4212757 171139 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 409 5 0 7 4.1 CC(C)c1cn2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)c2n1 10.1021/acs.jmedchem.8b00457
138376515 170567 5 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
ChEMBL 409 5 0 7 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)n2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4205936 170567 5 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
ChEMBL 409 5 0 7 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)n2n1 10.1021/acs.jmedchem.8b00457
145972573 171388 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
ChEMBL 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccc4cc(C(C)C)nn34)o2)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4215911 171388 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
ChEMBL 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccc4cc(C(C)C)nn34)o2)CC1 10.1021/acs.jmedchem.8b00457
138376515 170567 5 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
ChEMBL 409 5 0 7 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)n2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4205936 170567 5 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
ChEMBL 409 5 0 7 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)n2n1 10.1021/acs.jmedchem.8b00457
145972573 171388 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
ChEMBL 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccc4cc(C(C)C)nn34)o2)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4215911 171388 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
ChEMBL 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccc4cc(C(C)C)nn34)o2)CC1 10.1021/acs.jmedchem.8b00457
11225102 83199 3 None - 1 Human 8.2 pEC50 = 8.2 Binding
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.05.034
CHEMBL2059590 83199 3 None - 1 Human 8.2 pEC50 = 8.2 Binding
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.05.034
CHEMBL5280851 201426 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
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 344 6 2 5 2.2 CC(C)n1nc(C(=O)NC2CCN(CCCO)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315805 201426 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
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 344 6 2 5 2.2 CC(C)n1nc(C(=O)NC2CCN(CCCO)CC2)c2ccccc21 10.1021/acs.jmedchem.1c00703
127027375 144618 0 None - 0 Rat 5.2 pEC50 = 5.2 Binding
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 542 9 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCC(Cc3ccccc3)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3759928 144618 0 None - 0 Rat 5.2 pEC50 = 5.2 Binding
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 542 9 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCC(Cc3ccccc3)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL5267529 201412 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayAgonist 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 5 1 4 4.1 CC(C)n1nc(C(=O)NC2CC3CCC(C2)N3CC(C)(C)F)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315542 201412 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assayAgonist 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 5 1 4 4.1 CC(C)n1nc(C(=O)NC2CC3CCC(C2)N3CC(C)(C)F)c2ccccc21 10.1021/acs.jmedchem.1c00703
145972573 171388 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccc4cc(C(C)C)nn34)o2)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4215911 171388 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccc4cc(C(C)C)nn34)o2)CC1 10.1021/acs.jmedchem.8b00457
145978541 170524 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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)c2nc(C(C)C)c3ccccn23)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4205387 170524 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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)c2nc(C(C)C)c3ccccn23)CC1 10.1021/acs.jmedchem.8b00457
9800656 22322 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Concentration required to produce half-maximal response against 5-hydroxytryptamine receptor in the presence of 10 nM compound in isolated human atrial myocytesConcentration required to produce half-maximal response against 5-hydroxytryptamine receptor in the presence of 10 nM compound in isolated human atrial myocytes
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
CHEMBL121913 22322 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Concentration required to produce half-maximal response against 5-hydroxytryptamine receptor in the presence of 10 nM compound in isolated human atrial myocytesConcentration required to produce half-maximal response against 5-hydroxytryptamine receptor in the presence of 10 nM compound in isolated human atrial myocytes
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
CHEMBL5286398 201123 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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 365 5 0 6 4.3 CC(C)n1nc(-c2nnc(C3CCN(CC4CC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5288222 201190 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 399 7 1 8 3.0 COCCCN1CCC(O)(c2nnc(-c3nn(C(C)C)c4ccccc34)o2)CC1 10.1021/acs.jmedchem.1c00703
68592484 144496 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
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 420 8 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cccc2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758932 144496 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
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 420 8 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cccc2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
145968234 171561 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccn4cc(C(C)C)nc34)o2)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4218152 171561 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccn4cc(C(C)C)nc34)o2)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL5276881 201428 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 351 3 0 6 4.0 CC(C)n1nc(-c2nnc(C3CC4CCC(C3)N4C)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315816 201428 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 351 3 0 6 4.0 CC(C)n1nc(-c2nnc(C3CC4CCC(C3)N4C)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
145966863 170924 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 370 8 1 5 2.4 COCCCN1CC2C(CNC(=O)c3cccc4cc(C(C)C)nn34)C2C1 10.1021/acs.jmedchem.8b00457
CHEMBL4210176 170924 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 370 8 1 5 2.4 COCCCN1CC2C(CNC(=O)c3cccc4cc(C(C)C)nn34)C2C1 10.1021/acs.jmedchem.8b00457
CHEMBL5287000 201148 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 358 5 1 4 3.3 CC(C)n1nc(C(=O)NC2CC3CCC(C2)N3CCF)c2ccccc21 10.1021/acs.jmedchem.1c00703
68593479 144577 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
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 422 8 2 8 1.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cncn2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3759601 144577 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
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 422 8 2 8 1.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cncn2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
155558212 181505 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Inhibition of 5-HT4 receptor (unknown origin)Inhibition of 5-HT4 receptor (unknown origin)
ChEMBL 344 2 1 3 2.3 CC(C)N1C(=O)N(C(=O)NC2CC3CCC(C2)N3C)C2C=CC=CC21 10.1016/j.ejmech.2019.111569
CHEMBL4560185 181505 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Inhibition of 5-HT4 receptor (unknown origin)Inhibition of 5-HT4 receptor (unknown origin)
ChEMBL 344 2 1 3 2.3 CC(C)N1C(=O)N(C(=O)NC2CC3CCC(C2)N3C)C2C=CC=CC21 10.1016/j.ejmech.2019.111569
CHEMBL5286814 201137 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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 379 4 0 6 4.8 CC(C)n1nc(-c2nnc(C3CCN(C4CCCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
44343153 117124 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Tested for ability to stimulate production of cAMP mediated by 5-hydroxytryptamine 4 receptor in mouse Coliculi neuronsTested for ability to stimulate production of cAMP mediated by 5-hydroxytryptamine 4 receptor in mouse Coliculi neurons
ChEMBL 356 2 1 5 3.0 CC(C)n1c(=O)n(C(=O)NC2CC3CCCC(C2)N3C)c2ccccc21 10.1021/jm020099f
CHEMBL324057 117124 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Tested for ability to stimulate production of cAMP mediated by 5-hydroxytryptamine 4 receptor in mouse Coliculi neuronsTested for ability to stimulate production of cAMP mediated by 5-hydroxytryptamine 4 receptor in mouse Coliculi neurons
ChEMBL 356 2 1 5 3.0 CC(C)n1c(=O)n(C(=O)NC2CC3CCCC(C2)N3C)c2ccccc21 10.1021/jm020099f
9975257 55528 1 None - 0 Human 7.1 pEC50 = 7.1 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against cisaprideTested for 5-hydroxytryptamine 4 binding affinity against cisapride
ChEMBL 351 3 2 4 3.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2C(C)CCCC2C1 10.1021/jm020099f
CHEMBL15585 55528 1 None - 0 Human 7.1 pEC50 = 7.1 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against cisaprideTested for 5-hydroxytryptamine 4 binding affinity against cisapride
ChEMBL 351 3 2 4 3.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2C(C)CCCC2C1 10.1021/jm020099f
9797313 108706 2 None - 3 Human 7.1 pEC50 = 7.1 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against cisaprideTested for 5-hydroxytryptamine 4 binding affinity against cisapride
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1021/jm020099f
CHEMBL301039 108706 2 None - 3 Human 7.1 pEC50 = 7.1 Binding
Tested for 5-hydroxytryptamine 4 binding affinity against cisaprideTested for 5-hydroxytryptamine 4 binding affinity against cisapride
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1021/jm020099f
9928343 110247 0 None - 1 Guinea pig 7.1 pEC50 = 7.1 Binding
Effective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligandEffective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligand
ChEMBL 349 4 2 4 2.2 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
CHEMBL3085015 110247 0 None - 1 Guinea pig 7.1 pEC50 = 7.1 Binding
Effective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligandEffective concentration required towards 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as the radioligand
ChEMBL 349 4 2 4 2.2 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
145978151 170706 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
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 353 4 0 6 4.1 CC(C)c1nc(-c2nnc(C3CCN(C(C)C)CC3)o2)n2ccccc12 10.1021/acs.jmedchem.8b00457
CHEMBL4207406 170706 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
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 353 4 0 6 4.1 CC(C)c1nc(-c2nnc(C3CCN(C(C)C)CC3)o2)n2ccccc12 10.1021/acs.jmedchem.8b00457
145964746 170929 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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 399 6 1 6 2.7 CC(C)c1nc2c(C(=O)NCC3CCN(CC4CCOCC4)CC3)cccn2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4210213 170929 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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 399 6 1 6 2.7 CC(C)c1nc2c(C(=O)NCC3CCN(CC4CCOCC4)CC3)cccn2n1 10.1021/acs.jmedchem.8b00457
CHEMBL5277726 200723 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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 395 4 0 7 4.0 CC(C)n1nc(-c2nnc(C3CCN(C4CCOCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
145977409 170635 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
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 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3nc(C(C)C)c4ccccn34)o2)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4206608 170635 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
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 383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3nc(C(C)C)c4ccccn34)o2)CC1 10.1021/acs.jmedchem.8b00457
145978067 170514 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 453 6 1 6 2.8 COC(=O)N1CCC(CN2CC3C(CNC(=O)c4cccc5cc(C(C)C)nn45)C3C2)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4205273 170514 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 453 6 1 6 2.8 COC(=O)N1CCC(CN2CC3C(CNC(=O)c4cccc5cc(C(C)C)nn45)C3C2)CC1 10.1021/acs.jmedchem.8b00457
145965914 170914 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 441 5 1 6 3.1 COC(=O)N1CCC(N2CCC(CNC(=O)c3cccn4cc(C(C)C)nc34)CC2)CC1 10.1021/acs.jmedchem.8b00457
CHEMBL4210063 170914 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 441 5 1 6 3.1 COC(=O)N1CCC(N2CCC(CNC(=O)c3cccn4cc(C(C)C)nc34)CC2)CC1 10.1021/acs.jmedchem.8b00457
11961293 10541 19 None - 1 Guinea pig 8.1 pEC50 = 8.1 Binding
Agonist activity at 5-HT4 receptor in guinea pig colonAgonist activity at 5-HT4 receptor in guinea pig colon
ChEMBL 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 10.1016/j.ejmech.2015.08.051
8426 10541 19 None - 1 Guinea pig 8.1 pEC50 = 8.1 Binding
Agonist activity at 5-HT4 receptor in guinea pig colonAgonist activity at 5-HT4 receptor in guinea pig colon
ChEMBL 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 10.1016/j.ejmech.2015.08.051
CHEMBL2402904 10541 19 None - 1 Guinea pig 8.1 pEC50 = 8.1 Binding
Agonist activity at 5-HT4 receptor in guinea pig colonAgonist activity at 5-HT4 receptor in guinea pig colon
ChEMBL 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 10.1016/j.ejmech.2015.08.051
DB12725 10541 19 None - 1 Guinea pig 8.1 pEC50 = 8.1 Binding
Agonist activity at 5-HT4 receptor in guinea pig colonAgonist activity at 5-HT4 receptor in guinea pig colon
ChEMBL 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 10.1016/j.ejmech.2015.08.051
CHEMBL5283820 201009 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 353 4 0 6 4.3 CC(C)N1CCC(c2nc(-c3nn(C(C)C)c4ccccc34)no2)CC1 10.1021/acs.jmedchem.1c00703
183782 10171 20 None - 14 Rat 8.1 pEC50 = 8.1 Binding
Agonist activity at 5-HT4 receptor in Sprague-Dawley rat oesophagus assessed as relaxation of carbachol precontracted oesophagusAgonist activity at 5-HT4 receptor in Sprague-Dawley rat oesophagus assessed as relaxation of carbachol precontracted oesophagus
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2015.08.051
237 10171 20 None - 14 Rat 8.1 pEC50 = 8.1 Binding
Agonist activity at 5-HT4 receptor in Sprague-Dawley rat oesophagus assessed as relaxation of carbachol precontracted oesophagusAgonist activity at 5-HT4 receptor in Sprague-Dawley rat oesophagus assessed as relaxation of carbachol precontracted oesophagus
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2015.08.051
CHEMBL85251 10171 20 None - 14 Rat 8.1 pEC50 = 8.1 Binding
Agonist activity at 5-HT4 receptor in Sprague-Dawley rat oesophagus assessed as relaxation of carbachol precontracted oesophagusAgonist activity at 5-HT4 receptor in Sprague-Dawley rat oesophagus assessed as relaxation of carbachol precontracted oesophagus
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2015.08.051
145964157 171107 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 396 6 1 5 2.8 CC(C)c1cc2cccc(C(=O)NCC3C4CN(CC5CCOCC5)CC34)n2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4212433 171107 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 396 6 1 5 2.8 CC(C)c1cc2cccc(C(=O)NCC3C4CN(CC5CCOCC5)CC34)n2n1 10.1021/acs.jmedchem.8b00457
145977034 170395 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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)c1nc(C(=O)NCC2CCN(CC3CCOCC3)CC2)n2ccccc12 10.1021/acs.jmedchem.8b00457
CHEMBL4203734 170395 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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)c1nc(C(=O)NCC2CCN(CC3CCOCC3)CC2)n2ccccc12 10.1021/acs.jmedchem.8b00457
CHEMBL5290981 201442 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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(-c2nnc(C3CCN(CC4CCOCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5316123 201442 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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(-c2nnc(C3CCN(CC4CCOCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
145968730 171619 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 342 5 1 4 3.3 CC(C)c1cn2cccc(C(=O)NCC3CCN(C(C)C)CC3)c2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4218868 171619 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 342 5 1 4 3.3 CC(C)c1cn2cccc(C(=O)NCC3CCN(C(C)C)CC3)c2n1 10.1021/acs.jmedchem.8b00457
145974160 171359 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
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 342 5 1 4 3.3 CC(C)c1cc2cccc(C(=O)NCC3CCN(C(C)C)CC3)n2n1 10.1021/acs.jmedchem.8b00457
CHEMBL4215511 171359 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
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 342 5 1 4 3.3 CC(C)c1cc2cccc(C(=O)NCC3CCN(C(C)C)CC3)n2n1 10.1021/acs.jmedchem.8b00457
CHEMBL5280230 201435 0 None - 0 Human 6.0 pEC50 = 6 Binding
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 393 5 0 6 4.9 CC(C)n1nc(-c2nnc(CC3CCN(C4CCCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
CHEMBL5315982 201435 0 None - 0 Human 6.0 pEC50 = 6 Binding
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 393 5 0 6 4.9 CC(C)n1nc(-c2nnc(CC3CCN(C4CCCC4)CC3)o2)c2ccccc21 10.1021/acs.jmedchem.1c00703
15166837 129166 0 None - 1 Rat 5.9 pED50 = 5.9 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 337 5 2 4 2.5 CCOc1cc(N)c(Cl)cc1C(=O)NCC1CCN2CCCC12 10.1021/jm00086a019
CHEMBL36005 129166 0 None - 1 Rat 5.9 pED50 = 5.9 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 337 5 2 4 2.5 CCOc1cc(N)c(Cl)cc1C(=O)NCC1CCN2CCCC12 10.1021/jm00086a019
5 6927 72 None -117 53 Rat 7.8 pED50 = 7.8 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00086a019
5202 6927 72 None -117 53 Rat 7.8 pED50 = 7.8 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00086a019
CHEMBL39 6927 72 None -117 53 Rat 7.8 pED50 = 7.8 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00086a019
DB08839 6927 72 None -117 53 Rat 7.8 pED50 = 7.8 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00086a019
57391435 74505 0 None - 0 Rat 6.8 pED50 = 6.8 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 307 3 2 4 1.4 COc1cc(N)c(Cl)cc1C(=O)N[C@]12CN3CCC1C2C3 10.1021/jm00086a019
CHEMBL1907770 74505 0 None - 0 Rat 6.8 pED50 = 6.8 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 307 3 2 4 1.4 COc1cc(N)c(Cl)cc1C(=O)N[C@]12CN3CCC1C2C3 10.1021/jm00086a019
15166838 48466 0 None - 0 Rat 6.7 pED50 = 6.7 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 309 3 2 4 1.9 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCCC12 10.1021/jm00086a019
CHEMBL14923 48466 0 None - 0 Rat 6.7 pED50 = 6.7 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 309 3 2 4 1.9 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCCC12 10.1021/jm00086a019
10358856 126966 0 None - 1 Rat 5.6 pED50 = 5.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.3 CCOc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCCC12 10.1021/jm00086a019
CHEMBL35180 126966 0 None - 1 Rat 5.6 pED50 = 5.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.3 CCOc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCCC12 10.1021/jm00086a019
132337 10316 15 None - 2 Rat 7.6 pED50 = 7.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm00086a019
238 10316 15 None - 2 Rat 7.6 pED50 = 7.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm00086a019
CHEMBL34291 10316 15 None - 2 Rat 7.6 pED50 = 7.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm00086a019
1782 9296 84 None -11 23 Rat 4.6 pED50 = 4.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm00086a019
241 9296 84 None -11 23 Rat 4.6 pED50 = 4.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm00086a019
4168 9296 84 None -11 23 Rat 4.6 pED50 = 4.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm00086a019
CHEMBL86 9296 84 None -11 23 Rat 4.6 pED50 = 4.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm00086a019
DB01233 9296 84 None -11 23 Rat 4.6 pED50 = 4.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm00086a019
15095972 144323 0 None - 0 Rat 6.6 pED50 = 6.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN2CCCC12 10.1021/jm00086a019
CHEMBL37544 144323 0 None - 0 Rat 6.6 pED50 = 6.6 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN2CCCC12 10.1021/jm00086a019
15095973 143046 0 None - 0 Rat 6.5 pED50 = 6.5 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN2CCC[C@H]12 10.1021/jm00086a019
CHEMBL37333 143046 0 None - 0 Rat 6.5 pED50 = 6.5 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN2CCC[C@H]12 10.1021/jm00086a019
15166838 48466 0 None - 0 Rat 5.5 pED50 = 5.5 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 309 3 2 4 1.9 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCCC12 10.1021/jm00086a019
CHEMBL14923 48466 0 None - 0 Rat 5.5 pED50 = 5.5 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 309 3 2 4 1.9 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCCC12 10.1021/jm00086a019
44283512 146958 0 None - 0 Rat 7.4 pED50 = 7.4 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 341 3 0 5 3.3 CC(C)n1c(=O)n(C(=O)CC2CC3CCC(C2)N3C)c2ccccc21 10.1021/jm00086a019
CHEMBL38041 146958 0 None - 0 Rat 7.4 pED50 = 7.4 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 341 3 0 5 3.3 CC(C)n1c(=O)n(C(=O)CC2CC3CCC(C2)N3C)c2ccccc21 10.1021/jm00086a019
44374544 59927 0 None - 1 Rat 7.4 pED50 = 7.4 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCC1C2 10.1021/jm00086a019
CHEMBL159825 59927 0 None - 1 Rat 7.4 pED50 = 7.4 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCC1C2 10.1021/jm00086a019
9819593 105580 3 None 1 2 Rat 6.3 pED50 = 6.3 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 10.1021/jm00086a019
CHEMBL27846 105580 3 None 1 2 Rat 6.3 pED50 = 6.3 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 10.1021/jm00086a019
240 7731 43 None -8 25 Rat 7.3 pED50 = 7.3 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
2769 7731 43 None -8 25 Rat 7.3 pED50 = 7.3 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
44279790 7731 43 None -8 25 Rat 7.3 pED50 = 7.3 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
660 7731 43 None -8 25 Rat 7.3 pED50 = 7.3 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
CHEMBL1729 7731 43 None -8 25 Rat 7.3 pED50 = 7.3 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
CHEMBL560739 7731 43 None -8 25 Rat 7.3 pED50 = 7.3 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
DB00604 7731 43 None -8 25 Rat 7.3 pED50 = 7.3 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
15095972 144323 0 None - 0 Rat 7.2 pED50 = 7.2 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN2CCCC12 10.1021/jm00086a019
CHEMBL37544 144323 0 None - 0 Rat 7.2 pED50 = 7.2 Binding
Relaxation of carbachol induced contractions of rat tunica muscularis mucosaeRelaxation of carbachol induced contractions of rat tunica muscularis mucosae
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN2CCCC12 10.1021/jm00086a019
9864179 128132 0 None - 0 Guinea pig 10.6 pIC50 = 10.6 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 370 6 0 5 4.1 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1021/jm00024a002
CHEMBL358119 128132 0 None - 0 Guinea pig 10.6 pIC50 = 10.6 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 370 6 0 5 4.1 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1021/jm00024a002
9864179 128132 0 None - 0 Guinea pig 10.6 pIC50 = 10.6 Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
ChEMBL 370 6 0 5 4.1 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/S0960-894X(01)80176-1
CHEMBL358119 128132 0 None - 0 Guinea pig 10.6 pIC50 = 10.6 Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
ChEMBL 370 6 0 5 4.1 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/S0960-894X(01)80176-1
54575167 158811 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 454 8 2 5 4.4 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2ccc3ccccc32)CC1 nan
CHEMBL3967117 158811 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 454 8 2 5 4.4 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2ccc3ccccc32)CC1 nan
54575171 156843 2 None - 0 Human 10.2 pIC50 = 10.2 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 406 8 2 7 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2ccnn2)CC1 nan
CHEMBL3950712 156843 2 None - 0 Human 10.2 pIC50 = 10.2 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 406 8 2 7 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2ccnn2)CC1 nan
54575225 154789 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 440 6 2 5 4.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2cn(C)c3ccccc23)CC1 nan
CHEMBL3934371 154789 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 440 6 2 5 4.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2cn(C)c3ccccc23)CC1 nan
121881 10263 27 None 2 15 Guinea pig 10.1 pIC50 = 10.1 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1021/jm00024a002
256 10263 27 None 2 15 Guinea pig 10.1 pIC50 = 10.1 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1021/jm00024a002
CHEMBL68131 10263 27 None 2 15 Guinea pig 10.1 pIC50 = 10.1 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1021/jm00024a002
121881 10263 27 None 2 15 Guinea pig 10.1 pIC50 = 10.1 Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/S0960-894X(01)80176-1
256 10263 27 None 2 15 Guinea pig 10.1 pIC50 = 10.1 Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/S0960-894X(01)80176-1
CHEMBL68131 10263 27 None 2 15 Guinea pig 10.1 pIC50 = 10.1 Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/S0960-894X(01)80176-1
10617443 40821 0 None - 0 Guinea pig 10.0 pIC50 = 10 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 344 7 1 4 3.8 CCCCN1CCC(COC(=O)c2c(OC)[nH]c3ccccc23)CC1 10.1021/jm00024a002
CHEMBL142490 40821 0 None - 0 Guinea pig 10.0 pIC50 = 10 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 344 7 1 4 3.8 CCCCN1CCC(COC(=O)c2c(OC)[nH]c3ccccc23)CC1 10.1021/jm00024a002
10736989 43658 0 None - 0 Guinea pig 10.0 pIC50 = 10 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 356 6 0 5 3.7 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCO3)CC1 10.1021/jm00024a002
CHEMBL145075 43658 0 None - 0 Guinea pig 10.0 pIC50 = 10 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 356 6 0 5 3.7 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCO3)CC1 10.1021/jm00024a002
10736989 43658 0 None - 0 Guinea pig 10.0 pIC50 = 10 Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
ChEMBL 356 6 0 5 3.7 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCO3)CC1 10.1016/S0960-894X(01)80176-1
CHEMBL145075 43658 0 None - 0 Guinea pig 10.0 pIC50 = 10 Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
ChEMBL 356 6 0 5 3.7 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCO3)CC1 10.1016/S0960-894X(01)80176-1
54575170 153766 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 434 10 2 7 2.8 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCCCn2ccnn2)CC1 nan
CHEMBL3926377 153766 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 434 10 2 7 2.8 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCCCn2ccnn2)CC1 nan
54575227 149307 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 405 6 2 4 3.7 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2ccc(F)cc2)CC1 nan
CHEMBL3890747 149307 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 405 6 2 4 3.7 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2ccc(F)cc2)CC1 nan
10691444 42274 0 None - 0 Guinea pig 9.8 pIC50 = 9.8 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 384 6 0 5 4.5 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCCO3)CC1 10.1021/jm00024a002
CHEMBL143862 42274 0 None - 0 Guinea pig 9.8 pIC50 = 9.8 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 384 6 0 5 4.5 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCCO3)CC1 10.1021/jm00024a002
10691444 42274 0 None - 0 Guinea pig 9.8 pIC50 = 9.8 Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
ChEMBL 384 6 0 5 4.5 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCCO3)CC1 10.1016/S0960-894X(01)80176-1
CHEMBL143862 42274 0 None - 0 Guinea pig 9.8 pIC50 = 9.8 Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
ChEMBL 384 6 0 5 4.5 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCCO3)CC1 10.1016/S0960-894X(01)80176-1
54575166 161120 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 407 8 2 8 1.4 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2cnnn2)CC1 nan
CHEMBL3986866 161120 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 407 8 2 8 1.4 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2cnnn2)CC1 nan
54575223 157633 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 406 8 2 7 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2nccn2)CC1 nan
CHEMBL3957180 157633 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 406 8 2 7 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2nccn2)CC1 nan
66780300 156247 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 406 8 2 7 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2cncn2)CC1 nan
CHEMBL3946162 156247 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 406 8 2 7 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2cncn2)CC1 nan
54575168 153972 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 419 8 2 6 3.0 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2ccnc2C)CC1 nan
CHEMBL3928124 153972 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 419 8 2 6 3.0 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2ccnc2C)CC1 nan
54575224 160601 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 388 6 2 5 3.0 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2cccnc2)CC1 nan
CHEMBL3982522 160601 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 388 6 2 5 3.0 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2cccnc2)CC1 nan
240 7731 43 None -11 25 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 7731 43 None -11 25 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 7731 43 None -11 25 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 7731 43 None -11 25 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 7731 43 None -11 25 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 7731 43 None -11 25 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 7731 43 None -11 25 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
54575228 152965 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 403 6 3 5 3.3 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2ccc(O)cc2)CC1 nan
CHEMBL3920018 152965 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 403 6 3 5 3.3 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2ccc(O)cc2)CC1 nan
53472864 152347 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 390 6 2 5 2.9 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2cccn2C)CC1 nan
CHEMBL3915236 152347 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 390 6 2 5 2.9 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2cccn2C)CC1 nan
54575226 151767 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 377 6 3 5 2.3 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2ncc[nH]2)CC1 nan
CHEMBL3910849 151767 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT).
ChEMBL 377 6 3 5 2.3 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2ncc[nH]2)CC1 nan
10852772 41901 1 None - 0 Guinea pig 9.3 pIC50 = 9.3 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 314 6 1 3 3.8 CCCCN1CCC(COC(=O)c2c[nH]c3ccccc23)CC1 10.1021/jm00024a002
CHEMBL143426 41901 1 None - 0 Guinea pig 9.3 pIC50 = 9.3 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 314 6 1 3 3.8 CCCCN1CCC(COC(=O)c2c[nH]c3ccccc23)CC1 10.1021/jm00024a002
10852772 41901 1 None - 0 Guinea pig 9.3 pIC50 = 9.3 Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
ChEMBL 314 6 1 3 3.8 CCCCN1CCC(COC(=O)c2c[nH]c3ccccc23)CC1 10.1016/S0960-894X(01)80176-1
CHEMBL143426 41901 1 None - 0 Guinea pig 9.3 pIC50 = 9.3 Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
ChEMBL 314 6 1 3 3.8 CCCCN1CCC(COC(=O)c2c[nH]c3ccccc23)CC1 10.1016/S0960-894X(01)80176-1
9881053 127023 0 None - 1 Mouse 9.3 pIC50 = 9.3 Binding
Ability to displace [3H]GR-113808 from mouse 5-hydroxytryptamine 4 receptor in COS7 cellsAbility to displace [3H]GR-113808 from mouse 5-hydroxytryptamine 4 receptor in COS7 cells
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL35226 127023 0 None - 1 Mouse 9.3 pIC50 = 9.3 Binding
Ability to displace [3H]GR-113808 from mouse 5-hydroxytryptamine 4 receptor in COS7 cellsAbility to displace [3H]GR-113808 from mouse 5-hydroxytryptamine 4 receptor in COS7 cells
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
177336 9894 50 None 6 3 Human 9.2 pIC50 = 9.2 Binding
Binding affinity was determined against 5-hydroxytryptamine 3 receptorBinding affinity was determined against 5-hydroxytryptamine 3 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm00024a002
225 9894 50 None 6 3 Human 9.2 pIC50 = 9.2 Binding
Binding affinity was determined against 5-hydroxytryptamine 3 receptorBinding affinity was determined against 5-hydroxytryptamine 3 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm00024a002
CHEMBL356359 9894 50 None 6 3 Human 9.2 pIC50 = 9.2 Binding
Binding affinity was determined against 5-hydroxytryptamine 3 receptorBinding affinity was determined against 5-hydroxytryptamine 3 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm00024a002
DB04873 9894 50 None 6 3 Human 9.2 pIC50 = 9.2 Binding
Binding affinity was determined against 5-hydroxytryptamine 3 receptorBinding affinity was determined against 5-hydroxytryptamine 3 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm00024a002
90666907 116228 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 467 7 1 8 3.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2-c2cnccn2)CC1 10.1039/C1MD00213A
CHEMBL3220223 116228 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 467 7 1 8 3.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2-c2cnccn2)CC1 10.1039/C1MD00213A
44300153 204265 0 None - 1 Guinea pig 6.0 pIC50 = 6 Binding
Binding affinity towards 5-HT4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-HT4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 323 3 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC1CN2C 10.1016/s0960-894x(01)00693-x
CHEMBL56994 204265 0 None - 1 Guinea pig 6.0 pIC50 = 6 Binding
Binding affinity towards 5-HT4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-HT4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 323 3 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC1CN2C 10.1016/s0960-894x(01)00693-x
44300154 205177 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 323 3 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC1N(C)C2 10.1016/s0960-894x(01)00693-x
CHEMBL57686 205177 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 323 3 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC1N(C)C2 10.1016/s0960-894x(01)00693-x
3245407 54879 25 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptorDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL1550957 54879 25 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptorDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
10590554 215160 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
Displacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor in guinea pig striatum
ChEMBL 303 3 2 5 0.1 CN1CCN(CCNC(=O)n2c(=O)[nH]c3ccccc32)CC1 10.1021/jm981098j
CHEMBL99577 215160 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
Displacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor in guinea pig striatum
ChEMBL 303 3 2 5 0.1 CN1CCN(CCNC(=O)n2c(=O)[nH]c3ccccc32)CC1 10.1021/jm981098j
155525723 177864 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
ChEMBL 515 11 3 7 4.2 COc1cc(/C=C/C(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)ccc1O 10.1016/j.ejmech.2019.111596
CHEMBL4457426 177864 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
ChEMBL 515 11 3 7 4.2 COc1cc(/C=C/C(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)ccc1O 10.1016/j.ejmech.2019.111596
176155 10937 0 None -1 4 Guinea pig 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 377 4 1 3 4.7 C[S+]([O-])c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 nan
CHEMBL10 10937 0 None -1 4 Guinea pig 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 377 4 1 3 4.7 C[S+]([O-])c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 nan
2585 7590 103 None -57 22 Guinea pig 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 7590 103 None -57 22 Guinea pig 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 7590 103 None -57 22 Guinea pig 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 7590 103 None -57 22 Guinea pig 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 7590 103 None -57 22 Guinea pig 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
44385634 68882 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 465 10 3 6 3.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL177573 68882 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 465 10 3 6 3.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
90644473 119057 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assayAntagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 353 5 0 5 2.7 COc1cc2c3c(cccc3n1)C(=O)N(CCCN1CCCCC1)C2=O 10.1016/j.ejmech.2014.05.015
CHEMBL3291078 119057 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assayAntagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 353 5 0 5 2.7 COc1cc2c3c(cccc3n1)C(=O)N(CCCN1CCCCC1)C2=O 10.1016/j.ejmech.2014.05.015
127027374 144445 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 423 8 2 9 0.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2ncnn2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758523 144445 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 423 8 2 9 0.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2ncnn2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
119584 9373 102 None -1 6 Guinea pig 7.0 pIC50 = 7.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1016/s0960-894x(02)00060-4
1848 9373 102 None -1 6 Guinea pig 7.0 pIC50 = 7.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1016/s0960-894x(02)00060-4
242 9373 102 None -1 6 Guinea pig 7.0 pIC50 = 7.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1016/s0960-894x(02)00060-4
CHEMBL60889 9373 102 None -1 6 Guinea pig 7.0 pIC50 = 7.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1016/s0960-894x(02)00060-4
DB11675 9373 102 None -1 6 Guinea pig 7.0 pIC50 = 7.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1016/s0960-894x(02)00060-4
2274 9947 58 None -17 31 Guinea pig 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 9947 58 None -17 31 Guinea pig 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 9947 58 None -17 31 Guinea pig 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 9947 58 None -17 31 Guinea pig 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 9947 58 None -17 31 Guinea pig 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
127027397 144408 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 421 8 2 7 2.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2ccnc2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758199 144408 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 421 8 2 7 2.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2ccnc2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
68592173 144619 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
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 144619 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
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
31703 201496 63 None 1 3 Guinea pig 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
CHEMBL359744 201496 63 None 1 3 Guinea pig 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
CHEMBL53463 201496 63 None 1 3 Guinea pig 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
68593479 144577 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 422 8 2 8 1.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cncn2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3759601 144577 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 422 8 2 8 1.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cncn2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
44214754 67173 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 437 8 3 6 2.2 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL174935 67173 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 437 8 3 6 2.2 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
68592826 144459 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 496 8 2 7 3.0 CCCOC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
CHEMBL3758641 144459 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 496 8 2 7 3.0 CCCOC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
25016328 144603 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 480 7 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)C(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3759860 144603 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 480 7 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)C(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
3397 212267 112 None 1 2 Guinea pig 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
CHEMBL806 212267 112 None 1 2 Guinea pig 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
44384769 138141 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 451 8 3 6 2.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CC(C)CN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL368844 138141 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 451 8 3 6 2.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CC(C)CN)CC2)CC1 10.1016/s0960-894x(02)00060-4
44386218 172926 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 423 7 3 6 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL426216 172926 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 423 7 3 6 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
44386168 175061 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 453 8 4 7 1.2 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CC(O)CN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL433984 175061 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 453 8 4 7 1.2 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CC(O)CN)CC2)CC1 10.1016/s0960-894x(02)00060-4
155565664 182382 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
ChEMBL 432 8 2 6 4.5 COc1ccc(CN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1O 10.1016/j.ejmech.2019.111596
CHEMBL4580044 182382 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
ChEMBL 432 8 2 6 4.5 COc1ccc(CN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1O 10.1016/j.ejmech.2019.111596
16005860 194185 7 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT4 receptorInhibition of 5HT4 receptor
ChEMBL 388 5 1 2 4.8 CC(C)(C)CCN1CC[C@H](CNC(=O)c2cc(Cl)cc(Cl)c2)[C@H](F)C1 10.1021/jm800830n
CHEMBL493677 194185 7 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT4 receptorInhibition of 5HT4 receptor
ChEMBL 388 5 1 2 4.8 CC(C)(C)CCN1CC[C@H](CNC(=O)c2cc(Cl)cc(Cl)c2)[C@H](F)C1 10.1021/jm800830n
5 6927 72 None -117 53 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptorInhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970376w
5202 6927 72 None -117 53 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptorInhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970376w
CHEMBL39 6927 72 None -117 53 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptorInhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970376w
DB08839 6927 72 None -117 53 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptorInhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970376w
441383 27105 57 None -5 17 Guinea pig 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 27105 57 None -5 17 Guinea pig 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
10784420 127796 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 355 6 1 4 3.3 CCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCO3)CC1 10.1021/jm00024a002
CHEMBL356546 127796 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 355 6 1 4 3.3 CCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCO3)CC1 10.1021/jm00024a002
87509467 144461 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 496 7 2 6 3.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=S)C(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758674 144461 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 496 7 2 6 3.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=S)C(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
1043 8363 14 None -2884 29 Guinea pig 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 8363 14 None -2884 29 Guinea pig 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 8363 14 None -2884 29 Guinea pig 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 8363 14 None -2884 29 Guinea pig 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 8363 14 None -2884 29 Guinea pig 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
10645984 25589 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(Cl)c2)CC1 10.1039/C1MD00213A
CHEMBL127876 25589 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(Cl)c2)CC1 10.1039/C1MD00213A
133 9274 52 None -79 43 Guinea pig 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 9274 52 None -79 43 Guinea pig 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 9274 52 None -79 43 Guinea pig 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 9274 52 None -79 43 Guinea pig 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 9274 52 None -79 43 Guinea pig 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
10645103 171120 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 407 6 1 6 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2F)CC1 10.1039/C1MD00213A
CHEMBL421256 171120 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 407 6 1 6 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2F)CC1 10.1039/C1MD00213A
68593295 144565 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 480 8 2 6 2.8 CCCC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
CHEMBL3759546 144565 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 480 8 2 6 2.8 CCCC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
10669778 124253 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1ccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1039/C1MD00213A
CHEMBL339936 124253 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1ccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1039/C1MD00213A
3019427 67156 33 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 313 4 3 5 1.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCNCC1OC 10.1016/j.bmcl.2009.08.016
CHEMBL1748 67156 33 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 313 4 3 5 1.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCNCC1OC 10.1016/j.bmcl.2009.08.016
68593458 144621 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 468 6 2 7 2.2 COC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
CHEMBL3759969 144621 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 468 6 2 7 2.2 COC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
90644474 119058 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Partial agonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as effect on serotonin-induced receptor/Gbeta1 coupling by BRET assayPartial agonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as effect on serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 343 4 0 3 3.7 O=C1c2cc(Cl)nc3cccc(c23)CN1CCCN1CCCCC1 10.1016/j.ejmech.2014.05.015
CHEMBL3291079 119058 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Partial agonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as effect on serotonin-induced receptor/Gbeta1 coupling by BRET assayPartial agonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as effect on serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 343 4 0 3 3.7 O=C1c2cc(Cl)nc3cccc(c23)CN1CCCN1CCCCC1 10.1016/j.ejmech.2014.05.015
10591304 45215 2 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 313 6 2 2 3.4 CCCCN1CCC(CNC(=O)c2c[nH]c3ccccc23)CC1 10.1021/jm00024a002
CHEMBL146386 45215 2 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 313 6 2 2 3.4 CCCCN1CCC(CNC(=O)c2c[nH]c3ccccc23)CC1 10.1021/jm00024a002
44384896 67066 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 479 7 3 6 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(N)C(C)C)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL174284 67066 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 479 7 3 6 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(N)C(C)C)CC2)CC1 10.1016/s0960-894x(02)00060-4
44384728 66601 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 479 8 3 6 2.5 CCCC(N)C(=O)N1CCC(CN2CCC(NC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL172802 66601 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 479 8 3 6 2.5 CCCC(N)C(=O)N1CCC(CN2CCC(NC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1016/s0960-894x(02)00060-4
44384721 137443 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 465 6 3 6 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(C)(C)N)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL368213 137443 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 465 6 3 6 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(C)(C)N)CC2)CC1 10.1016/s0960-894x(02)00060-4
90644470 119055 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assayAntagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 328 6 0 5 3.3 COc1cc(C(=O)OCCCN2CCCCC2)c2ccccc2n1 10.1016/j.ejmech.2014.05.015
CHEMBL3291075 119055 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assayAntagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 328 6 0 5 3.3 COc1cc(C(=O)OCCCN2CCCCC2)c2ccccc2n1 10.1016/j.ejmech.2014.05.015
44385584 136963 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 515 10 3 7 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCNS(C)(=O)=O)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL367877 136963 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 515 10 3 7 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCNS(C)(=O)=O)CC2)CC1 10.1016/s0960-894x(02)00060-4
2353 107889 82 None -1 5 Guinea pig 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL12089 107889 82 None -1 5 Guinea pig 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL295124 107889 82 None -1 5 Guinea pig 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
4223 10764 94 None - 3 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
6918314 10764 94 None - 3 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
7427 10764 94 None - 3 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
CHEMBL439849 10764 94 None - 3 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
DB06684 10764 94 None - 3 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
240 7731 43 None -4 25 Guinea pig 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 7731 43 None -4 25 Guinea pig 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 7731 43 None -4 25 Guinea pig 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 7731 43 None -4 25 Guinea pig 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 7731 43 None -4 25 Guinea pig 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 7731 43 None -4 25 Guinea pig 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 7731 43 None -4 25 Guinea pig 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
10550242 24029 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2Cl)CC1 10.1039/C1MD00213A
CHEMBL125670 24029 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2Cl)CC1 10.1039/C1MD00213A
11796362 121879 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)c1 10.1039/C1MD00213A
CHEMBL334325 121879 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)c1 10.1039/C1MD00213A
44384735 66683 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 479 9 3 6 2.5 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CCCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL173089 66683 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 479 9 3 6 2.5 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CCCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
44384689 66409 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 465 8 3 6 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL172074 66409 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 465 8 3 6 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
5 6927 72 None -288 53 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111596
5202 6927 72 None -288 53 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111596
CHEMBL39 6927 72 None -288 53 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111596
DB08839 6927 72 None -288 53 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111596
260 10641 54 None -45 6 Guinea pig 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 nan
2775 10641 54 None -45 6 Guinea pig 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 nan
656665 10641 54 None -45 6 Guinea pig 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 nan
CHEMBL56564 10641 54 None -45 6 Guinea pig 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 nan
DB11699 10641 54 None -45 6 Guinea pig 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 nan
68592299 144532 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 466 7 2 6 2.4 CCC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
CHEMBL3759259 144532 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 466 7 2 6 2.4 CCC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
68593622 144431 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 482 7 2 7 2.6 CCOC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
CHEMBL3758398 144431 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 482 7 2 7 2.6 CCOC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
3168 16034 92 None -93 22 Guinea pig 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 16034 92 None -93 22 Guinea pig 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
44626295 204553 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 531 8 3 7 3.8 COc1cccc([C@]2(O)CCCC[C@H]2CN2CC[C@@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@@H](OC)C2)c1 10.1016/j.bmcl.2009.08.016
CHEMBL571799 204553 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 531 8 3 7 3.8 COc1cccc([C@]2(O)CCCC[C@H]2CN2CC[C@@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@@H](OC)C2)c1 10.1016/j.bmcl.2009.08.016
44385532 68058 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 453 8 4 7 1.2 COc1cc(N)c(Cl)cc1C(=O)NCC(O)CN1CCC(CN2CCC(N)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL176672 68058 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 453 8 4 7 1.2 COc1cc(N)c(Cl)cc1C(=O)NCC(O)CN1CCC(CN2CCC(N)CC2)CC1 10.1016/s0960-894x(02)00060-4
44384630 135796 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 479 7 3 6 1.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(C(=O)C2CCN(C(=O)CCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL366986 135796 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 479 7 3 6 1.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(C(=O)C2CCN(C(=O)CCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
12 8335 17 None - 7 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
6918513 8335 17 None - 7 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
CHEMBL267615 8335 17 None - 7 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
90644475 119059 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assayAntagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 357 4 0 4 3.4 O=C1c2cccc3nc(Cl)cc(c23)C(=O)N1CCCN1CCCCC1 10.1016/j.ejmech.2014.05.015
CHEMBL3291080 119059 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assayAntagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 357 4 0 4 3.4 O=C1c2cccc3nc(Cl)cc(c23)C(=O)N1CCCN1CCCCC1 10.1016/j.ejmech.2014.05.015
45485653 204363 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 531 8 3 7 3.8 COc1cccc([C@]2(O)CCCC[C@H]2CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)c1 10.1016/j.bmcl.2009.08.016
CHEMBL570487 204363 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 531 8 3 7 3.8 COc1cccc([C@]2(O)CCCC[C@H]2CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)c1 10.1016/j.bmcl.2009.08.016
5311047 211542 33 None -5 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
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 211542 33 None -5 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
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
182593 10168 6 None 1 3 Human 7.3 pIC50 = 7.3 Binding
Partial agonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as effect on serotonin-induced receptor/Gbeta1 coupling by BRET assayPartial agonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as effect on serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1016/j.ejmech.2014.05.015
254 10168 6 None 1 3 Human 7.3 pIC50 = 7.3 Binding
Partial agonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as effect on serotonin-induced receptor/Gbeta1 coupling by BRET assayPartial agonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as effect on serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1016/j.ejmech.2014.05.015
CHEMBL83954 10168 6 None 1 3 Human 7.3 pIC50 = 7.3 Binding
Partial agonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as effect on serotonin-induced receptor/Gbeta1 coupling by BRET assayPartial agonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as effect on serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1016/j.ejmech.2014.05.015
107715 207724 22 None -165 20 Guinea pig 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 207724 22 None -165 20 Guinea pig 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 207724 22 None -165 20 Guinea pig 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
68593871 144542 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 466 7 2 6 2.4 CCC(=O)N1CCCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)C1 10.1016/j.ejmech.2015.12.006
CHEMBL3759348 144542 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 466 7 2 6 2.4 CCC(=O)N1CCCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)C1 10.1016/j.ejmech.2015.12.006
44384684 66629 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 451 6 3 6 1.7 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(C)N)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL172899 66629 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 451 6 3 6 1.7 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(C)N)CC2)CC1 10.1016/s0960-894x(02)00060-4
44384624 172766 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 465 7 3 6 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(C)CN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL425329 172766 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 465 7 3 6 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(C)CN)CC2)CC1 10.1016/s0960-894x(02)00060-4
45485563 204579 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 475 9 3 6 3.7 COc1cccc([C@@]2(O)CCCC[C@@H]2CN(C)CCNC(=O)c2cc(Cl)c(N)cc2OC)c1 10.1016/j.bmcl.2009.08.016
CHEMBL572038 204579 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 475 9 3 6 3.7 COc1cccc([C@@]2(O)CCCC[C@@H]2CN(C)CCNC(=O)c2cc(Cl)c(N)cc2OC)c1 10.1016/j.bmcl.2009.08.016
68592632 144593 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 481 6 2 6 2.1 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)N(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3759759 144593 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 481 6 2 6 2.1 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)N(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
67922794 144498 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
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 144498 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
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
68593774 144471 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 406 7 2 6 2.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCn2cccc2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758721 144471 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 406 7 2 6 2.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCn2cccc2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
68591735 144544 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 452 6 2 6 2.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(C)=O)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3759362 144544 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 452 6 2 6 2.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(C)=O)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
87509988 144430 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 482 7 2 6 3.2 CCC(=S)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
CHEMBL3758397 144430 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 482 7 2 6 3.2 CCC(=S)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
9911674 138213 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 451 9 3 6 2.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL369037 138213 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 451 9 3 6 2.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
45485620 204199 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 531 8 3 7 3.8 COc1cccc([C@@]2(O)CCCC[C@@H]2CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)c1 10.1016/j.bmcl.2009.08.016
CHEMBL569585 204199 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 531 8 3 7 3.8 COc1cccc([C@@]2(O)CCCC[C@@H]2CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)c1 10.1016/j.bmcl.2009.08.016
10131112 8334 25 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
8428 8334 25 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
CHEMBL364005 8334 25 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
10812045 22293 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2OC)CC1 10.1039/C1MD00213A
CHEMBL121766 22293 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2OC)CC1 10.1039/C1MD00213A
68592484 144496 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 420 8 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cccc2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758932 144496 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 420 8 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cccc2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
127027375 144618 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 542 9 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCC(Cc3ccccc3)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3759928 144618 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 542 9 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCC(Cc3ccccc3)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
25016330 144421 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 480 7 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CCN(CC2CCN(C(=O)C(C)C)CC2)C[C@@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758309 144421 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 480 7 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CCN(CC2CCN(C(=O)C(C)C)CC2)C[C@@H]1OC 10.1016/j.ejmech.2015.12.006
155543353 180080 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
ChEMBL 418 7 3 6 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccc(O)c(O)c2)CC1 10.1016/j.ejmech.2019.111596
CHEMBL4526049 180080 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
ChEMBL 418 7 3 6 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccc(O)c(O)c2)CC1 10.1016/j.ejmech.2019.111596
10620001 40974 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 383 6 1 4 4.1 CCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCCO3)CC1 10.1021/jm00024a002
CHEMBL142621 40974 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 383 6 1 4 4.1 CCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCCO3)CC1 10.1021/jm00024a002
10717193 23554 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)cc2)CC1 10.1039/C1MD00213A
CHEMBL124485 23554 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)cc2)CC1 10.1039/C1MD00213A
68592631 144502 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 495 7 3 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)NC(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758976 144502 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 495 7 3 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)NC(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
3157 8252 71 None -27 12 Guinea pig 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
7170 8252 71 None -27 12 Guinea pig 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
954 8252 71 None -27 12 Guinea pig 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
CHEMBL707 8252 71 None -27 12 Guinea pig 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
DB00590 8252 71 None -27 12 Guinea pig 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
68593153 144437 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 494 8 2 6 3.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)CC(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758433 144437 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 494 8 2 6 3.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)CC(C)C)CC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
10545343 171665 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 343 7 2 3 3.4 CCCCN1CCC(CNC(=O)c2c(OC)[nH]c3ccccc23)CC1 10.1021/jm00024a002
CHEMBL422116 171665 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMPAbility to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP
ChEMBL 343 7 2 3 3.4 CCCCN1CCC(CNC(=O)c2c(OC)[nH]c3ccccc23)CC1 10.1021/jm00024a002
151537 169443 49 None - 1 Guinea pig 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 nan
41867 169443 49 None - 1 Guinea pig 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 nan
CHEMBL417 169443 49 None - 1 Guinea pig 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 nan
5991 210698 72 None 2 5 Guinea pig 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C nan
CHEMBL691 210698 72 None 2 5 Guinea pig 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C nan
68593732 144601 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 480 8 2 6 2.8 CCC(=O)N1CCC(CCN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
CHEMBL3759824 144601 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 480 8 2 6 2.8 CCC(=O)N1CCC(CCN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1 10.1016/j.ejmech.2015.12.006
119584 9373 102 None -1 6 Guinea pig 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
1848 9373 102 None -1 6 Guinea pig 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
242 9373 102 None -1 6 Guinea pig 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
CHEMBL60889 9373 102 None -1 6 Guinea pig 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
DB11675 9373 102 None -1 6 Guinea pig 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
44384672 66476 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 437 6 3 6 1.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL172314 66476 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 437 6 3 6 1.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CN)CC2)CC1 10.1016/s0960-894x(02)00060-4
44384738 67120 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 451 7 3 6 1.7 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
CHEMBL174524 67120 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligandInhibitory activity against 5-hydroxytryptamine 4 receptor of guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 451 7 3 6 1.7 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CCN)CC2)CC1 10.1016/s0960-894x(02)00060-4
1782 9296 84 None -12 23 Guinea pig 6.0 pIC50 = 6.0 Binding
Concentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatumConcentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm020270n
241 9296 84 None -12 23 Guinea pig 6.0 pIC50 = 6.0 Binding
Concentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatumConcentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm020270n
4168 9296 84 None -12 23 Guinea pig 6.0 pIC50 = 6.0 Binding
Concentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatumConcentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm020270n
CHEMBL86 9296 84 None -12 23 Guinea pig 6.0 pIC50 = 6.0 Binding
Concentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatumConcentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm020270n
DB01233 9296 84 None -12 23 Guinea pig 6.0 pIC50 = 6.0 Binding
Concentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatumConcentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm020270n
90644472 119056 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assayAntagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 339 5 0 4 3.1 COc1cc2c3c(cccc3n1)CN(CCCN1CCCCC1)C2=O 10.1016/j.ejmech.2014.05.015
CHEMBL3291077 119056 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assayAntagonist activity at Rluc-tagged human 5HT4R expressed in human SH-SY5Y cells assessed as inhibition of serotonin-induced receptor/Gbeta1 coupling by BRET assay
ChEMBL 339 5 0 4 3.1 COc1cc2c3c(cccc3n1)CN(CCCN1CCCCC1)C2=O 10.1016/j.ejmech.2014.05.015
127028946 144452 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 438 7 2 6 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCCC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758578 144452 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 438 7 2 6 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCCC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
10531 8202 21 None -87 24 Guinea pig 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 8202 21 None -87 24 Guinea pig 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 8202 21 None -87 24 Guinea pig 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 8202 21 None -87 24 Guinea pig 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 8202 21 None -87 24 Guinea pig 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
127027702 144434 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 454 7 2 7 1.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCOCC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
CHEMBL3758410 144434 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis
ChEMBL 454 7 2 7 1.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCOCC2)C[C@H]1OC 10.1016/j.ejmech.2015.12.006
3066250 77061 2 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
CHEMBL194305 77061 2 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
44626294 205778 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 517 7 4 7 3.5 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(C[C@@H]2CCCC[C@@]2(O)c2cccc(O)c2)C[C@H]1OC 10.1016/j.bmcl.2009.08.016
CHEMBL585567 205778 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
ChEMBL 517 7 4 7 3.5 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(C[C@@H]2CCCC[C@@]2(O)c2cccc(O)c2)C[C@H]1OC 10.1016/j.bmcl.2009.08.016
121881 10263 27 None 2 15 Guinea pig 10.7 pKd = 10.7 Binding
Binding affinity to 5HT4 receptor in guinea pig distal colonBinding affinity to 5HT4 receptor in guinea pig distal colon
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/j.bmcl.2013.09.097
256 10263 27 None 2 15 Guinea pig 10.7 pKd = 10.7 Binding
Binding affinity to 5HT4 receptor in guinea pig distal colonBinding affinity to 5HT4 receptor in guinea pig distal colon
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/j.bmcl.2013.09.097
CHEMBL68131 10263 27 None 2 15 Guinea pig 10.7 pKd = 10.7 Binding
Binding affinity to 5HT4 receptor in guinea pig distal colonBinding affinity to 5HT4 receptor in guinea pig distal colon
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/j.bmcl.2013.09.097
257 10266 13 None -1 4 Rat 9.5 pKd = 9.5 Binding
Binding affinity to 5HT4 receptor in rat striatal membranesBinding affinity to 5HT4 receptor in rat striatal membranes
ChEMBL 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1016/j.bmcl.2013.09.097
5311423 10266 13 None -1 4 Rat 9.5 pKd = 9.5 Binding
Binding affinity to 5HT4 receptor in rat striatal membranesBinding affinity to 5HT4 receptor in rat striatal membranes
ChEMBL 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1016/j.bmcl.2013.09.097
CHEMBL114112 10266 13 None -1 4 Rat 9.5 pKd = 9.5 Binding
Binding affinity to 5HT4 receptor in rat striatal membranesBinding affinity to 5HT4 receptor in rat striatal membranes
ChEMBL 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1016/j.bmcl.2013.09.097
76310958 112504 1 None -1 2 Rat 9.5 pKd = 9.5 Binding
Binding affinity to 5HT4 receptor in rat striatal membranesBinding affinity to 5HT4 receptor in rat striatal membranes
ChEMBL 340 3 1 6 2.2 CN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCCO3)CC1 10.1016/j.bmcl.2013.09.097
CHEMBL3126112 112504 1 None -1 2 Rat 9.5 pKd = 9.5 Binding
Binding affinity to 5HT4 receptor in rat striatal membranesBinding affinity to 5HT4 receptor in rat striatal membranes
ChEMBL 340 3 1 6 2.2 CN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCCO3)CC1 10.1016/j.bmcl.2013.09.097
CHEMBL5182119 112504 1 None -1 2 Rat 9.5 pKd = 9.5 Binding
Binding affinity to 5HT4 receptor in rat striatal membranesBinding affinity to 5HT4 receptor in rat striatal membranes
ChEMBL 340 3 1 6 2.2 CN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCCO3)CC1 10.1016/j.bmcl.2013.09.097
119376 8622 48 None -1 27 Human 7.8 pKd = 7.8 Binding
Binding affinity to human 5HT4 receptor expressed in HEK293 cells by saturation binding methodBinding affinity to human 5HT4 receptor expressed in HEK293 cells by saturation binding method
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/np0601760
247 8622 48 None -1 27 Human 7.8 pKd = 7.8 Binding
Binding affinity to human 5HT4 receptor expressed in HEK293 cells by saturation binding methodBinding affinity to human 5HT4 receptor expressed in HEK293 cells by saturation binding method
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/np0601760
CHEMBL33884 8622 48 None -1 27 Human 7.8 pKd = 7.8 Binding
Binding affinity to human 5HT4 receptor expressed in HEK293 cells by saturation binding methodBinding affinity to human 5HT4 receptor expressed in HEK293 cells by saturation binding method
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/np0601760
243 9976 91 None 12 34 Human 8.7 pKd = 8.7 Binding
Binding affinity to 5-HT4 receptor (unknown origin) assessed as dissociation constantBinding affinity to 5-HT4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.2c00633
3052762 9976 91 None 12 34 Human 8.7 pKd = 8.7 Binding
Binding affinity to 5-HT4 receptor (unknown origin) assessed as dissociation constantBinding affinity to 5-HT4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.2c00633
3502 9976 91 None 12 34 Human 8.7 pKd = 8.7 Binding
Binding affinity to 5-HT4 receptor (unknown origin) assessed as dissociation constantBinding affinity to 5-HT4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.2c00633
CHEMBL117287 9976 91 None 12 34 Human 8.7 pKd = 8.7 Binding
Binding affinity to 5-HT4 receptor (unknown origin) assessed as dissociation constantBinding affinity to 5-HT4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.2c00633
DB06480 9976 91 None 12 34 Human 8.7 pKd = 8.7 Binding
Binding affinity to 5-HT4 receptor (unknown origin) assessed as dissociation constantBinding affinity to 5-HT4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/acs.jmedchem.2c00633
121881 10263 27 None 2 15 Guinea pig 10.9 pKi = 10.9 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/S0960-894X(01)80414-5
256 10263 27 None 2 15 Guinea pig 10.9 pKi = 10.9 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/S0960-894X(01)80414-5
CHEMBL68131 10263 27 None 2 15 Guinea pig 10.9 pKi = 10.9 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/S0960-894X(01)80414-5
121881 10263 27 None -2 15 Human 10.8 pKi = 10.8 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/j.bmc.2008.11.045
256 10263 27 None -2 15 Human 10.8 pKi = 10.8 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/j.bmc.2008.11.045
CHEMBL68131 10263 27 None -2 15 Human 10.8 pKi = 10.8 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10.1016/j.bmc.2008.11.045
9936969 70908 0 None - 1 Human 10.8 pKi = 10.8 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 534 9 1 7 2.2 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(C3CCCC3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL180835 70908 0 None - 1 Human 10.8 pKi = 10.8 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 534 9 1 7 2.2 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(C3CCCC3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
44390256 71113 0 None - 1 Human 10.6 pKi = 10.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 522 10 1 7 2.0 CCC(C)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL181202 71113 0 None - 1 Human 10.6 pKi = 10.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 522 10 1 7 2.0 CCC(C)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
9914629 129893 0 None - 1 Human 10.6 pKi = 10.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 519 8 1 6 3.3 O=C(NCC1CCN(CCCS(=O)(=O)N2CCC3(CCCC3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL361118 129893 0 None - 1 Human 10.6 pKi = 10.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 519 8 1 6 3.3 O=C(NCC1CCN(CCCS(=O)(=O)N2CCC3(CCCC3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
9870916 71096 0 None - 1 Human 10.5 pKi = 10.5 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 508 10 1 7 1.6 CCCN1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL181126 71096 0 None - 1 Human 10.5 pKi = 10.5 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 508 10 1 7 1.6 CCCN1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
9892494 72242 0 None - 1 Human 10.5 pKi = 10.5 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 508 9 1 7 1.6 CC(C)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL182999 72242 0 None - 1 Human 10.5 pKi = 10.5 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 508 9 1 7 1.6 CC(C)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
9873926 136434 0 None - 1 Human 10.5 pKi = 10.5 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 624 10 1 8 1.8 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(S(=O)(=O)c3ccc(F)cc3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL367354 136434 0 None - 1 Human 10.5 pKi = 10.5 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 624 10 1 8 1.8 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(S(=O)(=O)c3ccc(F)cc3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
119376 8622 48 None -1 27 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.ejmech.2013.03.060
247 8622 48 None -1 27 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.ejmech.2013.03.060
CHEMBL33884 8622 48 None -1 27 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.ejmech.2013.03.060
119376 8622 48 None -1 27 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2013.09.004
247 8622 48 None -1 27 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2013.09.004
CHEMBL33884 8622 48 None -1 27 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2013.09.004
71455625 89739 0 None 54 6 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181170 89739 0 None 54 6 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1021/jm300943r
71455625 89739 0 None 54 6 Human 10.4 pKi = 10.4 Binding
Binding affinity to human 5HT4RBinding affinity to human 5HT4R
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1016/j.bmc.2013.08.061
CHEMBL2181170 89739 0 None 54 6 Human 10.4 pKi = 10.4 Binding
Binding affinity to human 5HT4RBinding affinity to human 5HT4R
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1016/j.bmc.2013.08.061
71455625 89739 0 None 54 6 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181170 89739 0 None 54 6 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1021/jm300943r
53325605 63221 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 489 9 1 6 4.4 O=C(CCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1)OCc1ccccc1 10.1016/j.bmc.2010.10.011
CHEMBL1632165 63221 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 489 9 1 6 4.4 O=C(CCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1)OCc1ccccc1 10.1016/j.bmc.2010.10.011
46935636 109349 0 None 31622 2 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 524 7 1 6 5.9 O=C(O)c1ccccc1-c1ccc(CN2CCC(COC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmc.2013.09.004
CHEMBL2440460 109349 0 None 31622 2 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 524 7 1 6 5.9 O=C(O)c1ccccc1-c1ccc(CN2CCC(COC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmc.2013.09.004
CHEMBL3040772 109349 0 None 31622 2 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 524 7 1 6 5.9 O=C(O)c1ccccc1-c1ccc(CN2CCC(COC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmc.2013.09.004
118712571 121010 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 538 9 2 6 4.5 CC(C)CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
CHEMBL3329805 121010 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 538 9 2 6 4.5 CC(C)CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
9807895 70724 0 None - 1 Human 10.3 pKi = 10.3 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 560 9 1 7 2.6 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(c3ccc(F)cc3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL180680 70724 0 None - 1 Human 10.3 pKi = 10.3 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 560 9 1 7 2.6 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(c3ccc(F)cc3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
9870390 172571 0 None - 1 Human 10.3 pKi = 10.3 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 494 9 1 7 1.3 CCN1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL424790 172571 0 None - 1 Human 10.3 pKi = 10.3 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 494 9 1 7 1.3 CCN1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
177336 9894 50 None 6 3 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2010.10.011
225 9894 50 None 6 3 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2010.10.011
CHEMBL356359 9894 50 None 6 3 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2010.10.011
DB04873 9894 50 None 6 3 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2010.10.011
50898776 63219 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 483 9 1 6 4.8 CC(C)(C)OC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632163 63219 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 483 9 1 6 4.8 CC(C)(C)OC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
46935596 99651 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 537 7 1 6 5.5 COC(=O)c1ccccc1-c1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmc.2013.09.004
CHEMBL2440457 99651 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 537 7 1 6 5.5 COC(=O)c1ccccc1-c1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmc.2013.09.004
9892465 70563 0 None - 1 Human 10.2 pKi = 10.2 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 507 10 1 6 3.1 CCCC1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL180201 70563 0 None - 1 Human 10.2 pKi = 10.2 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 507 10 1 6 3.1 CCCC1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
50898699 63224 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 541 11 1 8 4.5 CC(C)(C)C(=O)OCOC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632169 63224 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 541 11 1 8 4.5 CC(C)(C)C(=O)OCOC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
72545050 112502 0 None - 1 Rat 10.2 pKi = 10.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma counting
ChEMBL 386 6 1 6 2.9 Nc1c(Cl)cc(C(=O)OCC2CCN(CCCF)CC2)c2c1OCCO2 10.1016/j.bmcl.2013.09.097
CHEMBL3126108 112502 0 None - 1 Rat 10.2 pKi = 10.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma counting
ChEMBL 386 6 1 6 2.9 Nc1c(Cl)cc(C(=O)OCC2CCN(CCCF)CC2)c2c1OCCO2 10.1016/j.bmcl.2013.09.097
119376 8622 48 None -1 27 Human 10.1 pKi = 10.1 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
247 8622 48 None -1 27 Human 10.1 pKi = 10.1 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
CHEMBL33884 8622 48 None -1 27 Human 10.1 pKi = 10.1 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
9954930 91360 0 None 398 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 404 7 1 4 4.3 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccccc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2177130 91360 0 None 398 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 404 7 1 4 4.3 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccccc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2220969 91360 0 None 398 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 404 7 1 4 4.3 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccccc3)CC2)c2ccccc21 10.1021/jm300573d
91754444 121019 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 388 6 2 7 1.6 O=C(OCC1CCN(CC(O)CO)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmcl.2014.06.083
CHEMBL3329814 121019 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 388 6 2 7 1.6 O=C(OCC1CCN(CC(O)CO)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmcl.2014.06.083
21268036 129512 0 None - 1 Human 10.1 pKi = 10.1 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 599 10 1 8 0.6 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(S(=O)(=O)N3CCCC3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL360449 129512 0 None - 1 Human 10.1 pKi = 10.1 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 599 10 1 8 0.6 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(S(=O)(=O)N3CCCC3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
90667897 116307 0 None - 1 Rat 10.1 pKi = 10.1 Binding
Displacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 364 6 2 3 4.0 CCCCN1CCC(CNC(=S)c2cc(Cl)cc3[nH]cnc23)CC1 10.1039/C0MD00258E
CHEMBL3221572 116307 0 None - 1 Rat 10.1 pKi = 10.1 Binding
Displacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 364 6 2 3 4.0 CCCCN1CCC(CNC(=S)c2cc(Cl)cc3[nH]cnc23)CC1 10.1039/C0MD00258E
119376 8622 48 None -1 27 Human 10.0 pKi = 10 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
247 8622 48 None -1 27 Human 10.0 pKi = 10 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
CHEMBL33884 8622 48 None -1 27 Human 10.0 pKi = 10 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
250 10159 8 None -2 13 Guinea pig 10.0 pKi = 10 Binding
Compound was evaluated for binding affinity against 5-hydroxytryptamine 4 receptor using radioligand binding assay using [3H]GR as radioligandCompound was evaluated for binding affinity against 5-hydroxytryptamine 4 receptor using radioligand binding assay using [3H]GR as radioligand
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
5311416 10159 8 None -2 13 Guinea pig 10.0 pKi = 10 Binding
Compound was evaluated for binding affinity against 5-hydroxytryptamine 4 receptor using radioligand binding assay using [3H]GR as radioligandCompound was evaluated for binding affinity against 5-hydroxytryptamine 4 receptor using radioligand binding assay using [3H]GR as radioligand
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
CHEMBL69733 10159 8 None -2 13 Guinea pig 10.0 pKi = 10 Binding
Compound was evaluated for binding affinity against 5-hydroxytryptamine 4 receptor using radioligand binding assay using [3H]GR as radioligandCompound was evaluated for binding affinity against 5-hydroxytryptamine 4 receptor using radioligand binding assay using [3H]GR as radioligand
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
11153975 91341 7 None 1000 2 Human 10.0 pKi = 10 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 405 7 1 5 3.7 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccccn3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2179697 91341 7 None 1000 2 Human 10.0 pKi = 10 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 405 7 1 5 3.7 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccccn3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2220892 91341 7 None 1000 2 Human 10.0 pKi = 10 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 405 7 1 5 3.7 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccccn3)CC2)c2ccccc21 10.1021/jm300573d
177336 9894 50 None 6 3 Human 10.0 pKi = 10 Binding
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.ejmech.2013.03.060
225 9894 50 None 6 3 Human 10.0 pKi = 10 Binding
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.ejmech.2013.03.060
CHEMBL356359 9894 50 None 6 3 Human 10.0 pKi = 10 Binding
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.ejmech.2013.03.060
DB04873 9894 50 None 6 3 Human 10.0 pKi = 10 Binding
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.ejmech.2013.03.060
177336 9894 50 None 6 3 Human 10.0 pKi = 10 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
225 9894 50 None 6 3 Human 10.0 pKi = 10 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
CHEMBL356359 9894 50 None 6 3 Human 10.0 pKi = 10 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
DB04873 9894 50 None 6 3 Human 10.0 pKi = 10 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
21268033 70902 0 None - 1 Human 10.0 pKi = 10 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 560 9 1 8 1.7 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(C(=O)c3ccco3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL180830 70902 0 None - 1 Human 10.0 pKi = 10 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 560 9 1 8 1.7 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(C(=O)c3ccco3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
15485936 129385 0 None - 1 Human 10.0 pKi = 10 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 572 11 1 8 1.0 CCCS(=O)(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL360245 129385 0 None - 1 Human 10.0 pKi = 10 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 572 11 1 8 1.0 CCCS(=O)(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
53319410 63213 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 427 8 1 6 3.2 CCOC(=O)CCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632157 63213 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 427 8 1 6 3.2 CCOC(=O)CCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
50898777 63214 0 None 2951 8 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 441 9 1 6 3.6 COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632158 63214 0 None 2951 8 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 441 9 1 6 3.6 COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
10476858 119142 0 None - 1 Rat 10.0 pKi = 10.0 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 413 7 3 5 1.2 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL329487 119142 0 None - 1 Rat 10.0 pKi = 10.0 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 413 7 3 5 1.2 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
119376 8622 48 None 1 27 Guinea pig 10.0 pKi = 10.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm981098j
247 8622 48 None 1 27 Guinea pig 10.0 pKi = 10.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm981098j
CHEMBL33884 8622 48 None 1 27 Guinea pig 10.0 pKi = 10.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm981098j
10476858 119142 0 None - 1 Rat 10.0 pKi = 10.0 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 413 7 3 5 1.2 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL329487 119142 0 None - 1 Rat 10.0 pKi = 10.0 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 413 7 3 5 1.2 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
72698087 110765 0 None 81 3 Human 10.0 pKi = 10.0 Binding
Binding affinity to human 5HT4RBinding affinity to human 5HT4R
ChEMBL 407 5 0 4 5.0 Fc1cccc2c1nc(OCC1CCN(CCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
CHEMBL3093186 110765 0 None 81 3 Human 10.0 pKi = 10.0 Binding
Binding affinity to human 5HT4RBinding affinity to human 5HT4R
ChEMBL 407 5 0 4 5.0 Fc1cccc2c1nc(OCC1CCN(CCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
10476858 119142 0 None - 1 Rat 10.0 pKi = 10.0 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 413 7 3 5 1.2 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL329487 119142 0 None - 1 Rat 10.0 pKi = 10.0 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 413 7 3 5 1.2 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
46935743 97596 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
ChEMBL 490 7 1 6 4.9 CC(C)(C(=O)O)c1ccc(CN2CCC(COC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.ejmech.2013.03.060
CHEMBL2391994 97596 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
ChEMBL 490 7 1 6 4.9 CC(C)(C(=O)O)c1ccc(CN2CCC(COC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.ejmech.2013.03.060
21268037 69370 0 None - 1 Human 9.9 pKi = 9.9 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 493 8 1 6 2.7 CC1(C)CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL178285 69370 0 None - 1 Human 9.9 pKi = 9.9 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 493 8 1 6 2.7 CC1(C)CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
21268031 69773 0 None - 1 Human 9.9 pKi = 9.9 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 508 8 1 7 0.8 CC(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL178669 69773 0 None - 1 Human 9.9 pKi = 9.9 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 508 8 1 7 0.8 CC(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
44390214 70240 0 None - 1 Human 9.9 pKi = 9.9 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 572 10 1 8 1.0 CC(C)S(=O)(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL179833 70240 0 None - 1 Human 9.9 pKi = 9.9 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 572 10 1 8 1.0 CC(C)S(=O)(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
9952994 113747 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 366 6 1 5 3.5 CCCCN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCC3)CC1 10.1016/0960-894X(96)00002-9
CHEMBL315071 113747 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 366 6 1 5 3.5 CCCCN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCC3)CC1 10.1016/0960-894X(96)00002-9
50898775 63222 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 517 11 1 6 5.2 O=C(CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1)OCc1ccccc1 10.1016/j.bmc.2010.10.011
CHEMBL1632167 63222 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 517 11 1 6 5.2 O=C(CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1)OCc1ccccc1 10.1016/j.bmc.2010.10.011
119376 8622 48 None -2 27 Rat 9.8 pKi = 9.8 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm960853v
247 8622 48 None -2 27 Rat 9.8 pKi = 9.8 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm960853v
CHEMBL33884 8622 48 None -2 27 Rat 9.8 pKi = 9.8 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm960853v
119376 8622 48 None -2 27 Rat 9.8 pKi = 9.8 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm960320m
247 8622 48 None -2 27 Rat 9.8 pKi = 9.8 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm960320m
CHEMBL33884 8622 48 None -2 27 Rat 9.8 pKi = 9.8 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm960320m
90667896 116306 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Displacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 330 6 2 3 3.3 CCCCN1CCC(CNC(=S)c2cccc3[nH]cnc23)CC1 10.1039/C0MD00258E
CHEMBL3221571 116306 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Displacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 330 6 2 3 3.3 CCCCN1CCC(CNC(=S)c2cccc3[nH]cnc23)CC1 10.1039/C0MD00258E
53354764 9838 34 None 1 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
9059 9838 34 None 1 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
CHEMBL2152922 9838 34 None 1 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
DB12675 9838 34 None 1 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
119376 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2008.11.045
247 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2008.11.045
CHEMBL33884 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2008.11.045
177336 9894 50 None 6 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm300573d
225 9894 50 None 6 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm300573d
CHEMBL356359 9894 50 None 6 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm300573d
DB04873 9894 50 None 6 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm300573d
21252894 91371 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 410 7 1 4 5.0 CC(C)n1nc(C(=O)NCC2CCN(CCC3CCCCC3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2179699 91371 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 410 7 1 4 5.0 CC(C)n1nc(C(=O)NCC2CCN(CCC3CCCCC3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2221066 91371 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 410 7 1 4 5.0 CC(C)n1nc(C(=O)NCC2CCN(CCC3CCCCC3)CC2)c2ccccc21 10.1021/jm300573d
11317280 70752 0 None - 1 Human 9.8 pKi = 9.8 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 466 8 2 7 0.5 O=C(NCC1CCN(CCCS(=O)(=O)N2CCNCC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL180697 70752 0 None - 1 Human 9.8 pKi = 9.8 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 466 8 2 7 0.5 O=C(NCC1CCN(CCCS(=O)(=O)N2CCNCC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
44390243 71258 0 None - 1 Human 9.8 pKi = 9.8 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 557 10 1 8 1.8 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(Cc3cccnc3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL181415 71258 0 None - 1 Human 9.8 pKi = 9.8 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 557 10 1 8 1.8 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(Cc3cccnc3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
11493559 80188 0 None - 1 Guinea pig 9.7 pKi = 9.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 324 4 1 5 2.6 COc1cc(N)c(Cl)cc1C(=O)OC[C@@H]1CCN2CCC[C@@H]12 10.1021/jm0509501
CHEMBL201621 80188 0 None - 1 Guinea pig 9.7 pKi = 9.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 324 4 1 5 2.6 COc1cc(N)c(Cl)cc1C(=O)OC[C@@H]1CCN2CCC[C@@H]12 10.1021/jm0509501
44407083 80685 0 None 6 2 Guinea pig 9.7 pKi = 9.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 284 3 1 3 2.8 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1c[nH]c2ccccc12 10.1021/jm0509501
CHEMBL201946 80685 0 None 6 2 Guinea pig 9.7 pKi = 9.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 284 3 1 3 2.8 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1c[nH]c2ccccc12 10.1021/jm0509501
53317702 63215 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 497 13 1 6 5.2 COC(=O)CCCCCCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632159 63215 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 497 13 1 6 5.2 COC(=O)CCCCCCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
9823412 91385 0 None 398 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 419 7 2 5 3.9 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(N)cc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2221193 91385 0 None 398 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 419 7 2 5 3.9 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(N)cc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL3216126 91385 0 None 398 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 419 7 2 5 3.9 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(N)cc3)CC2)c2ccccc21 10.1021/jm300573d
118712569 121008 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 496 7 2 6 3.4 CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
CHEMBL3329803 121008 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 496 7 2 6 3.4 CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
118712572 121011 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 564 8 2 6 5.1 O=C(NCC1CCN(Cc2ccc(NS(=O)(=O)C3CCCCC3)cc2)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmcl.2014.06.083
CHEMBL3329806 121011 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 564 8 2 6 5.1 O=C(NCC1CCN(Cc2ccc(NS(=O)(=O)C3CCCCC3)cc2)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmcl.2014.06.083
118712573 121012 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 459 7 2 6 2.5 CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
CHEMBL3329807 121012 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 459 7 2 6 2.5 CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
118712575 121014 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 501 9 2 6 3.5 CC(C)CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
CHEMBL3329809 121014 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 501 9 2 6 3.5 CC(C)CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
44390192 71545 0 None - 1 Human 9.7 pKi = 9.7 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 465 8 1 6 2.1 O=C(NCC1CCN(CCCS(=O)(=O)N2CCCCC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL181928 71545 0 None - 1 Human 9.7 pKi = 9.7 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 465 8 1 6 2.1 O=C(NCC1CCN(CCCS(=O)(=O)N2CCCCC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
72698088 110766 0 None 20 5 Human 9.7 pKi = 9.7 Binding
Binding affinity to human 5HT4RBinding affinity to human 5HT4R
ChEMBL 421 6 0 4 5.4 Fc1cccc2c1nc(OCC1CCN(CCCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
CHEMBL3093187 110766 0 None 20 5 Human 9.7 pKi = 9.7 Binding
Binding affinity to human 5HT4RBinding affinity to human 5HT4R
ChEMBL 421 6 0 4 5.4 Fc1cccc2c1nc(OCC1CCN(CCCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
72545049 112503 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma counting
ChEMBL 372 5 1 6 2.5 Nc1c(Cl)cc(C(=O)OCC2CCN(CCF)CC2)c2c1OCCO2 10.1016/j.bmcl.2013.09.097
CHEMBL3126109 112503 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma counting
ChEMBL 372 5 1 6 2.5 Nc1c(Cl)cc(C(=O)OCC2CCN(CCF)CC2)c2c1OCCO2 10.1016/j.bmcl.2013.09.097
257 10266 13 None 1 4 Guinea pig 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1021/jm100668r
5311423 10266 13 None 1 4 Guinea pig 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1021/jm100668r
CHEMBL114112 10266 13 None 1 4 Guinea pig 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1021/jm100668r
49783421 24560 0 None 51 2 Guinea pig 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 352 9 1 5 3.3 CCCCN1CCC(COC(=O)c2ccc(N)c(OCCF)c2)CC1 10.1021/jm100668r
CHEMBL1258786 24560 0 None 51 2 Guinea pig 9.7 pKi = 9.7 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 352 9 1 5 3.3 CCCCN1CCC(COC(=O)c2ccc(N)c(OCCF)c2)CC1 10.1021/jm100668r
71459269 89735 0 None 10 8 Human 9.6 pKi = 9.6 Binding
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
CHEMBL2181166 89735 0 None 10 8 Human 9.6 pKi = 9.6 Binding
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
53320711 63218 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 455 7 1 6 4.0 CC(C)(C)OC(=O)CCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632162 63218 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 455 7 1 6 4.0 CC(C)(C)OC(=O)CCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
17984294 91383 0 None 39 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 420 7 2 5 4.0 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(O)cc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2179704 91383 0 None 39 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 420 7 2 5 4.0 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(O)cc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2221162 91383 0 None 39 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 420 7 2 5 4.0 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(O)cc3)CC2)c2ccccc21 10.1021/jm300573d
119376 8622 48 None -1 27 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmcl.2014.06.083
247 8622 48 None -1 27 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmcl.2014.06.083
CHEMBL33884 8622 48 None -1 27 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmcl.2014.06.083
118712574 121013 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 501 10 2 6 3.6 CCCCS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
CHEMBL3329808 121013 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 501 10 2 6 3.6 CCCCS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
177336 9894 50 None 6 3 Human 9.6 pKi = 9.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmcl.2005.01.039
225 9894 50 None 6 3 Human 9.6 pKi = 9.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmcl.2005.01.039
CHEMBL356359 9894 50 None 6 3 Human 9.6 pKi = 9.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmcl.2005.01.039
DB04873 9894 50 None 6 3 Human 9.6 pKi = 9.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmcl.2005.01.039
9869791 70700 20 None - 1 Human 9.6 pKi = 9.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 480 8 1 7 0.9 CN1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL180632 70700 20 None - 1 Human 9.6 pKi = 9.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 480 8 1 7 0.9 CN1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
44390227 129590 0 None - 1 Human 9.6 pKi = 9.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 543 9 1 8 1.8 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(c3ccccn3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL360531 129590 0 None - 1 Human 9.6 pKi = 9.6 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 543 9 1 8 1.8 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(c3ccccn3)CC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
10831066 195615 6 None - 1 Rat 9.6 pKi = 9.6 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1C[C@@H](C)C[C@@H](C)C1 10.1021/jm960853v
CHEMBL50660 195615 6 None - 1 Rat 9.6 pKi = 9.6 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1C[C@@H](C)C[C@@H](C)C1 10.1021/jm960853v
249 9343 4 None -1 2 Rat 9.6 pKi = 9.6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
9905972 9343 4 None -1 2 Rat 9.6 pKi = 9.6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
CHEMBL155917 9343 4 None -1 2 Rat 9.6 pKi = 9.6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
71457409 89737 0 None 17 6 Human 9.6 pKi = 9.6 Binding
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
ChEMBL 461 5 0 4 4.9 CCCN1CCC(COc2nc3c(I)cccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181168 89737 0 None 17 6 Human 9.6 pKi = 9.6 Binding
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
ChEMBL 461 5 0 4 4.9 CCCN1CCC(COc2nc3c(I)cccc3c3ncccc23)CC1 10.1021/jm300943r
71450132 89452 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 358 8 0 5 4.7 CCCCN1CCC(COc2noc3cccc(OC4CCC4)c23)CC1 10.1021/jm300953p
CHEMBL2179584 89452 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 358 8 0 5 4.7 CCCCN1CCC(COc2noc3cccc(OC4CCC4)c23)CC1 10.1021/jm300953p
10472977 103329 0 None - 1 Rat 9.5 pKi = 9.5 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 348 5 2 3 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL262950 103329 0 None - 1 Rat 9.5 pKi = 9.5 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 348 5 2 3 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
10472977 103329 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 348 5 2 3 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL262950 103329 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 348 5 2 3 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
71462651 89455 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 360 9 0 5 4.8 CCCCN1CCC(COc2noc3cccc(OCC(C)C)c23)CC1 10.1021/jm300953p
CHEMBL2179587 89455 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 360 9 0 5 4.8 CCCCN1CCC(COc2noc3cccc(OCC(C)C)c23)CC1 10.1021/jm300953p
10472977 103329 0 None - 1 Rat 9.5 pKi = 9.5 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 348 5 2 3 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL262950 103329 0 None - 1 Rat 9.5 pKi = 9.5 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 348 5 2 3 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
76310958 112504 1 None 1 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5-HT4 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 340 3 1 6 2.2 CN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCCO3)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL3126112 112504 1 None 1 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5-HT4 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 340 3 1 6 2.2 CN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCCO3)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5182119 112504 1 None 1 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5-HT4 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 340 3 1 6 2.2 CN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCCO3)CC1 10.1021/acs.jmedchem.2c00633
53354764 9838 34 None -1 2 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
9059 9838 34 None -1 2 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
CHEMBL2152922 9838 34 None -1 2 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
DB12675 9838 34 None -1 2 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
71712326 98161 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 554 9 3 7 1.7 CC(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cc(Cl)cc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402896 98161 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 554 9 3 7 1.7 CC(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cc(Cl)cc2[nH]1 10.1016/j.bmcl.2013.05.018
21252889 91351 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 421 8 2 6 1.6 CC(C)n1nc(C(=O)NCC2CCN(CCNS(C)(=O)=O)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2179702 91351 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 421 8 2 6 1.6 CC(C)n1nc(C(=O)NCC2CCN(CCNS(C)(=O)=O)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2220908 91351 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 421 8 2 6 1.6 CC(C)n1nc(C(=O)NCC2CCN(CCNS(C)(=O)=O)CC2)c2ccccc21 10.1021/jm300573d
118712580 121018 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 476 7 1 6 4.7 CC(C(=O)O)c1ccc(CN2CCC(COC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
CHEMBL3329813 121018 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 476 7 1 6 4.7 CC(C(=O)O)c1ccc(CN2CCC(COC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
44390250 70234 0 None - 1 Human 9.5 pKi = 9.5 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 544 9 1 8 0.2 CS(=O)(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL179799 70234 0 None - 1 Human 9.5 pKi = 9.5 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 544 9 1 8 0.2 CS(=O)(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
10089141 214351 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 348 6 2 3 3.5 CCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL94880 214351 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 348 6 2 3 3.5 CCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
10089141 214351 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 348 6 2 3 3.5 CCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1039/C0MD00258E
CHEMBL94880 214351 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 348 6 2 3 3.5 CCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1039/C0MD00258E
53354764 9838 34 None 1 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
9059 9838 34 None 1 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
CHEMBL2152922 9838 34 None 1 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
DB12675 9838 34 None 1 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
10089141 214351 0 None - 1 Rat 9.5 pKi = 9.5 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 348 6 2 3 3.5 CCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL94880 214351 0 None - 1 Rat 9.5 pKi = 9.5 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 348 6 2 3 3.5 CCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
10089141 214351 0 None - 1 Rat 9.5 pKi = 9.5 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 348 6 2 3 3.5 CCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL94880 214351 0 None - 1 Rat 9.5 pKi = 9.5 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 348 6 2 3 3.5 CCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
119376 8622 48 None -1 27 Human 9.5 pKi = 9.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
247 8622 48 None -1 27 Human 9.5 pKi = 9.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
CHEMBL33884 8622 48 None -1 27 Human 9.5 pKi = 9.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
49783419 24521 0 None 6 12 Guinea pig 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258671 24521 0 None 6 12 Guinea pig 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
49783420 24522 0 None 51 2 Guinea pig 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 338 8 1 5 3.2 CCCCN1CCC(COC(=O)c2ccc(N)c(OCF)c2)CC1 10.1021/jm100668r
CHEMBL1258672 24522 0 None 51 2 Guinea pig 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 338 8 1 5 3.2 CCCCN1CCC(COC(=O)c2ccc(N)c(OCF)c2)CC1 10.1021/jm100668r
44461527 212558 0 None - 1 Guinea pig 9.5 pKi = 9.5 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 567 14 2 8 4.1 COc1cc(COc2cc(N)c(Cl)cc2C(=O)CCC2CCN(CCCNS(C)(=O)=O)CC2)cc(OC)c1 10.1016/S0960-894X(01)80414-5
CHEMBL82976 212558 0 None - 1 Guinea pig 9.5 pKi = 9.5 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 567 14 2 8 4.1 COc1cc(COc2cc(N)c(Cl)cc2C(=O)CCC2CCN(CCCNS(C)(=O)=O)CC2)cc(OC)c1 10.1016/S0960-894X(01)80414-5
53319411 63216 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 525 15 1 6 5.9 COC(=O)CCCCCCCCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632160 63216 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 525 15 1 6 5.9 COC(=O)CCCCCCCCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
53324684 63223 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 561 8 1 8 4.8 CC(C)(C)C(=O)OCOC(=O)c1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmc.2010.10.011
CHEMBL1632168 63223 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 561 8 1 8 4.8 CC(C)(C)C(=O)OCOC(=O)c1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmc.2010.10.011
11496400 18580 0 None - 1 Guinea pig 9.5 pKi = 9.5 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 338 4 2 3 2.3 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CC[N@@+]2(C)CCC[C@@H]12 10.1021/jm0509501
CHEMBL1181946 18580 0 None - 1 Guinea pig 9.5 pKi = 9.5 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 338 4 2 3 2.3 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CC[N@@+]2(C)CCC[C@@H]12 10.1021/jm0509501
CHEMBL199866 18580 0 None - 1 Guinea pig 9.5 pKi = 9.5 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 338 4 2 3 2.3 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CC[N@@+]2(C)CCC[C@@H]12 10.1021/jm0509501
53354764 9838 34 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
9059 9838 34 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
CHEMBL2152922 9838 34 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
DB12675 9838 34 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
53357029 89457 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 418 8 1 7 3.5 CC(C)COc1cccc2onc(OCC3CCN(CC4(O)CCOCC4)CC3)c12 10.1021/jm300953p
CHEMBL2179589 89457 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 418 8 1 7 3.5 CC(C)COc1cccc2onc(OCC3CCN(CC4(O)CCOCC4)CC3)c12 10.1021/jm300953p
11961293 10541 19 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
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 10541 19 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
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 10541 19 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
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 10541 19 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
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
21252892 91349 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 413 7 1 6 2.4 CC(C)n1nc(C(=O)NCC2CCN(CCN3CCOCC3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2220906 91349 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 413 7 1 6 2.4 CC(C)n1nc(C(=O)NCC2CCN(CCN3CCOCC3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL3215681 91349 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 413 7 1 6 2.4 CC(C)n1nc(C(=O)NCC2CCN(CCN3CCOCC3)CC2)c2ccccc21 10.1021/jm300573d
177336 9894 50 None 6 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmcl.2014.06.083
225 9894 50 None 6 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmcl.2014.06.083
CHEMBL356359 9894 50 None 6 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmcl.2014.06.083
DB04873 9894 50 None 6 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmcl.2014.06.083
9912434 130631 0 None - 1 Human 9.4 pKi = 9.4 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 467 8 1 7 1.0 O=C(NCC1CCN(CCCS(=O)(=O)N2CCOCC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL362582 130631 0 None - 1 Human 9.4 pKi = 9.4 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 467 8 1 7 1.0 O=C(NCC1CCN(CCCS(=O)(=O)N2CCOCC2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
11522273 148123 0 None 6 2 Guinea pig 9.4 pKi = 9.4 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 299 3 0 5 2.2 Cn1nc(C(=O)OC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21 10.1021/jm0509501
CHEMBL383577 148123 0 None 6 2 Guinea pig 9.4 pKi = 9.4 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 299 3 0 5 2.2 Cn1nc(C(=O)OC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21 10.1021/jm0509501
119376 8622 48 None -1 27 Human 9.4 pKi = 9.4 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
247 8622 48 None -1 27 Human 9.4 pKi = 9.4 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
CHEMBL33884 8622 48 None -1 27 Human 9.4 pKi = 9.4 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
145988201 173870 0 None - 1 Guinea pig 9.4 pKi = 9.4 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 366 7 0 4 4.8 CCCCN1CCC(COC(=O)c2cc(C3CC3)nc3ccccc23)CC1 10.1039/C8MD00233A
CHEMBL4289793 173870 0 None - 1 Guinea pig 9.4 pKi = 9.4 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 366 7 0 4 4.8 CCCCN1CCC(COC(=O)c2cc(C3CC3)nc3ccccc23)CC1 10.1039/C8MD00233A
49783206 24349 0 None 74 2 Guinea pig 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 373 6 1 7 2.6 CCCCN1CCC(COC(=O)c2cc(C#N)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258108 24349 0 None 74 2 Guinea pig 9.4 pKi = 9.4 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 373 6 1 7 2.6 CCCCN1CCC(COC(=O)c2cc(C#N)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
53354764 9838 34 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
9059 9838 34 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
CHEMBL2152922 9838 34 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
DB12675 9838 34 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 10.1021/jm300953p
44461518 212723 0 None - 1 Guinea pig 9.3 pKi = 9.3 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 567 13 1 8 4.1 COc1cc(COc2cc(N)c(Cl)cc2C(=O)CCC2CCN(CCN(C)S(C)(=O)=O)CC2)cc(OC)c1 10.1016/S0960-894X(01)80414-5
CHEMBL84294 212723 0 None - 1 Guinea pig 9.3 pKi = 9.3 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 567 13 1 8 4.1 COc1cc(COc2cc(N)c(Cl)cc2C(=O)CCC2CCN(CCN(C)S(C)(=O)=O)CC2)cc(OC)c1 10.1016/S0960-894X(01)80414-5
19081854 111519 0 None - 1 Guinea pig 9.3 pKi = 9.3 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 488 12 1 6 6.0 CCCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OCc2cc(OC)cc(OC)c2)CC1 10.1016/S0960-894X(01)80414-5
CHEMBL310667 111519 0 None - 1 Guinea pig 9.3 pKi = 9.3 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 488 12 1 6 6.0 CCCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OCc2cc(OC)cc(OC)c2)CC1 10.1016/S0960-894X(01)80414-5
119376 8622 48 None -1 27 Human 9.3 pKi = 9.3 Binding
Binding affinity to Rluc fused 5HT4 receptor expressed in CHO cellsBinding affinity to Rluc fused 5HT4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm070552t
247 8622 48 None -1 27 Human 9.3 pKi = 9.3 Binding
Binding affinity to Rluc fused 5HT4 receptor expressed in CHO cellsBinding affinity to Rluc fused 5HT4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm070552t
CHEMBL33884 8622 48 None -1 27 Human 9.3 pKi = 9.3 Binding
Binding affinity to Rluc fused 5HT4 receptor expressed in CHO cellsBinding affinity to Rluc fused 5HT4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm070552t
53357011 89448 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
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 89448 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 446 7 2 8 2.8 O[C@@H]1CC[C@@H](Oc2cccc3onc(OCC4CCN(CC5(O)CCOCC5)CC4)c23)C1 10.1021/jm300953p
177336 9894 50 None 6 3 Human 9.3 pKi = 9.3 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2008.11.045
225 9894 50 None 6 3 Human 9.3 pKi = 9.3 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2008.11.045
CHEMBL356359 9894 50 None 6 3 Human 9.3 pKi = 9.3 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2008.11.045
DB04873 9894 50 None 6 3 Human 9.3 pKi = 9.3 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2008.11.045
71714540 98155 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 506 9 3 7 0.5 CCc1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402890 98155 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 506 9 3 7 0.5 CCc1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
71714541 98156 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 520 9 3 7 1.1 CC(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402891 98156 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 520 9 3 7 1.1 CC(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
71714542 98157 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 518 9 3 7 0.8 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]c(C5CC5)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402892 98157 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 518 9 3 7 0.8 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]c(C5CC5)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
66810955 98168 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 475 7 2 5 2.8 CC(C)c1nc2c(C(=O)NCC3CCN(CC4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402903 98168 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 475 7 2 5 2.8 CC(C)c1nc2c(C(=O)NCC3CCN(CC4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
177336 9894 50 None 6 3 Human 9.3 pKi = 9.3 Binding
Binding affinity was determined against 5-hydroxytryptamine 2C receptor using cloned rat receptors expressed in 293 cells radiolabeled with [3H]mesulergineBinding affinity was determined against 5-hydroxytryptamine 2C receptor using cloned rat receptors expressed in 293 cells radiolabeled with [3H]mesulergine
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm00024a002
225 9894 50 None 6 3 Human 9.3 pKi = 9.3 Binding
Binding affinity was determined against 5-hydroxytryptamine 2C receptor using cloned rat receptors expressed in 293 cells radiolabeled with [3H]mesulergineBinding affinity was determined against 5-hydroxytryptamine 2C receptor using cloned rat receptors expressed in 293 cells radiolabeled with [3H]mesulergine
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm00024a002
CHEMBL356359 9894 50 None 6 3 Human 9.3 pKi = 9.3 Binding
Binding affinity was determined against 5-hydroxytryptamine 2C receptor using cloned rat receptors expressed in 293 cells radiolabeled with [3H]mesulergineBinding affinity was determined against 5-hydroxytryptamine 2C receptor using cloned rat receptors expressed in 293 cells radiolabeled with [3H]mesulergine
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm00024a002
DB04873 9894 50 None 6 3 Human 9.3 pKi = 9.3 Binding
Binding affinity was determined against 5-hydroxytryptamine 2C receptor using cloned rat receptors expressed in 293 cells radiolabeled with [3H]mesulergineBinding affinity was determined against 5-hydroxytryptamine 2C receptor using cloned rat receptors expressed in 293 cells radiolabeled with [3H]mesulergine
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1021/jm00024a002
71457299 91382 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 385 7 2 5 2.2 CNC(=O)CCN1CCC(CNC(=O)c2nn(C(C)C)c3ccccc23)CC1 10.1021/jm300573d
CHEMBL2179703 91382 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 385 7 2 5 2.2 CNC(=O)CCN1CCC(CNC(=O)c2nn(C(C)C)c3ccccc23)CC1 10.1021/jm300573d
CHEMBL2221161 91382 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 385 7 2 5 2.2 CNC(=O)CCN1CCC(CNC(=O)c2nn(C(C)C)c3ccccc23)CC1 10.1021/jm300573d
119376 8622 48 None -1 27 Human 9.3 pKi = 9.3 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
247 8622 48 None -1 27 Human 9.3 pKi = 9.3 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
CHEMBL33884 8622 48 None -1 27 Human 9.3 pKi = 9.3 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm0009538
44327645 214896 0 None - 1 Rat 9.3 pKi = 9.3 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 362 7 2 3 3.8 CCCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL97955 214896 0 None - 1 Rat 9.3 pKi = 9.3 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 362 7 2 3 3.8 CCCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
44327645 214896 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 362 7 2 3 3.8 CCCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL97955 214896 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 362 7 2 3 3.8 CCCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
44327645 214896 0 None - 1 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 362 7 2 3 3.8 CCCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL97955 214896 0 None - 1 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 362 7 2 3 3.8 CCCCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
49783209 24381 0 None 3 26 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 24381 0 None 3 26 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
145987934 173833 0 None - 1 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 356 7 0 5 3.9 CCCCN1CCC(COC(=O)c2cc(OC)nc3ccccc23)CC1 10.1039/C8MD00233A
CHEMBL4289073 173833 0 None - 1 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 356 7 0 5 3.9 CCCCN1CCC(COC(=O)c2cc(OC)nc3ccccc23)CC1 10.1039/C8MD00233A
21252899 91362 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 390 6 1 4 4.3 CC(C)n1nc(C(=O)NCC2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2179696 91362 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 390 6 1 4 4.3 CC(C)n1nc(C(=O)NCC2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2220973 91362 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 390 6 1 4 4.3 CC(C)n1nc(C(=O)NCC2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm300573d
72697441 99652 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 523 7 2 5 5.4 O=C(O)c1ccccc1-c1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmc.2013.09.004
CHEMBL2440458 99652 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 523 7 2 5 5.4 O=C(O)c1ccccc1-c1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmc.2013.09.004
11014701 214408 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 392 6 2 3 3.6 CCCCN1CCC(CNC(=O)c2cc(Br)cc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL95178 214408 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 392 6 2 3 3.6 CCCCN1CCC(CNC(=O)c2cc(Br)cc3[nH]cnc23)CC1 10.1021/jm020807x
11014701 214408 0 None - 1 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 392 6 2 3 3.6 CCCCN1CCC(CNC(=O)c2cc(Br)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL95178 214408 0 None - 1 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 392 6 2 3 3.6 CCCCN1CCC(CNC(=O)c2cc(Br)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
11014701 214408 0 None - 1 Rat 9.2 pKi = 9.2 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 392 6 2 3 3.6 CCCCN1CCC(CNC(=O)c2cc(Br)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL95178 214408 0 None - 1 Rat 9.2 pKi = 9.2 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 392 6 2 3 3.6 CCCCN1CCC(CNC(=O)c2cc(Br)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
119376 8622 48 None -1 27 Human 9.2 pKi = 9.2 Binding
Binding affinity to YFP fused 5HT4 receptor expressed in CHO cellsBinding affinity to YFP fused 5HT4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm070552t
247 8622 48 None -1 27 Human 9.2 pKi = 9.2 Binding
Binding affinity to YFP fused 5HT4 receptor expressed in CHO cellsBinding affinity to YFP fused 5HT4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm070552t
CHEMBL33884 8622 48 None -1 27 Human 9.2 pKi = 9.2 Binding
Binding affinity to YFP fused 5HT4 receptor expressed in CHO cellsBinding affinity to YFP fused 5HT4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1021/jm070552t
11580890 80721 0 None 4 2 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 302 3 1 3 2.9 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1c[nH]c2ccc(F)cc12 10.1021/jm0509501
CHEMBL202122 80721 0 None 4 2 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 302 3 1 3 2.9 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1c[nH]c2ccc(F)cc12 10.1021/jm0509501
49783415 24450 0 None 3 12 Guinea pig 9.1 pKi = 9.1 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 24450 0 None 3 12 Guinea pig 9.1 pKi = 9.1 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
71451951 89453 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 372 8 0 5 5.0 CCCCN1CCC(COc2noc3cccc(OC4CCCC4)c23)CC1 10.1021/jm300953p
CHEMBL2179585 89453 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 372 8 0 5 5.0 CCCCN1CCC(COc2noc3cccc(OC4CCCC4)c23)CC1 10.1021/jm300953p
5145950 210266 7 None 5 2 Guinea pig 9.1 pKi = 9.1 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 553 13 2 8 3.7 COc1cc(COc2cc(N)c(Cl)cc2C(=O)CCC2CCN(CCNS(C)(=O)=O)CC2)cc(OC)c1 10.1016/S0960-894X(01)80414-5
CHEMBL586946 210266 7 None 5 2 Guinea pig 9.1 pKi = 9.1 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 553 13 2 8 3.7 COc1cc(COc2cc(N)c(Cl)cc2C(=O)CCC2CCN(CCNS(C)(=O)=O)CC2)cc(OC)c1 10.1016/S0960-894X(01)80414-5
CHEMBL66114 210266 7 None 5 2 Guinea pig 9.1 pKi = 9.1 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 553 13 2 8 3.7 COc1cc(COc2cc(N)c(Cl)cc2C(=O)CCC2CCN(CCNS(C)(=O)=O)CC2)cc(OC)c1 10.1016/S0960-894X(01)80414-5
53322003 63217 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 427 5 1 6 3.2 CC(C)(C)OC(=O)CN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632161 63217 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 427 5 1 6 3.2 CC(C)(C)OC(=O)CN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
71712327 98162 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 490 8 2 6 1.7 CC(C)c1nc2c(C(=O)NCC3CCN(CCN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402897 98162 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 490 8 2 6 1.7 CC(C)c1nc2c(C(=O)NCC3CCN(CCN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
9886435 99648 0 None -1 2 Guinea pig 9.1 pKi = 9.1 Binding
Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranesDisplacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes
ChEMBL 385 6 2 5 2.6 CC(O)CCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2013.09.004
CHEMBL2440453 99648 0 None -1 2 Guinea pig 9.1 pKi = 9.1 Binding
Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranesDisplacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes
ChEMBL 385 6 2 5 2.6 CC(O)CCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2013.09.004
9886435 99648 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]SB207710 from human recombinant 5-HT4 receptorDisplacement of [125I]SB207710 from human recombinant 5-HT4 receptor
ChEMBL 385 6 2 5 2.6 CC(O)CCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2013.09.004
CHEMBL2440453 99648 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]SB207710 from human recombinant 5-HT4 receptorDisplacement of [125I]SB207710 from human recombinant 5-HT4 receptor
ChEMBL 385 6 2 5 2.6 CC(O)CCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2013.09.004
68490431 89503 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 448 8 2 5 4.0 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(C(=O)O)cc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2179707 89503 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 448 8 2 5 4.0 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(C(=O)O)cc3)CC2)c2ccccc21 10.1021/jm300573d
21252902 91350 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 385 8 1 5 3.0 CC(C)n1nc(C(=O)NCC2CCN(CCCN(C)C)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2179701 91350 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 385 8 1 5 3.0 CC(C)n1nc(C(=O)NCC2CCN(CCCN(C)C)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2220907 91350 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 385 8 1 5 3.0 CC(C)n1nc(C(=O)NCC2CCN(CCCN(C)C)CC2)c2ccccc21 10.1021/jm300573d
70694780 83191 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 509 12 1 6 5.0 COC[C@@H]1CCCN1CCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
CHEMBL2059582 83191 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 509 12 1 6 5.0 COC[C@@H]1CCCN1CCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
252 10115 3 None -1 2 Human 9.1 pKi = 9.1 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 332 6 1 4 2.7 CCCCN1CCC(CC1)CNC(=O)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
44391713 10115 3 None -1 2 Human 9.1 pKi = 9.1 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 332 6 1 4 2.7 CCCCN1CCC(CC1)CNC(=O)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
CHEMBL182590 10115 3 None -1 2 Human 9.1 pKi = 9.1 Binding
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
ChEMBL 332 6 1 4 2.7 CCCCN1CCC(CC1)CNC(=O)c1cccc2c1OCCO2 10.1016/j.bmcl.2005.01.039
11508052 80612 0 None 4 2 Guinea pig 9.1 pKi = 9.1 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 285 3 1 4 2.2 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1[nH]nc2ccccc12 10.1021/jm0509501
CHEMBL201878 80612 0 None 4 2 Guinea pig 9.1 pKi = 9.1 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 285 3 1 4 2.2 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1[nH]nc2ccccc12 10.1021/jm0509501
19081848 212644 0 None - 1 Guinea pig 9.1 pKi = 9.1 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 502 13 1 6 6.4 CCCCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OCc2cc(OC)cc(OC)c2)CC1 10.1016/S0960-894X(01)80414-5
CHEMBL83755 212644 0 None - 1 Guinea pig 9.1 pKi = 9.1 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 502 13 1 6 6.4 CCCCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OCc2cc(OC)cc(OC)c2)CC1 10.1016/S0960-894X(01)80414-5
145981672 173327 0 None - 1 Guinea pig 9.1 pKi = 9.1 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 360 6 0 4 4.6 CCCCN1CCC(COC(=O)c2cc(Cl)nc3ccccc23)CC1 10.1039/C8MD00233A
CHEMBL4279446 173327 0 None - 1 Guinea pig 9.1 pKi = 9.1 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 360 6 0 4 4.6 CCCCN1CCC(COC(=O)c2cc(Cl)nc3ccccc23)CC1 10.1039/C8MD00233A
49783417 24486 0 None 18 2 Guinea pig 9.0 pKi = 9.0 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 306 6 1 5 2.6 CCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258560 24486 0 None 18 2 Guinea pig 9.0 pKi = 9.0 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 306 6 1 5 2.6 CCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
9973683 126585 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 326 5 1 5 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCCCC1 10.1021/jm960320m
CHEMBL348311 126585 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 326 5 1 5 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCCCC1 10.1021/jm960320m
10381762 56077 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 326 5 1 5 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(C)C1 10.1021/jm960320m
CHEMBL156349 56077 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 326 5 1 5 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(C)C1 10.1021/jm960320m
44213662 213376 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 324 4 1 5 2.5 Nc1c(Cl)cc(C(=O)OCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL88973 213376 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 324 4 1 5 2.5 Nc1c(Cl)cc(C(=O)OCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
118734523 125458 0 None - 1 Guinea pig 9.0 pKi = 9.0 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 394 6 1 5 4.4 COc1cc(N)c(Cl)cc1C(=O)OCC1CCN(CC2CCCCC2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3417008 125458 0 None - 1 Guinea pig 9.0 pKi = 9.0 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 394 6 1 5 4.4 COc1cc(N)c(Cl)cc1C(=O)OCC1CCN(CC2CCCCC2)CC1 10.1021/acs.jmedchem.5b00115
71462650 89454 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 372 9 0 5 4.9 CCCCN1CCC(COc2noc3cccc(OCC4CCC4)c23)CC1 10.1021/jm300953p
CHEMBL2179586 89454 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 372 9 0 5 4.9 CCCCN1CCC(COc2noc3cccc(OCC4CCC4)c23)CC1 10.1021/jm300953p
71712466 98016 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 439 6 2 4 3.4 CC(=O)N1CCC(CN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2401750 98016 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 439 6 2 4 3.4 CC(=O)N1CCC(CN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
15295138 57836 0 None - 1 Rat 9.0 pKi = 9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
CHEMBL157880 57836 0 None - 1 Rat 9.0 pKi = 9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
235 9342 42 None -4 3 Human 9.0 pKi = 9 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0307887
5311299 9342 42 None -4 3 Human 9.0 pKi = 9 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0307887
CHEMBL286136 9342 42 None -4 3 Human 9.0 pKi = 9 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0307887
9800656 22322 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
CHEMBL121913 22322 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
118712570 121009 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 538 10 2 6 4.6 CCCCS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
CHEMBL3329804 121009 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 538 10 2 6 4.6 CCCCS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmcl.2014.06.083
70696825 83187 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 479 10 1 5 5.4 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCCCC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059578 83187 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 479 10 1 5 5.4 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCCCC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
70696826 83189 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 467 11 1 5 5.2 CC(C)N(C)CCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
CHEMBL2059580 83189 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 467 11 1 5 5.2 CC(C)N(C)CCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
255 10262 21 None 1 2 Guinea pig 9.0 pKi = 9 Binding
In vitro by displacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor on guinea pig striatal membraneIn vitro by displacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor on guinea pig striatal membrane
ChEMBL 272 4 1 3 2.8 O=C(c1c[nH]c2c1cccc2)OCCN1CCCCC1 10.1021/jm960442e
3272300 10262 21 None 1 2 Guinea pig 9.0 pKi = 9 Binding
In vitro by displacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor on guinea pig striatal membraneIn vitro by displacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor on guinea pig striatal membrane
ChEMBL 272 4 1 3 2.8 O=C(c1c[nH]c2c1cccc2)OCCN1CCCCC1 10.1021/jm960442e
CHEMBL1255781 10262 21 None 1 2 Guinea pig 9.0 pKi = 9 Binding
In vitro by displacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor on guinea pig striatal membraneIn vitro by displacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor on guinea pig striatal membrane
ChEMBL 272 4 1 3 2.8 O=C(c1c[nH]c2c1cccc2)OCCN1CCCCC1 10.1021/jm960442e
10615668 193462 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 320 6 1 4 3.6 CCOc1ccccc1NC(=O)OCCN1C[C@@H](C)C[C@@H](C)C1 10.1021/jm960853v
CHEMBL48836 193462 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 320 6 1 4 3.6 CCOc1ccccc1NC(=O)OCCN1C[C@@H](C)C[C@@H](C)C1 10.1021/jm960853v
10690483 56074 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 369 6 2 6 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(C)=O)CC1 10.1021/jm960320m
CHEMBL156348 56074 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 369 6 2 6 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(C)=O)CC1 10.1021/jm960320m
235 9342 42 None 4 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80508-4
5311299 9342 42 None 4 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80508-4
CHEMBL286136 9342 42 None 4 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1016/S0960-894X(01)80508-4
235 9342 42 None 4 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm960853v
5311299 9342 42 None 4 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm960853v
CHEMBL286136 9342 42 None 4 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm960853v
235 9342 42 None 4 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm960320m
5311299 9342 42 None 4 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm960320m
CHEMBL286136 9342 42 None 4 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm960320m
53320712 63226 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 385 6 2 5 2.3 O=C(O)CCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632171 63226 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 385 6 2 5 2.3 O=C(O)CCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
71454555 86409 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 320 6 1 4 3.6 CCOc1ccccc1NC(=O)OCCN1C[C@H](C)C[C@@H](C)C1 10.1021/jm960853v
CHEMBL2115017 86409 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 320 6 1 4 3.6 CCOc1ccccc1NC(=O)OCCN1C[C@H](C)C[C@@H](C)C1 10.1021/jm960853v
71462776 89738 0 None 11 7 Human 8.9 pKi = 8.9 Binding
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181169 89738 0 None 11 7 Human 8.9 pKi = 8.9 Binding
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
71712325 98160 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 554 9 3 7 1.6 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]c(-c5ccccc5)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402895 98160 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 554 9 3 7 1.6 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]c(-c5ccccc5)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
71712463 98165 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
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 98165 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
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
11293856 91384 0 None 794 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 449 8 1 6 4.2 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc([N+](=O)[O-])cc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2179705 91384 0 None 794 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 449 8 1 6 4.2 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc([N+](=O)[O-])cc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2221192 91384 0 None 794 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 449 8 1 6 4.2 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc([N+](=O)[O-])cc3)CC2)c2ccccc21 10.1021/jm300573d
53322004 63220 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 477 10 1 7 4.1 CCOP(=O)(CCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1)OCC 10.1016/j.bmc.2010.10.011
CHEMBL1632164 63220 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 477 10 1 7 4.1 CCOP(=O)(CCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1)OCC 10.1016/j.bmc.2010.10.011
118712576 121015 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 527 8 2 6 4.2 O=C(NCC1CCN(Cc2ccc(NS(=O)(=O)C3CCCCC3)cc2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2014.06.083
CHEMBL3329810 121015 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 527 8 2 6 4.2 O=C(NCC1CCN(Cc2ccc(NS(=O)(=O)C3CCCCC3)cc2)CC1)c1cccc2c1OCCO2 10.1016/j.bmcl.2014.06.083
118712578 121016 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 440 6 1 6 3.8 O=C(OCC1CCN(CC2CCC(C(=O)O)C2)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmcl.2014.06.083
CHEMBL3329811 121016 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 440 6 1 6 3.8 O=C(OCC1CCN(CC2CCC(C(=O)O)C2)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmcl.2014.06.083
118712579 121017 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 454 6 1 6 4.2 O=C(OCC1CCN(CC2CCCC(C(=O)O)C2)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmcl.2014.06.083
CHEMBL3329812 121017 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 454 6 1 6 4.2 O=C(OCC1CCN(CC2CCCC(C(=O)O)C2)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmcl.2014.06.083
44248186 202240 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 567 15 3 5 6.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
CHEMBL552484 202240 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 567 15 3 5 6.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
119376 8622 48 None -1 27 Human 8.9 pKi = 8.9 Binding
Antagonist activity at 5-HT4 receptor in human HeLa cells assessed as inhibition of intracellular calcium mobilization incubated for 2 hrs by FLIPR assayAntagonist activity at 5-HT4 receptor in human HeLa cells assessed as inhibition of intracellular calcium mobilization incubated for 2 hrs by FLIPR assay
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2023.117256
247 8622 48 None -1 27 Human 8.9 pKi = 8.9 Binding
Antagonist activity at 5-HT4 receptor in human HeLa cells assessed as inhibition of intracellular calcium mobilization incubated for 2 hrs by FLIPR assayAntagonist activity at 5-HT4 receptor in human HeLa cells assessed as inhibition of intracellular calcium mobilization incubated for 2 hrs by FLIPR assay
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2023.117256
CHEMBL33884 8622 48 None -1 27 Human 8.9 pKi = 8.9 Binding
Antagonist activity at 5-HT4 receptor in human HeLa cells assessed as inhibition of intracellular calcium mobilization incubated for 2 hrs by FLIPR assayAntagonist activity at 5-HT4 receptor in human HeLa cells assessed as inhibition of intracellular calcium mobilization incubated for 2 hrs by FLIPR assay
ChEMBL 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10.1016/j.bmc.2023.117256
10524522 22297 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cnccn2)CC1 10.1021/jm0009538
CHEMBL121776 22297 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cnccn2)CC1 10.1021/jm0009538
10548505 119881 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccnn2)CC1 10.1021/jm0009538
CHEMBL331396 119881 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccnn2)CC1 10.1021/jm0009538
133999 81090 8 None 5 2 Guinea pig 8.9 pKi = 8.9 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 318 3 1 4 2.2 O=C(NC[C@@H]1CCN2CCC[C@@H]12)c1cc(Cl)cn2ccnc12 10.1021/jm0509501
CHEMBL202434 81090 8 None 5 2 Guinea pig 8.9 pKi = 8.9 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 318 3 1 4 2.2 O=C(NC[C@@H]1CCN2CCC[C@@H]12)c1cc(Cl)cn2ccnc12 10.1021/jm0509501
52945318 24315 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 348 6 1 6 2.7 CCCCN1CCC(COC(=O)c2ccc(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1257991 24315 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 348 6 1 6 2.7 CCCCN1CCC(COC(=O)c2ccc(N)c3c2OCCO3)CC1 10.1021/jm100668r
44592414 185949 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 332 3 2 3 2.8 C[C@@]12CCCN1CC[C@H]2CNC(=O)c1cc(Cl)cc2nc[nH]c12 10.1016/j.bmc.2008.11.045
CHEMBL472219 185949 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 332 3 2 3 2.8 C[C@@]12CCCN1CC[C@H]2CNC(=O)c1cc(Cl)cc2nc[nH]c12 10.1016/j.bmc.2008.11.045
9905514 126460 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(O)CC1 10.1021/jm960320m
CHEMBL347235 126460 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(O)CC1 10.1021/jm960320m
10570203 56326 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 355 6 2 6 1.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(N)=O)CC1 10.1021/jm960320m
CHEMBL156554 56326 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 355 6 2 6 1.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(N)=O)CC1 10.1021/jm960320m
10644148 120601 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 390 6 1 7 2.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccn2)CC1 10.1021/jm0009538
CHEMBL332553 120601 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 390 6 1 7 2.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccn2)CC1 10.1021/jm0009538
145980826 173430 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 326 6 0 4 3.9 CCCCN1CCC(COC(=O)c2ccnc3ccccc23)CC1 10.1039/C8MD00233A
CHEMBL4281416 173430 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 326 6 0 4 3.9 CCCCN1CCC(COC(=O)c2ccnc3ccccc23)CC1 10.1039/C8MD00233A
11166796 89451 0 None 2 2 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation counting
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 89451 0 None 2 2 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation counting
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
50898778 63229 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 427 9 2 5 3.5 O=C(O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632174 63229 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 427 9 2 5 3.5 O=C(O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
71712328 98163 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 470 7 2 6 2.5 COC(=O)N1CCN(CCN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402898 98163 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 470 7 2 6 2.5 COC(=O)N1CCN(CCN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
177336 9894 50 None -6 3 Guinea pig 8.8 pKi = 8.8 Binding
Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranesDisplacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
225 9894 50 None -6 3 Guinea pig 8.8 pKi = 8.8 Binding
Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranesDisplacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
CHEMBL356359 9894 50 None -6 3 Guinea pig 8.8 pKi = 8.8 Binding
Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranesDisplacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
DB04873 9894 50 None -6 3 Guinea pig 8.8 pKi = 8.8 Binding
Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranesDisplacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
177336 9894 50 None 6 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]SB207710 from human recombinant 5-HT4 receptorDisplacement of [125I]SB207710 from human recombinant 5-HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
225 9894 50 None 6 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]SB207710 from human recombinant 5-HT4 receptorDisplacement of [125I]SB207710 from human recombinant 5-HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
CHEMBL356359 9894 50 None 6 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]SB207710 from human recombinant 5-HT4 receptorDisplacement of [125I]SB207710 from human recombinant 5-HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
DB04873 9894 50 None 6 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]SB207710 from human recombinant 5-HT4 receptorDisplacement of [125I]SB207710 from human recombinant 5-HT4 receptor
ChEMBL 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 10.1016/j.bmc.2013.09.004
118712577 120918 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 464 6 1 6 3.5 O=C(OCC1CCN(CC2C3CC4C2C4C3C(=O)O)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmcl.2014.06.083
CHEMBL3329226 120918 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 464 6 1 6 3.5 O=C(OCC1CCN(CC2C3CC4C2C4C3C(=O)O)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmcl.2014.06.083
70688535 83193 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 586 13 2 7 4.2 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCC(CNS(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059584 83193 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 586 13 2 7 4.2 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCC(CNS(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
44248184 202941 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 525 12 3 5 5.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
CHEMBL561278 202941 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 525 12 3 5 5.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
11166796 89451 0 None -2 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
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 89451 0 None -2 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
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
10854687 55330 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 340 5 1 5 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(C)(C)C1 10.1021/jm960320m
CHEMBL155682 55330 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 340 5 1 5 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(C)(C)C1 10.1021/jm960320m
42636941 185728 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL470432 185728 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
23202543 212174 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 493 11 2 6 3.7 CS(=O)(=O)NCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OCc2ccccc2)CC1 10.1016/S0960-894X(01)80414-5
CHEMBL80026 212174 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
ChEMBL 493 11 2 6 3.7 CS(=O)(=O)NCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OCc2ccccc2)CC1 10.1016/S0960-894X(01)80414-5
44323244 19157 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
CHEMBL1185621 19157 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
CHEMBL423504 19157 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
22708808 213842 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 365 6 2 4 3.1 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)c3c2OCC3)CC1 10.1016/0960-894X(96)00002-9
CHEMBL91771 213842 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 365 6 2 4 3.1 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)c3c2OCC3)CC1 10.1016/0960-894X(96)00002-9
162662474 188833 0 None - 1 Guinea pig 8.7 pKi = 8.7 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 494 10 3 7 3.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(N)cc2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4781228 188833 0 None - 1 Guinea pig 8.7 pKi = 8.7 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 494 10 3 7 3.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(N)cc2)CC1 10.1016/j.ejmech.2016.05.048
71714544 98159 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 542 9 3 7 1.1 CC(F)(F)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402894 98159 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 542 9 3 7 1.1 CC(F)(F)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
44628200 89494 0 None 1584 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 456 7 1 5 5.0 CC(=O)Nc1ccc(CCN2CCC(COc3nc4ccccc4c4cn(C)cc34)CC2)cc1 10.1021/jm300573d
CHEMBL2179670 89494 0 None 1584 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 456 7 1 5 5.0 CC(=O)Nc1ccc(CCN2CCC(COc3nc4ccccc4c4cn(C)cc34)CC2)cc1 10.1021/jm300573d
44628198 89498 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 443 7 1 5 4.8 Cn1cc2c(OCC3CCN(CCc4ccc(C(=O)O)cc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2179674 89498 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 443 7 1 5 4.8 Cn1cc2c(OCC3CCN(CCc4ccc(C(=O)O)cc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
44629279 89499 0 None 39 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 399 6 0 4 5.1 Cn1cc2c(OCC3CCN(CCc4ccccc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2179678 89499 0 None 39 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 399 6 0 4 5.1 Cn1cc2c(OCC3CCN(CCc4ccccc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
53320713 63227 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 399 7 2 5 2.7 O=C(O)CCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632172 63227 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 399 7 2 5 2.7 O=C(O)CCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
70682173 83186 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 453 7 2 6 3.2 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCCCC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059577 83186 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 453 7 2 6 3.2 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCCCC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
44248189 91900499 201625 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
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 201625 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
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
44248315 202700 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 522 11 1 6 4.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCOCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL559322 202700 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 522 11 1 6 4.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCOCC2)cc2ccccc21 10.1021/jm900881j
9819953 128089 0 None - 1 Guinea pig 8.0 pKi = 8 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 353 6 1 4 4.5 CCCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL35808 128089 0 None - 1 Guinea pig 8.0 pKi = 8 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 353 6 1 4 4.5 CCCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
11520655 139609 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 792 19 4 12 4.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNC(=O)CCC(=O)NCCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL370181 139609 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 792 19 4 12 4.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNC(=O)CCC(=O)NCCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
17755141 85900 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to Rluc fused 5HT4 receptor expressed in CHO cellsBinding affinity to Rluc fused 5HT4 receptor expressed in CHO cells
ChEMBL 1183 28 4 16 9.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CCCc2ccc(CCCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
CHEMBL2113289 85900 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to Rluc fused 5HT4 receptor expressed in CHO cellsBinding affinity to Rluc fused 5HT4 receptor expressed in CHO cells
ChEMBL 1183 28 4 16 9.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CCCc2ccc(CCCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
17755141 85900 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to YFP fused 5HT4 receptor expressed in CHO cellsBinding affinity to YFP fused 5HT4 receptor expressed in CHO cells
ChEMBL 1183 28 4 16 9.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CCCc2ccc(CCCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
CHEMBL2113289 85900 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to YFP fused 5HT4 receptor expressed in CHO cellsBinding affinity to YFP fused 5HT4 receptor expressed in CHO cells
ChEMBL 1183 28 4 16 9.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCN(CCCc2ccc(CCCN(CCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)OC(C)(C)C)cc2)C(=O)OC(C)(C)C)CC1 10.1021/jm070552t
44628201 89496 0 None 3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 429 7 1 5 4.6 Cn1cc2c(OCC3CCN(CCc4ccc(CO)cc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2179672 89496 0 None 3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 429 7 1 5 4.6 Cn1cc2c(OCC3CCN(CCc4ccc(CO)cc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
11225102 83199 3 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.05.034
CHEMBL2059590 83199 3 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.05.034
11225102 83199 3 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.08.051
CHEMBL2059590 83199 3 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1 10.1016/j.bmcl.2012.08.051
44248679 202378 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 599 12 1 7 3.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL555693 202378 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 599 12 1 7 3.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44248925 203199 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 436 9 2 5 3.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2CCCCC2)CC1 10.1021/jm900881j
CHEMBL562902 203199 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 436 9 2 5 3.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2CCCCC2)CC1 10.1021/jm900881j
10712297 193888 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 341 5 2 5 3.2 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCC(C)C1 10.1021/jm960853v
CHEMBL49155 193888 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 341 5 2 5 3.2 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCC(C)C1 10.1021/jm960853v
10688750 215165 0 None - 1 Guinea pig 8.0 pKi = 8.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 343 4 1 6 0.9 CN1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL99590 215165 0 None - 1 Guinea pig 8.0 pKi = 8.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 343 4 1 6 0.9 CN1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
44281102 123493 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 312 4 1 5 2.6 CCN1CCC(OC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80508-4
CHEMBL33732 123493 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 312 4 1 5 2.6 CCN1CCC(OC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1016/S0960-894X(01)80508-4
10584 8245 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Agonist activity at 5-HT4R (unknown origin)Agonist activity at 5-HT4R (unknown origin)
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.ejmech.2018.10.064
86582973 8245 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Agonist activity at 5-HT4R (unknown origin)Agonist activity at 5-HT4R (unknown origin)
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.ejmech.2018.10.064
CHEMBL3417009 8245 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Agonist activity at 5-HT4R (unknown origin)Agonist activity at 5-HT4R (unknown origin)
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.ejmech.2018.10.064
10584 8245 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GR113808 from human 5-HT4 receptor expressed in Chem-1 cell membrane incubated for 60 mins by radiometric scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4 receptor expressed in Chem-1 cell membrane incubated for 60 mins by radiometric scintillation counting analysis
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.bmcl.2022.128873
86582973 8245 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GR113808 from human 5-HT4 receptor expressed in Chem-1 cell membrane incubated for 60 mins by radiometric scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4 receptor expressed in Chem-1 cell membrane incubated for 60 mins by radiometric scintillation counting analysis
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.bmcl.2022.128873
CHEMBL3417009 8245 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GR113808 from human 5-HT4 receptor expressed in Chem-1 cell membrane incubated for 60 mins by radiometric scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4 receptor expressed in Chem-1 cell membrane incubated for 60 mins by radiometric scintillation counting analysis
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.bmcl.2022.128873
9881054 133830 0 None - 1 Guinea pig 8.0 pKi = 8.0 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 339 4 1 4 4.1 CCN1CCC(COc2nc3ccccc3c3c2CCCCN3)CC1 10.1021/jm020954v
CHEMBL36558 133830 0 None - 1 Guinea pig 8.0 pKi = 8.0 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 339 4 1 4 4.1 CCN1CCC(COc2nc3ccccc3c3c2CCCCN3)CC1 10.1021/jm020954v
235 9342 42 None -4 3 Human 8.0 pKi = 8.0 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
5311299 9342 42 None -4 3 Human 8.0 pKi = 8.0 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
CHEMBL286136 9342 42 None -4 3 Human 8.0 pKi = 8.0 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
240 7731 43 None -11 25 Human 7.0 pKi = 7 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
2769 7731 43 None -11 25 Human 7.0 pKi = 7 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
44279790 7731 43 None -11 25 Human 7.0 pKi = 7 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
660 7731 43 None -11 25 Human 7.0 pKi = 7 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL1729 7731 43 None -11 25 Human 7.0 pKi = 7 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL560739 7731 43 None -11 25 Human 7.0 pKi = 7 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
DB00604 7731 43 None -11 25 Human 7.0 pKi = 7 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
5 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm900018b
5 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901126m
5202 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm900018b
5202 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901126m
CHEMBL39 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm900018b
CHEMBL39 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901126m
DB08839 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm900018b
DB08839 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901126m
71457412 89749 0 None - 1 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 348 5 0 3 5.2 CCCN1CCC(COc2nc3c(C)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181186 89749 0 None - 1 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 348 5 0 3 5.2 CCCN1CCC(COc2nc3c(C)cccc3c3ccccc23)CC1 10.1021/jm300943r
5311047 211542 33 None -5 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
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.bmcl.2012.05.034
CHEMBL74656 211542 33 None -5 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
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.bmcl.2012.05.034
70682705 84278 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 483 7 3 6 1.9 CNC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
CHEMBL2087329 84278 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 483 7 3 6 1.9 CNC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
70686942 84279 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 483 7 3 6 1.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNC(=O)N(C)C)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087330 84279 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 483 7 3 6 1.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNC(=O)N(C)C)cc2ccccc21 10.1016/j.bmcl.2012.08.051
5311047 211542 33 None -5 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
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.bmcl.2012.08.051
CHEMBL74656 211542 33 None -5 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
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.bmcl.2012.08.051
44248797 202491 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 353 7 2 4 3.3 CCCCCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
CHEMBL557053 202491 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 353 7 2 4 3.3 CCCCCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
5 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
5202 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
CHEMBL39 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
DB08839 6927 72 None -190 53 Guinea pig 7.0 pKi = 7 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
118712568 121007 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 516 9 3 4 4.8 O=C(NCC1CCN(Cc2ccc(NS(=O)(=O)Cc3ccccc3)cc2)CC1)c1c[nH]c2ccccc12 10.1016/j.bmcl.2014.06.083
CHEMBL3329802 121007 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 516 9 3 4 4.8 O=C(NCC1CCN(Cc2ccc(NS(=O)(=O)Cc3ccccc3)cc2)CC1)c1c[nH]c2ccccc12 10.1016/j.bmcl.2014.06.083
44249189 91900488 202181 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 447 6 2 6 2.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
CHEMBL552075 202181 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 447 6 2 6 2.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
44248310 203335 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 512 6 1 6 3.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
CHEMBL563799 203335 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 512 6 1 6 3.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
44575 204295 1 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 311 4 2 4 2.1 CCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
CHEMBL570074 204295 1 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 311 4 2 4 2.1 CCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
15544715 119572 4 None - 1 Rat 6.0 pKi = 6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 272 3 2 3 1.8 CCN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL330605 119572 4 None - 1 Rat 6.0 pKi = 6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 272 3 2 3 1.8 CCN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
44327586 170610 4 None - 1 Rat 6.0 pKi = 6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 286 4 2 3 2.2 CCCN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL420638 170610 4 None - 1 Rat 6.0 pKi = 6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 286 4 2 3 2.2 CCCN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
15544721 105749 4 None - 1 Rat 5.0 pKi = 5 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 259 2 1 4 1.8 CN1CCC(OC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL279823 105749 4 None - 1 Rat 5.0 pKi = 5 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 259 2 1 4 1.8 CN1CCC(OC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
155525723 177864 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assayBinding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assay
ChEMBL 515 11 3 7 4.2 COc1cc(/C=C/C(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)ccc1O 10.1016/j.ejmech.2019.111596
CHEMBL4457426 177864 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assayBinding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assay
ChEMBL 515 11 3 7 4.2 COc1cc(/C=C/C(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)ccc1O 10.1016/j.ejmech.2019.111596
71461048 89748 0 None -3 2 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3cc(F)ccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181185 89748 0 None -3 2 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3cc(F)ccc3c3ccccc23)CC1 10.1021/jm300943r
10712151 126943 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 339 5 2 4 2.6 COc1cc(N)c(Cl)cc1C(=O)NCCN1CC(C)CC(C)C1 10.1021/jm960320m
CHEMBL351557 126943 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 339 5 2 4 2.6 COc1cc(N)c(Cl)cc1C(=O)NCCN1CC(C)CC(C)C1 10.1021/jm960320m
10832327 10993 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 359 5 1 6 1.6 CCN1CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL100317 10993 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 359 5 1 6 1.6 CCN1CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
2780 117306 36 None -20 10 Rat 7.0 pKi = 7.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/0960-894X(95)00115-A
CHEMBL325109 117306 36 None -20 10 Rat 7.0 pKi = 7.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/0960-894X(95)00115-A
2780 117306 36 None -20 10 Guinea pig 7.0 pKi = 7.0 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1021/jm020270n
CHEMBL325109 117306 36 None -20 10 Guinea pig 7.0 pKi = 7.0 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1021/jm020270n
5 6927 72 None -288 53 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801327q
5202 6927 72 None -288 53 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801327q
CHEMBL39 6927 72 None -288 53 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801327q
DB08839 6927 72 None -288 53 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801327q
118734520 125455 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 421 8 1 5 5.4 CO/N=C(\CCC1CCN(CC2CCCCC2)CC1)c1cc(Cl)c(N)cc1OC 10.1021/acs.jmedchem.5b00115
CHEMBL3417005 125455 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 421 8 1 5 5.4 CO/N=C(\CCC1CCN(CC2CCCCC2)CC1)c1cc(Cl)c(N)cc1OC 10.1021/acs.jmedchem.5b00115
90644475 119059 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 357 4 0 4 3.4 O=C1c2cccc3nc(Cl)cc(c23)C(=O)N1CCCN1CCCCC1 10.1016/j.ejmech.2014.05.015
CHEMBL3291080 119059 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 357 4 0 4 3.4 O=C1c2cccc3nc(Cl)cc(c23)C(=O)N1CCCN1CCCCC1 10.1016/j.ejmech.2014.05.015
136118638 83091 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058698 83091 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
10594888 10949 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 363 4 1 6 1.3 CC(C)n1c(=O)n(C(=O)NCCN2CCN(C)CC2)c2cc(F)ccc21 10.1021/jm981098j
CHEMBL100088 10949 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 363 4 1 6 1.3 CC(C)n1c(=O)n(C(=O)NCCN2CCN(C)CC2)c2cc(F)ccc21 10.1021/jm981098j
5 6927 72 None -288 53 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2009.01.015
5202 6927 72 None -288 53 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2009.01.015
CHEMBL39 6927 72 None -288 53 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2009.01.015
DB08839 6927 72 None -288 53 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2009.01.015
11686484 139620 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 806 20 4 12 4.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNC(=O)CCCC(=O)NCCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL370182 139620 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 806 20 4 12 4.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNC(=O)CCCC(=O)NCCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
11629240 147853 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 806 20 4 12 4.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCCCC(=O)NCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL382543 147853 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 806 20 4 12 4.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCCCC(=O)NCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
49783421 24560 0 None -51 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 352 9 1 5 3.3 CCCCN1CCC(COC(=O)c2ccc(N)c(OCCF)c2)CC1 10.1021/jm100668r
CHEMBL1258786 24560 0 None -51 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 352 9 1 5 3.3 CCCCN1CCC(COC(=O)c2ccc(N)c(OCCF)c2)CC1 10.1021/jm100668r
44592282 185985 0 None - 1 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 355 6 0 5 4.5 C=CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL472481 185985 0 None - 1 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 355 6 0 5 4.5 C=CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
15544716 118172 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 379 7 3 5 0.6 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL327192 118172 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 379 7 3 5 0.6 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
15544716 118172 0 None - 1 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 379 7 3 5 0.6 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL327192 118172 0 None - 1 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 379 7 3 5 0.6 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
15544716 118172 0 None - 1 Rat 7.9 pKi = 7.9 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 379 7 3 5 0.6 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL327192 118172 0 None - 1 Rat 7.9 pKi = 7.9 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 379 7 3 5 0.6 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
10739944 85530 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 403 7 1 6 3.3 COc1cc(N)c(Cl)cc1C(=O)OCCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
CHEMBL2112621 85530 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 403 7 1 6 3.3 COc1cc(N)c(Cl)cc1C(=O)OCCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
44592148 185634 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 5 0 5 4.1 CCCN1CCC(COc2nc3sccc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL469582 185634 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 5 0 5 4.1 CCCN1CCC(COc2nc3sccc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
243 9976 91 None 12 34 Human 7.0 pKi = 7.0 Binding
Tested for selectivity for 5-hydroxytryptamine 4 receptorTested for selectivity for 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/jm020099f
3052762 9976 91 None 12 34 Human 7.0 pKi = 7.0 Binding
Tested for selectivity for 5-hydroxytryptamine 4 receptorTested for selectivity for 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/jm020099f
3502 9976 91 None 12 34 Human 7.0 pKi = 7.0 Binding
Tested for selectivity for 5-hydroxytryptamine 4 receptorTested for selectivity for 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/jm020099f
CHEMBL117287 9976 91 None 12 34 Human 7.0 pKi = 7.0 Binding
Tested for selectivity for 5-hydroxytryptamine 4 receptorTested for selectivity for 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/jm020099f
DB06480 9976 91 None 12 34 Human 7.0 pKi = 7.0 Binding
Tested for selectivity for 5-hydroxytryptamine 4 receptorTested for selectivity for 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1021/jm020099f
44582815 180007 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 621 11 3 9 3.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCN2C(=O)c3cccc4c(N)ccc(c34)C2=O)CC1 10.1021/jm801327q
CHEMBL452353 180007 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 621 11 3 9 3.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCN2C(=O)c3cccc4c(N)ccc(c34)C2=O)CC1 10.1021/jm801327q
11557207 85830 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 1203 39 7 18 10.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCNc2nc(NCCCCCCCCCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)nc(NCc3ccccc3)n2)CC1 10.1021/jm050234z
CHEMBL2113160 85830 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 1203 39 7 18 10.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCNc2nc(NCCCCCCCCCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)nc(NCc3ccccc3)n2)CC1 10.1021/jm050234z
10925529 214676 0 None - 1 Rat 6.9 pKi = 6.9 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 329 6 3 4 2.4 CCCCN1CCC(CNC(=O)c2ccc(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL96667 214676 0 None - 1 Rat 6.9 pKi = 6.9 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 329 6 3 4 2.4 CCCCN1CCC(CNC(=O)c2ccc(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
132164 213427 12 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 321 2 2 4 1.7 Nc1c(Cl)cc(C(=O)N[C@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL89259 213427 12 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 321 2 2 4 1.7 Nc1c(Cl)cc(C(=O)N[C@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
10925529 214676 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 329 6 3 4 2.4 CCCCN1CCC(CNC(=O)c2ccc(N)c3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL96667 214676 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 329 6 3 4 2.4 CCCCN1CCC(CNC(=O)c2ccc(N)c3[nH]cnc23)CC1 10.1021/jm020807x
71457408 89736 0 None - 1 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 536 7 0 3 6.7 Ic1ccc(CCCN2CCC(COc3nc4ccccc4c4ccccc34)CC2)cc1 10.1021/jm300943r
CHEMBL2181167 89736 0 None - 1 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 536 7 0 3 6.7 Ic1ccc(CCCN2CCC(COc3nc4ccccc4c4ccccc34)CC2)cc1 10.1021/jm300943r
10925529 214676 0 None - 1 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 329 6 3 4 2.4 CCCCN1CCC(CNC(=O)c2ccc(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL96667 214676 0 None - 1 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 329 6 3 4 2.4 CCCCN1CCC(CNC(=O)c2ccc(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
136118650 83098 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058705 83098 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
11039391 213063 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 617 11 2 9 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
CHEMBL86985 213063 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 617 11 2 9 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
42618251 193714 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 530 14 3 7 3.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCNCCCc2ccccc2)CC1 10.1021/jm801327q
CHEMBL490050 193714 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 530 14 3 7 3.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCNCCCc2ccccc2)CC1 10.1021/jm801327q
49783418 24487 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 334 8 1 5 3.3 CCCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258561 24487 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 334 8 1 5 3.3 CCCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
162652829 187166 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 508 11 1 7 4.5 COc1ccc(S(=O)(=O)CCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1016/j.ejmech.2016.05.048
CHEMBL4751840 187166 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 508 11 1 7 4.5 COc1ccc(S(=O)(=O)CCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1016/j.ejmech.2016.05.048
162650788 186966 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 509 11 2 7 3.6 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1016/j.ejmech.2016.05.048
CHEMBL4749344 186966 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 509 11 2 7 3.6 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1016/j.ejmech.2016.05.048
10270343 125817 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 367 7 1 4 4.9 CCCCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL34263 125817 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 367 7 1 4 4.9 CCCCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
10408029 23232 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
CHEMBL123377 23232 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
71714543 98158 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 534 8 3 7 1.2 CC(C)(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
CHEMBL2402893 98158 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 534 8 3 7 1.2 CC(C)(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1 10.1016/j.bmcl.2013.05.018
11168006 83198 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 502 7 1 7 1.9 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059589 83198 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 502 7 1 7 1.9 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
44224237 201569 8 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
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 201569 8 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
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 201569 8 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
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.2012.08.051
CHEMBL538635 201569 8 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
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.2012.08.051
44224237 201569 8 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
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 201569 8 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
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
10291662 126981 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 353 5 1 4 4.5 CCCN1CCC(COc2nc3ccccc3c3c2CCCCN3)CC1 10.1021/jm020954v
CHEMBL35196 126981 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 353 5 1 4 4.5 CCCN1CCC(COc2nc3ccccc3c3c2CCCCN3)CC1 10.1021/jm020954v
155565664 182382 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assayBinding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assay
ChEMBL 432 8 2 6 4.5 COc1ccc(CN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1O 10.1016/j.ejmech.2019.111596
CHEMBL4580044 182382 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assayBinding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assay
ChEMBL 432 8 2 6 4.5 COc1ccc(CN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1O 10.1016/j.ejmech.2019.111596
44592186 185638 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 5 0 5 4.1 Cc1csc2nc(OCCCN3CCCCC3)c3cccn3c12 10.1016/j.bmc.2008.11.045
CHEMBL469593 185638 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 5 0 5 4.1 Cc1csc2nc(OCCCN3CCCCC3)c3cccn3c12 10.1016/j.bmc.2008.11.045
4595 183494 106 None -3 14 Rat 5.9 pKi = 5.9 Binding
The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O 10.1021/jm00075a026
CHEMBL46 183494 106 None -3 14 Rat 5.9 pKi = 5.9 Binding
The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O 10.1021/jm00075a026
145957594 168757 0 None - 1 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 791 33 3 15 2.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCN=[N+]=[N-])CC1 10.1039/C6MD00458J
CHEMBL4159138 168757 0 None - 1 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 791 33 3 15 2.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCN=[N+]=[N-])CC1 10.1039/C6MD00458J
118734521 125456 0 None - 1 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 394 7 2 4 5.0 COc1cc(N)c(Cl)cc1C(O)CCC1CCN(CC2CCCCC2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3417006 125456 0 None - 1 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 394 7 2 4 5.0 COc1cc(N)c(Cl)cc1C(O)CCC1CCN(CC2CCCCC2)CC1 10.1021/acs.jmedchem.5b00115
10567201 191044 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 313 5 2 5 2.6 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCC1 10.1021/jm960853v
CHEMBL48379 191044 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 313 5 2 5 2.6 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCC1 10.1021/jm960853v
260 10641 54 None -45 6 Guinea pig 6.9 pKi = 6.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/s0960-894x(01)00693-x
2775 10641 54 None -45 6 Guinea pig 6.9 pKi = 6.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/s0960-894x(01)00693-x
656665 10641 54 None -45 6 Guinea pig 6.9 pKi = 6.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/s0960-894x(01)00693-x
CHEMBL56564 10641 54 None -45 6 Guinea pig 6.9 pKi = 6.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/s0960-894x(01)00693-x
DB11699 10641 54 None -45 6 Guinea pig 6.9 pKi = 6.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/s0960-894x(01)00693-x
240 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
Binding affinity to serotonin 5-HT4 receptor (unknown origin)Binding affinity to serotonin 5-HT4 receptor (unknown origin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
2769 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
Binding affinity to serotonin 5-HT4 receptor (unknown origin)Binding affinity to serotonin 5-HT4 receptor (unknown origin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
44279790 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
Binding affinity to serotonin 5-HT4 receptor (unknown origin)Binding affinity to serotonin 5-HT4 receptor (unknown origin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
660 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
Binding affinity to serotonin 5-HT4 receptor (unknown origin)Binding affinity to serotonin 5-HT4 receptor (unknown origin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL1729 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
Binding affinity to serotonin 5-HT4 receptor (unknown origin)Binding affinity to serotonin 5-HT4 receptor (unknown origin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL560739 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
Binding affinity to serotonin 5-HT4 receptor (unknown origin)Binding affinity to serotonin 5-HT4 receptor (unknown origin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
DB00604 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
Binding affinity to serotonin 5-HT4 receptor (unknown origin)Binding affinity to serotonin 5-HT4 receptor (unknown origin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
44629348 91358 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 427 7 0 4 6.1 CC(C)n1cc2c(OCC3CCN(CCc4ccccc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2179677 91358 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 427 7 0 4 6.1 CC(C)n1cc2c(OCC3CCN(CCc4ccccc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2220955 91358 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 427 7 0 4 6.1 CC(C)n1cc2c(OCC3CCN(CCc4ccccc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
44249315 201954 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 331 4 2 6 0.8 CC(C)n1c(=O)n(C(=O)NCCN2CCNCC2)c2ccccc21 10.1021/jm900881j
CHEMBL550459 201954 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 331 4 2 6 0.8 CC(C)n1c(=O)n(C(=O)NCCN2CCNCC2)c2ccccc21 10.1021/jm900881j
44248066 201965 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 473 7 2 7 0.7 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
CHEMBL550530 201965 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 473 7 2 7 0.7 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
44249055 91900481 202198 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 367 4 1 4 3.3 CCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
CHEMBL552218 202198 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 367 4 1 4 3.3 CCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
10643698 202231 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 383 5 2 5 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCO)cc2ccccc21 10.1021/jm900881j
CHEMBL552420 202231 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 383 5 2 5 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCO)cc2ccccc21 10.1021/jm900881j
3233 10285 44 None -933 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptorBinding affinity towards 5-hydroxytryptamine 4 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
3247 10285 44 None -933 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptorBinding affinity towards 5-hydroxytryptamine 4 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
6604889 10285 44 None -933 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptorBinding affinity towards 5-hydroxytryptamine 4 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
CHEMBL282199 10285 44 None -933 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptorBinding affinity towards 5-hydroxytryptamine 4 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
DB13988 10285 44 None -933 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptorBinding affinity towards 5-hydroxytryptamine 4 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
44249179 201602 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 312 5 3 5 0.6 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCNCC1 10.1021/jm900881j
CHEMBL539212 201602 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 312 5 3 5 0.6 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCNCC1 10.1021/jm900881j
3157 8252 71 None -27 12 Guinea pig 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
7170 8252 71 None -27 12 Guinea pig 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
954 8252 71 None -27 12 Guinea pig 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
CHEMBL707 8252 71 None -27 12 Guinea pig 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
DB00590 8252 71 None -27 12 Guinea pig 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
49845575 26131 0 None - 1 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 467 5 0 5 4.9 Cc1csc2nc(OCC3CCN(C/C=C/I)CC3)c3cccn3c12 10.1016/j.ejmech.2010.07.052
CHEMBL1290805 26131 0 None - 1 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 467 5 0 5 4.9 Cc1csc2nc(OCC3CCN(C/C=C/I)CC3)c3cccn3c12 10.1016/j.ejmech.2010.07.052
11577105 78939 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 510 16 3 7 4.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCN)CC1 10.1021/jm050234z
CHEMBL197965 78939 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 510 16 3 7 4.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCN)CC1 10.1021/jm050234z
11593090 78969 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 834 22 4 12 5.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNC(=O)CCCCCC(=O)NCCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL198052 78969 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 834 22 4 12 5.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNC(=O)CCCCCC(=O)NCCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
44404964 79247 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 736 15 5 12 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
CHEMBL198921 79247 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 736 15 5 12 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
130946 209537 2 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT4 receptorBinding affinity to 5HT4 receptor
ChEMBL 328 2 1 5 2.0 CCn1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1016/j.bmc.2008.12.025
CHEMBL62023 209537 2 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT4 receptorBinding affinity to 5HT4 receptor
ChEMBL 328 2 1 5 2.0 CCn1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1016/j.bmc.2008.12.025
145955141 169469 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 426 9 3 6 2.7 CCCCNC(=O)NC1CCN(CCOC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1039/C6MD00458J
CHEMBL4170461 169469 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 426 9 3 6 2.7 CCCCNC(=O)NC1CCN(CCOC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1039/C6MD00458J
9858485 129909 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 325 4 1 4 3.7 CCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL36120 129909 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 325 4 1 4 3.7 CCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
71462777 89740 0 None -1 4 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181171 89740 0 None -1 4 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3ncccc23)CC1 10.1021/jm300943r
10045643 214863 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 385 7 1 6 2.1 CCCCN1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL97755 214863 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 385 7 1 6 2.1 CCCCN1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
71462776 89738 0 None -11 7 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181169 89738 0 None -11 7 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
9839847 215025 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 314 6 2 3 2.8 CCCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL98734 215025 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 314 6 2 3 2.8 CCCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
9839847 215025 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 314 6 2 3 2.8 CCCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1039/C0MD00258E
CHEMBL98734 215025 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 314 6 2 3 2.8 CCCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1039/C0MD00258E
9839847 215025 0 None - 1 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 314 6 2 3 2.8 CCCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL98734 215025 0 None - 1 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 314 6 2 3 2.8 CCCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
9839847 215025 0 None - 1 Rat 7.9 pKi = 7.9 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 314 6 2 3 2.8 CCCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL98734 215025 0 None - 1 Rat 7.9 pKi = 7.9 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 314 6 2 3 2.8 CCCCN1CCC(CNC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
6604914 107160 3 None 1 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/0960-894X(96)00002-9
CHEMBL28992 107160 3 None 1 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/0960-894X(96)00002-9
151537 169443 49 None - 1 Guinea pig 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 nan
41867 169443 49 None - 1 Guinea pig 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 nan
CHEMBL417 169443 49 None - 1 Guinea pig 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 nan
5991 210698 72 None 2 5 Guinea pig 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C nan
CHEMBL691 210698 72 None 2 5 Guinea pig 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C nan
203435 170883 3 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 311 5 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCCCC1 10.1021/jm960320m
CHEMBL420969 170883 3 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 311 5 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCCCC1 10.1021/jm960320m
44404968 79130 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 711 20 3 8 6.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCC(=O)NC2CCN(Cc3ccccc3)CC2)CC1 10.1021/jm050234z
CHEMBL198504 79130 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 711 20 3 8 6.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCC(=O)NC2CCN(Cc3ccccc3)CC2)CC1 10.1021/jm050234z
42618250 176240 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 982 28 6 14 5.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCNCCCc2ccc(CCCNCCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)cc2)CC1 10.1021/jm801327q
CHEMBL442869 176240 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 982 28 6 14 5.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCNCCCc2ccc(CCCNCCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)cc2)CC1 10.1021/jm801327q
72698085 110763 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 420 6 0 3 6.0 Fc1cccc2c1nc(OCC1CCN(CCCC(F)(F)F)CC1)c1ccccc12 10.1016/j.bmc.2013.08.061
CHEMBL3093184 110763 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 420 6 0 3 6.0 Fc1cccc2c1nc(OCC1CCN(CCCC(F)(F)F)CC1)c1ccccc12 10.1016/j.bmc.2013.08.061
10408029 23232 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
CHEMBL123377 23232 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
118734516 125451 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 386 7 1 4 4.8 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3417001 125451 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 386 7 1 4 4.8 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.5b00115
240 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm020270n
2769 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm020270n
44279790 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm020270n
660 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm020270n
CHEMBL1729 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm020270n
CHEMBL560739 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm020270n
DB00604 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm020270n
10545215 195761 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 341 5 2 5 3.4 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCCCC1 10.1021/jm960853v
CHEMBL50852 195761 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 341 5 2 5 3.4 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCCCC1 10.1021/jm960853v
118734508 125275 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 350 7 1 4 4.0 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CC2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3414597 125275 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 350 7 1 4 4.0 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CC2)CC1 10.1021/acs.jmedchem.5b00115
42646835 201933 2 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation countingDisplacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting
ChEMBL 261 4 2 4 1.5 COc1ccc2[nH]cc(CNN3CCOCC3)c2c1 10.1016/j.ejmech.2009.01.015
CHEMBL550302 201933 2 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation countingDisplacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting
ChEMBL 261 4 2 4 1.5 COc1ccc2[nH]cc(CNN3CCOCC3)c2c1 10.1016/j.ejmech.2009.01.015
119584 9373 102 None -1 6 Guinea pig 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
1848 9373 102 None -1 6 Guinea pig 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
242 9373 102 None -1 6 Guinea pig 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
CHEMBL60889 9373 102 None -1 6 Guinea pig 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
DB11675 9373 102 None -1 6 Guinea pig 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
145991736 173623 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 355 7 1 4 3.5 CCCCN1CCC(CNC(=O)c2cc(OC)c3ccccc3n2)CC1 10.1039/C8MD00233A
CHEMBL4285302 173623 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 355 7 1 4 3.5 CCCCN1CCC(CNC(=O)c2cc(OC)c3ccccc3n2)CC1 10.1039/C8MD00233A
145979545 173506 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 314 5 0 5 2.9 COc1cc(C(=O)OCCN2CCCCC2)c2ccccc2n1 10.1039/C8MD00233A
CHEMBL4283020 173506 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 314 5 0 5 2.9 COc1cc(C(=O)OCCN2CCCCC2)c2ccccc2n1 10.1039/C8MD00233A
70695321 84275 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 455 7 4 6 1.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNC(N)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087326 84275 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 455 7 4 6 1.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNC(N)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
44247822 91900495 202294 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 571 10 1 7 3.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL553685 202294 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 571 10 1 7 3.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44248434 91900496 202418 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 613 13 1 7 4.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL556326 202418 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 613 13 1 7 4.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44248070 202603 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 557 13 2 7 3.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
CHEMBL558261 202603 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 557 13 2 7 3.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
44248552 91900486 202698 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 554 9 1 6 4.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
CHEMBL559317 202698 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 554 9 1 6 4.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
10615288 193788 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 315 7 2 5 2.8 CCN(CC)CCOC(=O)Nc1cc(Cl)c(N)cc1OC 10.1021/jm960853v
CHEMBL49072 193788 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 315 7 2 5 2.8 CCN(CC)CCOC(=O)Nc1cc(Cl)c(N)cc1OC 10.1021/jm960853v
134828069 180081 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 410 7 1 3 5.7 COc1c(C(=O)CCC2CCN(Cc3ccccc3)CC2)cc(Cl)c2[nH]ccc12 10.1016/j.ejmech.2018.10.064
CHEMBL4526050 180081 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 410 7 1 3 5.7 COc1c(C(=O)CCC2CCN(Cc3ccccc3)CC2)cc(Cl)c2[nH]ccc12 10.1016/j.ejmech.2018.10.064
9819593 105580 3 None 1 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 10.1021/jm960320m
CHEMBL27846 105580 3 None 1 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 10.1021/jm960320m
71461046 89743 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3ccccc3c3ccc(F)cc23)CC1 10.1021/jm300943r
CHEMBL2181175 89743 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3ccccc3c3ccc(F)cc23)CC1 10.1021/jm300943r
10531 8202 21 None -87 24 Guinea pig 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 8202 21 None -87 24 Guinea pig 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 8202 21 None -87 24 Guinea pig 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 8202 21 None -87 24 Guinea pig 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 8202 21 None -87 24 Guinea pig 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
108182 10903 22 None -1 17 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1016/0960-894X(96)00200-4
245 10903 22 None -1 17 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1016/0960-894X(96)00200-4
CHEMBL18041 10903 22 None -1 17 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1016/0960-894X(96)00200-4
9906933 41240 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.
ChEMBL 360 3 1 4 3.6 CC(C)n1cnc2c(C(=O)NC3CC4CCC(C3)N4C)cc(Cl)cc21 10.1016/0960-894X(96)00052-2
CHEMBL142852 41240 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.
ChEMBL 360 3 1 4 3.6 CC(C)n1cnc2c(C(=O)NC3CC4CCC(C3)N4C)cc(Cl)cc21 10.1016/0960-894X(96)00052-2
15231247 91900477 202431 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 309 3 3 4 1.9 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C[C@@H]2CC[C@H](C1)N2 10.1021/jm900881j
CHEMBL556438 202431 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 309 3 3 4 1.9 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C[C@@H]2CC[C@H](C1)N2 10.1021/jm900881j
42499 201716 23 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 283 3 3 4 1.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCNCC1 10.1021/jm900881j
CHEMBL541969 201716 23 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 283 3 3 4 1.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCNCC1 10.1021/jm900881j
44248794 202291 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 302 2 2 5 1.7 CC(C)n1c(=O)n(C(=O)NC2CCNCC2)c2ccccc21 10.1021/jm900881j
CHEMBL553658 202291 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 302 2 2 5 1.7 CC(C)n1c(=O)n(C(=O)NC2CCNCC2)c2ccccc21 10.1021/jm900881j
44247817 91900489 202754 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 489 9 2 6 3.4 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
CHEMBL559746 202754 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 489 9 2 6 3.4 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
9935387 106218 0 None -1995 14 Human 5.8 pKi = 5.8 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL282971 106218 0 None -1995 14 Human 5.8 pKi = 5.8 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
44247949 201893 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 475 12 3 6 3.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCS(=O)(=O)O)CC1 10.1021/jm900881j
CHEMBL549998 201893 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 475 12 3 6 3.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCS(=O)(=O)O)CC1 10.1021/jm900881j
11600413 74298 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 876 25 4 12 6.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCCCCCCCCC(=O)NCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL189580 74298 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 876 25 4 12 6.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCCCCCCCCC(=O)NCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
44404962 79320 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 834 22 5 12 5.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
CHEMBL199150 79320 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 834 22 5 12 5.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
44592076 179503 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 317 8 0 5 4.1 CCN(CC)CCCCOc1nc2ccsc2n2cccc12 10.1016/j.bmc.2008.11.045
CHEMBL450595 179503 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 317 8 0 5 4.1 CCN(CC)CCCCOc1nc2ccsc2n2cccc12 10.1016/j.bmc.2008.11.045
44592108 185865 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 5 0 5 4.1 CCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL471662 185865 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 5 0 5 4.1 CCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
10292429 126980 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 1 4 4.9 CCCCN1CCC(COc2nc3ccccc3c3c2CCCCN3)CC1 10.1021/jm020954v
CHEMBL35195 126980 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 367 6 1 4 4.9 CCCCN1CCC(COc2nc3ccccc3c3c2CCCCN3)CC1 10.1021/jm020954v
162676850 190299 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 635 10 2 6 5.1 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2cc(Br)ccc2Br)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4799839 190299 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 635 10 2 6 5.1 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2cc(Br)ccc2Br)CC1 10.1016/j.ejmech.2016.05.048
10645103 171120 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 407 6 1 6 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2F)CC1 10.1021/jm0009538
CHEMBL421256 171120 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 407 6 1 6 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2F)CC1 10.1021/jm0009538
10546395 10977 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 359 6 1 6 1.4 CCCN1CCN(CCNC(=O)n2c(=O)n(CC)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL100199 10977 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 359 6 1 6 1.4 CCCN1CCN(CCNC(=O)n2c(=O)n(CC)c3ccccc32)CC1 10.1021/jm981098j
10645984 25589 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm0009538
CHEMBL127876 25589 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm0009538
11841878 74371 4 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 332 2 2 3 3.0 CN1C2CCCC1CC(NC(=O)c1cc(Cl)cc3[nH]cnc13)C2 10.1016/0960-894X(96)00200-4
CHEMBL19022 74371 4 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 332 2 2 3 3.0 CN1C2CCCC1CC(NC(=O)c1cc(Cl)cc3[nH]cnc13)C2 10.1016/0960-894X(96)00200-4
11841878 74371 4 None - 1 Rat 6.8 pKi = 6.8 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 332 2 2 3 3.0 CN1C2CCCC1CC(NC(=O)c1cc(Cl)cc3[nH]cnc13)C2 10.1021/jm991076c
CHEMBL19022 74371 4 None - 1 Rat 6.8 pKi = 6.8 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 332 2 2 3 3.0 CN1C2CCCC1CC(NC(=O)c1cc(Cl)cc3[nH]cnc13)C2 10.1021/jm991076c
10859701 74357 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 304 2 2 3 2.0 O=C(NC1CN2CCC1CC2)c1cc(Cl)cc2nc[nH]c12 10.1016/0960-894X(96)00200-4
CHEMBL19006 74357 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 304 2 2 3 2.0 O=C(NC1CN2CCC1CC2)c1cc(Cl)cc2nc[nH]c12 10.1016/0960-894X(96)00200-4
10859701 74357 0 None - 1 Rat 6.8 pKi = 6.8 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 304 2 2 3 2.0 O=C(NC1CN2CCC1CC2)c1cc(Cl)cc2nc[nH]c12 10.1021/jm991076c
CHEMBL19006 74357 0 None - 1 Rat 6.8 pKi = 6.8 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 304 2 2 3 2.0 O=C(NC1CN2CCC1CC2)c1cc(Cl)cc2nc[nH]c12 10.1021/jm991076c
11841879 127791 7 None - 1 Rat 6.8 pKi = 6.8 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 348 2 2 3 2.1 O=C(NC1CN2CCC1CC2)c1cc(Br)cc2nc[nH]c12 10.1021/jm991076c
CHEMBL356521 127791 7 None - 1 Rat 6.8 pKi = 6.8 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 348 2 2 3 2.1 O=C(NC1CN2CCC1CC2)c1cc(Br)cc2nc[nH]c12 10.1021/jm991076c
9924349 182646 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 346 6 1 2 5.0 O=C(CCC1CCN(Cc2ccccc2)CC1)c1ccc2[nH]ccc2c1 10.1016/j.ejmech.2018.10.064
CHEMBL4585990 182646 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 346 6 1 2 5.0 O=C(CCC1CCN(Cc2ccccc2)CC1)c1ccc2[nH]ccc2c1 10.1016/j.ejmech.2018.10.064
9905225 213723 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 321 2 2 4 1.7 Nc1c(Cl)cc(C(=O)N[C@@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL91147 213723 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 321 2 2 4 1.7 Nc1c(Cl)cc(C(=O)N[C@@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
240 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
2769 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
44279790 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
660 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
CHEMBL1729 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
CHEMBL560739 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
DB00604 7731 43 None -4 25 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
49783417 24486 0 None -18 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 306 6 1 5 2.6 CCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258560 24486 0 None -18 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 306 6 1 5 2.6 CCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
49783420 24522 0 None -51 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 338 8 1 5 3.2 CCCCN1CCC(COC(=O)c2ccc(N)c(OCF)c2)CC1 10.1021/jm100668r
CHEMBL1258672 24522 0 None -51 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 338 8 1 5 3.2 CCCCN1CCC(COC(=O)c2ccc(N)c(OCF)c2)CC1 10.1021/jm100668r
71461049 89750 0 None 1 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3c(OC)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181187 89750 0 None 1 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3c(OC)cccc3c3ccccc23)CC1 10.1021/jm300943r
10669778 124253 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 419 7 1 7 2.9 COc1ccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1021/jm0009538
CHEMBL339936 124253 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 419 7 1 7 2.9 COc1ccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1021/jm0009538
11791805 114317 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 345 5 1 6 1.0 CCN1CCN(CCNC(=O)n2c(=O)n(CC)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL318764 114317 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 345 5 1 6 1.0 CCN1CCN(CCNC(=O)n2c(=O)n(CC)c3ccccc32)CC1 10.1021/jm981098j
10267187 213277 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 306 2 1 3 2.1 O=C(N[C@@H]1CN2CCC1CC2)c1cc(Cl)cc2c1OCC2 10.1016/0960-894X(96)00002-9
CHEMBL88310 213277 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 306 2 1 3 2.1 O=C(N[C@@H]1CN2CCC1CC2)c1cc(Cl)cc2c1OCC2 10.1016/0960-894X(96)00002-9
10331436 7112 10 None -851 6 Human 5.8 pKi = 5.8 Binding
Inhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligandInhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
160 7112 10 None -851 6 Human 5.8 pKi = 5.8 Binding
Inhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligandInhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
CHEMBL133455 7112 10 None -851 6 Human 5.8 pKi = 5.8 Binding
Inhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligandInhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
11146446 112731 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 603 10 2 9 2.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
CHEMBL312940 112731 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 603 10 2 9 2.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
90666003 116064 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 378 5 0 6 4.2 c1cc2c(OCC3CCN(Cc4ccncc4)CC3)nc3ccsc3n2c1 10.1039/C2MD20063E
CHEMBL3218875 116064 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 378 5 0 6 4.2 c1cc2c(OCC3CCN(Cc4ccncc4)CC3)nc3ccsc3n2c1 10.1039/C2MD20063E
176155 10937 0 None -1 4 Guinea pig 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 377 4 1 3 4.7 C[S+]([O-])c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 nan
CHEMBL10 10937 0 None -1 4 Guinea pig 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 377 4 1 3 4.7 C[S+]([O-])c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 nan
11714901 141110 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 904 27 4 12 7.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNC(=O)CCCCCCCCCCC(=O)NCCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL371718 141110 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 904 27 4 12 7.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNC(=O)CCCCCCCCCCC(=O)NCCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
162673811 189928 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 493 10 2 6 3.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4795251 189928 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 493 10 2 6 3.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1016/j.ejmech.2016.05.048
44592111 196587 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 4 0 5 4.0 CC(C)N1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL516340 196587 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 4 0 5 4.0 CC(C)N1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
162667581 189264 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 539 12 2 8 3.6 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)c(OC)c1 10.1016/j.ejmech.2016.05.048
CHEMBL4786794 189264 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 539 12 2 8 3.6 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)c(OC)c1 10.1016/j.ejmech.2016.05.048
10919426 212999 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 659 14 2 9 4.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
CHEMBL86624 212999 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 659 14 2 9 4.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
9856041 30886 3 None -489 8 Human 5.8 pKi = 5.8 Binding
Inhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligandInhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligand
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL133868 30886 3 None -489 8 Human 5.8 pKi = 5.8 Binding
Inhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligandInhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligand
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
11813759 213075 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 564 8 1 8 4.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CN2C(=O)c3cccc4c(N(C)C)ccc(c34)C2=O)CC1 10.1021/jm0307887
CHEMBL87063 213075 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 564 8 1 8 4.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CN2C(=O)c3cccc4c(N(C)C)ccc(c34)C2=O)CC1 10.1021/jm0307887
2585 7590 103 None -57 22 Guinea pig 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 7590 103 None -57 22 Guinea pig 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 7590 103 None -57 22 Guinea pig 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 7590 103 None -57 22 Guinea pig 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 7590 103 None -57 22 Guinea pig 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
11050452 55921 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 631 12 2 9 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
CHEMBL156206 55921 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 631 12 2 9 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
5 6927 72 None -117 53 Rat 6.7 pKi = 6.7 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960320m
5202 6927 72 None -117 53 Rat 6.7 pKi = 6.7 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960320m
CHEMBL39 6927 72 None -117 53 Rat 6.7 pKi = 6.7 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960320m
DB08839 6927 72 None -117 53 Rat 6.7 pKi = 6.7 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960320m
10615623 163902 0 None - 1 Rat 6.7 pKi = 6.7 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 319 2 3 4 1.6 Nc1c(Cl)cc(C(=O)NC2CN3CCC2CC3)c2[nH]cnc12 10.1021/jm991076c
CHEMBL407493 163902 0 None - 1 Rat 6.7 pKi = 6.7 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 319 2 3 4 1.6 Nc1c(Cl)cc(C(=O)NC2CN3CCC2CC3)c2[nH]cnc12 10.1021/jm991076c
11527897 141077 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 780 18 4 13 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCOCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL371707 141077 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 780 18 4 13 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCOCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
182593 10168 6 None -1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1039/C8MD00233A
254 10168 6 None -1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1039/C8MD00233A
CHEMBL83954 10168 6 None -1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1039/C8MD00233A
182593 10168 6 None -1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1016/j.ejmech.2014.05.015
254 10168 6 None -1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1016/j.ejmech.2014.05.015
CHEMBL83954 10168 6 None -1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1016/j.ejmech.2014.05.015
182593 10168 6 None -1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1039/C6MD00458J
254 10168 6 None -1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1039/C6MD00458J
CHEMBL83954 10168 6 None -1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1039/C6MD00458J
9861687 195978 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 315 4 0 5 3.7 CCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL511312 195978 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 315 4 0 5 3.7 CCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
67251061 89495 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 443 8 0 5 5.2 COCc1ccc(CCN2CCC(COc3nc4ccccc4c4cn(C)cc34)CC2)cc1 10.1021/jm300573d
CHEMBL2179671 89495 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 443 8 0 5 5.2 COCc1ccc(CCN2CCC(COc3nc4ccccc4c4cn(C)cc34)CC2)cc1 10.1021/jm300573d
11842633 10753 21 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
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 10753 21 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
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 10753 21 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
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
67276168 84283 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 490 8 3 7 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNS(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087334 84283 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 490 8 3 7 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNS(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
11432106 84284 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 504 8 2 7 1.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)S(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087335 84284 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 504 8 2 7 1.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)S(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
11519716 202275 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 559 8 2 8 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL553405 202275 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 559 8 2 8 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44247941 202567 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 498 9 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
CHEMBL557867 202567 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 498 9 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
71461047 89746 0 None - 1 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3cc(OC)ccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181183 89746 0 None - 1 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3cc(OC)ccc3c3ccccc23)CC1 10.1021/jm300943r
10028436 10305 5 None -954 12 Human 5.7 pKi = 5.7 Binding
Compound was tested for its binding affinity for 5-hydroxytryptamine 4 receptorCompound was tested for its binding affinity for 5-hydroxytryptamine 4 receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 10305 5 None -954 12 Human 5.7 pKi = 5.7 Binding
Compound was tested for its binding affinity for 5-hydroxytryptamine 4 receptorCompound was tested for its binding affinity for 5-hydroxytryptamine 4 receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 10305 5 None -954 12 Human 5.7 pKi = 5.7 Binding
Compound was tested for its binding affinity for 5-hydroxytryptamine 4 receptorCompound was tested for its binding affinity for 5-hydroxytryptamine 4 receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
11177588 101964 5 None -5 3 Human 5.7 pKi = 5.7 Binding
Displacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cellsDisplacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cells
ChEMBL 418 5 6 3 1.1 N=C(N)NCCC[C@@H]1NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)NC1=O 10.1021/np0601760
CHEMBL255898 101964 5 None -5 3 Human 5.7 pKi = 5.7 Binding
Displacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cellsDisplacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cells
ChEMBL 418 5 6 3 1.1 N=C(N)NCCC[C@@H]1NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)NC1=O 10.1021/np0601760
118734519 125454 0 None - 1 Guinea pig 6.7 pKi = 6.7 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 407 7 2 5 5.2 COc1cc(N)c(Cl)cc1/C(CCC1CCN(CC2CCCCC2)CC1)=N/O 10.1021/acs.jmedchem.5b00115
CHEMBL3417004 125454 0 None - 1 Guinea pig 6.7 pKi = 6.7 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 407 7 2 5 5.2 COc1cc(N)c(Cl)cc1/C(CCC1CCN(CC2CCCCC2)CC1)=N/O 10.1021/acs.jmedchem.5b00115
2274 9947 58 None -17 31 Guinea pig 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 9947 58 None -17 31 Guinea pig 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 9947 58 None -17 31 Guinea pig 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 9947 58 None -17 31 Guinea pig 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 9947 58 None -17 31 Guinea pig 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
10623729 119863 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 457 6 1 6 3.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm0009538
CHEMBL331264 119863 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 457 6 1 6 3.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm0009538
260 10641 54 None -38 6 Human 6.7 pKi = 6.7 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/j.bmc.2008.11.045
2775 10641 54 None -38 6 Human 6.7 pKi = 6.7 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/j.bmc.2008.11.045
656665 10641 54 None -38 6 Human 6.7 pKi = 6.7 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/j.bmc.2008.11.045
CHEMBL56564 10641 54 None -38 6 Human 6.7 pKi = 6.7 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/j.bmc.2008.11.045
DB11699 10641 54 None -38 6 Human 6.7 pKi = 6.7 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/j.bmc.2008.11.045
44628269 89497 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 443 7 1 5 4.8 Cn1cc2c(OCC3CCN(CCc4ccccc4C(=O)O)CC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2179673 89497 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 443 7 1 5 4.8 Cn1cc2c(OCC3CCN(CCc4ccccc4C(=O)O)CC3)nc3ccccc3c2c1 10.1021/jm300573d
44248317 202678 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 559 12 1 7 2.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN(C)CCCN(C)S(C)(=O)=O)cc2ccccc21 10.1021/jm900881j
CHEMBL559050 202678 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 559 12 1 7 2.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN(C)CCCN(C)S(C)(=O)=O)cc2ccccc21 10.1021/jm900881j
20030109 203130 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 327 5 3 5 1.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCO)CC1 10.1021/jm900881j
CHEMBL562477 203130 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 327 5 3 5 1.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCO)CC1 10.1021/jm900881j
15295138 57836 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
CHEMBL157880 57836 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
10741078 119617 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 425 6 1 8 2.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)nn2)CC1 10.1021/jm0009538
CHEMBL330848 119617 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 425 6 1 8 2.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)nn2)CC1 10.1021/jm0009538
42618252 193459 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 580 13 3 8 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm801327q
CHEMBL488325 193459 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 580 13 3 8 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm801327q
49783209 24381 0 None -3 26 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 24381 0 None -3 26 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
53321958 63228 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 413 8 2 5 3.1 O=C(O)CCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632173 63228 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 413 8 2 5 3.1 O=C(O)CCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
49783419 24521 0 None -6 12 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258671 24521 0 None -6 12 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
5324247 214834 1 None - 1 Rat 8.7 pKi = 8.7 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 362 5 1 4 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3C)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL97594 214834 1 None - 1 Rat 8.7 pKi = 8.7 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 362 5 1 4 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3C)CC1 10.1016/s0960-894x(01)00517-0
5324247 214834 1 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 362 5 1 4 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3C)CC1 10.1021/jm020807x
CHEMBL97594 214834 1 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 362 5 1 4 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3C)CC1 10.1021/jm020807x
71455625 89739 0 None -54 6 Guinea pig 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1016/j.bmc.2013.08.061
71455625 89739 0 None -54 6 Guinea pig 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181170 89739 0 None -54 6 Guinea pig 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1016/j.bmc.2013.08.061
CHEMBL2181170 89739 0 None -54 6 Guinea pig 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1021/jm300943r
257 10266 13 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1021/jm100668r
5311423 10266 13 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1021/jm100668r
CHEMBL114112 10266 13 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 10.1021/jm100668r
5324247 214834 1 None - 1 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 362 5 1 4 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3C)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL97594 214834 1 None - 1 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 362 5 1 4 3.3 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3C)CC1 10.1016/s0960-894x(01)00517-0
118734522 125457 0 None - 1 Guinea pig 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 393 6 2 4 4.0 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CC2CCCCC2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3417007 125457 0 None - 1 Guinea pig 8.7 pKi = 8.7 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 393 6 2 4 4.0 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CC2CCCCC2)CC1 10.1021/acs.jmedchem.5b00115
15544728 214332 0 None - 1 Rat 8.6 pKi = 8.6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 414 7 2 6 1.6 CS(=O)(=O)NCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL94784 214332 0 None - 1 Rat 8.6 pKi = 8.6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 414 7 2 6 1.6 CS(=O)(=O)NCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
15544728 214332 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 414 7 2 6 1.6 CS(=O)(=O)NCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL94784 214332 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 414 7 2 6 1.6 CS(=O)(=O)NCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
15544728 214332 0 None - 1 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 414 7 2 6 1.6 CS(=O)(=O)NCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL94784 214332 0 None - 1 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 414 7 2 6 1.6 CS(=O)(=O)NCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
249 9343 4 None -1 2 Rat 8.6 pKi = 8.6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
9905972 9343 4 None -1 2 Rat 8.6 pKi = 8.6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
CHEMBL155917 9343 4 None -1 2 Rat 8.6 pKi = 8.6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10.1021/jm960320m
10522209 108473 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 355 5 2 5 3.5 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CC(C)CC(C)C1 10.1021/jm960853v
CHEMBL299408 108473 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 355 5 2 5 3.5 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CC(C)CC(C)C1 10.1021/jm960853v
49783415 24450 0 None -3 12 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 24450 0 None -3 12 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
53318013 63230 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 511 15 2 5 5.9 O=C(O)CCCCCCCCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632175 63230 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 511 15 2 5 5.9 O=C(O)CCCCCCCCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
9800656 22322 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
CHEMBL121913 22322 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
118734513 127415 0 None - 1 Guinea pig 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 393 7 2 5 3.6 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CCNCC2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3416998 127415 0 None - 1 Guinea pig 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 393 7 2 5 3.6 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CCNCC2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3546835 127415 0 None - 1 Guinea pig 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 393 7 2 5 3.6 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CCNCC2)CC1 10.1021/acs.jmedchem.5b00115
71459269 89735 0 None -10 8 Guinea pig 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
CHEMBL2181166 89735 0 None -10 8 Guinea pig 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
243 9976 91 None 12 34 Human 8.6 pKi = 8.6 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.bmc.2008.11.045
3052762 9976 91 None 12 34 Human 8.6 pKi = 8.6 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.bmc.2008.11.045
3502 9976 91 None 12 34 Human 8.6 pKi = 8.6 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.bmc.2008.11.045
CHEMBL117287 9976 91 None 12 34 Human 8.6 pKi = 8.6 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.bmc.2008.11.045
DB06480 9976 91 None 12 34 Human 8.6 pKi = 8.6 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1016/j.bmc.2008.11.045
44629350 91357 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 408 6 0 6 3.2 Cn1cc2c(OCC3CCN(CCN4CCOCC4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2179676 91357 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 408 6 0 6 3.2 Cn1cc2c(OCC3CCN(CCN4CCOCC4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2220954 91357 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 408 6 0 6 3.2 Cn1cc2c(OCC3CCN(CCN4CCOCC4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
67472601 99650 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 548 7 1 8 5.3 O=C(OCC1CCN(Cc2ccc(-c3ccccc3-c3nnn[nH]3)cc2)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmc.2013.09.004
CHEMBL2440456 99650 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 548 7 1 8 5.3 O=C(OCC1CCN(Cc2ccc(-c3ccccc3-c3nnn[nH]3)cc2)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmc.2013.09.004
70686434 83192 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
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
CHEMBL2059583 83192 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
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
70684288 83195 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 558 11 1 7 3.5 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059586 83195 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 558 11 1 7 3.5 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
11504722 83197 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
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 83197 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
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
44248922 201679 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 627 14 2 7 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCC(CNS(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL540981 201679 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 627 14 2 7 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCC(CNS(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44248921 202025 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 520 11 1 5 5.7 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL551013 202025 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 520 11 1 5 5.7 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
41585 108398 3 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 292 6 1 4 3.1 CCOc1ccccc1NC(=O)OCCN1CCCCC1 10.1021/jm960853v
CHEMBL298920 108398 3 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 292 6 1 4 3.1 CCOc1ccccc1NC(=O)OCCN1CCCCC1 10.1021/jm960853v
10566592 192666 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 306 5 1 4 3.2 COc1ccccc1NC(=O)OCCN1C[C@@H](C)C[C@@H](C)C1 10.1021/jm960853v
CHEMBL48684 192666 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 306 5 1 4 3.2 COc1ccccc1NC(=O)OCCN1C[C@@H](C)C[C@@H](C)C1 10.1021/jm960853v
71451950 89450 8 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
53324017 63225 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 371 5 2 5 2.0 O=C(O)CN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632170 63225 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 371 5 2 5 2.0 O=C(O)CN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
15544727 114019 0 None - 1 Rat 8.5 pKi = 8.5 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 349 6 1 4 3.9 CCCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL316856 114019 0 None - 1 Rat 8.5 pKi = 8.5 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 349 6 1 4 3.9 CCCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
9881053 127023 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL35226 127023 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
15544727 114019 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 349 6 1 4 3.9 CCCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL316856 114019 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 349 6 1 4 3.9 CCCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
15544727 114019 0 None - 1 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 349 6 1 4 3.9 CCCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL316856 114019 0 None - 1 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 349 6 1 4 3.9 CCCCN1CCC(COC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
11622025 150524 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 848 23 4 12 6.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL390075 150524 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 848 23 4 12 6.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
240 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1039/C8MD00233A
2769 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1039/C8MD00233A
44279790 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1039/C8MD00233A
660 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1039/C8MD00233A
CHEMBL1729 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1039/C8MD00233A
CHEMBL560739 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1039/C8MD00233A
DB00604 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1039/C8MD00233A
240 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2014.05.015
2769 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2014.05.015
44279790 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2014.05.015
660 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2014.05.015
CHEMBL1729 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2014.05.015
CHEMBL560739 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2014.05.015
DB00604 7731 43 None -4 25 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2014.05.015
5311047 211542 33 None 5 2 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 465 9 2 6 3.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCOc2ccc(F)cc2)C[C@H]1OC 10.1039/C6MD00458J
CHEMBL74656 211542 33 None 5 2 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 465 9 2 6 3.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCOc2ccc(F)cc2)C[C@H]1OC 10.1039/C6MD00458J
71461050 89752 0 None -6 5 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1016/j.bmc.2013.08.061
71461050 89752 0 None -6 5 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181189 89752 0 None -6 5 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1016/j.bmc.2013.08.061
CHEMBL2181189 89752 0 None -6 5 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1021/jm300943r
118734517 125452 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 387 7 1 5 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2cccnc2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3417002 125452 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 387 7 1 5 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2cccnc2)CC1 10.1021/acs.jmedchem.5b00115
118734518 125453 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 387 7 1 5 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccncc2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3417003 125453 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 387 7 1 5 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccncc2)CC1 10.1021/acs.jmedchem.5b00115
44592183 185618 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 343 6 0 5 4.4 CCCCN1CCC(COc2nc3sccc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL469379 185618 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 343 6 0 5 4.4 CCCCN1CCC(COc2nc3sccc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
44592109 185866 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 343 6 0 5 4.4 CCCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL471663 185866 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 343 6 0 5 4.4 CCCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
11686510 79089 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 820 21 2 12 5.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCCCCCCCCC(=O)N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL198372 79089 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 820 21 2 12 5.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCCCCCCCCC(=O)N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
1235483 44774 1 None - 1 Rat 6.7 pKi = 6.7 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 304 2 2 3 2.0 O=C(N[C@H]1CN2CCC1CC2)c1cc(Cl)cc2nc[nH]c12 10.1021/jm991076c
CHEMBL146012 44774 1 None - 1 Rat 6.7 pKi = 6.7 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 304 2 2 3 2.0 O=C(N[C@H]1CN2CCC1CC2)c1cc(Cl)cc2nc[nH]c12 10.1021/jm991076c
31703 201496 63 None 1 3 Guinea pig 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
CHEMBL359744 201496 63 None 1 3 Guinea pig 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
CHEMBL53463 201496 63 None 1 3 Guinea pig 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
71452074 89742 0 None - 1 Guinea pig 6.7 pKi = 6.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3ccccc3c3cc(F)ccc23)CC1 10.1021/jm300943r
CHEMBL2181173 89742 0 None - 1 Guinea pig 6.7 pKi = 6.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3ccccc3c3cc(F)ccc23)CC1 10.1021/jm300943r
11650641 78864 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 736 15 4 12 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL197751 78864 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 736 15 4 12 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
132337 10316 15 None -1 2 Guinea pig 7.7 pKi = 7.7 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm020270n
238 10316 15 None -1 2 Guinea pig 7.7 pKi = 7.7 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm020270n
CHEMBL34291 10316 15 None -1 2 Guinea pig 7.7 pKi = 7.7 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm020270n
90666008 116069 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 383 5 0 5 5.1 Cc1csc2nc(OCC3CCN(CC4CCCC4)CC3)c3cccn3c12 10.1039/C2MD20063E
CHEMBL3218880 116069 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 383 5 0 5 5.1 Cc1csc2nc(OCC3CCN(CC4CCCC4)CC3)c3cccn3c12 10.1039/C2MD20063E
71462781 89753 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3ccccc3c3cccc(F)c23)CC1 10.1021/jm300943r
CHEMBL2181190 89753 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3ccccc3c3cccc(F)c23)CC1 10.1021/jm300943r
71450247 89751 0 None -4 9 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181188 89751 0 None -4 9 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
90666002 116063 0 None - 1 Guinea pig 6.7 pKi = 6.7 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 407 6 0 6 4.8 COc1ccc(CN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1039/C2MD20063E
CHEMBL3218874 116063 0 None - 1 Guinea pig 6.7 pKi = 6.7 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 407 6 0 6 4.8 COc1ccc(CN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1039/C2MD20063E
10760942 114068 0 None - 1 Guinea pig 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 359 4 1 6 1.5 Cc1cccc2c1n(C(C)C)c(=O)n2C(=O)NCCN1CCN(C)CC1 10.1021/jm981098j
CHEMBL317146 114068 0 None - 1 Guinea pig 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 359 4 1 6 1.5 Cc1cccc2c1n(C(C)C)c(=O)n2C(=O)NCCN1CCN(C)CC1 10.1021/jm981098j
44592283 196046 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 391 5 0 5 5.1 Cc1csc2nc(OCC3CCN(Cc4ccccc4)CC3)c3cccn3c12 10.1039/C2MD20063E
CHEMBL511837 196046 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 391 5 0 5 5.1 Cc1csc2nc(OCC3CCN(Cc4ccccc4)CC3)c3cccn3c12 10.1039/C2MD20063E
72697940 110767 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 406 5 0 3 5.6 Fc1cccc2c1nc(OCC1CCN(CCC(F)(F)F)CC1)c1ccccc12 10.1016/j.bmc.2013.08.061
CHEMBL3093194 110767 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 406 5 0 3 5.6 Fc1cccc2c1nc(OCC1CCN(CCC(F)(F)F)CC1)c1ccccc12 10.1016/j.bmc.2013.08.061
11810608 214833 0 None - 1 Rat 7.7 pKi = 7.7 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 363 6 3 4 3.0 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL97591 214833 0 None - 1 Rat 7.7 pKi = 7.7 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 363 6 3 4 3.0 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
11810608 214833 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 363 6 3 4 3.0 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)c3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL97591 214833 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 363 6 3 4 3.0 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)c3[nH]cnc23)CC1 10.1021/jm020807x
11810608 214833 0 None - 1 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 363 6 3 4 3.0 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL97591 214833 0 None - 1 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 363 6 3 4 3.0 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
162670887 189748 0 None 7 2 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 543 11 2 7 4.2 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Cl 10.1016/j.ejmech.2016.05.048
CHEMBL4793078 189748 0 None 7 2 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 543 11 2 7 4.2 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Cl 10.1016/j.ejmech.2016.05.048
71452073 89741 0 None 17 2 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3cnccc23)CC1 10.1021/jm300943r
CHEMBL2181172 89741 0 None 17 2 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3cnccc23)CC1 10.1021/jm300943r
136118637 83090 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
CHEMBL2058697 83090 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
3397 212267 112 None 1 2 Guinea pig 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
CHEMBL806 212267 112 None 1 2 Guinea pig 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
136118649 83097 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058704 83097 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
10618741 172458 0 None - 1 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 363 2 3 4 1.7 Nc1c(Br)cc(C(=O)NC2CN3CCC2CC3)c2[nH]cnc12 10.1021/jm991076c
CHEMBL424498 172458 0 None - 1 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 363 2 3 4 1.7 Nc1c(Br)cc(C(=O)NC2CN3CCC2CC3)c2[nH]cnc12 10.1021/jm991076c
44281492 125650 2 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 298 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OC1CCN(C)CC1 10.1016/S0960-894X(01)80508-4
CHEMBL34224 125650 2 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 298 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OC1CCN(C)CC1 10.1016/S0960-894X(01)80508-4
10408029 23232 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
CHEMBL123377 23232 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
10834000 23101 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 385 6 1 7 1.9 CCOC(=O)N1CCN(CCOC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm0009538
CHEMBL122818 23101 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 385 6 1 7 1.9 CCOC(=O)N1CCN(CCOC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm0009538
10669143 121031 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 407 6 1 6 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm0009538
CHEMBL333028 121031 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 407 6 1 6 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm0009538
6604794 44431 9 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.
ChEMBL 346 3 1 4 3.1 CC(C)n1cnc2c(C(=O)N[C@H]3CN4CCC3CC4)cc(Cl)cc21 10.1016/0960-894X(96)00052-2
CHEMBL145725 44431 9 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.
ChEMBL 346 3 1 4 3.1 CC(C)n1cnc2c(C(=O)N[C@H]3CN4CCC3CC4)cc(Cl)cc21 10.1016/0960-894X(96)00052-2
5 6927 72 None -190 53 Guinea pig 6.6 pKi = 6.6 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
5202 6927 72 None -190 53 Guinea pig 6.6 pKi = 6.6 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
CHEMBL39 6927 72 None -190 53 Guinea pig 6.6 pKi = 6.6 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
DB08839 6927 72 None -190 53 Guinea pig 6.6 pKi = 6.6 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
10069545 63350 0 None -831 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 399 5 2 4 3.9 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2Cc1ccccc1 10.1016/0960-894X(95)00115-A
CHEMBL164169 63350 0 None -831 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 399 5 2 4 3.9 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2Cc1ccccc1 10.1016/0960-894X(95)00115-A
71462780 89745 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3ccc(OC)cc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181181 89745 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3ccc(OC)cc3c3ccccc23)CC1 10.1021/jm300943r
10069545 63350 0 None -831 3 Guinea pig 6.6 pKi = 6.6 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 399 5 2 4 3.9 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2Cc1ccccc1 10.1021/jm020270n
CHEMBL164169 63350 0 None -831 3 Guinea pig 6.6 pKi = 6.6 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 399 5 2 4 3.9 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2Cc1ccccc1 10.1021/jm020270n
136118646 83094 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058701 83094 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
136118635 83087 0 None -6 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2cccc(Br)c12 10.1016/j.bmc.2013.09.011
CHEMBL2058694 83087 0 None -6 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2cccc(Br)c12 10.1016/j.bmc.2013.09.011
11549456 85827 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 736 15 4 12 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL2113157 85827 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 736 15 4 12 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
11146533 113828 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 616 13 2 8 5.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
CHEMBL315590 113828 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 616 13 2 8 5.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
162668604 189365 0 None 6 2 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 587 11 2 7 4.4 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Br 10.1016/j.ejmech.2016.05.048
CHEMBL4788022 189365 0 None 6 2 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 587 11 2 7 4.4 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Br 10.1016/j.ejmech.2016.05.048
15544722 214327 1 None - 1 Rat 7.6 pKi = 7.6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 315 6 1 4 3.2 CCCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL94756 214327 1 None - 1 Rat 7.6 pKi = 7.6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 315 6 1 4 3.2 CCCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
15544722 214327 1 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 315 6 1 4 3.2 CCCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL94756 214327 1 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 315 6 1 4 3.2 CCCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
15544722 214327 1 None - 1 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 315 6 1 4 3.2 CCCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL94756 214327 1 None - 1 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 315 6 1 4 3.2 CCCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
10811181 170274 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 403 7 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(Cc2ccccc2)CC1 10.1021/jm0009538
CHEMBL420166 170274 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 403 7 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(Cc2ccccc2)CC1 10.1021/jm0009538
44299805 107861 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity towards 5-HT4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-HT4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 324 3 1 5 2.6 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC1CN2C 10.1016/s0960-894x(01)00693-x
CHEMBL294894 107861 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity towards 5-HT4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-HT4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 324 3 1 5 2.6 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC1CN2C 10.1016/s0960-894x(01)00693-x
9947817 11819 0 None -436 9 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 4 receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 4 receptor
ChEMBL 286 3 2 3 2.7 CCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL105261 11819 0 None -436 9 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 4 receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 4 receptor
ChEMBL 286 3 2 3 2.7 CCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
107 6929 121 None -389 31 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation counting
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.ejmech.2009.01.015
1833 6929 121 None -389 31 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation counting
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.ejmech.2009.01.015
CHEMBL8165 6929 121 None -389 31 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation countingDisplacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation counting
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.ejmech.2009.01.015
5 6927 72 None -288 53 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assayBinding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111596
5202 6927 72 None -288 53 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assayBinding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111596
CHEMBL39 6927 72 None -288 53 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assayBinding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111596
DB08839 6927 72 None -288 53 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assayBinding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2019.111596
71459270 89744 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 348 5 0 3 5.2 CCCN1CCC(COc2nc3ccc(C)cc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181180 89744 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 348 5 0 3 5.2 CCCN1CCC(COc2nc3ccc(C)cc3c3ccccc23)CC1 10.1021/jm300943r
441383 27105 57 None -5 17 Guinea pig 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 27105 57 None -5 17 Guinea pig 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
155559813 181618 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 338 6 1 2 5.0 O=C(CCC1CCN(CC2CCCC2)CC1)c1ccc2[nH]ccc2c1 10.1016/j.ejmech.2018.10.064
CHEMBL4562793 181618 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 338 6 1 2 5.0 O=C(CCC1CCN(CC2CCCC2)CC1)c1ccc2[nH]ccc2c1 10.1016/j.ejmech.2018.10.064
10569278 194029 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 341 5 2 5 3.2 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCC(C)CC1 10.1021/jm960853v
CHEMBL49266 194029 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 341 5 2 5 3.2 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCC(C)CC1 10.1021/jm960853v
70695322 84277 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 469 7 4 6 1.6 CNC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
CHEMBL2087328 84277 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 469 7 4 6 1.6 CNC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
10737191 215098 0 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 359 5 1 6 1.4 CCn1c(=O)n(C(=O)NCCN2CCN(C(C)C)CC2)c2ccccc21 10.1021/jm981098j
CHEMBL99147 215098 0 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 359 5 1 6 1.4 CCn1c(=O)n(C(=O)NCCN2CCN(C(C)C)CC2)c2ccccc21 10.1021/jm981098j
44592110 195946 0 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 357 7 0 5 4.8 CCCCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL511148 195946 0 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 357 7 0 5 4.8 CCCCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
90666005 116066 0 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 355 5 0 5 4.4 c1cc2c(OCC3CCN(CC4CCC4)CC3)nc3ccsc3n2c1 10.1039/C2MD20063E
CHEMBL3218877 116066 0 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 355 5 0 5 4.4 c1cc2c(OCC3CCN(CC4CCC4)CC3)nc3ccsc3n2c1 10.1039/C2MD20063E
6604789 107824 5 None 12 10 Human 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptorBinding affinity against 5-hydroxytryptamine 4 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
CHEMBL294649 107824 5 None 12 10 Human 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptorBinding affinity against 5-hydroxytryptamine 4 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
71712613 98154 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 464 7 3 7 -0.3 CS(=O)(=O)N1CCN(CC(O)CN2CCC(NC(=O)c3cccc4[nH]cnc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402889 98154 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 464 7 3 7 -0.3 CS(=O)(=O)N1CCN(CC(O)CN2CCC(NC(=O)c3cccc4[nH]cnc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
44248793 91900478 202402 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 339 3 2 4 2.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)cc2ccccc21 10.1021/jm900881j
CHEMBL556235 202402 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 339 3 2 4 2.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)cc2ccccc21 10.1021/jm900881j
44249053 203280 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 394 6 2 5 2.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2CCCCC2)CC1 10.1021/jm900881j
CHEMBL563445 203280 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 394 6 2 5 2.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2CCCCC2)CC1 10.1021/jm900881j
6918647 107522 2 None -501 14 Human 5.6 pKi = 5.6 Binding
Compound was tested for its binding affinity against 5-hydroxytryptamine 4 receptorCompound was tested for its binding affinity against 5-hydroxytryptamine 4 receptor
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL292759 107522 2 None -501 14 Human 5.6 pKi = 5.6 Binding
Compound was tested for its binding affinity against 5-hydroxytryptamine 4 receptorCompound was tested for its binding affinity against 5-hydroxytryptamine 4 receptor
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
44247945 202849 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 391 6 3 6 1.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCS(=O)(=O)O)CC1 10.1021/jm900881j
CHEMBL560597 202849 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 391 6 3 6 1.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCS(=O)(=O)O)CC1 10.1021/jm900881j
10831381 214818 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 345 5 1 6 1.0 CCCn1c(=O)n(C(=O)NCCN2CCN(C)CC2)c2ccccc21 10.1021/jm981098j
CHEMBL97508 214818 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 345 5 1 6 1.0 CCCn1c(=O)n(C(=O)NCCN2CCN(C)CC2)c2ccccc21 10.1021/jm981098j
131725 207216 3 None -3 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 342 2 1 5 2.6 CC(C)n1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1021/jm960320m
CHEMBL59834 207216 3 None -3 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 342 2 1 5 2.6 CC(C)n1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1021/jm960320m
162649188 186876 0 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 523 12 2 7 4.0 COc1ccc(S(=O)(=O)NCCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1016/j.ejmech.2016.05.048
CHEMBL4748287 186876 0 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 523 12 2 7 4.0 COc1ccc(S(=O)(=O)NCCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1016/j.ejmech.2016.05.048
15544723 214215 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 380 7 2 6 1.0 CS(=O)(=O)NCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL94099 214215 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 380 7 2 6 1.0 CS(=O)(=O)NCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
15544723 214215 0 None - 1 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 380 7 2 6 1.0 CS(=O)(=O)NCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL94099 214215 0 None - 1 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 380 7 2 6 1.0 CS(=O)(=O)NCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
15544723 214215 0 None - 1 Rat 7.6 pKi = 7.6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 380 7 2 6 1.0 CS(=O)(=O)NCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL94099 214215 0 None - 1 Rat 7.6 pKi = 7.6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 380 7 2 6 1.0 CS(=O)(=O)NCCN1CCC(COC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
107 6929 121 None -389 31 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation countingDisplacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.ejmech.2009.01.015
1833 6929 121 None -389 31 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation countingDisplacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.ejmech.2009.01.015
CHEMBL8165 6929 121 None -389 31 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation countingDisplacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.ejmech.2009.01.015
10741712 215096 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 439 6 1 6 2.9 CC(C)n1c(=O)n(C(=O)NCCN2CCN(Cc3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm981098j
CHEMBL99141 215096 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 439 6 1 6 2.9 CC(C)n1c(=O)n(C(=O)NCCN2CCN(Cc3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm981098j
10897011 174944 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 560 9 2 8 3.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
CHEMBL433149 174944 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 560 9 2 8 3.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
1043 8363 14 None -2884 29 Guinea pig 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 8363 14 None -2884 29 Guinea pig 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 8363 14 None -2884 29 Guinea pig 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 8363 14 None -2884 29 Guinea pig 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 8363 14 None -2884 29 Guinea pig 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
11825705 114985 0 None - 1 Rat 7.6 pKi = 7.6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 407 6 3 4 3.2 CCCCN1CCC(CNC(=O)c2cc(Br)c(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL319663 114985 0 None - 1 Rat 7.6 pKi = 7.6 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 407 6 3 4 3.2 CCCCN1CCC(CNC(=O)c2cc(Br)c(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
11825705 114985 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 407 6 3 4 3.2 CCCCN1CCC(CNC(=O)c2cc(Br)c(N)c3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL319663 114985 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 407 6 3 4 3.2 CCCCN1CCC(CNC(=O)c2cc(Br)c(N)c3[nH]cnc23)CC1 10.1021/jm020807x
11825705 114985 0 None - 1 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 407 6 3 4 3.2 CCCCN1CCC(CNC(=O)c2cc(Br)c(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL319663 114985 0 None - 1 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 407 6 3 4 3.2 CCCCN1CCC(CNC(=O)c2cc(Br)c(N)c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
850953 45185 2 None - 1 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 348 2 2 3 2.1 O=C(N[C@H]1CN2CCC1CC2)c1cc(Br)cc2nc[nH]c12 10.1021/jm991076c
CHEMBL146368 45185 2 None - 1 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 348 2 2 3 2.1 O=C(N[C@H]1CN2CCC1CC2)c1cc(Br)cc2nc[nH]c12 10.1021/jm991076c
133 9274 52 None -79 43 Guinea pig 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 9274 52 None -79 43 Guinea pig 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 9274 52 None -79 43 Guinea pig 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 9274 52 None -79 43 Guinea pig 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 9274 52 None -79 43 Guinea pig 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
182593 10168 6 None -2 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1021/jm960320m
254 10168 6 None -2 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1021/jm960320m
CHEMBL83954 10168 6 None -2 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1021/jm960320m
10425296 170178 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 306 2 1 3 2.1 O=C(N[C@H]1CN2CCC1CC2)c1cc(Cl)cc2c1OCC2 10.1016/0960-894X(96)00002-9
CHEMBL419496 170178 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 306 2 1 3 2.1 O=C(N[C@H]1CN2CCC1CC2)c1cc(Cl)cc2c1OCC2 10.1016/0960-894X(96)00002-9
9819593 105580 3 None -1 2 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 10.1016/0960-894X(96)00052-2
CHEMBL27846 105580 3 None -1 2 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 10.1016/0960-894X(96)00052-2
90644472 119056 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 339 5 0 4 3.1 COc1cc2c3c(cccc3n1)CN(CCCN1CCCCC1)C2=O 10.1016/j.ejmech.2014.05.015
CHEMBL3291077 119056 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 339 5 0 4 3.1 COc1cc2c3c(cccc3n1)CN(CCCN1CCCCC1)C2=O 10.1016/j.ejmech.2014.05.015
44327605 214270 3 None - 1 Rat 6.5 pKi = 6.5 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 300 5 2 3 2.6 CCCCN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL94415 214270 3 None - 1 Rat 6.5 pKi = 6.5 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 300 5 2 3 2.6 CCCCN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
240 7731 43 None -11 25 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0205651
2769 7731 43 None -11 25 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0205651
44279790 7731 43 None -11 25 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0205651
660 7731 43 None -11 25 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0205651
CHEMBL1729 7731 43 None -11 25 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0205651
CHEMBL560739 7731 43 None -11 25 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0205651
DB00604 7731 43 None -11 25 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0205651
9906777 100019 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C2CC3CN(C2)CC31 10.1021/jm0509501
CHEMBL2448165 100019 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C2CC3CN(C2)CC31 10.1021/jm0509501
44592185 196175 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 327 5 0 5 3.8 C=CCN1CCC(COc2nc3sccc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL513020 196175 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 327 5 0 5 3.8 C=CCN1CCC(COc2nc3sccc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
5 6927 72 None -288 53 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation countingDisplacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2009.01.015
5202 6927 72 None -288 53 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation countingDisplacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2009.01.015
CHEMBL39 6927 72 None -288 53 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation countingDisplacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2009.01.015
DB08839 6927 72 None -288 53 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation countingDisplacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2009.01.015
11724799 17304 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 339 0 2 5 1.5 Nc1cc2c(cc1Cl)C(=O)NC1CCN(CCOCCO2)CC1 10.1016/0960-894X(95)00115-A
CHEMBL116913 17304 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 339 0 2 5 1.5 Nc1cc2c(cc1Cl)C(=O)NC1CCN(CCOCCO2)CC1 10.1016/0960-894X(95)00115-A
44327605 214270 3 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 300 5 2 3 2.6 CCCCN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL94415 214270 3 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 300 5 2 3 2.6 CCCCN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
44327605 214270 3 None - 1 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 300 5 2 3 2.6 CCCCN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL94415 214270 3 None - 1 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 300 5 2 3 2.6 CCCCN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
10550242 24029 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2Cl)CC1 10.1021/jm0009538
CHEMBL125670 24029 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2Cl)CC1 10.1021/jm0009538
11629268 79052 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 824 21 4 14 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCOCCOCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL198271 79052 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 824 21 4 14 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCOCCOCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
11796362 121879 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 419 7 1 7 2.9 COc1cccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)c1 10.1021/jm0009538
CHEMBL334325 121879 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 419 7 1 7 2.9 COc1cccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)c1 10.1021/jm0009538
118734510 125446 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 378 7 1 4 4.8 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CCCC2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3416996 125446 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 378 7 1 4 4.8 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CCCC2)CC1 10.1021/acs.jmedchem.5b00115
71461050 89752 0 None 6 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to human 5HT4RBinding affinity to human 5HT4R
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1016/j.bmc.2013.08.061
CHEMBL2181189 89752 0 None 6 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to human 5HT4RBinding affinity to human 5HT4R
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1016/j.bmc.2013.08.061
71461050 89752 0 None 6 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181189 89752 0 None 6 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1021/jm300943r
44247820 91900493 201578 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 534 12 1 5 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL538706 201578 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 534 12 1 5 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
44248435 202359 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 623 15 2 5 7.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
CHEMBL555210 202359 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 623 15 2 5 7.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
44247953 202597 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 581 12 2 5 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
CHEMBL558163 202597 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 581 12 2 5 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
44249183 203159 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 478 12 2 5 5.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2CCCCC2)CC1 10.1021/jm900881j
CHEMBL562636 203159 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 478 12 2 5 5.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2CCCCC2)CC1 10.1021/jm900881j
162669699 189500 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 607 12 2 9 3.3 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(OC)c(N3CCN(C)CC3)c2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4789661 189500 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 607 12 2 9 3.3 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(OC)c(N3CCN(C)CC3)c2)CC1 10.1016/j.ejmech.2016.05.048
235 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to YFP fused 5HT4 receptor expressed in CHO cellsBinding affinity to YFP fused 5HT4 receptor expressed in CHO cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm070552t
5311299 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to YFP fused 5HT4 receptor expressed in CHO cellsBinding affinity to YFP fused 5HT4 receptor expressed in CHO cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm070552t
CHEMBL286136 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to YFP fused 5HT4 receptor expressed in CHO cellsBinding affinity to YFP fused 5HT4 receptor expressed in CHO cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm070552t
9800656 22322 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
CHEMBL121913 22322 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
10715463 23123 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 390 6 1 7 2.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccncc2)CC1 10.1021/jm0009538
CHEMBL122914 23123 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 390 6 1 7 2.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccncc2)CC1 10.1021/jm0009538
71462652 89458 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 434 8 2 8 2.6 CC(C)(O)COc1cccc2onc(OCC3CCN(CC4(O)CCOCC4)CC3)c12 10.1021/jm300953p
CHEMBL2179590 89458 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 434 8 2 8 2.6 CC(C)(O)COc1cccc2onc(OCC3CCN(CC4(O)CCOCC4)CC3)c12 10.1021/jm300953p
235 9342 42 None -4 3 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
5311299 9342 42 None -4 3 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
CHEMBL286136 9342 42 None -4 3 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
183782 10171 20 None 1 14 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1039/C8MD00233A
237 10171 20 None 1 14 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1039/C8MD00233A
CHEMBL85251 10171 20 None 1 14 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1039/C8MD00233A
5145950 210266 7 None -5 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from 5-HT4 receptor in Sprague-Dawley rat striatum after 30 minsDisplacement of [3H]GR113808 from 5-HT4 receptor in Sprague-Dawley rat striatum after 30 mins
ChEMBL 553 13 2 8 3.7 COc1cc(COc2cc(N)c(Cl)cc2C(=O)CCC2CCN(CCNS(C)(=O)=O)CC2)cc(OC)c1 10.1021/jm400766k
CHEMBL586946 210266 7 None -5 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from 5-HT4 receptor in Sprague-Dawley rat striatum after 30 minsDisplacement of [3H]GR113808 from 5-HT4 receptor in Sprague-Dawley rat striatum after 30 mins
ChEMBL 553 13 2 8 3.7 COc1cc(COc2cc(N)c(Cl)cc2C(=O)CCC2CCN(CCNS(C)(=O)=O)CC2)cc(OC)c1 10.1021/jm400766k
CHEMBL66114 210266 7 None -5 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from 5-HT4 receptor in Sprague-Dawley rat striatum after 30 minsDisplacement of [3H]GR113808 from 5-HT4 receptor in Sprague-Dawley rat striatum after 30 mins
ChEMBL 553 13 2 8 3.7 COc1cc(COc2cc(N)c(Cl)cc2C(=O)CCC2CCN(CCNS(C)(=O)=O)CC2)cc(OC)c1 10.1021/jm400766k
118734511 125447 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 406 7 1 4 5.6 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CCCCCC2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3416997 125447 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 406 7 1 4 5.6 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CCCCCC2)CC1 10.1021/acs.jmedchem.5b00115
71451950 89450 8 None 1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation counting
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None 1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation counting
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
19081885 212123 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 338 7 1 4 4.0 CCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1039/C6MD00458J
CHEMBL79637 212123 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 338 7 1 4 4.0 CCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1039/C6MD00458J
135409453 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmc.2008.11.045
226 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmc.2008.11.045
CHEMBL76370 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmc.2008.11.045
135409453 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2013.05.018
226 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2013.05.018
CHEMBL76370 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2013.05.018
71712464 98166 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 445 8 3 6 2.2 COC(=O)N(C)CC(O)CN1CCC(CNC(=O)c2cccc3[nH]c(C(C)C)nc23)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402901 98166 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 445 8 3 6 2.2 COC(=O)N(C)CC(O)CN1CCC(CNC(=O)c2cccc3[nH]c(C(C)C)nc23)CC1 10.1016/j.bmcl.2013.05.018
71712465 98167 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 429 8 3 5 2.0 CC(=O)N(C)CC(O)CN1CCC(CNC(=O)c2cccc3[nH]c(C(C)C)nc23)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402902 98167 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 429 8 3 5 2.0 CC(=O)N(C)CC(O)CN1CCC(CNC(=O)c2cccc3[nH]c(C(C)C)nc23)CC1 10.1016/j.bmcl.2013.05.018
72697299 99649 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 547 7 2 7 4.9 O=C(NCC1CCN(Cc2ccc(-c3ccccc3-c3nnn[nH]3)cc2)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmc.2013.09.004
CHEMBL2440455 99649 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
ChEMBL 547 7 2 7 4.9 O=C(NCC1CCN(Cc2ccc(-c3ccccc3-c3nnn[nH]3)cc2)CC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmc.2013.09.004
135409453 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
226 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
CHEMBL76370 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.05.034
70688534 83188 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 441 8 2 6 3.0 CC(C)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
CHEMBL2059579 83188 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 441 8 2 6 3.0 CC(C)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
11677434 83190 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 483 9 2 7 2.8 COC[C@@H]1CCCN1CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
CHEMBL2059581 83190 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 483 9 2 7 2.8 COC[C@@H]1CCCN1CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2 10.1016/j.bmcl.2012.05.034
11606227 83194 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 532 8 2 8 1.3 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL2059585 83194 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 532 8 2 8 1.3 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCN(S(C)(=O)=O)CC2)c2ccccc21 10.1016/j.bmcl.2012.05.034
135409453 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.08.051
226 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.08.051
CHEMBL76370 10545 41 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1016/j.bmcl.2012.08.051
44248437 201615 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 597 12 1 6 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCN(c3ccccc3)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL539651 201615 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 597 12 1 6 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCN(c3ccccc3)CC2)cc2ccccc21 10.1021/jm900881j
10971995 169186 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 427 6 2 7 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)OC(C)(C)C)CC1 10.1039/C6MD00458J
CHEMBL4165966 169186 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 427 6 2 7 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)OC(C)(C)C)CC1 10.1039/C6MD00458J
145978961 173331 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 429 6 1 7 3.4 COc1cc(C(=O)OCCN2CCC(NC(=O)OC(C)(C)C)CC2)c2ccccc2n1 10.1039/C8MD00233A
CHEMBL4279553 173331 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 429 6 1 7 3.4 COc1cc(C(=O)OCCN2CCC(NC(=O)OC(C)(C)C)CC2)c2ccccc2n1 10.1039/C8MD00233A
10543526 215161 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 317 3 1 6 0.1 CN1CCN(CCNC(=O)n2c(=O)n(C)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL99578 215161 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 317 3 1 6 0.1 CN1CCN(CCNC(=O)n2c(=O)n(C)c3ccccc32)CC1 10.1021/jm981098j
11714709 85828 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 750 16 4 12 3.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL2113158 85828 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 750 16 4 12 3.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
11039730 213027 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 687 16 2 9 4.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
CHEMBL86777 213027 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 687 16 2 9 4.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
135409453 10545 41 None -2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cellsDisplacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cells
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1021/np0601760
226 10545 41 None -2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cellsDisplacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cells
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1021/np0601760
CHEMBL76370 10545 41 None -2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cellsDisplacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cells
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1021/np0601760
182593 10168 6 None 1 3 Human 7.5 pKi = 7.5 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1016/j.bmc.2008.11.045
254 10168 6 None 1 3 Human 7.5 pKi = 7.5 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1016/j.bmc.2008.11.045
CHEMBL83954 10168 6 None 1 3 Human 7.5 pKi = 7.5 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10.1016/j.bmc.2008.11.045
71459132 91342 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 419 7 1 3 4.4 CC(C)n1nc(C(=O)NCC2CC[N+](C)(CCc3ccccc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2179698 91342 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 419 7 1 3 4.4 CC(C)n1nc(C(=O)NCC2CC[N+](C)(CCc3ccccc3)CC2)c2ccccc21 10.1021/jm300573d
CHEMBL2220893 91342 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 419 7 1 3 4.4 CC(C)n1nc(C(=O)NCC2CC[N+](C)(CCc3ccccc3)CC2)c2ccccc21 10.1021/jm300573d
67276466 84273 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 454 7 3 6 1.8 CC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
CHEMBL2087324 84273 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 454 7 3 6 1.8 CC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
44248311 91900487 202409 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 596 12 1 6 5.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
CHEMBL556279 202409 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 596 12 1 6 5.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2C(=O)c3ccccc3C2=O)cc2ccccc21 10.1021/jm900881j
39736 191011 8 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 248 4 1 3 2.7 O=C(Nc1ccccc1)OCCN1CCCCC1 10.1021/jm960853v
CHEMBL48351 191011 8 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 248 4 1 3 2.7 O=C(Nc1ccccc1)OCCN1CCCCC1 10.1021/jm960853v
71712612 98153 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 490 7 3 7 0.2 CS(=O)(=O)N1CCN(CC(O)CN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cccc4[nH]cnc24)C3)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402888 98153 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 490 7 3 7 0.2 CS(=O)(=O)N1CCN(CC(O)CN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cccc4[nH]cnc24)C3)CC1 10.1016/j.bmcl.2013.05.018
9817713 201616 61 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 297 4 3 4 1.7 COc1cc(N)c(Cl)cc1C(=O)NCC1CCNCC1 10.1021/jm900881j
CHEMBL539652 201616 61 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 297 4 3 4 1.7 COc1cc(N)c(Cl)cc1C(=O)NCC1CCNCC1 10.1021/jm900881j
44249316 91900479 202131 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 328 2 2 5 2.2 CC(C)n1c(=O)n(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1021/jm900881j
CHEMBL551820 202131 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 328 2 2 5 2.2 CC(C)n1c(=O)n(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1021/jm900881j
44248796 202295 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 302 5 3 4 0.8 COc1ccc2[nH]cc(C(=O)NCCN3CCNCC3)c2c1 10.1021/jm900881j
CHEMBL553688 202295 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 302 5 3 4 0.8 COc1ccc2[nH]cc(C(=O)NCCN3CCNCC3)c2c1 10.1021/jm900881j
10346043 53894 0 None -3162 3 Human 5.5 pKi = 5.5 Binding
Compound was evaluated for the binding affinity against human cloned 5-hydroxytryptamine 4 receptor in HeLa cells using [3H]-LSD as the radioligandCompound was evaluated for the binding affinity against human cloned 5-hydroxytryptamine 4 receptor in HeLa cells using [3H]-LSD as the radioligand
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)ccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154274 53894 0 None -3162 3 Human 5.5 pKi = 5.5 Binding
Compound was evaluated for the binding affinity against human cloned 5-hydroxytryptamine 4 receptor in HeLa cells using [3H]-LSD as the radioligandCompound was evaluated for the binding affinity against human cloned 5-hydroxytryptamine 4 receptor in HeLa cells using [3H]-LSD as the radioligand
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)ccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
6918648 108336 1 None -5128 14 Human 5.5 pKi = 5.5 Binding
Compound was tested for its binding affinity against 5-hydroxytryptamine 4 receptorCompound was tested for its binding affinity against 5-hydroxytryptamine 4 receptor
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL29846 108336 1 None -5128 14 Human 5.5 pKi = 5.5 Binding
Compound was tested for its binding affinity against 5-hydroxytryptamine 4 receptorCompound was tested for its binding affinity against 5-hydroxytryptamine 4 receptor
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
44249311 202105 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 313 3 2 4 2.1 CC(C)n1c(=O)c(C(=O)NC2CCNCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL551614 202105 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 313 3 2 4 2.1 CC(C)n1c(=O)c(C(=O)NC2CCNCC2)cc2ccccc21 10.1021/jm900881j
44249317 91900480 202120 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 299 3 3 3 2.2 COc1ccc2[nH]cc(C(=O)N[C@@H]3C[C@@H]4CC[C@H](C3)N4)c2c1 10.1021/jm900881j
CHEMBL551743 202120 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 299 3 3 3 2.2 COc1ccc2[nH]cc(C(=O)N[C@@H]3C[C@@H]4CC[C@H](C3)N4)c2c1 10.1021/jm900881j
44249318 202647 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 273 3 3 3 1.7 COc1ccc2[nH]cc(C(=O)NC3CCNCC3)c2c1 10.1021/jm900881j
CHEMBL558757 202647 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 273 3 3 3 1.7 COc1ccc2[nH]cc(C(=O)NC3CCNCC3)c2c1 10.1021/jm900881j
6918648 108336 1 None -5128 14 Human 5.5 pKi = 5.5 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligand
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
CHEMBL29846 108336 1 None -5128 14 Human 5.5 pKi = 5.5 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligand
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
11841877 46622 1 None - 1 Rat 6.5 pKi = 6.5 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 318 2 2 3 2.6 CN1C2CCC1CC(NC(=O)c1cc(Cl)cc3[nH]cnc13)C2 10.1021/jm991076c
CHEMBL147725 46622 1 None - 1 Rat 6.5 pKi = 6.5 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 318 2 2 3 2.6 CN1C2CCC1CC(NC(=O)c1cc(Cl)cc3[nH]cnc13)C2 10.1021/jm991076c
11093246 118322 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 602 12 2 8 4.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
CHEMBL327999 118322 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 602 12 2 8 4.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
10408029 23232 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
CHEMBL123377 23232 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
49783206 24349 0 None -74 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 373 6 1 7 2.6 CCCCN1CCC(COC(=O)c2cc(C#N)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258108 24349 0 None -74 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 373 6 1 7 2.6 CCCCN1CCC(COC(=O)c2cc(C#N)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
71461048 89748 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3cc(F)ccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181185 89748 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3cc(F)ccc3c3ccccc23)CC1 10.1021/jm300943r
10667079 214125 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 373 7 1 6 1.8 CCCCN1CCN(CCNC(=O)n2c(=O)n(CC)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL93611 214125 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 373 7 1 6 1.8 CCCCN1CCN(CCNC(=O)n2c(=O)n(CC)c3ccccc32)CC1 10.1021/jm981098j
44281491 119251 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 312 4 1 5 2.6 CCN1CCCC(OC(=O)c2cc(Cl)c(N)cc2OC)C1 10.1016/S0960-894X(01)80508-4
CHEMBL32986 119251 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 312 4 1 5 2.6 CCN1CCCC(OC(=O)c2cc(Cl)c(N)cc2OC)C1 10.1016/S0960-894X(01)80508-4
90644478 119060 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 406 5 0 5 3.7 O=C1c2cccc3nc(N4CCCCC4)cc(c23)C(=O)N1CCCN1CCCCC1 10.1016/j.ejmech.2014.05.015
CHEMBL3291083 119060 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 406 5 0 5 3.7 O=C1c2cccc3nc(N4CCCCC4)cc(c23)C(=O)N1CCCN1CCCCC1 10.1016/j.ejmech.2014.05.015
71461049 89750 0 None -2 6 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3c(OC)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181187 89750 0 None -2 6 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3c(OC)cccc3c3ccccc23)CC1 10.1021/jm300943r
10018558 57525 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 314 5 1 6 1.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCOCC1 10.1021/jm960320m
CHEMBL157631 57525 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 314 5 1 6 1.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCOCC1 10.1021/jm960320m
44364334 46730 0 None - 1 Rat 6.5 pKi = 6.5 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 319 2 1 4 3.0 CN1C2CCC1CC(OC(=O)c1cc(Cl)cc3[nH]cnc13)C2 10.1021/jm991076c
CHEMBL147827 46730 0 None - 1 Rat 6.5 pKi = 6.5 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 319 2 1 4 3.0 CN1C2CCC1CC(OC(=O)c1cc(Cl)cc3[nH]cnc13)C2 10.1021/jm991076c
54677674 119586 4 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to 5HT4R (unknown origin)Binding affinity to 5HT4R (unknown origin)
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1016/j.ejmech.2014.05.015
CHEMBL3291085 119586 4 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to 5HT4R (unknown origin)Binding affinity to 5HT4R (unknown origin)
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1016/j.ejmech.2014.05.015
CHEMBL3306918 119586 4 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to 5HT4R (unknown origin)Binding affinity to 5HT4R (unknown origin)
ChEMBL 377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21 10.1016/j.ejmech.2014.05.015
11498641 85829 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 736 15 4 12 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL2113159 85829 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 736 15 4 12 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
49783212 24448 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 387 7 1 7 3.0 CCCCN1CCC(COC(=O)c2cc(C#N)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258450 24448 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 387 7 1 7 3.0 CCCCN1CCC(COC(=O)c2cc(C#N)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
44592145 196152 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 341 6 0 5 4.2 C=CCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL512841 196152 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 341 6 0 5 4.2 C=CCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
5 6927 72 None -117 53 Rat 7.4 pKi = 7.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(96)00002-9
5202 6927 72 None -117 53 Rat 7.4 pKi = 7.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(96)00002-9
CHEMBL39 6927 72 None -117 53 Rat 7.4 pKi = 7.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(96)00002-9
DB08839 6927 72 None -117 53 Rat 7.4 pKi = 7.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(96)00002-9
155517675 176968 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 386 6 1 2 6.1 O=C(CCC1CCN(CC2CCCCC2)CC1)c1cc(Cl)c2[nH]ccc2c1 10.1016/j.ejmech.2018.10.064
CHEMBL4444843 176968 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 386 6 1 2 6.1 O=C(CCC1CCN(CC2CCCCC2)CC1)c1cc(Cl)c2[nH]ccc2c1 10.1016/j.ejmech.2018.10.064
155545651 180243 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 352 6 1 2 5.4 O=C(CCC1CCN(CC2CCCCC2)CC1)c1ccc2[nH]ccc2c1 10.1016/j.ejmech.2018.10.064
CHEMBL4529710 180243 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 352 6 1 2 5.4 O=C(CCC1CCN(CC2CCCCC2)CC1)c1ccc2[nH]ccc2c1 10.1016/j.ejmech.2018.10.064
2353 107889 82 None -1 5 Guinea pig 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL12089 107889 82 None -1 5 Guinea pig 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL295124 107889 82 None -1 5 Guinea pig 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
146025727 178464 0 None -138 27 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]GR113808 from recombinant human 5HT4 receptor stably expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]GR113808 from recombinant human 5HT4 receptor stably expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 178464 0 None -138 27 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]GR113808 from recombinant human 5HT4 receptor stably expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]GR113808 from recombinant human 5HT4 receptor stably expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
10552840 171060 0 None - 1 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 483 9 1 7 3.2 CC(C)n1c(=O)n(C(=O)NCCN2CCN(CCCOc3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm981098j
CHEMBL421187 171060 0 None - 1 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 483 9 1 7 3.2 CC(C)n1c(=O)n(C(=O)NCCN2CCN(CCCOc3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm981098j
136118639 83092 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058699 83092 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
44592146 195146 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 301 3 0 5 3.3 CN1CCC(COc2nc3sccc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL501309 195146 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 301 3 0 5 3.3 CN1CCC(COc2nc3sccc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
850954 47030 2 None - 1 Rat 7.4 pKi = 7.4 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 348 2 2 3 2.1 O=C(N[C@@H]1CN2CCC1CC2)c1cc(Br)cc2nc[nH]c12 10.1021/jm991076c
CHEMBL148080 47030 2 None - 1 Rat 7.4 pKi = 7.4 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 348 2 2 3 2.1 O=C(N[C@@H]1CN2CCC1CC2)c1cc(Br)cc2nc[nH]c12 10.1021/jm991076c
10643950 115211 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 387 7 1 6 2.4 CCCCN1CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL319886 115211 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 387 7 1 6 2.4 CCCCN1CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
44352308 124265 0 None -46 12 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 4 receptor using [3H]5-HT as radioligandBinding affinity towards human 5-hydroxytryptamine 4 receptor using [3H]5-HT as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
CHEMBL339980 124265 0 None -46 12 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 4 receptor using [3H]5-HT as radioligandBinding affinity towards human 5-hydroxytryptamine 4 receptor using [3H]5-HT as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
6604914 107160 3 None 1 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/0960-894X(95)00115-A
CHEMBL28992 107160 3 None 1 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/0960-894X(95)00115-A
6604914 107160 3 None 1 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1021/jm960320m
CHEMBL28992 107160 3 None 1 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1021/jm960320m
6604914 107160 3 None -1 2 Guinea pig 6.4 pKi = 6.4 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1021/jm020270n
CHEMBL28992 107160 3 None -1 2 Guinea pig 6.4 pKi = 6.4 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1021/jm020270n
10568248 192757 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 327 5 2 5 3.0 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCCC1 10.1021/jm960853v
CHEMBL48698 192757 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatumBinding affinity (Ki+/-SEM) against 5-hydroxytryptamine 4 receptor from cheng Prusoff equation by using [3H]GR-113808 in rat striatum
ChEMBL 327 5 2 5 3.0 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCCC1 10.1021/jm960853v
145988372 174069 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 359 6 1 3 4.1 CCCCN1CCC(CNC(=O)c2cc(Cl)c3ccccc3n2)CC1 10.1039/C8MD00233A
CHEMBL4293603 174069 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 359 6 1 3 4.1 CCCCN1CCC(CNC(=O)c2cc(Cl)c3ccccc3n2)CC1 10.1039/C8MD00233A
10545158 57130 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 340 5 1 5 3.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1C(C)CCCC1C 10.1021/jm960320m
CHEMBL157233 57130 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 340 5 1 5 3.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1C(C)CCCC1C 10.1021/jm960320m
10666045 215184 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 357 5 1 6 1.3 CN1CCN(CCCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL99723 215184 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 357 5 1 6 1.3 CN1CCN(CCCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
67276147 84274 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 468 7 2 6 2.1 CC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
CHEMBL2087325 84274 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 468 7 2 6 2.1 CC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
70684790 84282 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 484 7 2 7 2.4 COC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
CHEMBL2087333 84282 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 484 7 2 7 2.4 COC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
44248191 201678 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 537 8 1 7 3.5 CCOC(=O)N1CCN(CCCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cc4ccccc4n(C(C)C)c2=O)C3)CC1 10.1021/jm900881j
CHEMBL540980 201678 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 537 8 1 7 3.5 CCOC(=O)N1CCN(CCCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cc4ccccc4n(C(C)C)c2=O)C3)CC1 10.1021/jm900881j
44247951 91900497 201691 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 539 9 2 5 5.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
CHEMBL541223 201691 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 539 9 2 5 5.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21 10.1021/jm900881j
44248076 201823 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 543 8 1 7 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL549449 201823 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 543 8 1 7 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44248195 201861 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 466 7 1 6 3.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCOCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL549650 201861 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 466 7 1 6 3.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCOCC2)cc2ccccc21 10.1021/jm900881j
44248072 202454 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 483 9 3 5 3.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
CHEMBL556595 202454 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 483 9 3 5 3.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN(C)CCc2c[nH]c3ccccc23)CC1 10.1021/jm900881j
44248068 202664 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 515 10 2 7 1.9 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
CHEMBL558924 202664 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 515 10 2 7 1.9 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2CCN(S(C)(=O)=O)CC2)CC1 10.1021/jm900881j
44247943 202727 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 540 12 2 6 4.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
CHEMBL559548 202727 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 540 12 2 6 4.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
44249188 202891 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 316 3 2 5 1.9 CC(C)n1c(=O)n(C(=O)NCC2CCNCC2)c2ccccc21 10.1021/jm900881j
CHEMBL560940 202891 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 316 3 2 5 1.9 CC(C)n1c(=O)n(C(=O)NCC2CCNCC2)c2ccccc21 10.1021/jm900881j
10337773 108362 0 None 31 10 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-Hydroxytryptamine 4 receptorBinding affinity against 5-Hydroxytryptamine 4 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
CHEMBL298612 108362 0 None 31 10 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-Hydroxytryptamine 4 receptorBinding affinity against 5-Hydroxytryptamine 4 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
67211178 89501 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 295 3 1 4 3.1 Cn1cc2c(OCC3CCNCC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2179680 89501 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 295 3 1 4 3.1 Cn1cc2c(OCC3CCNCC3)nc3ccccc3c2c1 10.1021/jm300573d
10493462 209266 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 286 3 2 4 2.1 CC(C)n1nc(C(=O)NC2CCNCC2)c2ccccc21 10.1021/jm900881j
CHEMBL61130 209266 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 286 3 2 4 2.1 CC(C)n1nc(C(=O)NC2CCNCC2)c2ccccc21 10.1021/jm900881j
10413595 168620 0 None -12589 11 Human 5.4 pKi = 5.4 Binding
Compound was evaluated for the binding affinity against human cloned 5-hydroxytryptamine 4 receptor in HeLa cells using [3H]-LSD as the radioligandCompound was evaluated for the binding affinity against human cloned 5-hydroxytryptamine 4 receptor in HeLa cells using [3H]-LSD as the radioligand
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL414628 168620 0 None -12589 11 Human 5.4 pKi = 5.4 Binding
Compound was evaluated for the binding affinity against human cloned 5-hydroxytryptamine 4 receptor in HeLa cells using [3H]-LSD as the radioligandCompound was evaluated for the binding affinity against human cloned 5-hydroxytryptamine 4 receptor in HeLa cells using [3H]-LSD as the radioligand
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
276 10286 50 None -2691 13 Human 5.4 pKi = 5.4 Binding
Compound was tested for its binding affinity against 5-hydroxytryptamine 4 receptorCompound was tested for its binding affinity against 5-hydroxytryptamine 4 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
5312149 10286 50 None -2691 13 Human 5.4 pKi = 5.4 Binding
Compound was tested for its binding affinity against 5-hydroxytryptamine 4 receptorCompound was tested for its binding affinity against 5-hydroxytryptamine 4 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
CHEMBL431298 10286 50 None -2691 13 Human 5.4 pKi = 5.4 Binding
Compound was tested for its binding affinity against 5-hydroxytryptamine 4 receptorCompound was tested for its binding affinity against 5-hydroxytryptamine 4 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
44248795 204410 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 287 4 3 3 1.9 COc1ccc2[nH]cc(C(=O)NCC3CCNCC3)c2c1 10.1021/jm900881j
CHEMBL570780 204410 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 287 4 3 3 1.9 COc1ccc2[nH]cc(C(=O)NCC3CCNCC3)c2c1 10.1021/jm900881j
276 10286 50 None -2691 13 Human 5.4 pKi = 5.4 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligand
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
5312149 10286 50 None -2691 13 Human 5.4 pKi = 5.4 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligand
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
CHEMBL431298 10286 50 None -2691 13 Human 5.4 pKi = 5.4 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligand
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
145957993 168959 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 692 19 5 11 1.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)NCCOCCOCCNC(=O)NCC(=O)OCc2ccccc2)CC1 10.1039/C6MD00458J
CHEMBL4162531 168959 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 692 19 5 11 1.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)NCCOCCOCCNC(=O)NCC(=O)OCc2ccccc2)CC1 10.1039/C6MD00458J
145951595 169576 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 854 21 6 14 2.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)NCCOCCOCCNC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1039/C6MD00458J
CHEMBL4172346 169576 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 854 21 6 14 2.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)NCCOCCOCCNC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1039/C6MD00458J
9973684 58248 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 326 5 1 5 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C)CC1 10.1021/jm960320m
CHEMBL158238 58248 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 326 5 1 5 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C)CC1 10.1021/jm960320m
10519226 108764 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 312 5 1 4 3.4 COc1ccc(Cl)cc1NC(=O)OCCN1CCCCC1 10.1021/jm960853v
CHEMBL301510 108764 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 312 5 1 4 3.4 COc1ccc(Cl)cc1NC(=O)OCCN1CCCCC1 10.1021/jm960853v
90666009 116070 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 397 5 0 5 5.5 Cc1csc2nc(OCC3CCN(CC4CCCCC4)CC3)c3cccn3c12 10.1039/C2MD20063E
CHEMBL3218881 116070 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 397 5 0 5 5.5 Cc1csc2nc(OCC3CCN(CC4CCCCC4)CC3)c3cccn3c12 10.1039/C2MD20063E
72698088 110766 0 None -20 5 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 421 6 0 4 5.4 Fc1cccc2c1nc(OCC1CCN(CCCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
CHEMBL3093187 110766 0 None -20 5 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 421 6 0 4 5.4 Fc1cccc2c1nc(OCC1CCN(CCCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
11166796 89451 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
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 89451 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
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
44213661 213856 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 338 5 1 5 2.9 Nc1c(Cl)cc(C(=O)OCCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL91842 213856 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 338 5 1 5 2.9 Nc1c(Cl)cc(C(=O)OCCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
53357016 89449 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 446 7 1 8 3.0 OC1(CN2CCC(COc3noc4cccc(OC5CCOCC5)c34)CC2)CCOCC1 10.1021/jm300953p
CHEMBL2179581 89449 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 446 7 1 8 3.0 OC1(CN2CCC(COc3noc4cccc(OC5CCOCC5)c34)CC2)CCOCC1 10.1021/jm300953p
49783210 24411 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 440 7 1 6 3.9 CCCCN1CCC(COC(=O)c2cc(Br)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258338 24411 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 440 7 1 6 3.9 CCCCN1CCC(COC(=O)c2cc(Br)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL4172315 220007 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL None None None COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)NCCCN(CCCCN(CCCNC(=O)NCc3cn(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)NC4CCN(CCOC(=O)c5cc(Cl)c(N)cc5OC)CC4)nn3)CCCNC(=O)NCc3cn(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)NC4CCN(CCOC(=O)c5cc(Cl)c(N)cc5OC)CC4)nn3)CCCNC(=O)NCc3cn(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)NC4CCN(CCOC(=O)c5cc(Cl)c(N)cc5OC)CC4)nn3)nn2)CC1 10.1039/C6MD00458J
71457409 89737 0 None -17 6 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 461 5 0 4 4.9 CCCN1CCC(COc2nc3c(I)cccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181168 89737 0 None -17 6 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 461 5 0 4 4.9 CCCN1CCC(COc2nc3c(I)cccc3c3ncccc23)CC1 10.1021/jm300943r
71451950 89450 8 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
15295138 57836 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
CHEMBL157880 57836 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1 10.1021/jm960320m
118734515 125450 0 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 406 7 1 4 5.4 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CCCCC2C)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3417000 125450 0 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 406 7 1 4 5.4 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CCCCC2C)CC1 10.1021/acs.jmedchem.5b00115
11166796 89451 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation counting
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 89451 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation counting
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
44374544 59927 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCC1C2 10.1021/jm020270n
CHEMBL159825 59927 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCC1C2 10.1021/jm020270n
134828071 180540 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 416 7 1 3 6.1 COc1c(C(=O)CCC2CCN(CC3CCCCC3)CC2)cc(Cl)c2[nH]ccc12 10.1016/j.ejmech.2018.10.064
CHEMBL4537101 180540 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 416 7 1 3 6.1 COc1c(C(=O)CCC2CCN(CC3CCCCC3)CC2)cc(Cl)c2[nH]ccc12 10.1016/j.ejmech.2018.10.064
10020895 11477 0 None -524 8 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 4 receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 4 receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
CHEMBL103479 11477 0 None -524 8 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 4 receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 4 receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
71452073 89741 0 None -17 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3cnccc23)CC1 10.1021/jm300943r
CHEMBL2181172 89741 0 None -17 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3cnccc23)CC1 10.1021/jm300943r
44213663 213360 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 323 4 2 4 2.1 Nc1c(Cl)cc(C(=O)NCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL88867 213360 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 323 4 2 4 2.1 Nc1c(Cl)cc(C(=O)NCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
44592003 196254 0 None - 1 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 301 4 0 5 3.4 c1cc2c(OCCN3CCCCC3)nc3ccsc3n2c1 10.1016/j.bmc.2008.11.045
CHEMBL513740 196254 0 None - 1 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 301 4 0 5 3.4 c1cc2c(OCCN3CCCCC3)nc3ccsc3n2c1 10.1016/j.bmc.2008.11.045
44323269 18844 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
CHEMBL1183709 18844 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
CHEMBL314198 18844 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 10.1016/0960-894X(96)00002-9
6604914 107160 3 None -1 2 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/0960-894X(96)00052-2
CHEMBL28992 107160 3 None -1 2 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum.
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2 10.1016/0960-894X(96)00052-2
90644473 119057 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 353 5 0 5 2.7 COc1cc2c3c(cccc3n1)C(=O)N(CCCN1CCCCC1)C2=O 10.1016/j.ejmech.2014.05.015
CHEMBL3291078 119057 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 353 5 0 5 2.7 COc1cc2c3c(cccc3n1)C(=O)N(CCCN1CCCCC1)C2=O 10.1016/j.ejmech.2014.05.015
135446149 214964 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 393 7 2 5 3.4 CCCCN1CCC(CNC(=O)c2cc(Cl)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL98397 214964 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 393 7 2 5 3.4 CCCCN1CCC(CNC(=O)c2cc(Cl)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1021/jm020807x
135446149 214964 0 None - 1 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 393 7 2 5 3.4 CCCCN1CCC(CNC(=O)c2cc(Cl)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL98397 214964 0 None - 1 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 393 7 2 5 3.4 CCCCN1CCC(CNC(=O)c2cc(Cl)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
135446149 214964 0 None - 1 Rat 7.4 pKi = 7.4 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 393 7 2 5 3.4 CCCCN1CCC(CNC(=O)c2cc(Cl)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL98397 214964 0 None - 1 Rat 7.4 pKi = 7.4 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 393 7 2 5 3.4 CCCCN1CCC(CNC(=O)c2cc(Cl)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
90666006 116067 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 369 5 0 5 4.8 c1cc2c(OCC3CCN(CC4CCCC4)CC3)nc3ccsc3n2c1 10.1039/C2MD20063E
CHEMBL3218878 116067 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 369 5 0 5 4.8 c1cc2c(OCC3CCN(CC4CCCC4)CC3)nc3ccsc3n2c1 10.1039/C2MD20063E
10566528 168919 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 305 2 1 4 2.5 O=C(OC1CN2CCC1CC2)c1cc(Cl)cc2nc[nH]c12 10.1016/0960-894X(96)00200-4
CHEMBL416172 168919 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 305 2 1 4 2.5 O=C(OC1CN2CCC1CC2)c1cc(Cl)cc2nc[nH]c12 10.1016/0960-894X(96)00200-4
10566528 168919 0 None - 1 Rat 6.4 pKi = 6.4 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 305 2 1 4 2.5 O=C(OC1CN2CCC1CC2)c1cc(Cl)cc2nc[nH]c12 10.1021/jm991076c
CHEMBL416172 168919 0 None - 1 Rat 6.4 pKi = 6.4 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 305 2 1 4 2.5 O=C(OC1CN2CCC1CC2)c1cc(Cl)cc2nc[nH]c12 10.1021/jm991076c
240 7731 43 None -4 25 Guinea pig 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 7731 43 None -4 25 Guinea pig 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 7731 43 None -4 25 Guinea pig 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 7731 43 None -4 25 Guinea pig 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 7731 43 None -4 25 Guinea pig 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 7731 43 None -4 25 Guinea pig 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 7731 43 None -4 25 Guinea pig 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
41581 196602 5 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 278 5 1 4 2.7 COc1cccc(NC(=O)OCCN2CCCCC2)c1 10.1021/jm960853v
CHEMBL51647 196602 5 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 278 5 1 4 2.7 COc1cccc(NC(=O)OCCN2CCCCC2)c1 10.1021/jm960853v
44404969 79037 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 930 18 4 13 6.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCc2ccc3c(c2)oc2cc(CCC(=O)NC4CCN(CCOC(=O)c5cc(Cl)c(N)cc5OC)CC4)ccc23)CC1 10.1021/jm050234z
CHEMBL198226 79037 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 930 18 4 13 6.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCc2ccc3c(c2)oc2cc(CCC(=O)NC4CCN(CCOC(=O)c5cc(Cl)c(N)cc5OC)CC4)ccc23)CC1 10.1021/jm050234z
10802184 60932 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 272 5 1 5 1.6 COc1cc(N)c(Cl)cc1C(=O)OCCN(C)C 10.1021/jm960320m
CHEMBL160705 60932 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 272 5 1 5 1.6 COc1cc(N)c(Cl)cc1C(=O)OCCN(C)C 10.1021/jm960320m
135442121 119151 0 None - 1 Rat 7.3 pKi = 7.3 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 437 7 2 5 3.5 CCCCN1CCC(CNC(=O)c2cc(Br)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL329545 119151 0 None - 1 Rat 7.3 pKi = 7.3 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 437 7 2 5 3.5 CCCCN1CCC(CNC(=O)c2cc(Br)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
136118648 83096 0 None -9 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058703 83096 0 None -9 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
9797313 108706 2 None -154 3 Rat 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1016/0960-894X(95)00115-A
CHEMBL301039 108706 2 None -154 3 Rat 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1016/0960-894X(95)00115-A
9797313 108706 2 None -151 3 Guinea pig 7.3 pKi = 7.3 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1021/jm020270n
CHEMBL301039 108706 2 None -151 3 Guinea pig 7.3 pKi = 7.3 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1021/jm020270n
135442121 119151 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 437 7 2 5 3.5 CCCCN1CCC(CNC(=O)c2cc(Br)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL329545 119151 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 437 7 2 5 3.5 CCCCN1CCC(CNC(=O)c2cc(Br)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1021/jm020807x
135442121 119151 0 None - 1 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 437 7 2 5 3.5 CCCCN1CCC(CNC(=O)c2cc(Br)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL329545 119151 0 None - 1 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 437 7 2 5 3.5 CCCCN1CCC(CNC(=O)c2cc(Br)c([N+](=O)[O-])c3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
9797313 108706 2 None -154 3 Rat 7.3 pKi = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1021/jm960320m
CHEMBL301039 108706 2 None -154 3 Rat 7.3 pKi = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C 10.1021/jm960320m
44592184 185637 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 357 7 0 5 4.8 CCCCCN1CCC(COc2nc3sccc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL469592 185637 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 357 7 0 5 4.8 CCCCCN1CCC(COc2nc3sccc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
10757374 169871 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
CHEMBL41769 169871 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
11520559 79088 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 750 16 2 12 3.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCCCC(=O)N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL198371 79088 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 750 16 2 12 3.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCCCC(=O)N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
10757374 169871 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1021/jm960320m
CHEMBL41769 169871 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2 10.1021/jm960320m
9956365 202297 0 None -131 3 Guinea pig 6.3 pKi = 6.3 Binding
In vitro binding affinity at 5-hydroxytryptamine 4 receptor in guinea pig striatum using 3[H]GR-113808 as the radioligandIn vitro binding affinity at 5-hydroxytryptamine 4 receptor in guinea pig striatum using 3[H]GR-113808 as the radioligand
ChEMBL 470 7 2 4 4.1 CNC(=O)Cn1c2c(c3ccccc31)CCN(CCCCC13CCCc4cccc(c41)NC3=O)C2 10.1021/jm0104264
CHEMBL553794 202297 0 None -131 3 Guinea pig 6.3 pKi = 6.3 Binding
In vitro binding affinity at 5-hydroxytryptamine 4 receptor in guinea pig striatum using 3[H]GR-113808 as the radioligandIn vitro binding affinity at 5-hydroxytryptamine 4 receptor in guinea pig striatum using 3[H]GR-113808 as the radioligand
ChEMBL 470 7 2 4 4.1 CNC(=O)Cn1c2c(c3ccccc31)CCN(CCCCC13CCCc4cccc(c41)NC3=O)C2 10.1021/jm0104264
10687803 215136 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 329 3 1 6 0.9 CN1CCN(CNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL99452 215136 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 329 3 1 6 0.9 CN1CCN(CNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
155544687 181810 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 312 7 1 2 4.6 CCCCN1CCC(CCC(=O)c2ccc3[nH]ccc3c2)CC1 10.1016/j.ejmech.2018.10.064
CHEMBL4567394 181810 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 312 7 1 2 4.6 CCCCN1CCC(CCC(=O)c2ccc3[nH]ccc3c2)CC1 10.1016/j.ejmech.2018.10.064
90665997 116060 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 391 6 0 5 4.9 c1ccc(CCN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1039/C2MD20063E
CHEMBL3218869 116060 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 391 6 0 5 4.9 c1ccc(CCN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1039/C2MD20063E
235 9342 42 None -4 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm050234z
5311299 9342 42 None -4 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm050234z
CHEMBL286136 9342 42 None -4 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm050234z
44404965 78860 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 764 17 5 12 3.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
CHEMBL197745 78860 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 764 17 5 12 3.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
44404960 78866 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 736 15 5 12 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
CHEMBL197752 78866 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 736 15 5 12 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
11629247 79169 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 812 16 4 12 4.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCc2cccc(CNC(=O)C3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)c2)CC1 10.1021/jm050234z
CHEMBL198668 79169 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 812 16 4 12 4.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCc2cccc(CNC(=O)C3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)c2)CC1 10.1021/jm050234z
235 9342 42 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm801327q
5311299 9342 42 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm801327q
CHEMBL286136 9342 42 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm801327q
42618248 193807 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 479 8 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)Cc2ccccc2Cl)CC1 10.1021/jm801327q
CHEMBL490852 193807 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation countingDisplacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
ChEMBL 479 8 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)Cc2ccccc2Cl)CC1 10.1021/jm801327q
71450247 89751 0 None 4 9 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181188 89751 0 None 4 9 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
71712329 98164 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 454 7 2 5 2.3 CC(=O)N1CCN(CCN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402899 98164 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 454 7 2 5 2.3 CC(=O)N1CCN(CCN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
44628133 91356 0 None 50 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 414 6 1 5 4.6 Cn1cc2c(OCC3CCN(CCc4ccc(N)cc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2179675 91356 0 None 50 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 414 6 1 5 4.6 Cn1cc2c(OCC3CCN(CCc4ccc(N)cc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
CHEMBL2220953 91356 0 None 50 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 414 6 1 5 4.6 Cn1cc2c(OCC3CCN(CCc4ccc(N)cc4)CC3)nc3ccccc3c2c1 10.1021/jm300573d
53320666 63231 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 447 6 2 5 3.8 O=C(O)c1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmc.2010.10.011
CHEMBL1632176 63231 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 447 6 2 5 3.8 O=C(O)c1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1 10.1016/j.bmc.2010.10.011
44248319 202274 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 615 16 1 7 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN(C)CCCN(C)S(C)(=O)=O)cc2ccccc21 10.1021/jm900881j
CHEMBL553404 202274 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 615 16 1 7 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN(C)CCCN(C)S(C)(=O)=O)cc2ccccc21 10.1021/jm900881j
44248680 202361 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 571 10 2 7 3.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCC(CNS(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL555223 202361 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 571 10 2 7 3.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCC(CNS(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
44248313 91900492 202643 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 492 9 1 5 5.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL558719 202643 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 492 9 1 5 5.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
132337 10316 15 None -1 2 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm0509501
238 10316 15 None -1 2 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm0509501
CHEMBL34291 10316 15 None -1 2 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 10.1021/jm0509501
71460941 89456 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 374 8 0 5 5.1 CCCCN1CCC(COc2noc3cccc(OCC(C)(C)C)c23)CC1 10.1021/jm300953p
CHEMBL2179588 89456 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 374 8 0 5 5.1 CCCCN1CCC(COc2noc3cccc(OCC(C)(C)C)c23)CC1 10.1021/jm300953p
258 10340 31 None -2 8 Rat 8.3 pKi = 8.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80508-4
5191 10340 31 None -2 8 Rat 8.3 pKi = 8.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80508-4
CHEMBL287045 10340 31 None -2 8 Rat 8.3 pKi = 8.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80508-4
162663493 188781 0 None 30 4 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 572 10 3 7 3.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4780536 188781 0 None 30 4 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 572 10 3 7 3.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
10447437 56840 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 298 5 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC1 10.1021/jm960320m
CHEMBL156970 56840 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 298 5 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC1 10.1021/jm960320m
44592233 196138 0 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 357 6 0 5 4.7 CCCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL512679 196138 0 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 357 6 0 5 4.7 CCCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
10498232 58140 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 352 5 1 5 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC2CCC(CC2)C1 10.1021/jm960320m
CHEMBL158147 58140 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 352 5 1 5 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC2CCC(CC2)C1 10.1021/jm960320m
258 10340 31 None -2 8 Rat 8.3 pKi = 8.3 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960853v
5191 10340 31 None -2 8 Rat 8.3 pKi = 8.3 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960853v
CHEMBL287045 10340 31 None -2 8 Rat 8.3 pKi = 8.3 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960853v
258 10340 31 None -2 8 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960320m
5191 10340 31 None -2 8 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960320m
CHEMBL287045 10340 31 None -2 8 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm960320m
11166796 89451 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
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 89451 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
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
235 9342 42 None -4 3 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
5311299 9342 42 None -4 3 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
CHEMBL286136 9342 42 None -4 3 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
235 9342 42 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to Rluc fused 5HT4 receptor expressed in CHO cellsBinding affinity to Rluc fused 5HT4 receptor expressed in CHO cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm070552t
5311299 9342 42 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to Rluc fused 5HT4 receptor expressed in CHO cellsBinding affinity to Rluc fused 5HT4 receptor expressed in CHO cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm070552t
CHEMBL286136 9342 42 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to Rluc fused 5HT4 receptor expressed in CHO cellsBinding affinity to Rluc fused 5HT4 receptor expressed in CHO cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm070552t
155543353 180080 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assayBinding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assay
ChEMBL 418 7 3 6 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccc(O)c(O)c2)CC1 10.1016/j.ejmech.2019.111596
CHEMBL4526049 180080 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assayBinding affinity to recombinant human brain 5HT4 receptor by radio ligand binding assay
ChEMBL 418 7 3 6 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccc(O)c(O)c2)CC1 10.1016/j.ejmech.2019.111596
11643822 164638 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 1158 38 6 15 8.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCN(CCCCCCCCCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC(=O)NCC2CCNCC2)CC1 10.1021/jm050234z
CHEMBL408379 164638 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 1158 38 6 15 8.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCCCCCCN(CCCCCCCCCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC(=O)NCC2CCNCC2)CC1 10.1021/jm050234z
162652332 187127 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 550 10 2 8 3.4 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc3c(c2)N(C)CCO3)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4751353 187127 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 550 10 2 8 3.4 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc3c(c2)N(C)CCO3)CC1 10.1016/j.ejmech.2016.05.048
49783414 24449 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)cc2OC)CC1 10.1021/jm100668r
CHEMBL1258451 24449 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)cc2OC)CC1 10.1021/jm100668r
70691118 84276 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 469 7 3 6 1.7 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)C(N)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087327 84276 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 469 7 3 6 1.7 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)C(N)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
70686943 84280 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 497 7 2 6 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)C(=O)N(C)C)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087331 84280 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 497 7 2 6 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)C(=O)N(C)C)cc2ccccc21 10.1016/j.bmcl.2012.08.051
70684789 84281 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 470 7 3 7 2.0 COC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
CHEMBL2087332 84281 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 470 7 3 7 2.0 COC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1016/j.bmcl.2012.08.051
70695323 84285 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 504 8 2 7 1.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@H](O)CN(C)S(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
CHEMBL2087336 84285 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells
ChEMBL 504 8 2 7 1.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@H](O)CN(C)S(C)(=O)=O)cc2ccccc21 10.1016/j.bmcl.2012.08.051
44248923 201715 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
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
CHEMBL541968 201715 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
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
44248080 91900498 202655 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 493 8 2 6 2.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCC[C@@H]2C(N)=O)cc2ccccc21 10.1021/jm900881j
CHEMBL558855 202655 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 493 8 2 6 2.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCC[C@@H]2C(N)=O)cc2ccccc21 10.1021/jm900881j
44249057 91900485 202878 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 467 11 2 5 4.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCO)cc2ccccc21 10.1021/jm900881j
CHEMBL560876 202878 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 467 11 2 5 4.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCO)cc2ccccc21 10.1021/jm900881j
5 6927 72 None -288 53 Human 6.3 pKi = 6.3 Binding
Displacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cellsDisplacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/np0601760
5202 6927 72 None -288 53 Human 6.3 pKi = 6.3 Binding
Displacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cellsDisplacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/np0601760
CHEMBL39 6927 72 None -288 53 Human 6.3 pKi = 6.3 Binding
Displacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cellsDisplacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/np0601760
DB08839 6927 72 None -288 53 Human 6.3 pKi = 6.3 Binding
Displacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cellsDisplacement of [N-methyl-3H]GR-113808 from human 5HT4 receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/np0601760
118712567 121006 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 508 8 3 4 4.9 O=C(NCC1CCN(Cc2ccc(NS(=O)(=O)C3CCCCC3)cc2)CC1)c1c[nH]c2ccccc12 10.1016/j.bmcl.2014.06.083
CHEMBL3329801 121006 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
ChEMBL 508 8 3 4 4.9 O=C(NCC1CCN(Cc2ccc(NS(=O)(=O)C3CCCCC3)cc2)CC1)c1c[nH]c2ccccc12 10.1016/j.bmcl.2014.06.083
189 10265 39 None -2089 17 Rat 5.3 pKi = 5.3 Binding
Binding affinity against rat 5-hydroxytryptamine 4 receptorBinding affinity against rat 5-hydroxytryptamine 4 receptor
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm00014a004
5163 10265 39 None -2089 17 Rat 5.3 pKi = 5.3 Binding
Binding affinity against rat 5-hydroxytryptamine 4 receptorBinding affinity against rat 5-hydroxytryptamine 4 receptor
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm00014a004
CHEMBL297784 10265 39 None -2089 17 Rat 5.3 pKi = 5.3 Binding
Binding affinity against rat 5-hydroxytryptamine 4 receptorBinding affinity against rat 5-hydroxytryptamine 4 receptor
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm00014a004
9913554 107769 0 None -6309 14 Human 5.3 pKi = 5.3 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29433 107769 0 None -6309 14 Human 5.3 pKi = 5.3 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
9928343 110247 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor in rat was determined by rat tunica muscularis mucosae assayBinding affinity for 5-hydroxytryptamine 4 receptor in rat was determined by rat tunica muscularis mucosae assay
ChEMBL 349 4 2 4 2.2 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
CHEMBL3085015 110247 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor in rat was determined by rat tunica muscularis mucosae assayBinding affinity for 5-hydroxytryptamine 4 receptor in rat was determined by rat tunica muscularis mucosae assay
ChEMBL 349 4 2 4 2.2 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
155523661 177683 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 382 7 1 3 5.4 COc1c(C(=O)CCC2CCN(CC3CCCCC3)CC2)ccc2[nH]ccc12 10.1016/j.ejmech.2018.10.064
CHEMBL4454706 177683 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 382 7 1 3 5.4 COc1c(C(=O)CCC2CCN(CC3CCCCC3)CC2)ccc2[nH]ccc12 10.1016/j.ejmech.2018.10.064
71453895 89264 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 334 5 0 3 4.9 CCCN1CCC(COc2nc3ccccc3c3ccccc23)CC1 10.1016/j.bmc.2013.08.061
71453895 89264 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 334 5 0 3 4.9 CCCN1CCC(COc2nc3ccccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2177145 89264 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 334 5 0 3 4.9 CCCN1CCC(COc2nc3ccccc3c3ccccc23)CC1 10.1016/j.bmc.2013.08.061
CHEMBL2177145 89264 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 334 5 0 3 4.9 CCCN1CCC(COc2nc3ccccc3c3ccccc23)CC1 10.1021/jm300943r
135453290 140384 33 None -169 8 Human 6.3 pKi = 6.3 Binding
Inhibitory activity against 5HT4 receptorInhibitory activity against 5HT4 receptor
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 140384 33 None -169 8 Human 6.3 pKi = 6.3 Binding
Inhibitory activity against 5HT4 receptorInhibitory activity against 5HT4 receptor
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
90644470 119055 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 328 6 0 5 3.3 COc1cc(C(=O)OCCCN2CCCCC2)c2ccccc2n1 10.1016/j.ejmech.2014.05.015
CHEMBL3291075 119055 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 328 6 0 5 3.3 COc1cc(C(=O)OCCCN2CCCCC2)c2ccccc2n1 10.1016/j.ejmech.2014.05.015
44592041 185807 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 315 5 0 5 3.8 c1cc2c(OCCCN3CCCCC3)nc3ccsc3n2c1 10.1016/j.bmc.2008.11.045
CHEMBL471234 185807 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 315 5 0 5 3.8 c1cc2c(OCCCN3CCCCC3)nc3ccsc3n2c1 10.1016/j.bmc.2008.11.045
44592284 185806 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 377 5 0 5 4.8 c1ccc(CN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1039/C2MD20063E
CHEMBL471231 185806 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 377 5 0 5 4.8 c1ccc(CN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1039/C2MD20063E
90666004 116065 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 341 5 0 5 4.1 c1cc2c(OCC3CCN(CC4CC4)CC3)nc3ccsc3n2c1 10.1039/C2MD20063E
CHEMBL3218876 116065 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 341 5 0 5 4.1 c1cc2c(OCC3CCN(CC4CC4)CC3)nc3ccsc3n2c1 10.1039/C2MD20063E
15544720 73942 0 None - 1 Rat 7.3 pKi = 7.3 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 292 2 2 3 2.0 CN1CCC(NC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL18769 73942 0 None - 1 Rat 7.3 pKi = 7.3 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 292 2 2 3 2.0 CN1CCC(NC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
136118640 83093 0 None -4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058700 83093 0 None -4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
15544720 73942 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 292 2 2 3 2.0 CN1CCC(NC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL18769 73942 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 292 2 2 3 2.0 CN1CCC(NC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1021/jm020807x
260 10641 54 None -45 6 Guinea pig 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 nan
2775 10641 54 None -45 6 Guinea pig 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 nan
656665 10641 54 None -45 6 Guinea pig 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 nan
CHEMBL56564 10641 54 None -45 6 Guinea pig 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 nan
DB11699 10641 54 None -45 6 Guinea pig 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 nan
15544720 73942 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 292 2 2 3 2.0 CN1CCC(NC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/0960-894X(96)00200-4
CHEMBL18769 73942 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 292 2 2 3 2.0 CN1CCC(NC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/0960-894X(96)00200-4
15544720 73942 0 None - 1 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 292 2 2 3 2.0 CN1CCC(NC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL18769 73942 0 None - 1 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 292 2 2 3 2.0 CN1CCC(NC(=O)c2cc(Cl)cc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
1782 9296 84 None -12 23 Guinea pig 6.3 pKi = 6.3 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm020270n
241 9296 84 None -12 23 Guinea pig 6.3 pKi = 6.3 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm020270n
4168 9296 84 None -12 23 Guinea pig 6.3 pKi = 6.3 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm020270n
CHEMBL86 9296 84 None -12 23 Guinea pig 6.3 pKi = 6.3 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm020270n
DB01233 9296 84 None -12 23 Guinea pig 6.3 pKi = 6.3 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1021/jm020270n
10408029 23232 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
CHEMBL123377 23232 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells
ChEMBL 389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1 10.1021/jm0009538
10744356 18145 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 386 6 1 5 1.9 C=CC[N+]1(C)CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL1179774 18145 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 386 6 1 5 1.9 C=CC[N+]1(C)CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL99299 18145 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 386 6 1 5 1.9 C=CC[N+]1(C)CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
90644474 119058 0 None - 1 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 343 4 0 3 3.7 O=C1c2cc(Cl)nc3cccc(c23)CN1CCCN1CCCCC1 10.1016/j.ejmech.2014.05.015
CHEMBL3291079 119058 0 None - 1 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 minsDisplacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins
ChEMBL 343 4 0 3 3.7 O=C1c2cc(Cl)nc3cccc(c23)CN1CCCN1CCCCC1 10.1016/j.ejmech.2014.05.015
44288600 107894 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor in rat was determined by rat tunica muscularis mucosae assayBinding affinity for 5-hydroxytryptamine 4 receptor in rat was determined by rat tunica muscularis mucosae assay
ChEMBL 335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
CHEMBL295155 107894 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity for 5-hydroxytryptamine 4 receptor in rat was determined by rat tunica muscularis mucosae assayBinding affinity for 5-hydroxytryptamine 4 receptor in rat was determined by rat tunica muscularis mucosae assay
ChEMBL 335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2 10.1016/j.bmcl.2004.09.005
44592077 196091 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 6 0 5 4.2 c1cc2c(OCCCCN3CCCCC3)nc3ccsc3n2c1 10.1016/j.bmc.2008.11.045
CHEMBL512303 196091 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 6 0 5 4.2 c1cc2c(OCCCCN3CCCCC3)nc3ccsc3n2c1 10.1016/j.bmc.2008.11.045
56850385 78252 0 None -72 3 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation counting
ChEMBL 351 7 1 3 3.1 O=C1C2CCCN2C(=O)N1CCCCNCc1ccc2ccccc2c1 10.1021/jm2007886
CHEMBL1926730 78252 0 None -72 3 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation counting
ChEMBL 351 7 1 3 3.1 O=C1C2CCCN2C(=O)N1CCCCNCc1ccc2ccccc2c1 10.1021/jm2007886
CHEMBL1962454 78252 0 None -72 3 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation counting
ChEMBL 351 7 1 3 3.1 O=C1C2CCCN2C(=O)N1CCCCNCc1ccc2ccccc2c1 10.1021/jm2007886
3277217 185511 5 None -6 2 Guinea pig 5.2 pKi = 5.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 271 3 1 4 1.4 O=C(O)CN1CCN(c2ccc3ccccc3n2)CC1 10.1021/jm900018b
715494 185511 5 None -6 2 Guinea pig 5.2 pKi = 5.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 271 3 1 4 1.4 O=C(O)CN1CCN(c2ccc3ccccc3n2)CC1 10.1021/jm900018b
CHEMBL468498 185511 5 None -6 2 Guinea pig 5.2 pKi = 5.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 271 3 1 4 1.4 O=C(O)CN1CCN(c2ccc3ccccc3n2)CC1 10.1021/jm900018b
11174673 180410 0 None - 1 Human 7.2 pKi = 7.2 Binding
Agonist activity at 5-HT4 receptor (unknown origin)Agonist activity at 5-HT4 receptor (unknown origin)
ChEMBL 321 3 3 5 1.6 Cc1cn2c(N)c(Cl)cc(C(=O)NCC3CCNCC3)c2n1 10.1016/j.ejmech.2019.111569
CHEMBL4533922 180410 0 None - 1 Human 7.2 pKi = 7.2 Binding
Agonist activity at 5-HT4 receptor (unknown origin)Agonist activity at 5-HT4 receptor (unknown origin)
ChEMBL 321 3 3 5 1.6 Cc1cn2c(N)c(Cl)cc(C(=O)NCC3CCNCC3)c2n1 10.1016/j.ejmech.2019.111569
44592107 185864 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 301 3 0 5 3.3 CN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL471661 185864 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 301 3 0 5 3.3 CN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
11135810 213283 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 606 11 1 8 5.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCCCN2C(=O)c3cccc4c(N(C)C)ccc(c34)C2=O)CC1 10.1021/jm0307887
CHEMBL88355 213283 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 606 11 1 8 5.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCCCN2C(=O)c3cccc4c(N(C)C)ccc(c34)C2=O)CC1 10.1021/jm0307887
56850387 78253 0 None -13 3 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation counting
ChEMBL 365 8 1 3 3.2 O=C1C2CCCN2C(=O)N1CCCCNCCc1ccc2ccccc2c1 10.1021/jm2007886
CHEMBL1926731 78253 0 None -13 3 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation counting
ChEMBL 365 8 1 3 3.2 O=C1C2CCCN2C(=O)N1CCCCNCCc1ccc2ccccc2c1 10.1021/jm2007886
CHEMBL1962455 78253 0 None -13 3 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation counting
ChEMBL 365 8 1 3 3.2 O=C1C2CCCN2C(=O)N1CCCCNCCc1ccc2ccccc2c1 10.1021/jm2007886
44404955 140298 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 868 24 4 15 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCCOCCOCCOCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL370796 140298 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 868 24 4 15 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCCOCCOCCOCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
235 9342 42 None -5 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1039/C8MD00233A
5311299 9342 42 None -5 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1039/C8MD00233A
CHEMBL286136 9342 42 None -5 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1039/C8MD00233A
42636941 185728 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1039/C2MD20063E
CHEMBL470432 185728 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1039/C2MD20063E
235 9342 42 None -5 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1039/C6MD00458J
5311299 9342 42 None -5 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1039/C6MD00458J
CHEMBL286136 9342 42 None -5 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1039/C6MD00458J
10764565 55787 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 339 5 1 4 2.7 COc1cc(N)c(Cl)cc1C(=O)OCC[N+]12CCC(CC1)CC2 10.1021/jm960320m
CHEMBL156088 55787 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 339 5 1 4 2.7 COc1cc(N)c(Cl)cc1C(=O)OCC[N+]12CCC(CC1)CC2 10.1021/jm960320m
10548275 55285 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 307 5 1 4 2.1 COc1cc(N)c(Cl)cc1C(=O)OCC[n+]1ccccc1 10.1021/jm960320m
CHEMBL155631 55285 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 307 5 1 4 2.1 COc1cc(N)c(Cl)cc1C(=O)OCC[n+]1ccccc1 10.1021/jm960320m
162648923 186733 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 550 10 3 8 2.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc3c(c2)NC(=O)CO3)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4746550 186733 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 550 10 3 8 2.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc3c(c2)NC(=O)CO3)CC1 10.1016/j.ejmech.2016.05.048
44371350 126946 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 342 5 1 6 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC(C)OC(C)C1 10.1021/jm960320m
CHEMBL351570 126946 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 342 5 1 6 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC(C)OC(C)C1 10.1021/jm960320m
71451950 89450 8 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
49783208 24380 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 362 6 1 6 3.0 CCCCN1CCC(COC(=O)c2cc(C)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258222 24380 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 362 6 1 6 3.0 CCCCN1CCC(COC(=O)c2cc(C)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
258 10340 31 None -1 8 Human 8.2 pKi = 8.2 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/j.bmc.2008.11.045
5191 10340 31 None -1 8 Human 8.2 pKi = 8.2 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/j.bmc.2008.11.045
CHEMBL287045 10340 31 None -1 8 Human 8.2 pKi = 8.2 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/j.bmc.2008.11.045
71712611 98152 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 478 8 3 7 -0.1 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]cnc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
CHEMBL2402887 98152 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human recombinant 5HT4 receptorBinding affinity to human recombinant 5HT4 receptor
ChEMBL 478 8 3 7 -0.1 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]cnc34)CC2)CC1 10.1016/j.bmcl.2013.05.018
44248439 202971 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 464 7 1 5 4.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL561398 202971 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 464 7 1 5 4.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
44592235 179346 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 343 4 0 5 4.4 Cc1csc2nc(OCC3CCN(C(C)C)CC3)c3cccn3c12 10.1016/j.bmc.2008.11.045
CHEMBL448702 179346 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 343 4 0 5 4.4 Cc1csc2nc(OCC3CCN(C(C)C)CC3)c3cccn3c12 10.1016/j.bmc.2008.11.045
10584 8245 0 None 1 2 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1021/acs.jmedchem.5b00115
86582973 8245 0 None 1 2 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1021/acs.jmedchem.5b00115
CHEMBL3417009 8245 0 None 1 2 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1021/acs.jmedchem.5b00115
10584 8245 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from human 5-HT4R membrane in Tris buffer assessed as inhibitory constant measured after 60 mins by filter binding methodDisplacement of [3H]GR113808 from human 5-HT4R membrane in Tris buffer assessed as inhibitory constant measured after 60 mins by filter binding method
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.ejmech.2019.02.076
86582973 8245 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from human 5-HT4R membrane in Tris buffer assessed as inhibitory constant measured after 60 mins by filter binding methodDisplacement of [3H]GR113808 from human 5-HT4R membrane in Tris buffer assessed as inhibitory constant measured after 60 mins by filter binding method
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.ejmech.2019.02.076
CHEMBL3417009 8245 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from human 5-HT4R membrane in Tris buffer assessed as inhibitory constant measured after 60 mins by filter binding methodDisplacement of [3H]GR113808 from human 5-HT4R membrane in Tris buffer assessed as inhibitory constant measured after 60 mins by filter binding method
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.ejmech.2019.02.076
10666935 214729 0 None 1 2 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 371 5 1 6 1.7 CC(C)N1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL97019 214729 0 None 1 2 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 371 5 1 6 1.7 CC(C)N1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
71451950 89450 8 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
CHEMBL2179582 89450 8 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21 10.1021/jm300953p
11603514 78265 0 None -5 4 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation counting
ChEMBL 390 11 1 5 4.0 O=C1CSC(=O)N1CCCCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926760 78265 0 None -5 4 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation counting
ChEMBL 390 11 1 5 4.0 O=C1CSC(=O)N1CCCCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962492 78265 0 None -5 4 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley albinus rat striatal membranes after 30 mins by scintillation counting
ChEMBL 390 11 1 5 4.0 O=C1CSC(=O)N1CCCCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
209710 108624 1 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 282 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)OCCN1CCCCC1 10.1021/jm960853v
CHEMBL300476 108624 1 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 282 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)OCCN1CCCCC1 10.1021/jm960853v
44240743 13529 15 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity to 5HT4 receptorBinding affinity to 5HT4 receptor
ChEMBL 370 7 2 3 4.3 O=C(NCCCCN1CCCCC1)Nc1ccc(-c2ccc(F)cc2)nc1 10.1021/jm901692q
CHEMBL1083787 13529 15 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity to 5HT4 receptorBinding affinity to 5HT4 receptor
ChEMBL 370 7 2 3 4.3 O=C(NCCCCN1CCCCC1)Nc1ccc(-c2ccc(F)cc2)nc1 10.1021/jm901692q
136118651 83099 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058706 83099 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
145955685 169247 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 602 17 6 10 0.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)NCCOCCOCCNC(=O)NCC(=O)O)CC1 10.1039/C6MD00458J
CHEMBL4167048 169247 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL 602 17 6 10 0.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)NCCOCCOCCNC(=O)NCC(=O)O)CC1 10.1039/C6MD00458J
44592039 195077 0 None - 1 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 301 4 1 5 3.5 c1cc2c(OCCC3CCCCN3)nc3ccsc3n2c1 10.1016/j.bmc.2008.11.045
CHEMBL500336 195077 0 None - 1 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 301 4 1 5 3.5 c1cc2c(OCCC3CCCCN3)nc3ccsc3n2c1 10.1016/j.bmc.2008.11.045
260 10641 54 None -19 6 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/0960-894X(96)00200-4
2775 10641 54 None -19 6 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/0960-894X(96)00200-4
656665 10641 54 None -19 6 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/0960-894X(96)00200-4
CHEMBL56564 10641 54 None -19 6 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/0960-894X(96)00200-4
DB11699 10641 54 None -19 6 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1016/0960-894X(96)00200-4
76313431 110147 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 330 2 2 5 1.5 COc1ccc2[nH]c(=O)n(C(=O)N[C@H]3C[C@@H]4CC[C@H](C3)N4C)c2c1 10.1016/j.bmc.2008.11.045
CHEMBL3084582 110147 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
ChEMBL 330 2 2 5 1.5 COc1ccc2[nH]c(=O)n(C(=O)N[C@H]3C[C@@H]4CC[C@H](C3)N4C)c2c1 10.1016/j.bmc.2008.11.045
9839803 99647 0 None -1 2 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranesDisplacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes
ChEMBL 313 3 2 4 2.2 O=C(NCC1CCNCC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmc.2013.09.004
CHEMBL2440452 99647 0 None -1 2 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranesDisplacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes
ChEMBL 313 3 2 4 2.2 O=C(NCC1CCNCC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmc.2013.09.004
9839803 99647 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]SB207710 from human recombinant 5-HT4 receptorDisplacement of [125I]SB207710 from human recombinant 5-HT4 receptor
ChEMBL 313 3 2 4 2.2 O=C(NCC1CCNCC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmc.2013.09.004
CHEMBL2440452 99647 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]SB207710 from human recombinant 5-HT4 receptorDisplacement of [125I]SB207710 from human recombinant 5-HT4 receptor
ChEMBL 313 3 2 4 2.2 O=C(NCC1CCNCC1)c1c2n(c3ccccc13)CCCO2 10.1016/j.bmc.2013.09.004
44592284 185806 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 377 5 0 5 4.8 c1ccc(CN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1016/j.bmc.2008.11.045
CHEMBL471231 185806 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 377 5 0 5 4.8 c1ccc(CN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1016/j.bmc.2008.11.045
10757502 91929739 201904 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 312 3 2 4 2.6 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1016/j.bmcl.2012.05.034
CHEMBL550064 201904 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
ChEMBL 312 3 2 4 2.6 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1016/j.bmcl.2012.05.034
10757502 91929739 201904 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 312 3 2 4 2.6 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1021/jm900881j
CHEMBL550064 201904 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 312 3 2 4 2.6 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21 10.1021/jm900881j
44248312 91900490 201909 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 531 12 2 6 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
CHEMBL550122 201909 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 531 12 2 6 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCS(=O)(=O)O)cc2ccccc21 10.1021/jm900881j
44248187 91900482 202159 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 409 7 1 4 4.5 CCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
CHEMBL551941 202159 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 409 7 1 4 4.5 CCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
44247811 202250 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 369 8 3 5 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCO)CC1 10.1021/jm900881j
CHEMBL552693 202250 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 369 8 3 5 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCO)CC1 10.1021/jm900881j
44249056 91900483 203116 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 451 10 1 4 5.7 CCCCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
CHEMBL562400 203116 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 451 10 1 4 5.7 CCCCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2 10.1021/jm900881j
10574402 91900484 203251 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 425 8 2 5 3.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCO)cc2ccccc21 10.1021/jm900881j
CHEMBL563261 203251 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 425 8 2 5 3.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCO)cc2ccccc21 10.1021/jm900881j
44248433 91900494 203520 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 529 7 1 7 1.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL565146 203520 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 529 7 1 7 1.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21 10.1021/jm900881j
131725 207216 3 None 3 2 Guinea pig 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 342 2 1 5 2.6 CC(C)n1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1021/jm981098j
CHEMBL59834 207216 3 None 3 2 Guinea pig 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 342 2 1 5 2.6 CC(C)n1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 10.1021/jm981098j
44247947 202112 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 433 9 3 6 2.2 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCS(=O)(=O)O)CC1 10.1021/jm900881j
CHEMBL551678 202112 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 433 9 3 6 2.2 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCS(=O)(=O)O)CC1 10.1021/jm900881j
3168 16034 92 None -93 22 Guinea pig 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 16034 92 None -93 22 Guinea pig 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
10347130 212813 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 536 7 2 8 3.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CN2C(=O)c3cccc4c(N)ccc(c34)C2=O)CC1 10.1021/jm0307887
CHEMBL85125 212813 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 536 7 2 8 3.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CN2C(=O)c3cccc4c(N)ccc(c34)C2=O)CC1 10.1021/jm0307887
10812045 22293 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 419 7 1 7 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2OC)CC1 10.1021/jm0009538
CHEMBL121766 22293 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 419 7 1 7 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2OC)CC1 10.1021/jm0009538
14403199 123388 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 324 3 1 5 2.7 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC(C1)N2C 10.1016/S0960-894X(01)80508-4
CHEMBL33676 123388 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 324 3 1 5 2.7 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC(C1)N2C 10.1016/S0960-894X(01)80508-4
14403199 123388 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 324 3 1 5 2.7 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC(C1)N2C 10.1021/jm960320m
CHEMBL33676 123388 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 324 3 1 5 2.7 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC(C1)N2C 10.1021/jm960320m
10530233 18129 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 402 7 1 5 2.5 CCCC[N+]1(C)CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL1179716 18129 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 402 7 1 5 2.5 CCCC[N+]1(C)CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL95968 18129 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 402 7 1 5 2.5 CCCC[N+]1(C)CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
10381927 169878 1 None 1 2 Guinea pig 5.2 pKi = 5.2 Binding
Displacement of [3H]-GR113808 from 5-HT4 receptor of guinea pig striatumDisplacement of [3H]-GR113808 from 5-HT4 receptor of guinea pig striatum
ChEMBL 329 1 0 3 3.8 CN1CCN(c2nc3ccccc3c3c2CCc2ccccc2-3)CC1 10.1021/jm00014a021
CHEMBL417706 169878 1 None 1 2 Guinea pig 5.2 pKi = 5.2 Binding
Displacement of [3H]-GR113808 from 5-HT4 receptor of guinea pig striatumDisplacement of [3H]-GR113808 from 5-HT4 receptor of guinea pig striatum
ChEMBL 329 1 0 3 3.8 CN1CCN(c2nc3ccccc3c3c2CCc2ccccc2-3)CC1 10.1021/jm00014a021
11799162 18140 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 360 4 1 5 1.3 CC(C)n1c(=O)n(C(=O)NCCN2CC[N+](C)(C)CC2)c2ccccc21 10.1021/jm981098j
CHEMBL1179748 18140 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 360 4 1 5 1.3 CC(C)n1c(=O)n(C(=O)NCCN2CC[N+](C)(C)CC2)c2ccccc21 10.1021/jm981098j
CHEMBL97903 18140 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 360 4 1 5 1.3 CC(C)n1c(=O)n(C(=O)NCCN2CC[N+](C)(C)CC2)c2ccccc21 10.1021/jm981098j
21588627 113399 0 None - 1 Rat 7.2 pKi = 7.2 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 438 7 1 4 4.8 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3Cc2ccccc2)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL314299 113399 0 None - 1 Rat 7.2 pKi = 7.2 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 438 7 1 4 4.8 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3Cc2ccccc2)CC1 10.1016/s0960-894x(01)00517-0
21588627 113399 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 438 7 1 4 4.8 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3Cc2ccccc2)CC1 10.1021/jm020807x
CHEMBL314299 113399 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 438 7 1 4 4.8 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3Cc2ccccc2)CC1 10.1021/jm020807x
21588627 113399 0 None - 1 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 438 7 1 4 4.8 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3Cc2ccccc2)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL314299 113399 0 None - 1 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 438 7 1 4 4.8 CC(C)CN1CCC(CNC(=O)c2cc(Cl)cc3c2ncn3Cc2ccccc2)CC1 10.1016/s0960-894x(01)00517-0
119584 9373 102 None -1 6 Guinea pig 7.2 pKi = 7.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1021/jm020270n
1848 9373 102 None -1 6 Guinea pig 7.2 pKi = 7.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1021/jm020270n
242 9373 102 None -1 6 Guinea pig 7.2 pKi = 7.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1021/jm020270n
CHEMBL60889 9373 102 None -1 6 Guinea pig 7.2 pKi = 7.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1021/jm020270n
DB11675 9373 102 None -1 6 Guinea pig 7.2 pKi = 7.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1021/jm020270n
10335971 107686 1 None - 1 Guinea pig 5.2 pKi = 5.2 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.
ChEMBL 317 1 0 4 3.9 CN1CCN(c2nc3ccccc3c3c2oc2ccccc23)CC1 10.1021/jm00014a021
CHEMBL293866 107686 1 None - 1 Guinea pig 5.2 pKi = 5.2 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand.
ChEMBL 317 1 0 4 3.9 CN1CCN(c2nc3ccccc3c3c2oc2ccccc23)CC1 10.1021/jm00014a021
71450246 89747 0 None - 1 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 348 5 0 3 5.2 CCCN1CCC(COc2nc3cc(C)ccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181184 89747 0 None - 1 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 348 5 0 3 5.2 CCCN1CCC(COc2nc3cc(C)ccc3c3ccccc23)CC1 10.1021/jm300943r
44404958 79182 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 764 17 5 12 3.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCCCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
CHEMBL198719 79182 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 764 17 5 12 3.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCCCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
11813852 118794 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 574 10 2 8 4.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
CHEMBL328918 118794 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 574 10 2 8 4.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
11596009 80149 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 342 3 1 5 2.4 CC(C)n1c(=O)n(C(=O)NC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21 10.1021/jm0509501
CHEMBL201414 80149 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
ChEMBL 342 3 1 5 2.4 CC(C)n1c(=O)n(C(=O)NC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21 10.1021/jm0509501
9800656 22322 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
CHEMBL121913 22322 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
49783211 24412 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 488 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(I)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258339 24412 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 488 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(I)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
11005668 213421 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 504 9 2 11 3.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNc2ccc([N+](=O)[O-])c3nonc23)CC1 10.1021/jm0307887
CHEMBL89225 213421 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 504 9 2 11 3.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNc2ccc([N+](=O)[O-])c3nonc23)CC1 10.1021/jm0307887
71462777 89740 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181171 89740 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cellsDisplacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3ncccc23)CC1 10.1021/jm300943r
10788092 60362 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 416 7 1 6 3.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)c2ccccc2)CC1 10.1021/jm960320m
CHEMBL160237 60362 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 416 7 1 6 3.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)c2ccccc2)CC1 10.1021/jm960320m
162645470 186323 0 None 107 2 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 536 11 3 7 3.5 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(NC(C)=O)cc2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4741579 186323 0 None 107 2 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 536 11 3 7 3.5 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(NC(C)=O)cc2)CC1 10.1016/j.ejmech.2016.05.048
10449091 126743 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 326 5 1 5 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCCC1C 10.1021/jm960320m
CHEMBL349809 126743 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 326 5 1 5 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCCC1C 10.1021/jm960320m
49780155 23912 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 393 7 1 8 2.6 CCCCN1CCC(COC(=O)c2cc([N+](=O)[O-])c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1255606 23912 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 393 7 1 8 2.6 CCCCN1CCC(COC(=O)c2cc([N+](=O)[O-])c(N)c3c2OCCO3)CC1 10.1021/jm100668r
44629280 89500 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 351 6 0 4 4.6 CCCCN1CCC(COc2nc3ccccc3c3cn(C)cc23)CC1 10.1021/jm300573d
CHEMBL2179679 89500 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
ChEMBL 351 6 0 4 4.6 CCCCN1CCC(COc2nc3ccccc3c3cn(C)cc23)CC1 10.1021/jm300573d
11627949 83196 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
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
CHEMBL2059587 83196 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells
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
44248193 201588 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 593 12 1 7 5.0 CCOC(=O)N1CCN(CCCCCCCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cc4ccccc4n(C(C)C)c2=O)C3)CC1 10.1021/jm900881j
CHEMBL538956 201588 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 593 12 1 7 5.0 CCOC(=O)N1CCN(CCCCCCCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cc4ccccc4n(C(C)C)c2=O)C3)CC1 10.1021/jm900881j
21252890 202255 1 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 300 4 2 4 2.3 CC(C)n1nc(C(=O)NCC2CCNCC2)c2ccccc21 10.1021/jm900881j
CHEMBL552796 202255 1 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 300 4 2 4 2.3 CC(C)n1nc(C(=O)NCC2CCNCC2)c2ccccc21 10.1021/jm900881j
44248321 202360 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 541 8 1 6 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCN(c3ccccc3)CC2)cc2ccccc21 10.1021/jm900881j
CHEMBL555222 202360 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 541 8 1 6 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCN(c3ccccc3)CC2)cc2ccccc21 10.1021/jm900881j
235 9342 42 None -4 3 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
5311299 9342 42 None -4 3 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
CHEMBL286136 9342 42 None -4 3 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
10717193 23554 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm0009538
CHEMBL124485 23554 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm0009538
15544714 73057 7 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 258 2 2 3 1.4 CN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
CHEMBL18473 73057 7 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
ChEMBL 258 2 2 3 1.4 CN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1021/jm020807x
15544714 73057 7 None - 1 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 258 2 2 3 1.4 CN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/0960-894X(96)00200-4
CHEMBL18473 73057 7 None - 1 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
ChEMBL 258 2 2 3 1.4 CN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/0960-894X(96)00200-4
15544714 73057 7 None - 1 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 258 2 2 3 1.4 CN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL18473 73057 7 None - 1 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 258 2 2 3 1.4 CN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
1471834 10401 42 None -4 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT4Binding affinity to human 5HT4
ChEMBL 366 2 0 2 5.5 O=C1C(=Nc2cccc(c2)C(F)(F)F)c2c(N1c1ccccc1)cccc2 10.1021/jm060001n
6126 10401 42 None -4 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT4Binding affinity to human 5HT4
ChEMBL 366 2 0 2 5.5 O=C1C(=Nc2cccc(c2)C(F)(F)F)c2c(N1c1ccccc1)cccc2 10.1021/jm060001n
CHEMBL210288 10401 42 None -4 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT4Binding affinity to human 5HT4
ChEMBL 366 2 0 2 5.5 O=C1C(=Nc2cccc(c2)C(F)(F)F)c2c(N1c1ccccc1)cccc2 10.1021/jm060001n
15544714 73057 7 None - 1 Rat 6.1 pKi = 6.1 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 258 2 2 3 1.4 CN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
CHEMBL18473 73057 7 None - 1 Rat 6.1 pKi = 6.1 Binding
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
ChEMBL 258 2 2 3 1.4 CN1CCC(NC(=O)c2cccc3[nH]cnc23)CC1 10.1016/s0960-894x(01)00517-0
30049 194982 1 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 282 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)OCCN1CCCCC1 10.1021/jm960853v
CHEMBL49907 194982 1 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 282 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)OCCN1CCCCC1 10.1021/jm960853v
15485875 195508 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 301 5 0 5 3.4 c1cc2c(OCCCN3CCCC3)nc3ccsc3n2c1 10.1016/j.bmc.2008.11.045
CHEMBL504904 195508 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 301 5 0 5 3.4 c1cc2c(OCCCN3CCCC3)nc3ccsc3n2c1 10.1016/j.bmc.2008.11.045
10664258 215147 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 331 4 1 6 0.6 CCn1c(=O)n(C(=O)NCCN2CCN(C)CC2)c2ccccc21 10.1021/jm981098j
CHEMBL99515 215147 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 331 4 1 6 0.6 CCn1c(=O)n(C(=O)NCCN2CCN(C)CC2)c2ccccc21 10.1021/jm981098j
90665998 116061 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 405 7 0 5 5.3 c1ccc(CCCN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1039/C2MD20063E
CHEMBL3218870 116061 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 405 7 0 5 5.3 c1ccc(CCCN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1039/C2MD20063E
108182 10903 22 None -1 17 Rat 6.1 pKi = 6.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1016/S0960-894X(01)80508-4
245 10903 22 None -1 17 Rat 6.1 pKi = 6.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1016/S0960-894X(01)80508-4
CHEMBL18041 10903 22 None -1 17 Rat 6.1 pKi = 6.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1016/S0960-894X(01)80508-4
139188853 173661 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 341 6 2 4 3.2 CCCCN1CCC(CNC(=O)c2ccc3cccc(O)c3n2)CC1 10.1039/C8MD00233A
CHEMBL4285988 173661 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 341 6 2 4 3.2 CCCCN1CCC(CNC(=O)c2ccc3cccc(O)c3n2)CC1 10.1039/C8MD00233A
11966400 213623 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 588 11 2 8 4.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
CHEMBL90559 213623 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 588 11 2 8 4.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
10779499 44848 0 None - 1 Rat 6.1 pKi = 6.1 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 285 2 3 4 1.0 Nc1ccc(C(=O)NC2CN3CCC2CC3)c2[nH]cnc12 10.1021/jm991076c
CHEMBL146068 44848 0 None - 1 Rat 6.1 pKi = 6.1 Binding
In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.In vitro affinity at serotonergic 5-hydroxytryptamine 4 receptor by radioligand binding assay using [3H]GR-113808 in rat striatum membranes.
ChEMBL 285 2 3 4 1.0 Nc1ccc(C(=O)NC2CN3CCC2CC3)c2[nH]cnc12 10.1021/jm991076c
44247808 202158 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 395 10 2 4 4.5 CCCCCCCCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
CHEMBL551940 202158 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 395 10 2 4 4.5 CCCCCCCCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1 10.1021/jm900881j
44247813 202371 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 411 11 3 5 3.5 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCO)CC1 10.1021/jm900881j
CHEMBL555447 202371 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 411 11 3 5 3.5 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCO)CC1 10.1021/jm900881j
10837280 91900491 202601 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 450 6 1 5 3.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL558259 202601 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 450 6 1 5 3.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCCCC2)cc2ccccc21 10.1021/jm900881j
9857899 128951 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 311 3 1 4 3.3 CN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL35972 128951 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorAbility to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptor
ChEMBL 311 3 1 4 3.3 CN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
90666007 116068 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 383 5 0 5 5.2 c1cc2c(OCC3CCN(CC4CCCCC4)CC3)nc3ccsc3n2c1 10.1039/C2MD20063E
CHEMBL3218879 116068 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 383 5 0 5 5.2 c1cc2c(OCC3CCN(CC4CCCCC4)CC3)nc3ccsc3n2c1 10.1039/C2MD20063E
73354085 99646 0 None -1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranesDisplacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes
ChEMBL 385 6 2 5 3.4 CCCCN1CCC(CNC(=O)c2c3n(c4cc(O)ccc24)CCCO3)CC1 10.1016/j.bmc.2013.09.004
CHEMBL2440451 99646 0 None -1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranesDisplacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes
ChEMBL 385 6 2 5 3.4 CCCCN1CCC(CNC(=O)c2c3n(c4cc(O)ccc24)CCCO3)CC1 10.1016/j.bmc.2013.09.004
73354085 99646 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]SB207710 from human recombinant 5-HT4 receptorDisplacement of [125I]SB207710 from human recombinant 5-HT4 receptor
ChEMBL 385 6 2 5 3.4 CCCCN1CCC(CNC(=O)c2c3n(c4cc(O)ccc24)CCCO3)CC1 10.1016/j.bmc.2013.09.004
CHEMBL2440451 99646 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]SB207710 from human recombinant 5-HT4 receptorDisplacement of [125I]SB207710 from human recombinant 5-HT4 receptor
ChEMBL 385 6 2 5 3.4 CCCCN1CCC(CNC(=O)c2c3n(c4cc(O)ccc24)CCCO3)CC1 10.1016/j.bmc.2013.09.004
44249186 202095 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 327 4 2 4 2.3 CC(C)n1c(=O)c(C(=O)NCC2CCNCC2)cc2ccccc21 10.1021/jm900881j
CHEMBL551535 202095 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 327 4 2 4 2.3 CC(C)n1c(=O)c(C(=O)NCC2CCNCC2)cc2ccccc21 10.1021/jm900881j
44247815 203254 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 456 6 2 6 2.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
CHEMBL563276 203254 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [H]GR-113808 from human 5HT4C receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 456 6 2 6 2.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2C(=O)c3ccccc3C2=O)CC1 10.1021/jm900881j
24865727 199892 0 None -5011 11 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from human cloned 5HT4 receptorDisplacement of radioligand from human cloned 5HT4 receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL522708 199892 0 None -5011 11 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from human cloned 5HT4 receptorDisplacement of radioligand from human cloned 5HT4 receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
11686414 78524 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 764 17 4 12 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCC(=O)NCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL196633 78524 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 764 17 4 12 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCC(=O)NCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
44404966 140227 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 834 22 5 12 5.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCCCCCCCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
CHEMBL370646 140227 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 834 22 5 12 5.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)NCCCCCCCCCCNC(=O)C2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
145990064 173748 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 344 6 1 6 2.1 COc1cc(C(=O)OCCN2CCC(CO)CC2)c2ccccc2n1 10.1039/C8MD00233A
CHEMBL4287473 173748 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding methodDisplacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method
ChEMBL 344 6 1 6 2.1 COc1cc(C(=O)OCCN2CCC(CO)CC2)c2ccccc2n1 10.1039/C8MD00233A
9800656 22322 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
CHEMBL121913 22322 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 10.1021/jm0009538
11726706 214503 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 371 6 1 6 1.7 CCCN1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL95661 214503 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 371 6 1 6 1.7 CCCN1CCN(CCNC(=O)n2c(=O)n(C3CC3)c3ccccc32)CC1 10.1021/jm981098j
162658420 187879 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 539 12 2 8 3.6 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1OC 10.1016/j.ejmech.2016.05.048
CHEMBL4760149 187879 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 539 12 2 8 3.6 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1OC 10.1016/j.ejmech.2016.05.048
118734514 125448 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 406 8 1 4 5.6 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCC2CCCCC2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3416999 125448 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 406 8 1 4 5.6 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCC2CCCCC2)CC1 10.1021/acs.jmedchem.5b00115
44323264 213891 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 322 2 1 5 2.1 Nc1c(Cl)cc(C(=O)O[C@@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL92100 213891 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 322 2 1 5 2.1 Nc1c(Cl)cc(C(=O)O[C@@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
235 9342 42 None -4 3 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
5311299 9342 42 None -4 3 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
CHEMBL286136 9342 42 None -4 3 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells
ChEMBL 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10.1021/jm0009538
44592281 196197 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 341 5 0 5 4.1 C=CCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL513254 196197 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 341 5 0 5 4.1 C=CCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
162675700 190240 0 None 16 2 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 650 10 3 7 4.7 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2cc(Br)c(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4799043 190240 0 None 16 2 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 minsDisplacement of [3H]-GR113808 from guinea pig brain 5HT4 receptor in presence of serotonin incubated for 30 mins
ChEMBL 650 10 3 7 4.7 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2cc(Br)c(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
44592144 185632 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 327 5 0 5 3.8 C=CCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL469575 185632 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 327 5 0 5 3.8 C=CCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
118734509 125445 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 364 7 1 4 4.4 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CCC2)CC1 10.1021/acs.jmedchem.5b00115
CHEMBL3416995 125445 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 364 7 1 4 4.4 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CC2CCC2)CC1 10.1021/acs.jmedchem.5b00115
151758 196115 4 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 278 5 1 4 2.7 COc1ccccc1NC(=O)OCCN1CCCCC1 10.1021/jm960853v
CHEMBL51251 196115 4 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 278 5 1 4 2.7 COc1ccccc1NC(=O)OCCN1CCCCC1 10.1021/jm960853v
10541689 108830 4 None - 1 Rat 7.1 pKi = 7.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 292 6 1 4 3.1 COc1ccccc1NC(=O)OCCCN1CCCCC1 10.1021/jm960853v
CHEMBL301967 108830 4 None - 1 Rat 7.1 pKi = 7.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
ChEMBL 292 6 1 4 3.1 COc1ccccc1NC(=O)OCCCN1CCCCC1 10.1021/jm960853v
107715 207724 22 None -165 20 Guinea pig 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 207724 22 None -165 20 Guinea pig 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 207724 22 None -165 20 Guinea pig 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
44299805 107861 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 324 3 1 5 2.6 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC1CN2C 10.1016/s0960-894x(01)00693-x
CHEMBL294894 107861 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated
ChEMBL 324 3 1 5 2.6 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC1CN2C 10.1016/s0960-894x(01)00693-x
44573 63767 1 None -1 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 297 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(C)CC1 10.1016/0960-894X(95)00115-A
CHEMBL164425 63767 1 None -1 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 297 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(C)CC1 10.1016/0960-894X(95)00115-A
44573 63767 1 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 297 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(C)CC1 10.1021/jm020270n
CHEMBL164425 63767 1 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 297 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(C)CC1 10.1021/jm020270n
119584 9373 102 None -1 6 Guinea pig 7.1 pKi = 7.1 Binding
Tested for affinity against 5-hydroxytryptamine 4 receptor in the myenteric plexus of the guinea pig ileum.Tested for affinity against 5-hydroxytryptamine 4 receptor in the myenteric plexus of the guinea pig ileum.
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1021/jm020099f
1848 9373 102 None -1 6 Guinea pig 7.1 pKi = 7.1 Binding
Tested for affinity against 5-hydroxytryptamine 4 receptor in the myenteric plexus of the guinea pig ileum.Tested for affinity against 5-hydroxytryptamine 4 receptor in the myenteric plexus of the guinea pig ileum.
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1021/jm020099f
242 9373 102 None -1 6 Guinea pig 7.1 pKi = 7.1 Binding
Tested for affinity against 5-hydroxytryptamine 4 receptor in the myenteric plexus of the guinea pig ileum.Tested for affinity against 5-hydroxytryptamine 4 receptor in the myenteric plexus of the guinea pig ileum.
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1021/jm020099f
CHEMBL60889 9373 102 None -1 6 Guinea pig 7.1 pKi = 7.1 Binding
Tested for affinity against 5-hydroxytryptamine 4 receptor in the myenteric plexus of the guinea pig ileum.Tested for affinity against 5-hydroxytryptamine 4 receptor in the myenteric plexus of the guinea pig ileum.
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1021/jm020099f
DB11675 9373 102 None -1 6 Guinea pig 7.1 pKi = 7.1 Binding
Tested for affinity against 5-hydroxytryptamine 4 receptor in the myenteric plexus of the guinea pig ileum.Tested for affinity against 5-hydroxytryptamine 4 receptor in the myenteric plexus of the guinea pig ileum.
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1021/jm020099f
49783416 24485 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 319 7 2 4 2.5 CCCCN1CCC(CNC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258559 24485 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 319 7 2 4 2.5 CCCCN1CCC(CNC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
12861897 83866 0 None -35 2 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 347 7 2 4 2.8 COc1cc(N)c(Cl)cc1C(=O)NCCN(C)Cc1ccccc1 10.1021/jm020270n
CHEMBL20748 83866 0 None -35 2 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
ChEMBL 347 7 2 4 2.8 COc1cc(N)c(Cl)cc1C(=O)NCCN(C)Cc1ccccc1 10.1021/jm020270n
10761897 214522 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 373 6 1 6 2.0 CCCN1CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL95808 214522 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 373 6 1 6 2.0 CCCN1CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
10761898 214422 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 373 5 1 6 2.0 CC(C)N1CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
CHEMBL95235 214422 0 None - 1 Guinea pig 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 373 5 1 6 2.0 CC(C)N1CCN(CCNC(=O)n2c(=O)n(C(C)C)c3ccccc32)CC1 10.1021/jm981098j
45276946 26130 0 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 339 4 0 5 3.6 C#CCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.ejmech.2010.07.052
CHEMBL1290804 26130 0 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
ChEMBL 339 4 0 5 3.6 C#CCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.ejmech.2010.07.052
44404961 139792 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 764 17 5 12 4.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
CHEMBL370227 139792 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 764 17 5 12 4.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3O)CC2)CC1 10.1021/jm050234z
11693471 142017 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 778 18 4 12 4.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCC(=O)NCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
CHEMBL372479 142017 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808Binding affinity for 5-HT4 receptor using [3H]GR-113808
ChEMBL 778 18 4 12 4.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCC(=O)NCC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1 10.1021/jm050234z
72698087 110765 0 None -81 3 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 407 5 0 4 5.0 Fc1cccc2c1nc(OCC1CCN(CCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
CHEMBL3093186 110765 0 None -81 3 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 407 5 0 4 5.0 Fc1cccc2c1nc(OCC1CCN(CCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
CHEMBL4164469 219999 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation countingDisplacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting
ChEMBL None None None COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)NCCCN(C)CCCNC(=O)NCc3cn(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)NC4CCN(CCOC(=O)c5cc(Cl)c(N)cc5OC)CC4)nn3)nn2)CC1 10.1039/C6MD00458J
10757373 56361 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 310 5 1 5 2.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC=CCC1 10.1021/jm960320m
CHEMBL156579 56361 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 310 5 1 5 2.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC=CCC1 10.1021/jm960320m
49783207 24350 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 362 7 1 6 3.2 CCCCN1CCC(COC(=O)c2ccc(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258109 24350 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor expressed in HEK293 cells
ChEMBL 362 7 1 6 3.2 CCCCN1CCC(COC(=O)c2ccc(NC)c3c2OCCO3)CC1 10.1021/jm100668r
11794824 24708 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cncnc2)CC1 10.1021/jm0009538
CHEMBL125926 24708 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cncnc2)CC1 10.1021/jm0009538
44371317 56837 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 338 5 1 5 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1C2CCCC1CC2 10.1021/jm960320m
CHEMBL156965 56837 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 338 5 1 5 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1C2CCCC1CC2 10.1021/jm960320m
183782 10171 20 None 1 14 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1021/acs.jmedchem.5b00115
237 10171 20 None 1 14 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1021/acs.jmedchem.5b00115
CHEMBL85251 10171 20 None 1 14 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assayDisplacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1021/acs.jmedchem.5b00115
183782 10171 20 None -1 14 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2018.10.064
237 10171 20 None -1 14 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2018.10.064
CHEMBL85251 10171 20 None -1 14 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.ejmech.2018.10.064
10584 8245 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.ejmech.2018.10.064
86582973 8245 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.ejmech.2018.10.064
CHEMBL3417009 8245 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 minsDisplacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
ChEMBL 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 10.1016/j.ejmech.2018.10.064
44592188 196038 0 None - 1 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 4 0 5 4.0 CCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL511794 196038 0 None - 1 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane
ChEMBL 329 4 0 5 4.0 CCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
9927789 118279 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 337 5 2 4 2.5 Nc1c(Cl)cc(C(=O)NCCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL327798 118279 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 337 5 2 4 2.5 Nc1c(Cl)cc(C(=O)NCCCN2CCCCC2)c2c1CCO2 10.1016/0960-894X(96)00002-9
10526438 24067 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 425 6 1 8 2.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cnc(Cl)nc2)CC1 10.1021/jm0009538
CHEMBL125716 24067 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
ChEMBL 425 6 1 8 2.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cnc(Cl)nc2)CC1 10.1021/jm0009538
1782 9296 84 None -11 23 Rat 6.1 pKi = 6.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(96)00002-9
241 9296 84 None -11 23 Rat 6.1 pKi = 6.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(96)00002-9
4168 9296 84 None -11 23 Rat 6.1 pKi = 6.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(96)00002-9
CHEMBL86 9296 84 None -11 23 Rat 6.1 pKi = 6.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(96)00002-9
DB01233 9296 84 None -11 23 Rat 6.1 pKi = 6.1 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(96)00002-9
10688893 215166 0 None -1 2 Guinea pig 7.0 pKi = 7.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 345 4 1 6 1.2 CC(C)n1c(=O)n(C(=O)NCCN2CCN(C)CC2)c2ccccc21 10.1021/jm981098j
CHEMBL99591 215166 0 None -1 2 Guinea pig 7.0 pKi = 7.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
ChEMBL 345 4 1 6 1.2 CC(C)n1c(=O)n(C(=O)NCCN2CCN(C)CC2)c2ccccc21 10.1021/jm981098j
10828800 106965 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
CHEMBL288199 106965 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1016/S0960-894X(01)80508-4
10828800 106965 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1021/jm960320m
CHEMBL288199 106965 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
ChEMBL 310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2 10.1021/jm960320m
72698086 110764 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 375 5 0 4 4.3 Fc1cccc2c1nc(OCC1CCN(CC(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
CHEMBL3093185 110764 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
ChEMBL 375 5 0 4 4.3 Fc1cccc2c1nc(OCC1CCN(CC(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
75201901 173204 19 None -676 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]GR113808 from recombinant human 5HT4 receptor stably expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]GR113808 from recombinant human 5HT4 receptor stably expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 173204 19 None -676 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]GR113808 from recombinant human 5HT4 receptor stably expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]GR113808 from recombinant human 5HT4 receptor stably expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
136118647 83095 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 240 1 3 2 1.2 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058702 83095 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]GR113808 from human recombinant 5HT4 receptorDisplacement of [3H]GR113808 from human recombinant 5HT4 receptor
ChEMBL 240 1 3 2 1.2 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
44323245 113801 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 322 2 1 5 2.1 Nc1c(Cl)cc(C(=O)O[C@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
CHEMBL315443 113801 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
ChEMBL 322 2 1 5 2.1 Nc1c(Cl)cc(C(=O)O[C@H]2CN3CCC2CC3)c2c1CCO2 10.1016/0960-894X(96)00002-9
10930618 113816 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 729 19 2 9 5.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
CHEMBL315526 113816 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
ChEMBL 729 19 2 9 5.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(C(=O)CCCCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm0307887
6918107 84921 16 None -1 5 Rat 6.0 pKi = 6.0 Binding
The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.
ChEMBL 319 2 0 4 3.5 Cc1nccn1C[C@H]1CCc2c(c3cccc4c3n2CCC4)C1=O 10.1021/jm00075a026
CHEMBL2103778 84921 16 None -1 5 Rat 6.0 pKi = 6.0 Binding
The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.
ChEMBL 319 2 0 4 3.5 Cc1nccn1C[C@H]1CCc2c(c3cccc4c3n2CCC4)C1=O 10.1021/jm00075a026
1782 9296 84 None -11 23 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(95)00115-A
241 9296 84 None -11 23 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(95)00115-A
4168 9296 84 None -11 23 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(95)00115-A
CHEMBL86 9296 84 None -11 23 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(95)00115-A
DB01233 9296 84 None -11 23 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/0960-894X(95)00115-A
1782 9296 84 None -11 23 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80508-4
241 9296 84 None -11 23 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80508-4
4168 9296 84 None -11 23 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80508-4
CHEMBL86 9296 84 None -11 23 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80508-4
DB01233 9296 84 None -11 23 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1016/S0960-894X(01)80508-4
90666001 116062 0 None - 1 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 395 5 0 5 5.0 Fc1ccc(CN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1039/C2MD20063E
CHEMBL3218873 116062 0 None - 1 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's methodDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor by Grossman's method
ChEMBL 395 5 0 5 5.0 Fc1ccc(CN2CCC(COc3nc4ccsc4n4cccc34)CC2)cc1 10.1039/C2MD20063E
5 6927 72 None -117 53 Rat 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8813606
5202 6927 72 None -117 53 Rat 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8813606
CHEMBL39 6927 72 None -117 53 Rat 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8813606
DB08839 6927 72 None -117 53 Rat 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8813606
5 6927 72 None -288 53 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10646498
5202 6927 72 None -288 53 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10646498
CHEMBL39 6927 72 None -288 53 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10646498
DB08839 6927 72 None -288 53 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10646498
236 10170 0 None -4 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
239 10170 0 None -4 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
5311417 10170 0 None -4 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
CHEMBL1908857 10170 0 None -4 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
236 10170 0 None 4 2 Guinea pig 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
239 10170 0 None 4 2 Guinea pig 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
5311417 10170 0 None 4 2 Guinea pig 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
CHEMBL1908857 10170 0 None 4 2 Guinea pig 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
121881 10263 27 3H-GR-113808 2 15 Guinea pig 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
256 10263 27 3H-GR-113808 2 15 Guinea pig 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
CHEMBL68131 10263 27 3H-GR-113808 2 15 Guinea pig 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
119376 8622 48 3H-GR-113808 -1 27 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
119376 8622 48 3H-GR-113808 -2 27 Rat 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 -1 27 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 -2 27 Rat 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 -1 27 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 -2 27 Rat 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
119376 8622 48 3H-GR-113808 -2 27 Rat 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 -2 27 Rat 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 -2 27 Rat 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
119376 8622 48 3H-GR-113808 1 27 Guinea pig 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 1 27 Guinea pig 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 1 27 Guinea pig 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
121881 10263 27 3H-GR-113808 2 15 Guinea pig 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
256 10263 27 3H-GR-113808 2 15 Guinea pig 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
CHEMBL68131 10263 27 3H-GR-113808 2 15 Guinea pig 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
119376 8622 48 3H-GR-113808 -1 27 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 -1 27 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 -1 27 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
121881 10263 27 3H-GR-113808 -2 15 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
256 10263 27 3H-GR-113808 -2 15 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
CHEMBL68131 10263 27 3H-GR-113808 -2 15 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
119376 8622 48 3H-GR-113808 -1 27 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 -1 27 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 -1 27 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
119376 8622 48 3H-GR-113808 -1 27 Mouse 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 -1 27 Mouse 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 -1 27 Mouse 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
119376 8622 48 3H-GR-113808 1 27 Guinea pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
119376 8622 48 3H-GR-113808 -1 27 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 1 27 Guinea pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 -1 27 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 1 27 Guinea pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 -1 27 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
119376 8622 48 3H-GR-113808 1 27 Guinea pig 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
119376 8622 48 3H-GR-113808 -1 27 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 1 27 Guinea pig 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 -1 27 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 1 27 Guinea pig 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 -1 27 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
121881 10263 27 3H-RS 57639 -27 15 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
256 10263 27 3H-RS 57639 -27 15 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
CHEMBL68131 10263 27 3H-RS 57639 -27 15 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
119376 8622 48 3H-GR-113808 1 27 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 1 27 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 1 27 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
121881 10263 27 3H-GR-113808 -27 15 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
256 10263 27 3H-GR-113808 -27 15 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
CHEMBL68131 10263 27 3H-GR-113808 -27 15 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
121881 10263 27 3H-5HT -27 15 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
256 10263 27 3H-5HT -27 15 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
CHEMBL68131 10263 27 3H-5HT -27 15 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
None 222806 0 3H-GR-113808 251 13 Guinea pig 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 453 9 2 6 2.6 COC1=CC(=C(C=C1C(=O)CCC2CCN(CC2)CCNS(=O)(=O)C)Cl)N.Cl None
119376 8622 48 3H-GR-113808 -2 27 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-GR-113808 -2 27 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-GR-113808 -2 27 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
183782 10171 20 3H-GR-113808 1 14 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
237 10171 20 3H-GR-113808 1 14 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL85251 10171 20 3H-GR-113808 1 14 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
240 7731 43 3H-5HT -8 25 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-5HT -8 25 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-5HT -8 25 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-5HT -8 25 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-5HT -8 25 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-5HT -8 25 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-5HT -8 25 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
None 222790 0 3H-GR-113808 1 6 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
108182 10903 22 3H-5HT -1 17 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-5HT -1 17 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-5HT -1 17 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
57174031 222719 0 3H-5HT -33 20 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
3035240 222757 0 3H-GR-113808 -1 5 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
1809 6922 32 3H-5HT -46773 37 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 6922 32 3H-GR-113808 -46773 37 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -46773 37 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-113808 -46773 37 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -46773 37 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-113808 -46773 37 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
107 6929 121 3H-GR-113808 -389 31 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -389 31 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -389 31 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1220 6975 55 3H-GR-113808 -2511 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-GR-113808 -2511 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-GR-113808 -2511 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-GR-113808 -2511 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
202 8290 77 UNDEFINED -9 33 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 8290 77 UNDEFINED -9 33 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 8290 77 UNDEFINED -9 33 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 8290 77 UNDEFINED -9 33 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 8290 77 UNDEFINED -9 33 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
1524 8962 96 3H-GR-113808 -758 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-GR-113808 -758 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-GR-113808 -758 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-GR-113808 -758 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-GR-113808 -758 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-GR-113808 -758 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1621 9207 17 3H-GR-113808 -3235 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 9207 17 3H-GR-113808 -3235 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 9207 17 3H-GR-113808 -3235 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 9207 17 3H-GR-113808 -3235 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 9207 17 3H-GR-113808 -3235 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2543 10479 68 3H-GR-113808 -281 32 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-GR-113808 -281 32 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-GR-113808 -281 32 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-GR-113808 -281 32 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-GR-113808 -281 32 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
108182 10903 22 3H-GR-113808 -1 17 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
108182 10903 22 3H-RS 57639 -1 17 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 -1 17 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-RS 57639 -1 17 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 -1 17 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-RS 57639 -1 17 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
5656 209845 87 UNDEFINED -7 43 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 209845 87 UNDEFINED -7 43 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
54841 209906 52 UNDEFINED -1 30 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 209906 52 UNDEFINED -1 30 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
None 223158 0 UNDEFINED -1122 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 243 3 1 4 2.7 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N None
None 223859 0 UNDEFINED - 1 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 394 5 1 4 5.1 CC1=CC(=C(C=C1)OC)NC(=O)OC2CC3CCCC(C2)N3CC4=CC=CC=C4 None
1809 6922 32 3H-GR-113808 -87096 37 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 6922 32 3H-GR-113808 -109647 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 6922 32 3H-GR-113808 -109647 37 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 6922 32 3H-GR-113808 -46773 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-113808 -87096 37 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-113808 -109647 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-113808 -109647 37 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-113808 -46773 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-113808 -87096 37 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-113808 -109647 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-113808 -109647 37 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-113808 -46773 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1220 6975 55 3H-GR-113808 -2511 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-GR-113808 -2511 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-GR-113808 -2511 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-GR-113808 -2511 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
179 7188 115 3H-GR-113808 -4365 50 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 3H-GR-113808 -4365 50 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 3H-GR-113808 -4365 50 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 3H-GR-113808 -4365 50 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 3H-GR-113808 -4365 50 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2477 7532 59 3H-GR-113808 -1548 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 7532 59 3H-GR-113808 -1548 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 7532 59 3H-GR-113808 -1548 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 7532 59 3H-GR-113808 -1548 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 7532 59 3H-GR-113808 -1548 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
135398737 7745 93 3H-GR-113808 -4168 90 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-GR-113808 -4168 90 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-GR-113808 -4168 90 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-GR-113808 -4168 90 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-GR-113808 -4168 90 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
107780 8625 54 3H-5HT -10715 18 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 3H-5HT -10715 18 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 3H-5HT -10715 18 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
1353 8692 93 3H-GR-113808 -6918 85 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-GR-113808 -6918 85 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-GR-113808 -6918 85 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-GR-113808 -6918 85 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-GR-113808 -6918 85 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2402 10143 62 3H-GR-113808 -549 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 10143 62 3H-GR-113808 -549 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 10143 62 3H-GR-113808 -549 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 10143 62 3H-GR-113808 -549 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 10143 62 3H-GR-113808 -549 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
1150 10650 121 3H-5HT -436 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 10650 121 3H-5HT -436 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 10650 121 3H-5HT -436 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 10650 121 3H-5HT -436 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
44208932 147485 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 147485 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
None 223101 0 3H-GR-113808 -331 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 390 4 1 4 3.2 C1CN(CCN1CCN2C3=CC=CC=C3NC2=O)C4=CC=C(C=C4)C(F)(F)F None
None 223229 0 Functional -660 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 223229 0 UNDEFINED -660 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
108182 10903 22 3H-GR-113808 1 17 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 1 17 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 1 17 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
107 6929 121 3H-5HT -257 31 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-5HT -257 31 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-5HT -257 31 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
3035240 222757 0 3H-GR-113808 1 5 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
4595 183494 106 3H-GR113808 -3 14 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 183494 106 3H-GR113808 -3 14 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
240 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
107 6929 121 3H-GR-113808 -257 31 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -257 31 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -257 31 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
5 6927 72 3H-GR-113808 -288 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 3H-GR-113808 -117 53 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -288 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -117 53 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -288 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -117 53 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -288 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -117 53 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
240 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-GR-113808 -8 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
108182 10903 22 3H-5HT -1 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-5HT -1 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-5HT -1 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
3035240 222757 0 3H-GR-113808 -1 5 Guinea pig 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
108182 10903 22 3H-GR-113808 -1 17 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
108182 10903 22 3H-RS 57639 -1 17 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 -1 17 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-RS 57639 -1 17 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 -1 17 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-RS 57639 -1 17 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
130946 209537 2 UNDEFINED - 1 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 328 2 1 5 2.0 CCn1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 None
CHEMBL62023 209537 2 UNDEFINED - 1 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 328 2 1 5 2.0 CCn1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21 None
3035240 222757 0 3H-GR-113808 -1 5 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
108182 10903 22 3H-5HT -1 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-5HT -1 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-5HT -1 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
5 6927 72 3H-GR-113808 -117 53 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -117 53 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -117 53 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -117 53 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
152 7152 29 3H-GR-113808 -89 19 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 7152 29 3H-GR-113808 -89 19 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 7152 29 3H-GR-113808 -89 19 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
107 6929 121 3H-GR-113808 -389 31 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -389 31 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -389 31 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
5 6927 72 3H-GR-113808 -117 53 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -117 53 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -117 53 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -117 53 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
240 7731 43 3H-GR-113808 -11 25 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
240 7731 43 3H-RS 57639 -8 25 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-GR-113808 -11 25 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-RS 57639 -8 25 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-GR-113808 -11 25 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-RS 57639 -8 25 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-GR-113808 -11 25 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-RS 57639 -8 25 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-GR-113808 -11 25 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-RS 57639 -8 25 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-GR-113808 -11 25 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-RS 57639 -8 25 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-GR-113808 -11 25 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-RS 57639 -8 25 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
108182 10903 22 3H-GR-113808 -1 17 Guinea pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 -1 17 Guinea pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 -1 17 Guinea pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
57174031 222719 0 3H-GR-113808 -8 20 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
None 222790 0 3H-RS 57639 -2 6 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
152 7152 29 3H-GR-113808 -208 19 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 7152 29 3H-GR-113808 -208 19 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 7152 29 3H-GR-113808 -208 19 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
57174031 222719 0 3H-5HT -33 20 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
3035240 222757 0 3H-GR-113808 -2 5 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
None 222790 0 3H-GR-113808 1 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
108182 10903 22 3H-GR-113808 -1 17 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 -1 17 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 -1 17 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
258 10340 31 3H-5HT -2 8 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
258 10340 31 3H-GR-113808 -2 8 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
5191 10340 31 3H-5HT -2 8 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
5191 10340 31 3H-GR-113808 -2 8 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL287045 10340 31 3H-5HT -2 8 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL287045 10340 31 3H-GR-113808 -2 8 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
108182 10903 22 3H-GR-113808 1 17 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 1 17 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 1 17 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
5 6927 72 3H-RS 57639 -117 53 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-RS 57639 -117 53 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-RS 57639 -117 53 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-RS 57639 -117 53 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
108182 10903 22 3H-GR-113808 -1 17 Guinea pig 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 -1 17 Guinea pig 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 -1 17 Guinea pig 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
57174031 222719 0 3H-GR-113808 -14 20 Guinea pig 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
57174031 222719 0 3H-GR-113808 -6 20 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
258 10340 31 3H-GR-113808 1 8 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
5191 10340 31 3H-GR-113808 1 8 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL287045 10340 31 3H-GR-113808 1 8 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
5 6927 72 3H-5HT -117 53 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -117 53 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -117 53 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -117 53 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
130 10273 47 35S-GTPGammaS -562 13 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 10273 47 35S-GTPGammaS -562 13 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 10273 47 35S-GTPGammaS -562 13 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
None 222790 0 3H-GR-113808 -2 6 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
None 222790 0 3H-ZACOPRIDE -2 6 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
108182 10903 22 3H-GR-113808 1 17 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 1 17 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 1 17 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
None 222752 0 3H-GR-113808 4 2 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 336 1 2 4 1.9 CN1C2CCC1CC(C2)NC(=O)N3C4=CC=CC=C4NC3=O.Cl None
107 6929 121 3H-GR-113808 -457 31 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -457 31 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -457 31 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
3035240 222757 0 3H-GR-113808 1 5 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
240 7731 43 3H-5HT -8 25 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-5HT -8 25 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-5HT -8 25 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-5HT -8 25 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-5HT -8 25 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-5HT -8 25 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-5HT -8 25 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
258 10340 31 3H-RS 57639 -2 8 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
5191 10340 31 3H-RS 57639 -2 8 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL287045 10340 31 3H-RS 57639 -2 8 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
3035240 222757 0 3H-5HT 1 5 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
None 222790 0 3H-GR-113808 -1 6 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
107 6929 121 3H-GR-113808 -549 31 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -549 31 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -549 31 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
108182 10903 22 3H-GR-113808 -1 17 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 -1 17 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 -1 17 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
57174031 222719 0 3H-GR-113808 -33 20 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
3035240 222757 0 3H-GR-113808 -2 5 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
3035240 222757 0 3H-GR-113808 1 5 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
3035240 222757 0 3H-RS 57639 1 5 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
None 222790 0 3H-GR-113808 -1 6 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
152 7152 29 3H-5HT -89 19 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 7152 29 3H-5HT -89 19 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 7152 29 3H-5HT -89 19 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
3035240 222757 0 3H-5HT 1 5 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
1267 10576 49 3H-GR-113808 -1174 27 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 10576 49 3H-GR-113808 -1174 27 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 10576 49 3H-GR-113808 -1174 27 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
108182 10903 22 3H-GR-113808 -2 17 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 -2 17 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 -2 17 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
240 7731 43 3H-GR113808 -11 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-GR113808 -11 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-GR113808 -11 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-GR113808 -11 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-GR113808 -11 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-GR113808 -11 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-GR113808 -11 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
119376 8622 48 3H-5HT -2 27 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-5HT -2 27 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-5HT -2 27 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
119376 8622 48 3H-RS 57639 -2 27 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-RS 57639 -2 27 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-RS 57639 -2 27 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
108182 10903 22 3H-GR-113808 1 17 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 1 17 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 1 17 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
240 7731 43 3H-GR-113808 -4 25 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-GR-113808 -4 25 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-GR-113808 -4 25 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-GR-113808 -4 25 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-GR-113808 -4 25 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-GR-113808 -4 25 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-GR-113808 -4 25 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
107 6929 121 3H-5HT -257 31 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-5HT -257 31 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-5HT -257 31 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
108182 10903 22 3H-5HT -1 17 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-5HT -1 17 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-5HT -1 17 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
5 6927 72 3H-GR-113808 -288 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -288 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -288 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -288 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107 6929 121 3H-GR-113808 -549 31 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 6929 121 3H-RS 57639 -257 31 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -549 31 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-RS 57639 -257 31 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -549 31 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-RS 57639 -257 31 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
108182 10903 22 3H-5HT -1 17 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-5HT -1 17 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-5HT -1 17 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
1809 6922 32 3H-5HT -46773 37 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 6922 32 3H-GR-113808 -46773 37 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -46773 37 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-113808 -46773 37 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -46773 37 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-113808 -46773 37 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
240 7731 43 3H-GR-113808 -5 25 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-GR-113808 -5 25 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-GR-113808 -5 25 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-GR-113808 -5 25 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-GR-113808 -5 25 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-GR-113808 -5 25 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-GR-113808 -5 25 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
5 6927 72 3H-GR-113808 -117 53 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -117 53 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -117 53 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -117 53 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 3H-GR-113808 -190 53 Guinea pig 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -190 53 Guinea pig 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -190 53 Guinea pig 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -190 53 Guinea pig 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107 6929 121 3H-5HT -257 31 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-5HT -257 31 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-5HT -257 31 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 6929 121 3H-GR-113808 -257 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -257 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -257 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1782 9296 84 3H-GR-113808 -25 23 Mouse 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 9296 84 3H-GR-113808 -25 23 Mouse 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 9296 84 3H-GR-113808 -25 23 Mouse 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 9296 84 3H-GR-113808 -25 23 Mouse 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 9296 84 3H-GR-113808 -25 23 Mouse 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
107 6929 121 3H-GR-113808 -257 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -257 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -257 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
235 9342 42 3H-GR-113808 -4 3 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl None
5311299 9342 42 3H-GR-113808 -4 3 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl None
CHEMBL286136 9342 42 3H-GR-113808 -4 3 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl None
None 222790 0 3H-GR-113808 -2 6 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
441383 27105 57 None -5 17 Guinea pig 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL1306 27105 57 None -5 17 Guinea pig 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
3397 212267 112 None 1 2 Guinea pig 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 None
CHEMBL806 212267 112 None 1 2 Guinea pig 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 None
31703 201496 63 None 1 3 Guinea pig 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 None
CHEMBL359744 201496 63 None 1 3 Guinea pig 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 None
CHEMBL53463 201496 63 None 1 3 Guinea pig 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 None
151537 169443 49 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 None
41867 169443 49 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 None
CHEMBL417 169443 49 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 None
5991 210698 72 None 2 5 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C None
CHEMBL691 210698 72 None 2 5 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C None
4595 183494 106 None -3 14 Rat 8.2 pKi = 8.2 Binding
The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.
Drug Central 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 183494 106 None -3 14 Rat 8.2 pKi = 8.2 Binding
The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.
Drug Central 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
5 6927 72 3H-GR-113808 -190 53 Guinea pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -190 53 Guinea pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -190 53 Guinea pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -190 53 Guinea pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107 6929 121 3H-GR-113808 -389 31 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 6929 121 3H-GR-113808 -257 31 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -389 31 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -257 31 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -389 31 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -257 31 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1782 9296 84 3H-GR-113808 -12 23 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 9296 84 3H-GR-113808 -12 23 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 9296 84 3H-GR-113808 -12 23 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 9296 84 3H-GR-113808 -12 23 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 9296 84 3H-GR-113808 -12 23 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
108182 10903 22 3H-GR-113808 -1 17 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 -1 17 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 -1 17 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
57174031 222719 0 3H-GR-113808 -33 20 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
57174031 222719 0 3H-RS 57639 -33 20 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
1809 6922 32 3H-RS 57639 -46773 37 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-RS 57639 -46773 37 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-RS 57639 -46773 37 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
None 222993 0 UNDEFINED -446 14 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 438 5 1 4 4.8 C1CC(CCC1CCN2CCC3=C(C2)C=CC(=C3)C#N)NC(=O)C4=CC=NC5=CC=CC=C45 None
240 7731 43 3H-GR-113808 -5 25 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-GR-113808 -5 25 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-GR-113808 -5 25 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-GR-113808 -5 25 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-GR-113808 -5 25 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-GR-113808 -5 25 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-GR-113808 -5 25 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
107 6929 121 3H-GR-113808 -457 31 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -457 31 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -457 31 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
2780 117306 36 3H-GR-113808 -41 10 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
CHEMBL325109 117306 36 3H-GR-113808 -41 10 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
None 223033 0 3H-GR-113808 -436 20 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
None 222790 0 3H-GR-113808 -1 6 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
57174031 222719 0 3H-Cyclic AMP -14 20 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
57174031 222719 0 3H-GR-113808 -33 20 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
5 6927 72 3H-GR-113808 -288 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 3H-GR-113808 -154 53 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -288 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -154 53 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -288 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -154 53 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -288 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -154 53 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1782 9296 84 None -25 23 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 9296 84 None -25 23 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 9296 84 None -25 23 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 9296 84 None -25 23 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 9296 84 None -25 23 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
1782 9296 84 None -11 23 Rat 8.2 pKi = 8.2 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 9296 84 None -11 23 Rat 8.2 pKi = 8.2 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 9296 84 None -11 23 Rat 8.2 pKi = 8.2 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 9296 84 None -11 23 Rat 8.2 pKi = 8.2 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 9296 84 None -11 23 Rat 8.2 pKi = 8.2 Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
107715 207724 22 None -165 20 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 207724 22 None -165 20 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 207724 22 None -165 20 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
3168 16034 92 None -93 22 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 16034 92 None -93 22 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
1782 9296 84 None -12 23 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 9296 84 None -12 23 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 9296 84 None -12 23 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 9296 84 None -12 23 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 9296 84 None -12 23 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
5 6927 72 3H-5HT -117 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -117 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -117 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -117 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
258 10340 31 3H-GR-113808 1 8 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
258 10340 31 3H-GR-113808 -1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
258 10340 31 3H-GR-113808 -1 8 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
5191 10340 31 3H-GR-113808 1 8 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
5191 10340 31 3H-GR-113808 -1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
5191 10340 31 3H-GR-113808 -1 8 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL287045 10340 31 3H-GR-113808 1 8 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL287045 10340 31 3H-GR-113808 -1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL287045 10340 31 3H-GR-113808 -1 8 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
133 9274 52 None -79 43 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 None -79 43 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 None -79 43 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 None -79 43 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 None -79 43 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
11954224 222732 0 None -93 59 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
2274 9947 58 None -17 31 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 None -17 31 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 None -17 31 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 None -17 31 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 None -17 31 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2585 7590 103 None -57 22 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 7590 103 None -57 22 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 7590 103 None -57 22 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 7590 103 None -57 22 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 7590 103 None -57 22 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
10531 8202 21 None -87 24 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 8202 21 None -87 24 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 8202 21 None -87 24 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 8202 21 None -87 24 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 8202 21 None -87 24 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
57174031 222719 0 None -6 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
57174031 222719 0 None -14 20 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluatedBinding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated
Drug Central 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
3157 8252 71 None -27 12 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
7170 8252 71 None -27 12 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
954 8252 71 None -27 12 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
CHEMBL707 8252 71 None -27 12 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
DB00590 8252 71 None -27 12 Guinea pig 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
119584 9373 102 None -1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
1848 9373 102 None -1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
242 9373 102 None -1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
CHEMBL60889 9373 102 None -1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
DB11675 9373 102 None -1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
2780 117306 36 None -20 10 Rat 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
CHEMBL325109 117306 36 None -20 10 Rat 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatumBinding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
2780 117306 36 None -20 10 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
CHEMBL325109 117306 36 None -20 10 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
240 7731 43 3H-GR-113808 -4 25 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
240 7731 43 3H-GR-113808 -11 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-GR-113808 -4 25 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-GR-113808 -11 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-GR-113808 -4 25 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-GR-113808 -11 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-GR-113808 -4 25 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-GR-113808 -11 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-GR-113808 -4 25 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-GR-113808 -11 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-GR-113808 -4 25 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-GR-113808 -11 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-GR-113808 -4 25 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-GR-113808 -11 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
57174031 222719 0 3H-GR-113808 -14 20 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
None 222790 0 3H-GR-113808 1 6 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
None 222790 0 3H-GR-113808 -2 6 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
107 6929 121 3H-GR-113808 -549 31 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-113808 -549 31 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-113808 -549 31 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1782 9296 84 3H-GR-113808 -12 23 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 9296 84 3H-GR-113808 -12 23 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 9296 84 3H-GR-113808 -12 23 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 9296 84 3H-GR-113808 -12 23 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 9296 84 3H-GR-113808 -12 23 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
1809 6922 32 3H-GR-113808 -87096 37 Guinea pig 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-113808 -87096 37 Guinea pig 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-113808 -87096 37 Guinea pig 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
57174031 222719 0 None -8 20 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
119584 9373 102 None -1 6 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
1848 9373 102 None -1 6 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
242 9373 102 None -1 6 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
CHEMBL60889 9373 102 None -1 6 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
DB11675 9373 102 None -1 6 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
57174031 222719 0 None -33 20 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptorDisplacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
Drug Central 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
240 7731 43 None -5 25 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 None -5 25 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 None -5 25 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 None -5 25 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 None -5 25 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 None -5 25 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 None -5 25 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
240 7731 43 None -11 25 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 None -11 25 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 None -11 25 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 None -11 25 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 None -11 25 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 None -11 25 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 None -11 25 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptorBinding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
258 10340 31 3H-GR-113808 -1 8 Mouse 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
5191 10340 31 3H-GR-113808 -1 8 Mouse 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL287045 10340 31 3H-GR-113808 -1 8 Mouse 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
240 7731 43 None -4 25 Guinea pig 8.1 pKi = 8.1 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 None -4 25 Guinea pig 8.1 pKi = 8.1 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 None -4 25 Guinea pig 8.1 pKi = 8.1 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 None -4 25 Guinea pig 8.1 pKi = 8.1 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 None -4 25 Guinea pig 8.1 pKi = 8.1 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 None -4 25 Guinea pig 8.1 pKi = 8.1 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 None -4 25 Guinea pig 8.1 pKi = 8.1 Binding
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptorInhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
5 6927 72 3H-5HT -117 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -117 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -117 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -117 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
258 10340 31 3H-GR-113808 1 8 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
5191 10340 31 3H-GR-113808 1 8 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL287045 10340 31 3H-GR-113808 1 8 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC None
5 6927 72 3H-GR-113808 -190 53 Guinea pig 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 3H-GR-113808 -154 53 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -190 53 Guinea pig 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-113808 -154 53 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -190 53 Guinea pig 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-113808 -154 53 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -190 53 Guinea pig 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-113808 -154 53 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
240 7731 43 3H-GR-113808 -8 25 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 3H-GR-113808 -8 25 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 3H-GR-113808 -8 25 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 3H-GR-113808 -8 25 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 3H-GR-113808 -8 25 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 3H-GR-113808 -8 25 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 3H-GR-113808 -8 25 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
None 222790 0 3H-5HT -2 6 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
108182 10903 22 3H-GR-113808 -1 17 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
108182 10903 22 3H-RS 57639 -1 17 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 -1 17 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-RS 57639 -1 17 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 -1 17 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-RS 57639 -1 17 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
240 7731 43 None -8 25 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 None -8 25 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 None -8 25 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 None -8 25 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 None -8 25 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 None -8 25 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 None -8 25 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
135526515 224504 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
Drug Central 301 7 4 3 2.8 CCCCCNC(=N)NN=CC1=CNC2=C1C=C(OC)C=C2 None
243 9976 91 None 12 34 Human 8.1 pKi = 8.1 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 9976 91 None 12 34 Human 8.1 pKi = 8.1 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 9976 91 None 12 34 Human 8.1 pKi = 8.1 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 9976 91 None 12 34 Human 8.1 pKi = 8.1 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 9976 91 None 12 34 Human 8.1 pKi = 8.1 Binding
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
108182 10903 22 3H-GR-113808 -1 17 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-GR-113808 -1 17 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-GR-113808 -1 17 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
57174031 222719 0 3H-GR-113808 -8 20 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
1782 9296 84 3H-GR-113808 -25 23 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 9296 84 3H-GR-113808 -25 23 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 9296 84 3H-GR-113808 -25 23 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 9296 84 3H-GR-113808 -25 23 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 9296 84 3H-GR-113808 -25 23 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
1809 6922 32 3H-GR-113808 -46773 37 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-113808 -46773 37 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-113808 -46773 37 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
3035240 222757 0 3H-GR-113808 -1 5 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 359 3 2 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N.Cl None
1809 6922 32 3H-GR-113808 -109647 37 Mouse 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-113808 -109647 37 Mouse 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-113808 -109647 37 Mouse 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
57174031 222719 0 3H-ZACOPRIDE -33 20 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
53354764 9838 34 None 1 2 Human 9.8 pKi = 9.8 Binding
Measured at the 5-HT<sub>4d</sub> receptor.Measured at the 5-HT<sub>4d</sub> receptor.
Guide to Pharmacology 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 22974325
9059 9838 34 None 1 2 Human 9.8 pKi = 9.8 Binding
Measured at the 5-HT<sub>4d</sub> receptor.Measured at the 5-HT<sub>4d</sub> receptor.
Guide to Pharmacology 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 22974325
CHEMBL2152922 9838 34 None 1 2 Human 9.8 pKi = 9.8 Binding
Measured at the 5-HT<sub>4d</sub> receptor.Measured at the 5-HT<sub>4d</sub> receptor.
Guide to Pharmacology 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 22974325
DB12675 9838 34 None 1 2 Human 9.8 pKi = 9.8 Binding
Measured at the 5-HT<sub>4d</sub> receptor.Measured at the 5-HT<sub>4d</sub> receptor.
Guide to Pharmacology 432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1 22974325
121881 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10646498
121881 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10683202
121881 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 11030734
121881 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 9349523
256 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10646498
256 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10683202
256 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 11030734
256 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 9349523
CHEMBL68131 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10646498
CHEMBL68131 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 10683202
CHEMBL68131 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 11030734
CHEMBL68131 10263 27 None -2 15 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 9349523
250 10159 8 None 2 13 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 15351779
250 10159 8 None 2 13 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 9351641
5311416 10159 8 None 2 13 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 15351779
5311416 10159 8 None 2 13 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 9351641
CHEMBL69733 10159 8 None 2 13 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 15351779
CHEMBL69733 10159 8 None 2 13 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 9351641
1782 9296 84 None -25 23 Mouse 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 8946946
241 9296 84 None -25 23 Mouse 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 8946946
4168 9296 84 None -25 23 Mouse 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 8946946
CHEMBL86 9296 84 None -25 23 Mouse 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 8946946
DB01233 9296 84 None -25 23 Mouse 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 8946946
240 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10646498
240 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10683202
240 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11030734
240 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11218067
240 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 7796807
240 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9349523
2769 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10646498
2769 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10683202
2769 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11030734
2769 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11218067
2769 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 7796807
2769 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9349523
44279790 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10646498
44279790 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10683202
44279790 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11030734
44279790 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11218067
44279790 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 7796807
44279790 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9349523
660 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10646498
660 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10683202
660 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11030734
660 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11218067
660 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 7796807
660 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9349523
CHEMBL1729 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10646498
CHEMBL1729 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10683202
CHEMBL1729 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11030734
CHEMBL1729 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11218067
CHEMBL1729 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 7796807
CHEMBL1729 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9349523
CHEMBL560739 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10646498
CHEMBL560739 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10683202
CHEMBL560739 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11030734
CHEMBL560739 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11218067
CHEMBL560739 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 7796807
CHEMBL560739 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9349523
DB00604 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10646498
DB00604 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10683202
DB00604 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11030734
DB00604 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 11218067
DB00604 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 7796807
DB00604 7731 43 None -11 25 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9349523
234 7448 0 None -1 3 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 2.6 CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)n1c(=O)n(c2c1cccc2)C(C)C 9351641
5311029 7448 0 None -1 3 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 2.6 CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)n1c(=O)n(c2c1cccc2)C(C)C 9351641
11842633 10753 21 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18415081
11842633 10753 21 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22959244
8425 10753 21 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18415081
8425 10753 21 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22959244
CHEMBL2087337 10753 21 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 18415081
CHEMBL2087337 10753 21 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 22959244
10584 8245 0 None 1 2 Guinea pig 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 25157130
86582973 8245 0 None 1 2 Guinea pig 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 25157130
CHEMBL3417009 8245 0 None 1 2 Guinea pig 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl 25157130
45275554 10085 0 None 6 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
8427 10085 0 None 6 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
CHEMBL3544975 10085 0 None 6 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
DB12798 10085 0 None 6 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
235 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10683202
235 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10821780
235 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 11030734
235 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 12801225
235 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 9603189
5311299 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10683202
5311299 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10821780
5311299 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 11030734
5311299 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 12801225
5311299 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 9603189
CHEMBL286136 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10683202
CHEMBL286136 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 10821780
CHEMBL286136 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 11030734
CHEMBL286136 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 12801225
CHEMBL286136 9342 42 None -4 3 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl 9603189
11961293 10541 19 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 23756062
8426 10541 19 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 23756062
CHEMBL2402904 10541 19 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 23756062
DB12725 10541 19 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C 23756062
119376 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10646498
119376 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 11030734
119376 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 11218067
119376 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 15351779
119376 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9349523
119376 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9351641
119376 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9603189
247 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10646498
247 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 11030734
247 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 11218067
247 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 15351779
247 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9349523
247 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9351641
247 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9603189
CHEMBL33884 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 10646498
CHEMBL33884 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 11030734
CHEMBL33884 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 11218067
CHEMBL33884 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 15351779
CHEMBL33884 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9349523
CHEMBL33884 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9351641
CHEMBL33884 8622 48 None -1 27 Human 9.8 pKi = 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9603189
257 10266 13 None -1 4 Human 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 11218067
5311423 10266 13 None -1 4 Human 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 11218067
CHEMBL114112 10266 13 None -1 4 Human 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N 11218067
248 8623 0 None -2 2 Human 10.3 pKi None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 8 2 6 1.7 COc1[nH]c2c(c1C(=O)OCC1CCN(CC1)CCNS(=O)(=O)C)cc(cc2)F 9349523
248 8623 0 None -2 2 Human 10.3 pKi None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 8 2 6 1.7 COc1[nH]c2c(c1C(=O)OCC1CCN(CC1)CCNS(=O)(=O)C)cc(cc2)F 9351641
4284721 8623 0 None -2 2 Human 10.3 pKi None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 8 2 6 1.7 COc1[nH]c2c(c1C(=O)OCC1CCN(CC1)CCNS(=O)(=O)C)cc(cc2)F 9349523
4284721 8623 0 None -2 2 Human 10.3 pKi None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 8 2 6 1.7 COc1[nH]c2c(c1C(=O)OCC1CCN(CC1)CCNS(=O)(=O)C)cc(cc2)F 9351641
CHEMBL471233 8623 0 None -2 2 Human 10.3 pKi None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 8 2 6 1.7 COc1[nH]c2c(c1C(=O)OCC1CCN(CC1)CCNS(=O)(=O)C)cc(cc2)F 9349523
CHEMBL471233 8623 0 None -2 2 Human 10.3 pKi None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 8 2 6 1.7 COc1[nH]c2c(c1C(=O)OCC1CCN(CC1)CCNS(=O)(=O)C)cc(cc2)F 9351641
248 8623 0 None 2 2 Mouse 10.6 pKi None 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 8 2 6 1.7 COc1[nH]c2c(c1C(=O)OCC1CCN(CC1)CCNS(=O)(=O)C)cc(cc2)F 8946946
4284721 8623 0 None 2 2 Mouse 10.6 pKi None 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 8 2 6 1.7 COc1[nH]c2c(c1C(=O)OCC1CCN(CC1)CCNS(=O)(=O)C)cc(cc2)F 8946946
CHEMBL471233 8623 0 None 2 2 Mouse 10.6 pKi None 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 8 2 6 1.7 COc1[nH]c2c(c1C(=O)OCC1CCN(CC1)CCNS(=O)(=O)C)cc(cc2)F 8946946
108182 10903 22 None -2 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 7796807
108182 10903 22 None -2 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 9351641
108182 10903 22 None -2 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 9603189
245 10903 22 None -2 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 7796807
245 10903 22 None -2 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 9351641
245 10903 22 None -2 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 9603189
CHEMBL18041 10903 22 None -2 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 7796807
CHEMBL18041 10903 22 None -2 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 9351641
CHEMBL18041 10903 22 None -2 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 9603189
152 7152 29 None -208 19 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15466450
152 7152 29 None -208 19 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 7796807
2107 7152 29 None -208 19 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15466450
2107 7152 29 None -208 19 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 7796807
CHEMBL275854 7152 29 None -208 19 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15466450
CHEMBL275854 7152 29 None -208 19 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 7796807
152 7152 29 None -89 19 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8813606
152 7152 29 None -89 19 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 9225293
2107 7152 29 None -89 19 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8813606
2107 7152 29 None -89 19 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 9225293
CHEMBL275854 7152 29 None -89 19 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8813606
CHEMBL275854 7152 29 None -89 19 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 9225293
107 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10646498
107 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10683202
107 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 11030734
107 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 11218067
107 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9349523
107 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9603189
1833 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10646498
1833 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10683202
1833 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 11030734
1833 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 11218067
1833 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9349523
1833 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9603189
CHEMBL8165 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10646498
CHEMBL8165 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10683202
CHEMBL8165 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 11030734
CHEMBL8165 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 11218067
CHEMBL8165 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9349523
CHEMBL8165 6929 121 None -389 31 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9603189
244 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 10683202
244 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 11030734
244 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 11218067
244 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 7796807
244 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 9351641
244 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 9603189
3086547 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 10683202
3086547 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 11030734
3086547 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 11218067
3086547 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 7796807
3086547 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 9351641
3086547 10087 0 None -5 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 9603189
108182 10903 22 None -1 17 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 8813606
108182 10903 22 None -1 17 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 9225293
245 10903 22 None -1 17 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 8813606
245 10903 22 None -1 17 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 9225293
CHEMBL18041 10903 22 None -1 17 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 8813606
CHEMBL18041 10903 22 None -1 17 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 9225293
5 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10646498
5 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10683202
5 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10821780
5 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11030734
5 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11218067
5 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15351779
5 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
5 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9349523
5 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9351641
5 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9603189
5202 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10646498
5202 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10683202
5202 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10821780
5202 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11030734
5202 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11218067
5202 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15351779
5202 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
5202 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9349523
5202 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9351641
5202 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9603189
CHEMBL39 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10646498
CHEMBL39 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10683202
CHEMBL39 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10821780
CHEMBL39 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11030734
CHEMBL39 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11218067
CHEMBL39 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15351779
CHEMBL39 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
CHEMBL39 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9349523
CHEMBL39 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9351641
CHEMBL39 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9603189
DB08839 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10646498
DB08839 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10683202
DB08839 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10821780
DB08839 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11030734
DB08839 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11218067
DB08839 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15351779
DB08839 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
DB08839 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9349523
DB08839 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9351641
DB08839 6927 72 None -288 53 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9603189
119584 9373 102 None -1 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10646498
1848 9373 102 None -1 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10646498
242 9373 102 None -1 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10646498
CHEMBL60889 9373 102 None -1 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10646498
DB11675 9373 102 None -1 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10646498
107 6929 121 None -457 31 Mouse 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8946946
1833 6929 121 None -457 31 Mouse 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8946946
CHEMBL8165 6929 121 None -457 31 Mouse 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8946946
260 10641 54 None -38 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 11218067
260 10641 54 None -38 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 9349523
2775 10641 54 None -38 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 11218067
2775 10641 54 None -38 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 9349523
656665 10641 54 None -38 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 11218067
656665 10641 54 None -38 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 9349523
CHEMBL56564 10641 54 None -38 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 11218067
CHEMBL56564 10641 54 None -38 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 9349523
DB11699 10641 54 None -38 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 11218067
DB11699 10641 54 None -38 6 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 9349523
108182 10903 22 None 1 17 Mouse 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 8946946
245 10903 22 None 1 17 Mouse 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 8946946
CHEMBL18041 10903 22 None 1 17 Mouse 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 8946946
260 10641 54 None -19 6 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 8813606
2775 10641 54 None -19 6 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 8813606
656665 10641 54 None -19 6 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 8813606
CHEMBL56564 10641 54 None -19 6 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 8813606
DB11699 10641 54 None -19 6 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 8813606
107 6929 121 None -257 31 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 7796807
107 6929 121 None -257 31 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8813606
107 6929 121 None -257 31 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9225293
1833 6929 121 None -257 31 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 7796807
1833 6929 121 None -257 31 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8813606
1833 6929 121 None -257 31 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9225293
CHEMBL8165 6929 121 None -257 31 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 7796807
CHEMBL8165 6929 121 None -257 31 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8813606
CHEMBL8165 6929 121 None -257 31 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9225293
244 10087 0 None -1 3 Mouse 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 8946946
3086547 10087 0 None -1 3 Mouse 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 8946946
244 10087 0 None 1 3 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 8813606
244 10087 0 None 1 3 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 9225293
3086547 10087 0 None 1 3 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 8813606
3086547 10087 0 None 1 3 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 2 4 2.1 COc1cc(N)c(cc1C(=O)N[C@H]1CCN2C[C@@H]1CCC2)Cl 9225293
260 10641 54 None -15 6 Mouse 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 8946946
2775 10641 54 None -15 6 Mouse 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 8946946
656665 10641 54 None -15 6 Mouse 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 8946946
CHEMBL56564 10641 54 None -15 6 Mouse 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 8946946
DB11699 10641 54 None -15 6 Mouse 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 8946946
5 6927 72 None -154 53 Mouse 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8946946
5202 6927 72 None -154 53 Mouse 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8946946
CHEMBL39 6927 72 None -154 53 Mouse 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8946946
DB08839 6927 72 None -154 53 Mouse 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8946946
129928 8111 0 None -5 2 Mouse 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 2 1 6 1.9 COc1ccc2c(c1)n(C(=O)OC1CC3CCC(C1)N3C)c(=O)[nH]2 8946946
246 8111 0 None -5 2 Mouse 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 2 1 6 1.9 COc1ccc2c(c1)n(C(=O)OC1CC3CCC(C1)N3C)c(=O)[nH]2 8946946
CHEMBL1194556 8111 0 None -5 2 Mouse 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 2 1 6 1.9 COc1ccc2c(c1)n(C(=O)OC1CC3CCC(C1)N3C)c(=O)[nH]2 8946946
233 7447 0 None -1 2 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 2 1 5 2.0 CCn1c(=O)n(c2c1cccc2)C(=O)NC1CC2CC[C@@H](C1)N2C 10683202
233 7447 0 None -1 2 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 2 1 5 2.0 CCn1c(=O)n(c2c1cccc2)C(=O)NC1CC2CC[C@@H](C1)N2C 11030734
233 7447 0 None -1 2 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 2 1 5 2.0 CCn1c(=O)n(c2c1cccc2)C(=O)NC1CC2CC[C@@H](C1)N2C 9603189
9929033 7447 0 None -1 2 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 2 1 5 2.0 CCn1c(=O)n(c2c1cccc2)C(=O)NC1CC2CC[C@@H](C1)N2C 10683202
9929033 7447 0 None -1 2 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 2 1 5 2.0 CCn1c(=O)n(c2c1cccc2)C(=O)NC1CC2CC[C@@H](C1)N2C 11030734
9929033 7447 0 None -1 2 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 2 1 5 2.0 CCn1c(=O)n(c2c1cccc2)C(=O)NC1CC2CC[C@@H](C1)N2C 9603189
240 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8813606
240 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9225293
2769 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8813606
2769 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9225293
44279790 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8813606
44279790 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9225293
660 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8813606
660 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9225293
CHEMBL1729 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8813606
CHEMBL1729 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9225293
CHEMBL560739 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8813606
CHEMBL560739 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9225293
DB00604 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8813606
DB00604 7731 43 None -8 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 9225293
234 7448 0 None -1 3 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 2.6 CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)n1c(=O)n(c2c1cccc2)C(C)C 8946946
5311029 7448 0 None -1 3 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 2.6 CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)n1c(=O)n(c2c1cccc2)C(C)C 8946946
5 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7796807
5 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8813606
5 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225293
5202 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7796807
5202 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8813606
5202 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225293
CHEMBL39 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7796807
CHEMBL39 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8813606
CHEMBL39 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225293
DB08839 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7796807
DB08839 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8813606
DB08839 6927 72 None -117 53 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225293
234 7448 0 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 2.6 CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)n1c(=O)n(c2c1cccc2)C(C)C 9225293
5311029 7448 0 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 2.6 CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)n1c(=O)n(c2c1cccc2)C(C)C 9225293
233 7447 0 None 1 2 Mouse 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 2 1 5 2.0 CCn1c(=O)n(c2c1cccc2)C(=O)NC1CC2CC[C@@H](C1)N2C 8946946
9929033 7447 0 None 1 2 Mouse 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 2 1 5 2.0 CCn1c(=O)n(c2c1cccc2)C(=O)NC1CC2CC[C@@H](C1)N2C 8946946
240 7731 43 None -5 25 Mouse 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8946946
2769 7731 43 None -5 25 Mouse 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8946946
44279790 7731 43 None -5 25 Mouse 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8946946
660 7731 43 None -5 25 Mouse 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8946946
CHEMBL1729 7731 43 None -5 25 Mouse 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8946946
CHEMBL560739 7731 43 None -5 25 Mouse 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8946946
DB00604 7731 43 None -5 25 Mouse 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 8946946
258 10340 31 None -2 8 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 9225293
5191 10340 31 None -2 8 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 9225293
CHEMBL287045 10340 31 None -2 8 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 9225293
243 9976 91 None 12 34 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10646498
243 9976 91 None 12 34 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 11438309
3052762 9976 91 None 12 34 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10646498
3052762 9976 91 None 12 34 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 11438309
3502 9976 91 None 12 34 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10646498
3502 9976 91 None 12 34 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 11438309
CHEMBL117287 9976 91 None 12 34 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10646498
CHEMBL117287 9976 91 None 12 34 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 11438309
DB06480 9976 91 None 12 34 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10646498
DB06480 9976 91 None 12 34 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 11438309
135409453 10545 41 None -2 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10646498
135409453 10545 41 None -2 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 15466450
226 10545 41 None -2 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10646498
226 10545 41 None -2 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 15466450
CHEMBL76370 10545 41 None -2 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10646498
CHEMBL76370 10545 41 None -2 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 15466450
129928 8111 0 None 5 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 2 1 6 1.9 COc1ccc2c(c1)n(C(=O)OC1CC3CCC(C1)N3C)c(=O)[nH]2 9351641
246 8111 0 None 5 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 2 1 6 1.9 COc1ccc2c(c1)n(C(=O)OC1CC3CCC(C1)N3C)c(=O)[nH]2 9351641
CHEMBL1194556 8111 0 None 5 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 2 1 6 1.9 COc1ccc2c(c1)n(C(=O)OC1CC3CCC(C1)N3C)c(=O)[nH]2 9351641
132337 10316 15 None 1 2 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 8946946
238 10316 15 None 1 2 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 8946946
CHEMBL34291 10316 15 None 1 2 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl 8946946
258 10340 31 None -1 8 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 7498967
5191 10340 31 None -1 8 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 7498967
CHEMBL287045 10340 31 None -1 8 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC 7498967
182593 10168 6 None 1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10683202
182593 10168 6 None 1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 11030734
182593 10168 6 None 1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 15351779
254 10168 6 None 1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10683202
254 10168 6 None 1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 11030734
254 10168 6 None 1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 15351779
CHEMBL83954 10168 6 None 1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 10683202
CHEMBL83954 10168 6 None 1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 11030734
CHEMBL83954 10168 6 None 1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl 15351779
183782 10171 20 None -1 14 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10683202
183782 10171 20 None -1 14 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 11030734
237 10171 20 None -1 14 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10683202
237 10171 20 None -1 14 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 11030734
CHEMBL85251 10171 20 None -1 14 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 10683202
CHEMBL85251 10171 20 None -1 14 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N 11030734
119376 8622 48 None -2 27 Rat 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9225293
247 8622 48 None -2 27 Rat 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9225293
CHEMBL33884 8622 48 None -2 27 Rat 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 9225293
236 10170 0 None -4 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
239 10170 0 None -4 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
5311417 10170 0 None -4 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
CHEMBL1908857 10170 0 None -4 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 7 4.2 COc1cc(N)c(cc1C(=O)OCC1CCN(CC1)CCCc1ccc2c(c1)OCCO2)Cl 9225293
255 10262 21 None -1 2 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 4 1 3 2.8 O=C(c1c[nH]c2c1cccc2)OCCN1CCCCC1 11218067
3272300 10262 21 None -1 2 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 4 1 3 2.8 O=C(c1c[nH]c2c1cccc2)OCCN1CCCCC1 11218067
CHEMBL1255781 10262 21 None -1 2 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 4 1 3 2.8 O=C(c1c[nH]c2c1cccc2)OCCN1CCCCC1 11218067
121881 10263 27 None -27 15 Rat 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 9225293
256 10263 27 None -27 15 Rat 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 9225293
CHEMBL68131 10263 27 None -27 15 Rat 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N 9225293
29 7579 0 None 1584 9 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
9805719 7579 0 None 1584 9 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
CHEMBL2027925 7579 0 None 1584 9 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
252 10115 3 None 1 2 Mouse 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 6 1 4 2.7 CCCCN1CCC(CC1)CNC(=O)c1cccc2c1OCCO2 11976337
44391713 10115 3 None 1 2 Mouse 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 6 1 4 2.7 CCCCN1CCC(CC1)CNC(=O)c1cccc2c1OCCO2 11976337
CHEMBL182590 10115 3 None 1 2 Mouse 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 6 1 4 2.7 CCCCN1CCC(CC1)CNC(=O)c1cccc2c1OCCO2 11976337
249 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10683202
249 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10821780
249 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 11030734
249 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 15466450
249 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 9603189
9905972 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10683202
9905972 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10821780
9905972 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 11030734
9905972 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 15466450
9905972 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 9603189
CHEMBL155917 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10683202
CHEMBL155917 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 10821780
CHEMBL155917 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 11030734
CHEMBL155917 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 15466450
CHEMBL155917 9343 4 None 1 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl 9603189
10404587 10163 5 None - 1 Mouse 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 6 0 5 3.1 CCCCN1CCC(CC1)COC(=O)c1cccc2c1OCCO2 11976337
251 10163 5 None - 1 Mouse 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 6 0 5 3.1 CCCCN1CCC(CC1)COC(=O)c1cccc2c1OCCO2 11976337
CHEMBL130040 10163 5 None - 1 Mouse 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 6 0 5 3.1 CCCCN1CCC(CC1)COC(=O)c1cccc2c1OCCO2 11976337
177336 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
177336 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
177336 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 9351641
225 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
225 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
225 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 9351641
CHEMBL356359 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
CHEMBL356359 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
CHEMBL356359 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 9351641
DB04873 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
DB04873 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
DB04873 9894 50 None 6 3 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 9351641
119376 8622 48 None -1 27 Mouse 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 8946946
247 8622 48 None -1 27 Mouse 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 8946946
CHEMBL33884 8622 48 None -1 27 Mouse 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C 8946946