Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL1258451 5ht4r_human Human No 9.8 EC50 = 0.2 Funct
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
320 8 1 5 3.1 CCCCN1CCC(CC1)COC(=O)C2=C(C=C(C=C2)N)OC
CHEMBL1258451 5ht4r_human Human No 9.8 EC50 = 0.2 Funct
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
320 8 1 5 3.1 CCCCN1CCC(CC1)COC(=O)C2=C(C=C(C=C2)N)OC
CHEMBL2152922 5ht4r_human Human Yes 9.7 EC50 = 0.2 Funct
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
433 7 1 8 2.4 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O
CHEMBL2152922 5ht4r_human Human Yes 9.6 EC50 = 0.3 Funct
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
433 7 1 8 2.4 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O
CHEMBL2152922 5ht4r_human Human Yes 9.6 EC50 = 0.3 Funct
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
433 7 1 8 2.4 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O
CHEMBL2152922 5ht4r_human Human Yes 9.4 EC50 = 0.4 Funct
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
433 7 1 8 2.4 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O
CHEMBL2179583 5ht4r_human Human No 9.4 EC50 = 0.4 Funct
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
449 5 2 6 2.3 CC(C)N1C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL2059588 5ht4r_human Human No 9.4 EC50 = 0.4 Funct
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
533 8 2 8 1.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL538635 5ht4r_human Human Yes 9.4 EC50 = 0.4 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL539713 5ht4r_human Human No 9.4 EC50 = 0.4 Funct
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
550 12 2 5 4.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCCC5C(=O)N
CHEMBL538635 5ht4r_human Human Yes 9.4 EC50 = 0.4 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL2402900 5ht4r_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
466 9 3 7 1.4 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC(CN(C)S(=O)(=O)C)O
CHEMBL2059588 5ht4r_human Human No 9.4 EC50 = 0.4 Funct
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
533 8 2 8 1.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL538635 5ht4r_human Human Yes 9.4 EC50 = 0.4 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL539713 5ht4r_human Human No 9.4 EC50 = 0.4 Funct
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
550 12 2 5 4.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCCC5C(=O)N
CHEMBL538635 5ht4r_human Human Yes 9.4 EC50 = 0.4 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL2179580 5ht4r_human Human No 9.4 EC50 = 0.4 Funct
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
447 7 2 8 2.6 C1CC(CC1O)OC2=CC=CC3=C2C(=NO3)OCC4CCN(CC4)CC5(CCOCC5)O
CHEMBL2152922 5ht4r_human Human Yes 9.3 EC50 = 0.5 Funct
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
433 7 1 8 2.4 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O
CHEMBL3741376 5ht4r_human Human Yes 9.3 EC50 = 0.5 Funct
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
431 5 2 5 2.2 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL3741376 5ht4r_human Human Yes 9.3 EC50 = 0.5 Funct
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
431 5 2 5 2.2 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL2402904 5ht4r_human Human Yes 9.3 EC50 = 0.5 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
456 7 2 5 3.4 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC4CCN(CC4)C(=O)OC
CHEMBL2152922 5ht4r_rat Rat Yes 9.2 EC50 = 0.6 Funct
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
433 7 1 8 2.4 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O
CHEMBL2152922 5ht4r_rat Rat Yes 9.2 EC50 = 0.6 Funct
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
433 7 1 8 2.4 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O
CHEMBL2087337 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
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
505 8 2 7 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)S(=O)(=O)C)O
CHEMBL2087337 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
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
505 8 2 7 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)S(=O)(=O)C)O
CHEMBL2059583 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
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
561 10 3 8 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCC(CC5)CNS(=O)(=O)C)O
CHEMBL2059583 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
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
561 10 3 8 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCC(CC5)CNS(=O)(=O)C)O
CHEMBL540981 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
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
628 14 2 7 4.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCC(CC5)CNS(=O)(=O)C
CHEMBL558163 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
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
582 12 2 4 6.2 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCN(C)CCC5=CNC6=CC=CC=C65
CHEMBL553404 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
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
616 16 1 7 4.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN(C)CCCN(C)S(=O)(=O)C
CHEMBL540981 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
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
628 14 2 7 4.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCC(CC5)CNS(=O)(=O)C
CHEMBL558163 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
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
582 12 2 4 6.2 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCN(C)CCC5=CNC6=CC=CC=C65
CHEMBL553404 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
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
616 16 1 7 4.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN(C)CCCN(C)S(=O)(=O)C
CHEMBL2402891 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
521 9 3 8 1.2 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC(CN4CCN(CC4)S(=O)(=O)C)O
CHEMBL2402892 5ht4r_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
519 9 3 8 0.6 CS(=O)(=O)N1CCN(CC1)CC(CN2CCC(CC2)CNC(=O)C3=C4C(=CC=C3)NC(=N4)C5CC5)O
CHEMBL2152922 5ht4r_rat Rat Yes 9.2 EC50 = 0.7 Funct
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
433 7 1 8 2.4 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O
CHEMBL2059585 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
533 8 2 8 1.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL2059582 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
510 12 1 5 5.0 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCCCCCN5CCCC5COC
CHEMBL2059587 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
533 8 2 8 1.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL552484 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
568 15 3 5 6.3 CN(CCCCCCCCN1CCC(CC1)NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCC3=CNC4=CC=CC=C43
CHEMBL551013 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
521 11 1 4 5.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCCCC5
CHEMBL555222 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
542 8 1 5 5.0 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCN(CC5)C6=CC=CC=C6
CHEMBL553405 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL2402894 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
543 9 3 10 0.9 CC(C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC(CN4CCN(CC4)S(=O)(=O)C)O)(F)F
CHEMBL2402897 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
491 8 2 7 1.8 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CCN4CCN(CC4)S(=O)(=O)C
CHEMBL2059585 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
533 8 2 8 1.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL2059582 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
510 12 1 5 5.0 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCCCCCN5CCCC5COC
CHEMBL2059587 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
533 8 2 8 1.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL552484 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
568 15 3 5 6.3 CN(CCCCCCCCN1CCC(CC1)NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCC3=CNC4=CC=CC=C43
CHEMBL551013 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
521 11 1 4 5.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCCCC5
CHEMBL555222 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
542 8 1 5 5.0 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCN(CC5)C6=CC=CC=C6
CHEMBL553405 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL2179582 5ht4r_human Human Yes 9.1 EC50 = 0.8 Funct
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
434 4 2 6 2.5 CC1(C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O)C
CHEMBL2179584 5ht4r_human Human No 9.1 EC50 = 0.8 Funct
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
358 8 0 5 4.9 CCCCN1CCC(CC1)COC2=NOC3=C2C(=CC=C3)OC4CCC4
CHEMBL2179583 5ht4r_human Human No 9.1 EC50 = 0.9 Funct
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
449 5 2 6 2.3 CC(C)N1C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL2179582 5ht4r_human Human Yes 9.1 EC50 = 0.9 Funct
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
434 4 2 6 2.5 CC1(C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O)C
CHEMBL2179583 5ht4r_rat Rat No 9.1 EC50 = 0.9 Funct
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
449 5 2 6 2.3 CC(C)N1C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL2179583 5ht4r_rat Rat No 9.0 EC50 = 1.0 Funct
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
449 5 2 6 2.3 CC(C)N1C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL2179589 5ht4r_human Human No 9.0 EC50 = 1.0 Funct
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
419 8 1 7 3.6 CC(C)COC1=CC=CC2=C1C(=NO2)OCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL2179583 5ht4r_human Human No 9.0 EC50 = 1.0 Funct
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
449 5 2 6 2.3 CC(C)N1C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL76370 5ht4r_human Human Yes 9.0 EC50 = 1 Funct
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
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL555223 5ht4r_human Human No 9.0 EC50 = 1 Funct
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
572 10 2 7 3.3 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCC(CC5)CNS(=O)(=O)C
CHEMBL558719 5ht4r_human Human No 9.0 EC50 = 1 Funct
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
493 9 1 4 5.0 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCN5CCCCC5
CHEMBL555210 5ht4r_human Human No 9.0 EC50 = 1 Funct
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
624 15 2 4 7.6 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCN(C)CCC5=CNC6=CC=CC=C65
CHEMBL76370 5ht4r_human Human Yes 9.0 EC50 = 1 Funct
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
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL555223 5ht4r_human Human No 9.0 EC50 = 1 Funct
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
572 10 2 7 3.3 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCC(CC5)CNS(=O)(=O)C
CHEMBL558719 5ht4r_human Human No 9.0 EC50 = 1 Funct
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
493 9 1 4 5.0 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCN5CCCCC5
CHEMBL555210 5ht4r_human Human No 9.0 EC50 = 1 Funct
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
624 15 2 4 7.6 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCN(C)CCC5=CNC6=CC=CC=C65
CHEMBL2402903 5ht4r_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
476 7 2 6 2.7 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC4CCN(CC4)S(=O)(=O)C
CHEMBL2402890 5ht4r_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
507 9 3 8 0.9 CCC1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC(CN4CCN(CC4)S(=O)(=O)C)O
CHEMBL2179586 5ht4r_human Human No 9.0 EC50 = 1.1 Funct
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
373 9 0 5 5.3 CCCCN1CCC(CC1)COC2=NOC3=C2C(=CC=C3)OCC4CCC4
CHEMBL2179582 5ht4r_rat Rat Yes 8.9 EC50 = 1.2 Funct
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
434 4 2 6 2.5 CC1(C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O)C
CHEMBL2179583 5ht4r_human Human No 8.9 EC50 = 1.2 Funct
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
449 5 2 6 2.3 CC(C)N1C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL2179585 5ht4r_human Human No 8.9 EC50 = 1.2 Funct
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
373 8 0 5 5.3 CCCCN1CCC(CC1)COC2=NOC3=C2C(=CC=C3)OC4CCCC4
CHEMBL2179587 5ht4r_human Human No 8.9 EC50 = 1.2 Funct
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
360 9 0 5 5.3 CCCCN1CCC(CC1)COC2=NOC3=C2C(=CC=C3)OCC(C)C
CHEMBL2179582 5ht4r_human Human Yes 8.9 EC50 = 1.2 Funct
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
434 4 2 6 2.5 CC1(C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O)C
CHEMBL541968 5ht4r_human Human No 8.9 EC50 = 1.3 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL541223 5ht4r_human Human No 8.9 EC50 = 1.3 Funct
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
540 9 2 4 5.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCN(C)CCC5=CNC6=CC=CC=C65
CHEMBL538706 5ht4r_human Human No 8.9 EC50 = 1.3 Funct
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
535 12 1 4 6.4 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCN5CCCCC5
CHEMBL561278 5ht4r_human Human No 8.9 EC50 = 1.3 Funct
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
526 12 3 5 4.9 CN(CCCCCN1CCC(CC1)NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCC3=CNC4=CC=CC=C43
CHEMBL553685 5ht4r_human Human No 8.9 EC50 = 1.3 Funct
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
572 10 1 7 3.2 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCN5CCN(CC5)S(=O)(=O)C
CHEMBL541968 5ht4r_human Human No 8.9 EC50 = 1.3 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL541223 5ht4r_human Human No 8.9 EC50 = 1.3 Funct
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
540 9 2 4 5.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCN(C)CCC5=CNC6=CC=CC=C65
CHEMBL538706 5ht4r_human Human No 8.9 EC50 = 1.3 Funct
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
535 12 1 4 6.4 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCN5CCCCC5
CHEMBL561278 5ht4r_human Human No 8.9 EC50 = 1.3 Funct
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
526 12 3 5 4.9 CN(CCCCCN1CCC(CC1)NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCC3=CNC4=CC=CC=C43
CHEMBL553685 5ht4r_human Human No 8.9 EC50 = 1.3 Funct
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
572 10 1 7 3.2 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCN5CCN(CC5)S(=O)(=O)C
CHEMBL3741376 5ht4r_human Human Yes 8.9 EC50 = 1.3 Funct
Agonist activity at 5-HT4D receptor (unknown origin)Agonist activity at 5-HT4D receptor (unknown origin)
431 5 2 5 2.2 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL2152922 5ht4r_human Human Yes 8.9 EC50 = 1.3 Funct
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
433 7 1 8 2.4 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O
CHEMBL3741376 5ht4r_human Human Yes 8.9 EC50 = 1.3 Funct
Agonist activity at 5-HT4D receptor (unknown origin)Agonist activity at 5-HT4D receptor (unknown origin)
431 5 2 5 2.2 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL2179582 5ht4r_human Human Yes 8.9 EC50 = 1.3 Funct
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
434 4 2 6 2.5 CC1(C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O)C
CHEMBL2152922 5ht4r_human Human Yes 8.9 EC50 = 1.3 Funct
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
433 7 1 8 2.4 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O
CHEMBL201621 5ht4r_rat Rat No 8.8 EC50 = 1.5 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
325 5 1 5 2.7 COC1=CC(=C(C=C1C(=O)OCC2CCN3C2CCC3)Cl)N
CHEMBL2402904 5ht4r_human Human Yes 8.8 EC50 = 1.5 Funct
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
456 7 2 5 3.4 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC4CCN(CC4)C(=O)OC
CHEMBL2152922 5ht4r_human Human Yes 8.8 EC50 = 1.5 Funct
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
433 7 1 8 2.4 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O
CHEMBL201621 5ht4r_rat Rat No 8.8 EC50 = 1.5 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
325 5 1 5 2.7 COC1=CC(=C(C=C1C(=O)OCC2CCN3C2CCC3)Cl)N
CHEMBL2402904 5ht4r_human Human Yes 8.8 EC50 = 1.5 Funct
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
456 7 2 5 3.4 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC4CCN(CC4)C(=O)OC
CHEMBL2179582 5ht4r_rat Rat Yes 8.8 EC50 = 1.5 Funct
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
434 4 2 6 2.5 CC1(C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O)C
CHEMBL2059584 5ht4r_human Human No 8.8 EC50 = 1.6 Funct
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
587 13 2 7 4.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCCCCCN5CCC(CC5)CNS(=O)(=O)C
CHEMBL2059584 5ht4r_human Human No 8.8 EC50 = 1.6 Funct
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
587 13 2 7 4.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCCCCCN5CCC(CC5)CNS(=O)(=O)C
CHEMBL549449 5ht4r_human Human No 8.8 EC50 = 1.6 Funct
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
544 8 1 7 2.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCN(CC5)S(=O)(=O)C
CHEMBL549449 5ht4r_human Human No 8.8 EC50 = 1.6 Funct
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
544 8 1 7 2.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCN(CC5)S(=O)(=O)C
CHEMBL2402898 5ht4r_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
471 8 2 6 2.4 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CCN4CCN(CC4)C(=O)OC
CHEMBL2401750 5ht4r_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
440 6 2 4 3.0 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC4CCN(CC4)C(=O)C
CHEMBL2402895 5ht4r_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
555 9 3 8 1.7 CS(=O)(=O)N1CCN(CC1)CC(CN2CCC(CC2)CNC(=O)C3=C4C(=CC=C3)NC(=N4)C5=CC=CC=C5)O
CHEMBL2402902 5ht4r_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
430 8 3 5 1.6 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC(CN(C)C(=O)C)O
CHEMBL2179583 5ht4r_rat Rat No 8.8 EC50 = 1.6 Funct
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
449 5 2 6 2.3 CC(C)N1C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O
CHEMBL2179590 5ht4r_human Human No 8.8 EC50 = 1.7 Funct
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
435 8 2 8 2.2 CC(C)(COC1=CC=CC2=C1C(=NO2)OCC3CCN(CC3)CC4(CCOCC4)O)O
CHEMBL315071 5ht4r_rat Rat No 8.7 EC50 = 1.9 Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
367 7 1 5 3.8 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL2179581 5ht4r_human Human No 8.7 EC50 = 1.9 Funct
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
447 7 1 8 2.7 C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOCC4)CC5(CCOCC5)O
CHEMBL2059577 5ht4r_human Human No 8.7 EC50 = 2.0 Funct
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
454 7 2 5 3.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCCCC5)O
CHEMBL2059577 5ht4r_human Human No 8.7 EC50 = 2.0 Funct
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
454 7 2 5 3.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCCCC5)O
CHEMBL561398 5ht4r_human Human No 8.7 EC50 = 2.0 Funct
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
465 7 1 4 4.3 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCCCC5
CHEMBL561398 5ht4r_human Human No 8.7 EC50 = 2.0 Funct
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
465 7 1 4 4.3 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCCCC5
CHEMBL538635 5ht4r_human Human Yes 8.7 EC50 = 2.0 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL76370 5ht4r_human Human Yes 8.7 EC50 = 2.0 Funct
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
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL538635 5ht4r_human Human Yes 8.7 EC50 = 2.0 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL76370 5ht4r_human Human Yes 8.7 EC50 = 2.0 Funct
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
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL2402901 5ht4r_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
446 9 3 6 2.0 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC(CN(C)C(=O)OC)O
CHEMBL538635 5ht4r_human Human Yes 8.7 EC50 = 2.0 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL538635 5ht4r_human Human Yes 8.7 EC50 = 2.0 Funct
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
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL1258338 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
441 8 1 6 4.2 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)NC)Br
CHEMBL2059590 5ht4r_cavpo Guinea pig No 8.0 EC50 = 10 Funct
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
467 6 1 5 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)C(=O)C
CHEMBL558259 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
451 6 1 4 3.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCN5CCCCC5
CHEMBL559050 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
560 12 1 7 3.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN(C)CCCN(C)S(=O)(=O)C
CHEMBL2059590 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
467 6 1 5 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)C(=O)C
CHEMBL3741608 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
399 6 1 4 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CCN(CC3)CC4CCOCC4
CHEMBL2087335 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
505 8 2 7 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)S(=O)(=O)C)O
CHEMBL2087333 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
485 8 2 6 2.3 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(=O)OC)O
CHEMBL2059590 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
467 6 1 5 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)C(=O)C
CHEMBL84398 5ht4r_human Human No 8.0 EC50 = 10 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
337 7 1 4 3.2 COC1=CC(=C(C=C1C(=O)CCC2CCN(CC2)CC=C)Cl)N
CHEMBL1258338 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
441 8 1 6 4.2 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)NC)Br
CHEMBL2059590 5ht4r_cavpo Guinea pig No 8.0 EC50 = 10 Funct
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
467 6 1 5 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)C(=O)C
CHEMBL558259 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
451 6 1 4 3.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCN5CCCCC5
CHEMBL559050 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
560 12 1 7 3.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN(C)CCCN(C)S(=O)(=O)C
CHEMBL2059590 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
467 6 1 5 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)C(=O)C
CHEMBL3741608 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
399 6 1 4 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CCN(CC3)CC4CCOCC4
CHEMBL2087335 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
505 8 2 7 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)S(=O)(=O)C)O
CHEMBL2087333 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
485 8 2 6 2.3 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(=O)OC)O
CHEMBL2059590 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
467 6 1 5 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)C(=O)C
CHEMBL2181171 5ht4r_human Human No 8.0 EC50 = 10 Funct
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
335 5 0 4 4.4 CCCN1CCC(CC1)COC2=NC3=CC=CC=C3C4=C2C=CC=N4
CHEMBL62023 5ht4r_rat Rat No 8.0 EC50 = 10 Funct
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
328 2 1 3 2.1 CCN1C2=CC=CC=C2N(C1=O)C(=O)NC3CC4CCC(C3)N4C
CHEMBL3759944 5ht4r_rat Rat No 7.0 EC50 = 100 Funct
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
495 7 2 6 2.9 CC(C)(C)C(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL551535 5ht4r_human Human No 7.0 EC50 = 100 Funct
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
327 4 2 3 2.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NCC3CCNCC3
CHEMBL556438 5ht4r_human Human No 7.0 EC50 = 100 Funct
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
310 3 3 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CC3CCC(C2)N3)Cl)N
CHEMBL563445 5ht4r_human Human No 7.0 EC50 = 100 Funct
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
395 6 2 5 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCN3CCCCC3)Cl)N
CHEMBL3759944 5ht4r_rat Rat No 7.0 EC50 = 100 Funct
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
495 7 2 6 2.9 CC(C)(C)C(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL551535 5ht4r_human Human No 7.0 EC50 = 100 Funct
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
327 4 2 3 2.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NCC3CCNCC3
CHEMBL556438 5ht4r_human Human No 7.0 EC50 = 100 Funct
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
310 3 3 4 2.6 COC1=CC(=C(C=C1C(=O)NC2CC3CCC(C2)N3)Cl)N
CHEMBL563445 5ht4r_human Human No 7.0 EC50 = 100 Funct
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
395 6 2 5 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCN3CCCCC3)Cl)N
CHEMBL1358628 5ht4r_cavpo Guinea pig Yes 7.0 EC50 = 100 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_cavpo Guinea pig Yes 7.0 EC50 = 100 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_cavpo Guinea pig Yes 7.0 EC50 = 100 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL50852 5ht4r_cavpo Guinea pig No 7.0 EC50 = 100 Funct
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.
342 6 2 5 2.7 COC1=C(C=C(C(=C1)N)Cl)NC(=O)OCCN2CCCCCC2
CHEMBL549998 5ht4r_human Human No 6.0 EC50 = 1000 Funct
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
476 12 3 7 0.8 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCCCCS(=O)(=O)O)Cl)N
CHEMBL549998 5ht4r_human Human No 6.0 EC50 = 1000 Funct
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
476 12 3 7 0.8 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCCCCS(=O)(=O)O)Cl)N
CHEMBL1358628 5ht4r_rat Rat Yes 7.0 EC50 = 102.3 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_rat Rat Yes 7.0 EC50 = 102.3 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_rat Rat Yes 7.0 EC50 = 102.3 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1358628 5ht4r_rat Rat Yes 7.0 EC50 = 102.3 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_rat Rat Yes 7.0 EC50 = 102.3 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_rat Rat Yes 7.0 EC50 = 102.3 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL3758945 5ht4r_rat Rat No 6.0 EC50 = 1047.1 Funct
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
453 7 2 6 1.5 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCC(=O)N3CCCCC3
CHEMBL3758945 5ht4r_rat Rat No 6.0 EC50 = 1047.1 Funct
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
453 7 2 6 1.5 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCC(=O)N3CCCCC3
CHEMBL3739689 5ht4r_human Human No 6.0 EC50 = 1061 Funct
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
383 5 1 4 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3C4C3CN(C4)CC5CCOCC5
CHEMBL3739689 5ht4r_human Human No 6.0 EC50 = 1061 Funct
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
383 5 1 4 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3C4C3CN(C4)CC5CCOCC5
CHEMBL3739862 5ht4r_human Human No 8.0 EC50 = 11 Funct
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
385 5 1 4 3.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CCN(CC3)C4CCOCC4
CHEMBL3739862 5ht4r_human Human No 8.0 EC50 = 11 Funct
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
385 5 1 4 3.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CCN(CC3)C4CCOCC4
CHEMBL92100 5ht4r_rat Rat No 8.0 EC50 = 11.1 Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
323 3 1 5 2.3 C1CN2CCC1C(C2)OC(=O)C3=CC(=C(C4=C3OCC4)N)Cl
CHEMBL3417009 5ht4r_human Human No 8.0 EC50 = 11.3 Funct
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
393 7 1 4 5.0 COC1=CC(=C(C=C1C(=O)CCC2CCN(CC2)CC3CCCCC3)Cl)N
CHEMBL3417009 5ht4r_human Human No 8.0 EC50 = 11.3 Funct
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
393 7 1 4 5.0 COC1=CC(=C(C=C1C(=O)CCC2CCN(CC2)CC3CCCCC3)Cl)N
CHEMBL34224 5ht4r_cavpo Guinea pig Yes 7.0 EC50 = 110 Funct
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
299 4 1 5 2.3 CN1CCC(CC1)OC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL41769 5ht4r_cavpo Guinea pig No 7.0 EC50 = 110 Funct
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
311 4 1 5 2.3 COC1=CC(=C(C=C1C(=O)OC2CN3CCC2CC3)Cl)N
CHEMBL41769 5ht4r_cavpo Guinea pig No 7.0 EC50 = 110 Funct
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
311 4 1 5 2.3 COC1=CC(=C(C=C1C(=O)OC2CN3CCC2CC3)Cl)N
CHEMBL15585 5ht4r_human Human No 6.0 EC50 = 1122.0 Funct
Tested for 5-hydroxytryptamine 4 binding affinity against zacoprideTested for 5-hydroxytryptamine 4 binding affinity against zacopride
352 3 2 4 3.1 CC1CCCC2N1CCC(C2)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL301039 5ht4r_human Human No 6.0 EC50 = 1122.0 Funct
Tested for 5-hydroxytryptamine 4 binding affinity against zacoprideTested for 5-hydroxytryptamine 4 binding affinity against zacopride
324 3 2 4 2.3 CN1C2CCC1CC(C2)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL157631 5ht4r_cavpo Guinea pig No 7.0 EC50 = 113 Funct
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
315 6 1 6 1.4 COC1=CC(=C(C=C1C(=O)OCCN2CCOCC2)Cl)N
CHEMBL114112 5ht4r_human Human Yes 7.9 EC50 = 12.6 Funct
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
474 7 1 6 3.5 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)N)I
CHEMBL2087337 5ht4r_cavpo Guinea pig No 7.9 EC50 = 12.6 Funct
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
505 8 2 7 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)S(=O)(=O)C)O
CHEMBL2059586 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
559 11 1 7 3.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCCCCCN5CCN(CC5)S(=O)(=O)C
CHEMBL556235 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
339 3 2 3 2.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4
CHEMBL559746 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
490 9 2 6 0.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCS(=O)(=O)O
CHEMBL558924 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
516 10 2 8 1.9 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCN3CCN(CC3)S(=O)(=O)C)Cl)N
CHEMBL2087328 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
470 7 4 5 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CNC(=O)NC)O
CHEMBL2087325 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
469 7 2 5 1.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(=O)C)O
CHEMBL28499 5ht4r_rat Rat No 7.9 EC50 = 12.6 Funct
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
356 1 1 4 2.7 C1CN2CCC1C(C2)N3C(=O)C4=CC=CC5=C4C(=CC(=C5N)Cl)C3=O
CHEMBL79637 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
339 7 1 4 3.5 CCCN1CCC(CC1)CCC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL114112 5ht4r_human Human Yes 7.9 EC50 = 12.6 Funct
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
474 7 1 6 3.5 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)N)I
CHEMBL2087337 5ht4r_cavpo Guinea pig No 7.9 EC50 = 12.6 Funct
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
505 8 2 7 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)S(=O)(=O)C)O
CHEMBL2059586 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
559 11 1 7 3.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCCCCCN5CCN(CC5)S(=O)(=O)C
CHEMBL556235 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
339 3 2 3 2.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4
CHEMBL559746 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
490 9 2 6 0.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCS(=O)(=O)O
CHEMBL558924 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
516 10 2 8 1.9 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCN3CCN(CC3)S(=O)(=O)C)Cl)N
CHEMBL2087328 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
470 7 4 5 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CNC(=O)NC)O
CHEMBL2087325 5ht4r_human Human No 7.9 EC50 = 12.6 Funct
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
469 7 2 5 1.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(=O)C)O
CHEMBL76370 5ht4r_cavpo Guinea pig Yes 7.9 EC50 = 12.6 Funct
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
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL59834 5ht4r_rat Rat No 7.9 EC50 = 12.6 Funct
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
342 2 1 3 2.5 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NC3CC4CCC(C3)N4C
CHEMBL571799 5ht4r_human Human No 6.9 EC50 = 120 Funct
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
532 8 3 7 3.6 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCCCC3(C4=CC(=CC=C4)OC)O
CHEMBL571799 5ht4r_human Human No 6.9 EC50 = 120 Funct
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
532 8 3 7 3.6 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCCCC3(C4=CC(=CC=C4)OC)O
CHEMBL310451 5ht4r_human Human No 6.9 EC50 = 125.9 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
326 6 2 4 3.1 COC1=CC(=C(C=C1C(=O)NCCCN2CCCCC2)Cl)N
CHEMBL82833 5ht4r_human Human No 6.9 EC50 = 125.9 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
297 5 2 4 2.1 COC1=CC(=C(C=C1C(=O)CCC2CCNCC2)Cl)N
CHEMBL15585 5ht4r_human Human No 6.9 EC50 = 125.9 Funct
Tested for 5-hydroxytryptamine 4 binding affinity against renzaprideTested for 5-hydroxytryptamine 4 binding affinity against renzapride
352 3 2 4 3.1 CC1CCCC2N1CCC(C2)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL301039 5ht4r_human Human No 6.9 EC50 = 125.9 Funct
Tested for 5-hydroxytryptamine 4 binding affinity against renzaprideTested for 5-hydroxytryptamine 4 binding affinity against renzapride
324 3 2 4 2.3 CN1C2CCC1CC(C2)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL156348 5ht4r_cavpo Guinea pig No 7.9 EC50 = 13 Funct
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
370 7 2 6 1.6 CC(=O)NC1CCN(CC1)CCOC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL3741224 5ht4r_human Human No 7.9 EC50 = 13.2 Funct
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
367 6 1 3 4.3 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC5CCC5
CHEMBL3741224 5ht4r_human Human No 7.9 EC50 = 13.2 Funct
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
367 6 1 3 4.3 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC5CCC5
CHEMBL3742086 5ht4r_human Human No 6.9 EC50 = 132 Funct
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
360 5 1 4 4.2 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC(C)(C)F
CHEMBL3742086 5ht4r_human Human No 6.9 EC50 = 132 Funct
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
360 5 1 4 4.2 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC(C)(C)F
CHEMBL3740278 5ht4r_human Human No 5.9 EC50 = 1358 Funct
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
417 6 1 5 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CC4CCOCC4)F
CHEMBL3740278 5ht4r_human Human No 5.9 EC50 = 1358 Funct
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
417 6 1 5 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CC4CCOCC4)F
CHEMBL347235 5ht4r_cavpo Guinea pig No 7.9 EC50 = 14 Funct
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
329 6 2 6 1.6 COC1=CC(=C(C=C1C(=O)OCCN2CCC(CC2)O)Cl)N
CHEMBL325494 5ht4r_human Human No 7.9 EC50 = 14 Funct
Compound was tested for 5-hydroxytryptamine 4 binding affinityCompound was tested for 5-hydroxytryptamine 4 binding affinity
350 4 2 4 2.4 C1CC2(CCCN2C1)CCNC(=O)C3=CC(=C(C4=C3OCC4)N)Cl
CHEMBL1258223 5ht4r_human Human No 7.9 EC50 = 14.1 Funct
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
397 8 1 6 4.1 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)NC)Cl
CHEMBL1258223 5ht4r_human Human No 7.9 EC50 = 14.1 Funct
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
397 8 1 6 4.1 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)NC)Cl
CHEMBL3742190 5ht4r_human Human No 6.8 EC50 = 144 Funct
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
344 6 1 4 3.1 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CCOC
CHEMBL3740708 5ht4r_human Human No 6.8 EC50 = 144 Funct
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
401 5 2 5 2.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC4(CCOCC4)O
CHEMBL3742190 5ht4r_human Human No 6.8 EC50 = 144 Funct
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
344 6 1 4 3.1 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CCOC
CHEMBL3740708 5ht4r_human Human No 6.8 EC50 = 144 Funct
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
401 5 2 5 2.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC4(CCOCC4)O
CHEMBL156349 5ht4r_cavpo Guinea pig No 7.8 EC50 = 15 Funct
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
327 6 1 5 3.0 CC1CCCN(C1)CCOC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL3741826 5ht4r_human Human No 7.8 EC50 = 15.5 Funct
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
354 5 1 3 4.5 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC4CCC4
CHEMBL3741826 5ht4r_human Human No 7.8 EC50 = 15.5 Funct
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
354 5 1 3 4.5 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC4CCC4
CHEMBL76370 5ht4r_human Human Yes 7.8 EC50 = 15.9 Funct
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL1258450 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
387 8 1 7 3.8 CCCCN1CCC(CC1)COC(=O)C2=C3C(=C(C(=C2)C#N)NC)OCCO3
CHEMBL551820 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
328 2 2 3 2.1 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NC3CC4CCC(C3)N4
CHEMBL560876 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
468 11 2 4 4.8 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCO
CHEMBL560940 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
316 3 2 3 2.2 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NCC3CCNCC3
CHEMBL552693 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
370 8 3 5 2.1 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCO)Cl)N
CHEMBL556595 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
484 9 3 5 3.8 CN(CCC1=CNC2=CC=CC=C21)CCN3CCC(CC3)NC(=O)C4=CC(=C(C=C4OC)N)Cl
CHEMBL555447 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
412 11 3 5 3.5 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCCCCO)Cl)N
CHEMBL76370 5ht4r_human Human Yes 7.8 EC50 = 15.9 Funct
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL82360 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
325 6 1 4 3.0 CCN1CCC(CC1)CCC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL1258450 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
387 8 1 7 3.8 CCCCN1CCC(CC1)COC(=O)C2=C3C(=C(C(=C2)C#N)NC)OCCO3
CHEMBL551820 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
328 2 2 3 2.1 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NC3CC4CCC(C3)N4
CHEMBL560876 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
468 11 2 4 4.8 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCO
CHEMBL560940 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
316 3 2 3 2.2 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NCC3CCNCC3
CHEMBL552693 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
370 8 3 5 2.1 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCO)Cl)N
CHEMBL556595 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
484 9 3 5 3.8 CN(CCC1=CNC2=CC=CC=C21)CCN3CCC(CC3)NC(=O)C4=CC(=C(C=C4OC)N)Cl
CHEMBL555447 5ht4r_human Human No 7.8 EC50 = 15.9 Funct
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
412 11 3 5 3.5 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCCCCO)Cl)N
CHEMBL288199 5ht4r_cavpo Guinea pig No 6.8 EC50 = 153 Funct
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
311 4 1 5 2.3 COC1=CC(=C(C=C1C(=O)OC2CN3CCC2CC3)Cl)N
CHEMBL288199 5ht4r_cavpo Guinea pig No 6.8 EC50 = 153 Funct
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
311 4 1 5 2.3 COC1=CC(=C(C=C1C(=O)OC2CN3CCC2CC3)Cl)N
CHEMBL3759348 5ht4r_rat Rat No 5.8 EC50 = 1548.8 Funct
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
467 7 2 6 2.0 CCC(=O)N1CCCC(C1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759348 5ht4r_rat Rat No 5.8 EC50 = 1548.8 Funct
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
467 7 2 6 2.0 CCC(=O)N1CCCC(C1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL551614 5ht4r_human Human No 6.8 EC50 = 158.5 Funct
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
313 3 2 3 1.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CCNCC3
CHEMBL551614 5ht4r_human Human No 6.8 EC50 = 158.5 Funct
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
313 3 2 3 1.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CCNCC3
CHEMBL560597 5ht4r_human Human No 5.8 EC50 = 1584.9 Funct
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
392 6 3 7 -1.7 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCS(=O)(=O)O)Cl)N
CHEMBL560597 5ht4r_human Human No 5.8 EC50 = 1584.9 Funct
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
392 6 3 7 -1.7 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCS(=O)(=O)O)Cl)N
CHEMBL34291 5ht4r_rat Rat Yes 7.8 EC50 = 16.5 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
324 4 2 4 2.1 COC1=CC(=C(C=C1C(=O)NCC2CCN3C2CCC3)Cl)N
CHEMBL34291 5ht4r_rat Rat Yes 7.8 EC50 = 16.5 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
324 4 2 4 2.1 COC1=CC(=C(C=C1C(=O)NCC2CCN3C2CCC3)Cl)N
CHEMBL67554 5ht4r_rat Rat No 5.8 EC50 = 1658 Funct
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
350 5 2 4 2.2 COC1=CC(=C(C=C1C(=O)NCCC23CC4CN(C2)CC4C3)Cl)N
CHEMBL27846 5ht4r_cavpo Guinea pig No 6.8 EC50 = 166 Funct
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
310 3 2 4 1.7 COC1=CC(=C(C=C1C(=O)NC2CN3CCC2CC3)Cl)N
CHEMBL3306918 5ht4r_human Human Yes 7.8 EC50 = 17 Funct
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
378 6 2 5 3.5 CC(C)N1C2=C(C=CS2)C(=C(C1=O)C(=O)NCCCN3CCCCC3)O
CHEMBL3306918 5ht4r_human Human Yes 7.8 EC50 = 17 Funct
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
378 6 2 5 3.5 CC(C)N1C2=C(C=CS2)C(=C(C1=O)C(=O)NCCCN3CCCCC3)O
CHEMBL155631 5ht4r_cavpo Guinea pig No 7.8 EC50 = 17 Funct
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
308 6 1 4 2.4 COC1=CC(=C(C=C1C(=O)OCC[N+]2=CC=CC=C2)Cl)N
CHEMBL3306918 5ht4r_human Human Yes 7.8 EC50 = 17 Funct
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
378 6 2 5 3.5 CC(C)N1C2=C(C=CS2)C(=C(C1=O)C(=O)NCCCN3CCCCC3)O
CHEMBL490852 5ht4r_human Human No 7.8 EC50 = 18 Funct
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
480 9 2 6 3.8 COC1=CC(=C(C=C1C(=O)OCCN2CCC(CC2)NC(=O)CC3=CC=CC=C3Cl)Cl)N
CHEMBL3741595 5ht4r_human Human No 7.8 EC50 = 18 Funct
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
372 6 1 4 3.9 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC(C)(C)F
CHEMBL3739931 5ht4r_human Human No 7.8 EC50 = 18 Funct
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
352 5 1 3 3.9 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)C5CCC5
CHEMBL490852 5ht4r_human Human No 7.8 EC50 = 18 Funct
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
480 9 2 6 3.8 COC1=CC(=C(C=C1C(=O)OCCN2CCC(CC2)NC(=O)CC3=CC=CC=C3Cl)Cl)N
CHEMBL3741595 5ht4r_human Human No 7.8 EC50 = 18 Funct
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
372 6 1 4 3.9 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC(C)(C)F
CHEMBL3739931 5ht4r_human Human No 7.8 EC50 = 18 Funct
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
352 5 1 3 3.9 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)C5CCC5
CHEMBL3740844 5ht4r_human Human No 7.7 EC50 = 18.3 Funct
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
340 5 1 3 3.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)C(C)C
CHEMBL3740844 5ht4r_human Human No 7.7 EC50 = 18.3 Funct
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
340 5 1 3 3.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)C(C)C
CHEMBL91147 5ht4r_rat Rat No 7.7 EC50 = 18.6 Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
322 2 2 4 1.8 C1CN2CCC1C(C2)NC(=O)C3=CC(=C(C4=C3OCC4)N)Cl
CHEMBL160705 5ht4r_cavpo Guinea pig No 6.8 EC50 = 180 Funct
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
273 6 1 5 1.7 CN(C)CCOC(=O)C1=CC(=C(C=C1OC)N)Cl
CHEMBL156554 5ht4r_cavpo Guinea pig No 7.7 EC50 = 19 Funct
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
356 7 2 6 1.1 COC1=CC(=C(C=C1C(=O)OCCN2CCC(CC2)C(=O)N)Cl)N
CHEMBL327798 5ht4r_rat Rat No 7.7 EC50 = 19.3 Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
338 5 2 4 2.4 C1CCN(CC1)CCCNC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL3741918 5ht4r_human Human No 7.7 EC50 = 19.8 Funct
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
399 8 1 4 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC(C)(C)COC
CHEMBL3741918 5ht4r_human Human No 7.7 EC50 = 19.8 Funct
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
399 8 1 4 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC(C)(C)COC
CHEMBL1258339 5ht4r_human Human No 7.7 EC50 = 20.0 Funct
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
488 8 1 6 4.2 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)NC)I
CHEMBL1358628 5ht4r_human Human Yes 7.7 EC50 = 20.0 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_human Human Yes 7.7 EC50 = 20.0 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_human Human Yes 7.7 EC50 = 20.0 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL550122 5ht4r_human Human No 7.7 EC50 = 20.0 Funct
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
532 12 2 6 2.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCS(=O)(=O)O
CHEMBL550530 5ht4r_human Human No 7.7 EC50 = 20.0 Funct
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
474 7 2 8 0.8 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCN3CCN(CC3)S(=O)(=O)C)Cl)N
CHEMBL2087331 5ht4r_human Human No 7.7 EC50 = 20.0 Funct
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
498 7 2 5 1.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(=O)N(C)C)O
CHEMBL2087327 5ht4r_human Human No 7.7 EC50 = 20.0 Funct
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
470 7 3 5 1.3 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(=O)N)O
CHEMBL34291 5ht4r_human Human Yes 7.7 EC50 = 20.0 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
324 4 2 4 2.1 COC1=CC(=C(C=C1C(=O)NCC2CCN3C2CCC3)Cl)N
CHEMBL1258339 5ht4r_human Human No 7.7 EC50 = 20.0 Funct
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
488 8 1 6 4.2 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)NC)I
CHEMBL1358628 5ht4r_human Human Yes 7.7 EC50 = 20.0 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_human Human Yes 7.7 EC50 = 20.0 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_human Human Yes 7.7 EC50 = 20.0 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL550122 5ht4r_human Human No 7.7 EC50 = 20.0 Funct
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
532 12 2 6 2.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCS(=O)(=O)O
CHEMBL550530 5ht4r_human Human No 7.7 EC50 = 20.0 Funct
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
474 7 2 8 0.8 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCN3CCN(CC3)S(=O)(=O)C)Cl)N
CHEMBL2087331 5ht4r_human Human No 7.7 EC50 = 20.0 Funct
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
498 7 2 5 1.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(=O)N(C)C)O
CHEMBL2087327 5ht4r_human Human No 7.7 EC50 = 20.0 Funct
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
470 7 3 5 1.3 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(=O)N)O
CHEMBL201019 5ht4r_rat Rat No 6.7 EC50 = 195 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
338 5 2 4 2.5 CCOC1=CC(=C(C=C1C(=O)NCC2CCN3C2CCC3)Cl)N
CHEMBL201019 5ht4r_rat Rat No 6.7 EC50 = 195 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
338 5 2 4 2.5 CCOC1=CC(=C(C=C1C(=O)NCC2CCN3C2CCC3)Cl)N
CHEMBL89259 5ht4r_rat Rat No 6.7 EC50 = 195 Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
322 2 2 4 1.8 C1CN2CCC1C(C2)NC(=O)C3=CC(=C(C4=C3OCC4)N)Cl
CHEMBL3741703 5ht4r_human Human No 6.7 EC50 = 196 Funct
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
403 5 1 5 3.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC4(CCOCC4)F
CHEMBL3741703 5ht4r_human Human No 6.7 EC50 = 196 Funct
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
403 5 1 5 3.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC4(CCOCC4)F
CHEMBL61130 5ht4r_human Human No 6.7 EC50 = 199.5 Funct
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
286 3 2 3 2.0 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CCNCC3
CHEMBL61130 5ht4r_human Human No 6.7 EC50 = 199.5 Funct
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
286 3 2 3 2.0 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CCNCC3
CHEMBL311325 5ht4r_rat Rat No 5.7 EC50 = 1995.3 Funct
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
353 9 1 4 3.9 CCCOC1=CC(=C(C=C1C(=O)CCCCN2CCCCC2)Cl)N
CHEMBL88973 5ht4r_rat Rat No 8.7 EC50 = 2.0 Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
325 5 1 5 2.6 C1CCN(CC1)CCOC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL2179582 5ht4r_rat Rat Yes 8.7 EC50 = 2.2 Funct
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
434 4 2 6 2.5 CC1(C2=C(C=C(C=C2)F)N(C1=O)C(=O)NCC3CCN(CC3)CC4(CCOCC4)O)C
CHEMBL83899 5ht4r_human Human Yes 8.6 EC50 = 2.5 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
418 9 2 7 1.7 COC1=CC(=C(C=C1C(=O)CCC2CCN(CC2)CCNS(=O)(=O)C)Cl)N
CHEMBL2059581 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
484 9 2 6 2.9 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCCC5COC)O
CHEMBL2059578 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
480 10 1 4 5.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCCCCCN5CCCCC5
CHEMBL2059590 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
467 6 1 5 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)C(=O)C
CHEMBL2059581 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
484 9 2 6 2.9 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN5CCCC5COC)O
CHEMBL2059578 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
480 10 1 4 5.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCCCCCN5CCCCC5
CHEMBL2059590 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
467 6 1 5 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)C(=O)C
CHEMBL559322 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
523 11 1 5 4.6 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCOCC5
CHEMBL540980 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
538 9 1 6 3.5 CCOC(=O)N1CCN(CC1)CCCN2C3CCC2CC(C3)NC(=O)C4=CC5=CC=CC=C5N(C4=O)C(C)C
CHEMBL549650 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
467 7 1 5 3.0 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCOCC5
CHEMBL555693 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
600 12 1 7 4.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCN(CC5)S(=O)(=O)C
CHEMBL559322 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
523 11 1 5 4.6 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCOCC5
CHEMBL540980 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
538 9 1 6 3.5 CCOC(=O)N1CCN(CC1)CCCN2C3CCC2CC(C3)NC(=O)C4=CC5=CC=CC=C5N(C4=O)C(C)C
CHEMBL549650 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
467 7 1 5 3.0 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCOCC5
CHEMBL555693 5ht4r_human Human No 8.6 EC50 = 2.5 Funct
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
600 12 1 7 4.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCN(CC5)S(=O)(=O)C
CHEMBL76370 5ht4r_human Human Yes 8.6 EC50 = 2.5 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL76370 5ht4r_human Human Yes 8.6 EC50 = 2.5 Funct
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
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL76370 5ht4r_human Human Yes 8.6 EC50 = 2.5 Funct
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
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL2402904 5ht4r_cavpo Guinea pig Yes 8.6 EC50 = 2.5 Funct
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
456 7 2 5 3.4 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC4CCN(CC4)C(=O)OC
CHEMBL3740472 5ht4r_human Human No 7.7 EC50 = 20 Funct
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
370 8 1 4 3.2 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CCCOC
CHEMBL3740472 5ht4r_human Human No 7.7 EC50 = 20 Funct
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
370 8 1 4 3.2 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CCCOC
CHEMBL3740472 5ht4r_rat Rat No 7.7 EC50 = 20 Funct
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
370 8 1 4 3.2 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CCCOC
CHEMBL3740472 5ht4r_human Human No 7.7 EC50 = 20 Funct
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
370 8 1 4 3.2 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CCCOC
CHEMBL3740472 5ht4r_human Human No 7.7 EC50 = 20 Funct
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
370 8 1 4 3.2 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CCCOC
CHEMBL3740472 5ht4r_rat Rat No 7.7 EC50 = 20 Funct
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
370 8 1 4 3.2 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CCCOC
CHEMBL3740612 5ht4r_human Human No 7.7 EC50 = 20.7 Funct
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
383 5 1 4 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)C5CCOCC5
CHEMBL3740612 5ht4r_human Human No 7.7 EC50 = 20.7 Funct
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
383 5 1 4 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)C5CCOCC5
CHEMBL48379 5ht4r_cavpo Guinea pig No 6.7 EC50 = 200 Funct
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.
314 6 2 5 1.9 COC1=C(C=C(C(=C1)N)Cl)NC(=O)OCCN2CCCC2
CHEMBL67555 5ht4r_rat Rat No 6.7 EC50 = 217 Funct
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
336 4 2 4 1.8 COC1=CC(=C(C=C1C(=O)NCC23CC4CN(C2)CC4C3)Cl)N
CHEMBL3740472 5ht4r_human Human No 7.7 EC50 = 22 Funct
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
370 8 1 4 3.2 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CCCOC
CHEMBL33732 5ht4r_cavpo Guinea pig No 7.7 EC50 = 22 Funct
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
313 5 1 5 2.7 CCN1CCC(CC1)OC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL3740472 5ht4r_human Human No 7.7 EC50 = 22 Funct
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
370 8 1 4 3.2 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CCCOC
CHEMBL3742300 5ht4r_human Human No 5.7 EC50 = 2247 Funct
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
356 5 1 4 3.3 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CN(CCO3)C4CCC4
CHEMBL3742300 5ht4r_human Human No 5.7 EC50 = 2247 Funct
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
356 5 1 4 3.3 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CN(CCO3)C4CCC4
CHEMBL34291 5ht4r_rat Rat Yes 7.6 EC50 = 23 Funct
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
324 4 2 4 2.1 COC1=CC(=C(C=C1C(=O)NCC2CCN3C2CCC3)Cl)N
CHEMBL34291 5ht4r_rat Rat Yes 7.6 EC50 = 23.7 Funct
Efficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosaeEfficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosae
324 4 2 4 2.1 COC1=CC(=C(C=C1C(=O)NCC2CCN3C2CCC3)Cl)N
CHEMBL3740732 5ht4r_human Human No 7.6 EC50 = 25 Funct
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
370 5 1 4 3.5 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC4CCOC4
CHEMBL3740732 5ht4r_human Human No 7.6 EC50 = 25 Funct
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
370 5 1 4 3.5 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC4CCOC4
CHEMBL559317 5ht4r_human Human No 7.6 EC50 = 25.1 Funct
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
555 9 1 5 4.8 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCN5C(=O)C6=CC=CC=C6C5=O
CHEMBL563261 5ht4r_human Human No 7.6 EC50 = 25.1 Funct
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
426 8 2 4 3.4 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCO
CHEMBL557053 5ht4r_human Human No 7.6 EC50 = 25.1 Funct
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
354 7 2 4 3.5 CCCCCN1CCC(CC1)NC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL2087336 5ht4r_human Human No 7.6 EC50 = 25.1 Funct
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
505 8 2 7 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)S(=O)(=O)C)O
CHEMBL559317 5ht4r_human Human No 7.6 EC50 = 25.1 Funct
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
555 9 1 5 4.8 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCN5C(=O)C6=CC=CC=C6C5=O
CHEMBL563261 5ht4r_human Human No 7.6 EC50 = 25.1 Funct
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
426 8 2 4 3.4 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCO
CHEMBL557053 5ht4r_human Human No 7.6 EC50 = 25.1 Funct
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
354 7 2 4 3.5 CCCCCN1CCC(CC1)NC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL2087336 5ht4r_human Human No 7.6 EC50 = 25.1 Funct
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
505 8 2 7 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)S(=O)(=O)C)O
CHEMBL2181188 5ht4r_human Human No 6.6 EC50 = 251 Funct
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
369 5 0 3 6.0 CCCN1CCC(CC1)COC2=NC3=C(C=CC=C3Cl)C4=CC=CC=C42
CHEMBL3758199 5ht4r_rat Rat No 6.6 EC50 = 251.2 Funct
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
422 8 2 6 1.3 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3C=CN=C3
CHEMBL420969 5ht4r_human Human No 6.6 EC50 = 251.2 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
312 5 2 4 2.7 COC1=CC(=C(C=C1C(=O)NCCN2CCCCC2)Cl)N
CHEMBL3758199 5ht4r_rat Rat No 6.6 EC50 = 251.2 Funct
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
422 8 2 6 1.3 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3C=CN=C3
CHEMBL2402888 5ht4r_human Human No 6.6 EC50 = 251.2 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
491 7 3 8 0.5 CS(=O)(=O)N1CCN(CC1)CC(CN2C3CCC2CC(C3)NC(=O)C4=C5C(=CC=C4)NC=N5)O
CHEMBL551743 5ht4r_human Human No 5.6 EC50 = 2511.9 Funct
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
299 3 3 3 2.0 COC1=CC2=C(C=C1)NC=C2C(=O)NC3CC4CCC(C3)N4
CHEMBL551743 5ht4r_human Human No 5.6 EC50 = 2511.9 Funct
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
299 3 3 3 2.0 COC1=CC2=C(C=C1)NC=C2C(=O)NC3CC4CCC(C3)N4
CHEMBL117287 5ht4r_human Human Yes 7.6 EC50 = 26 Funct
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
368 6 2 5 2.0 COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL117287 5ht4r_rat Rat Yes 7.6 EC50 = 26 Funct
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
368 6 2 5 2.0 COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL117287 5ht4r_rat Rat Yes 7.6 EC50 = 26 Funct
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
368 6 2 5 2.0 COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL18041 5ht4r_cavpo Guinea pig Yes 6.6 EC50 = 260 Funct
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
310 3 2 4 1.7 COC1=CC(=C(C=C1C(=O)NC2CN3CCC2CC3)Cl)N
CHEMBL295155 5ht4r_cavpo Guinea pig No 6.6 EC50 = 262 Funct
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
336 3 2 4 2.0 COC1=CC(=C(C=C1C(=O)NC2C3CC4CC2CN(C4)C3)Cl)N
CHEMBL295155 5ht4r_rat Rat No 6.6 EC50 = 262 Funct
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
336 3 2 4 2.0 COC1=CC(=C(C=C1C(=O)NC2C3CC4CC2CN(C4)C3)Cl)N
CHEMBL33676 5ht4r_cavpo Guinea pig No 7.6 EC50 = 27 Funct
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
325 4 1 5 2.9 CN1C2CCC1CC(C2)OC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL33676 5ht4r_cavpo Guinea pig No 7.6 EC50 = 27 Funct
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
325 4 1 5 2.9 CN1C2CCC1CC(C2)OC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL156579 5ht4r_cavpo Guinea pig No 7.5 EC50 = 29 Funct
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
311 6 1 5 2.4 COC1=CC(=C(C=C1C(=O)OCCN2CCC=CC2)Cl)N
CHEMBL1748 5ht4r_human Human Yes 6.5 EC50 = 290 Funct
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
314 4 3 5 0.8 COC1CNCCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL1748 5ht4r_human Human Yes 6.5 EC50 = 290 Funct
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
314 4 3 5 0.8 COC1CNCCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL158238 5ht4r_cavpo Guinea pig No 8.5 EC50 = 3 Funct
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
327 6 1 5 3.0 CC1CCN(CC1)CCOC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL538956 5ht4r_human Human No 8.5 EC50 = 3.2 Funct
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
594 13 1 6 5.1 CCOC(=O)N1CCN(CC1)CCCCCCCN2C3CCC2CC(C3)NC(=O)C4=CC5=CC=CC=C5N(C4=O)C(C)C
CHEMBL556326 5ht4r_human Human No 8.5 EC50 = 3.2 Funct
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
614 13 1 7 4.6 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCN5CCN(CC5)S(=O)(=O)C
CHEMBL559548 5ht4r_human Human No 8.5 EC50 = 3.2 Funct
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
541 12 2 6 4.9 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCCCCN3C(=O)C4=CC=CC=C4C3=O)Cl)N
CHEMBL562636 5ht4r_human Human No 8.5 EC50 = 3.2 Funct
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
479 12 2 5 5.1 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCCCCN3CCCCC3)Cl)N
CHEMBL538956 5ht4r_human Human No 8.5 EC50 = 3.2 Funct
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
594 13 1 6 5.1 CCOC(=O)N1CCN(CC1)CCCCCCCN2C3CCC2CC(C3)NC(=O)C4=CC5=CC=CC=C5N(C4=O)C(C)C
CHEMBL556326 5ht4r_human Human No 8.5 EC50 = 3.2 Funct
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
614 13 1 7 4.6 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCN5CCN(CC5)S(=O)(=O)C
CHEMBL559548 5ht4r_human Human No 8.5 EC50 = 3.2 Funct
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
541 12 2 6 4.9 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCCCCN3C(=O)C4=CC=CC=C4C3=O)Cl)N
CHEMBL562636 5ht4r_human Human No 8.5 EC50 = 3.2 Funct
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
479 12 2 5 5.1 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCCCCN3CCCCC3)Cl)N
CHEMBL2402899 5ht4r_human Human No 8.5 EC50 = 3.2 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
455 7 2 5 2.0 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CCN4CCN(CC4)C(=O)C
CHEMBL2402893 5ht4r_human Human No 8.5 EC50 = 3.2 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
535 9 3 8 1.7 CC(C)(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC(CN4CCN(CC4)S(=O)(=O)C)O
CHEMBL3739521 5ht4r_human Human No 8.5 EC50 = 3.4 Funct
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
328 4 1 3 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)C(C)C
CHEMBL3739521 5ht4r_human Human No 8.5 EC50 = 3.4 Funct
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
328 4 1 3 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)C(C)C
CHEMBL3740908 5ht4r_human Human No 8.4 EC50 = 3.9 Funct
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
332 5 1 4 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CCF
CHEMBL3740908 5ht4r_human Human No 8.4 EC50 = 3.9 Funct
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
332 5 1 4 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CCF
CHEMBL538635 5ht4r_human Human Yes 8.4 EC50 = 4.0 Funct
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL538635 5ht4r_human Human Yes 8.4 EC50 = 4.0 Funct
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
560 8 2 8 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN5CCN(CC5)S(=O)(=O)C)O
CHEMBL2059589 5ht4r_human Human No 8.4 EC50 = 4.0 Funct
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
503 7 1 7 2.2 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)S(=O)(=O)C
CHEMBL2059589 5ht4r_human Human No 8.4 EC50 = 4.0 Funct
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
503 7 1 7 2.2 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)S(=O)(=O)C
CHEMBL558855 5ht4r_human Human No 8.4 EC50 = 4.0 Funct
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
494 8 2 5 2.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCCC5C(=O)N
CHEMBL558855 5ht4r_human Human No 8.4 EC50 = 4.0 Funct
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
494 8 2 5 2.9 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCN5CCCC5C(=O)N
CHEMBL83954 5ht4r_cavpo Guinea pig Yes 7.5 EC50 = 30 Funct
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
327 7 1 5 2.9 COC1=CC(=C(C=C1C(=O)OCCCN2CCCCC2)Cl)N
CHEMBL49072 5ht4r_cavpo Guinea pig No 6.5 EC50 = 300 Funct
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.
316 8 2 5 2.2 CCN(CC)CCOC(=O)NC1=C(C=C(C(=C1)Cl)N)OC
CHEMBL3739647 5ht4r_human Human No 7.5 EC50 = 31 Funct
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
397 6 1 4 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC5CCOCC5
CHEMBL3739647 5ht4r_human Human No 7.5 EC50 = 31 Funct
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
397 6 1 4 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC5CCOCC5
CHEMBL552218 5ht4r_human Human No 7.5 EC50 = 31.6 Funct
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
367 4 1 3 3.4 CCN1C2CCC1CC(C2)NC(=O)C3=CC4=CC=CC=C4N(C3=O)C(C)C
CHEMBL552420 5ht4r_human Human No 7.5 EC50 = 31.6 Funct
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
383 5 2 4 2.3 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCO
CHEMBL2087329 5ht4r_human Human No 7.5 EC50 = 31.6 Funct
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
484 7 3 5 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(=O)NC)O
CHEMBL27966 5ht4r_rat Rat No 7.5 EC50 = 31.6 Funct
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
344 1 1 4 2.7 CN1CCC(CC1)N2C(=O)C3=CC=CC4=C3C(=CC(=C4N)Cl)C2=O
CHEMBL552218 5ht4r_human Human No 7.5 EC50 = 31.6 Funct
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
367 4 1 3 3.4 CCN1C2CCC1CC(C2)NC(=O)C3=CC4=CC=CC=C4N(C3=O)C(C)C
CHEMBL552420 5ht4r_human Human No 7.5 EC50 = 31.6 Funct
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
383 5 2 4 2.3 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCO
CHEMBL2087329 5ht4r_human Human No 7.5 EC50 = 31.6 Funct
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
484 7 3 5 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(=O)NC)O
CHEMBL3740030 5ht4r_human Human No 6.5 EC50 = 315.7 Funct
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
389 8 2 5 2.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CCCOC)O
CHEMBL3740030 5ht4r_human Human No 6.5 EC50 = 315.7 Funct
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
389 8 2 5 2.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CCCOC)O
CHEMBL553658 5ht4r_human Human No 6.5 EC50 = 316.2 Funct
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
302 2 2 3 1.5 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NC3CCNCC3
CHEMBL309655 5ht4r_human Human No 6.5 EC50 = 316.2 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
311 6 1 4 2.7 COC1=CC(=C(C=C1C(=O)CCCN2CCCCC2)Cl)N
CHEMBL553658 5ht4r_human Human No 6.5 EC50 = 316.2 Funct
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
302 2 2 3 1.5 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NC3CCNCC3
CHEMBL37333 5ht4r_rat Rat No 6.5 EC50 = 323 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
324 4 2 4 2.1 COC1=CC(=C(C=C1C(=O)NCC2CCN3C2CCC3)Cl)N
CHEMBL37333 5ht4r_rat Rat No 6.5 EC50 = 323 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
324 4 2 4 2.1 COC1=CC(=C(C=C1C(=O)NCC2CCN3C2CCC3)Cl)N
CHEMBL303877 5ht4r_rat Rat No 5.5 EC50 = 3335 Funct
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
364 4 2 4 1.7 CC(=O)NC1=C(C=C(C(=C1)OC)C(=O)NC2C3CC4CC2CN4C3)Cl
CHEMBL3741377 5ht4r_human Human No 7.5 EC50 = 34 Funct
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
370 6 2 4 2.9 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC(C)(C)O
CHEMBL3741377 5ht4r_human Human No 7.5 EC50 = 34 Funct
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
370 6 2 4 2.9 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC(C)(C)O
CHEMBL88867 5ht4r_rat Rat No 7.5 EC50 = 35.4 Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
324 4 2 4 2.0 C1CCN(CC1)CCNC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL325603 5ht4r_mouse Mouse No 6.4 EC50 = 360 Funct
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
342 2 1 3 2.5 CCN1C2=CC=CC=C2N(C1=O)C(=O)NC3CC4CCCC(C3)N4C
CHEMBL201414 5ht4r_rat Rat No 6.4 EC50 = 374.2 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
342 3 1 3 2.9 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NCC3CCN4C3CCC4
CHEMBL201414 5ht4r_rat Rat No 6.4 EC50 = 374.2 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
342 3 1 3 2.9 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NCC3CCN4C3CCC4
CHEMBL3759259 5ht4r_rat Rat No 6.4 EC50 = 380.2 Funct
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
467 7 2 6 2.0 CCC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759259 5ht4r_rat Rat No 6.4 EC50 = 380.2 Funct
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
467 7 2 6 2.0 CCC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL66768 5ht4r_rat Rat No 6.4 EC50 = 382 Funct
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
322 3 2 4 1.8 COC1=CC(=C(C=C1C(=O)NC2C3CC4CC2CN4C3)Cl)N
CHEMBL315443 5ht4r_rat Rat No 6.4 EC50 = 385 Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
323 3 1 5 2.3 C1CN2CCC1C(C2)OC(=O)C3=CC(=C(C4=C3OCC4)N)Cl
CHEMBL2448137 5ht4r_rat Rat No 5.4 EC50 = 3870 Funct
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
322 3 2 4 1.7 COC1=CC(=C(C=C1C(=O)NC2C3CC4C2CN(C4)C3)Cl)N
CHEMBL3739826 5ht4r_human Human No 7.4 EC50 = 39 Funct
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
385 5 2 4 3.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CC4CCC(C3)N4CC(C)(C)O
CHEMBL3739826 5ht4r_human Human No 7.4 EC50 = 39 Funct
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
385 5 2 4 3.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CC4CCC(C3)N4CC(C)(C)O
CHEMBL550064 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
312 3 2 3 2.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4
CHEMBL558261 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
558 13 2 8 3.3 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCCCCN3CCN(CC3)S(=O)(=O)C)Cl)N
CHEMBL550064 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
312 3 2 3 2.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4
CHEMBL551940 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
396 10 2 4 5.1 CCCCCCCCN1CCC(CC1)NC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL562400 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
452 10 1 3 6.4 CCCCCCCCN1C2CCC1CC(C2)NC(=O)C3=CC4=CC=CC=C4N(C3=O)C(C)C
CHEMBL551941 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
410 7 1 3 4.8 CCCCCN1C2CCC1CC(C2)NC(=O)C3=CC4=CC=CC=C4N(C3=O)C(C)C
CHEMBL80015 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
311 5 1 4 2.6 CN1CCC(CC1)CCC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL83841 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
325 7 1 4 3.1 COC1=CC(=C(C=C1C(=O)CCCCN2CCCCC2)Cl)N
CHEMBL550064 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
312 3 2 3 2.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4
CHEMBL558261 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
558 13 2 8 3.3 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCCCCN3CCN(CC3)S(=O)(=O)C)Cl)N
CHEMBL550064 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
312 3 2 3 2.6 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4
CHEMBL551940 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
396 10 2 4 5.1 CCCCCCCCN1CCC(CC1)NC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL562400 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
452 10 1 3 6.4 CCCCCCCCN1C2CCC1CC(C2)NC(=O)C3=CC4=CC=CC=C4N(C3=O)C(C)C
CHEMBL551941 5ht4r_human Human No 7.4 EC50 = 39.8 Funct
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
410 7 1 3 4.8 CCCCCN1C2CCC1CC(C2)NC(=O)C3=CC4=CC=CC=C4N(C3=O)C(C)C
CHEMBL83841 5ht4r_rat Rat No 7.4 EC50 = 39.8 Funct
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
325 7 1 4 3.1 COC1=CC(=C(C=C1C(=O)CCCCN2CCCCC2)Cl)N
CHEMBL539652 5ht4r_human Human Yes 6.4 EC50 = 398.1 Funct
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
298 4 3 4 2.2 COC1=CC(=C(C=C1C(=O)NCC2CCNCC2)Cl)N
CHEMBL541969 5ht4r_human Human Yes 6.4 EC50 = 398.1 Funct
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
284 3 3 4 2.0 COC1=CC(=C(C=C1C(=O)NC2CCNCC2)Cl)N
CHEMBL551678 5ht4r_human Human No 6.4 EC50 = 398.1 Funct
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
434 9 3 7 -0.6 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCS(=O)(=O)O)Cl)N
CHEMBL539652 5ht4r_human Human Yes 6.4 EC50 = 398.1 Funct
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
298 4 3 4 2.2 COC1=CC(=C(C=C1C(=O)NCC2CCNCC2)Cl)N
CHEMBL541969 5ht4r_human Human Yes 6.4 EC50 = 398.1 Funct
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
284 3 3 4 2.0 COC1=CC(=C(C=C1C(=O)NC2CCNCC2)Cl)N
CHEMBL551678 5ht4r_human Human No 6.4 EC50 = 398.1 Funct
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
434 9 3 7 -0.6 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCS(=O)(=O)O)Cl)N
CHEMBL452353 5ht4r_human Human No 8.4 EC50 = 4 Funct
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
622 12 3 9 3.5 COC1=CC(=C(C=C1C(=O)OCCN2CCC(CC2)NC(=O)CCCCN3C(=O)C4=C5C(=C(C=C4)N)C=CC=C5C3=O)Cl)N
CHEMBL157880 5ht4r_cavpo Guinea pig No 8.4 EC50 = 4 Funct
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
329 6 2 6 1.6 COC1=CC(=C(C=C1C(=O)OCCN2CCCC(C2)O)Cl)N
CHEMBL452353 5ht4r_human Human No 8.4 EC50 = 4 Funct
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
622 12 3 9 3.5 COC1=CC(=C(C=C1C(=O)OCCN2CCC(CC2)NC(=O)CCCCN3C(=O)C4=C5C(=C(C=C4)N)C=CC=C5C3=O)Cl)N
CHEMBL348311 5ht4r_cavpo Guinea pig No 8.4 EC50 = 4.4 Funct
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
327 6 1 5 2.9 COC1=CC(=C(C=C1C(=O)OCCN2CCCCCC2)Cl)N
CHEMBL91771 5ht4r_rat Rat No 8.4 EC50 = 4.5 Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
366 6 2 4 3.2 CCCCN1CCC(CC1)CNC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL121913 5ht4r_human Human No 8.4 EC50 = 4.5 Funct
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
392 7 1 8 1.9 COC1=CC(=C(C=C1C(=O)OCCN2CCN(CC2)C3=NC=CC=N3)Cl)N
CHEMBL3741821 5ht4r_human Human No 8.3 EC50 = 4.8 Funct
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
373 8 1 4 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CCN(CC3)CCCOC
CHEMBL3741821 5ht4r_human Human No 8.3 EC50 = 4.8 Funct
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
373 8 1 4 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CCN(CC3)CCCOC
CHEMBL3741776 5ht4r_human Human No 7.4 EC50 = 40 Funct
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
358 7 1 4 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CCCOC
CHEMBL3739611 5ht4r_human Human No 7.4 EC50 = 40 Funct
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
358 5 2 4 3.1 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC(C)(C)O
CHEMBL156970 5ht4r_cavpo Guinea pig No 7.4 EC50 = 40 Funct
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
299 6 1 5 2.2 COC1=CC(=C(C=C1C(=O)OCCN2CCCC2)Cl)N
CHEMBL156965 5ht4r_cavpo Guinea pig No 7.4 EC50 = 40 Funct
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
339 6 1 5 3.2 COC1=CC(=C(C=C1C(=O)OCCN2C3CCCC2CC3)Cl)N
CHEMBL3741776 5ht4r_human Human No 7.4 EC50 = 40 Funct
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
358 7 1 4 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CCCOC
CHEMBL3739611 5ht4r_human Human No 7.4 EC50 = 40 Funct
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
358 5 2 4 3.1 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC(C)(C)O
CHEMBL324057 5ht4r_rat Rat No 7.4 EC50 = 40.3 Funct
Efficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosaeEfficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosae
356 2 1 3 2.9 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NC3CC4CCCC(C3)N4C
CHEMBL59834 5ht4r_cavpo Guinea pig No 7.4 EC50 = 43 Funct
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
342 2 1 3 2.5 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NC3CC4CCC(C3)N4C
CHEMBL32986 5ht4r_cavpo Guinea pig No 7.4 EC50 = 44 Funct
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
313 5 1 5 2.7 CCN1CCCC(C1)OC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL318154 5ht4r_rat Rat No 6.4 EC50 = 449 Funct
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
338 4 2 4 2.3 CC12CCCN1CCC2CNC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759860 5ht4r_rat Rat No 7.3 EC50 = 45.7 Funct
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
481 7 2 6 2.6 CC(C)C(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759860 5ht4r_rat Rat No 7.3 EC50 = 45.7 Funct
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
481 7 2 6 2.6 CC(C)C(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3741508 5ht4r_human Human No 6.3 EC50 = 467 Funct
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
386 5 1 5 2.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CN(CCO3)C4CCOCC4
CHEMBL3741508 5ht4r_human Human No 6.3 EC50 = 467 Funct
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
386 5 1 5 2.8 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CN(CCO3)C4CCOCC4
CHEMBL3739933 5ht4r_human Human No 7.3 EC50 = 47 Funct
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
387 7 1 4 4.3 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC(C)(C)COC
CHEMBL3739933 5ht4r_human Human No 7.3 EC50 = 47 Funct
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
387 7 1 4 4.3 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC(C)(C)COC
CHEMBL3741322 5ht4r_human Human No 7.3 EC50 = 49 Funct
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
370 4 1 4 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)C4CCOCC4
CHEMBL3739470 5ht4r_human Human No 7.3 EC50 = 49 Funct
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
340 5 1 3 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC4CC4
CHEMBL3741322 5ht4r_human Human No 7.3 EC50 = 49 Funct
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
370 4 1 4 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)C4CCOCC4
CHEMBL3739470 5ht4r_human Human No 7.3 EC50 = 49 Funct
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
340 5 1 3 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CCN(CC3)CC4CC4
CHEMBL2059580 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
468 11 1 4 5.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCCCCCN(C)C(C)C
CHEMBL2059579 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
442 8 2 5 3.3 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(C)C)O
CHEMBL2059580 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
468 11 1 4 5.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCCCCCN(C)C(C)C
CHEMBL2059579 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
442 8 2 5 3.3 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CC(CN(C)C(C)C)O
CHEMBL557867 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
499 9 2 6 3.5 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCN3C(=O)C4=CC=CC=C4C3=O)Cl)N
CHEMBL562902 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
437 9 2 5 3.7 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCN3CCCCC3)Cl)N
CHEMBL557867 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
499 9 2 6 3.5 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCN3C(=O)C4=CC=CC=C4C3=O)Cl)N
CHEMBL562902 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
437 9 2 5 3.7 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCCCCN3CCCCC3)Cl)N
CHEMBL2087337 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
505 8 2 7 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)S(=O)(=O)C)O
CHEMBL2087326 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
456 7 4 5 1.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CNC(=O)N)O
CHEMBL2087337 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
505 8 2 7 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CN(C)S(=O)(=O)C)O
CHEMBL2087326 5ht4r_human Human No 8.3 EC50 = 5.0 Funct
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
456 7 4 5 1.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CNC(=O)N)O
CHEMBL117287 5ht4r_human Human Yes 8.3 EC50 = 5.2 Funct
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
368 6 2 5 2.0 COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL117287 5ht4r_human Human Yes 8.3 EC50 = 5.2 Funct
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
368 6 2 5 2.0 COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL117287 5ht4r_human Human Yes 8.3 EC50 = 5.2 Funct
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
368 6 2 5 2.0 COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL156088 5ht4r_cavpo Guinea pig No 8.3 EC50 = 5.3 Funct
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
340 6 1 4 2.6 COC1=CC(=C(C=C1C(=O)OCC[N+]23CCC(CC2)CC3)Cl)N
CHEMBL3741548 5ht4r_human Human No 8.2 EC50 = 5.7 Funct
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
385 7 2 4 3.5 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC(C)(C)CO
CHEMBL3741548 5ht4r_human Human No 8.2 EC50 = 5.7 Funct
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
385 7 2 4 3.5 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC(C)(C)CO
CHEMBL1258671 5ht4r_human Human No 8.2 EC50 = 5.9 Funct
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
366 7 1 7 2.9 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)N)F
CHEMBL1258671 5ht4r_human Human No 8.2 EC50 = 5.9 Funct
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
366 7 1 7 2.9 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)N)F
CHEMBL3740400 5ht4r_human Human No 7.3 EC50 = 50 Funct
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
314 4 1 3 3.6 CCN1CCC(CC1)NC(=O)C2=C3C=CC=CN3C(=N2)C(C)C
CHEMBL3740400 5ht4r_human Human No 7.3 EC50 = 50 Funct
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
314 4 1 3 3.6 CCN1CCC(CC1)NC(=O)C2=C3C=CC=CN3C(=N2)C(C)C
CHEMBL556279 5ht4r_human Human No 7.3 EC50 = 50.1 Funct
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
597 12 1 5 6.2 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCN5C(=O)C6=CC=CC=C6C5=O
CHEMBL556279 5ht4r_human Human No 7.3 EC50 = 50.1 Funct
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
597 12 1 5 6.2 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCCN5C(=O)C6=CC=CC=C6C5=O
CHEMBL3740313 5ht4r_human Human No 6.3 EC50 = 500 Funct
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
353 4 0 5 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C3=NN=C(O3)C4CCN(CC4)C(C)C
CHEMBL3740313 5ht4r_human Human No 6.3 EC50 = 500 Funct
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
353 4 0 5 4.0 CC(C)C1=NC(=C2N1C=CC=C2)C3=NN=C(O3)C4CCN(CC4)C(C)C
CHEMBL539212 5ht4r_human Human Yes 6.3 EC50 = 501.2 Funct
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
313 5 3 5 1.2 COC1=CC(=C(C=C1C(=O)NCCN2CCNCC2)Cl)N
CHEMBL27846 5ht4r_rat Rat No 6.3 EC50 = 501.2 Funct
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
310 3 2 4 1.7 COC1=CC(=C(C=C1C(=O)NC2CN3CCC2CC3)Cl)N
CHEMBL539212 5ht4r_human Human Yes 6.3 EC50 = 501.2 Funct
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
313 5 3 5 1.2 COC1=CC(=C(C=C1C(=O)NCCN2CCNCC2)Cl)N
CHEMBL2448165 5ht4r_rat Rat No 7.3 EC50 = 51 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
322 3 2 4 1.7 COC1=CC(=C(C=C1C(=O)NC2C3CC4C2CN(C4)C3)Cl)N
CHEMBL2448165 5ht4r_rat Rat No 7.3 EC50 = 51 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
322 3 2 4 1.7 COC1=CC(=C(C=C1C(=O)NC2C3CC4C2CN(C4)C3)Cl)N
CHEMBL2448165 5ht4r_rat Rat No 7.3 EC50 = 51.3 Funct
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
322 3 2 4 1.7 COC1=CC(=C(C=C1C(=O)NC2C3CC4C2CN(C4)C3)Cl)N
CHEMBL3739455 5ht4r_human Human No 6.3 EC50 = 520 Funct
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
380 5 0 5 4.4 CC(C)C1=NC(=C2N1C=CC=C2)C3=NN=C(O3)C4CCN(CC4)CC5CCC5
CHEMBL3739455 5ht4r_human Human No 6.3 EC50 = 520 Funct
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
380 5 0 5 4.4 CC(C)C1=NC(=C2N1C=CC=C2)C3=NN=C(O3)C4CCN(CC4)CC5CCC5
CHEMBL3741062 5ht4r_human Human No 7.3 EC50 = 53 Funct
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
413 6 1 4 4.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CC4CCOCC4)C
CHEMBL3741062 5ht4r_human Human No 7.3 EC50 = 53 Funct
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
413 6 1 4 4.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CC4CCOCC4)C
CHEMBL295155 5ht4r_cavpo Guinea pig No 6.3 EC50 = 538 Funct
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
336 3 2 4 2.0 COC1=CC(=C(C=C1C(=O)NC2C3CC4CC2CN(C4)C3)Cl)N
CHEMBL295155 5ht4r_cavpo Guinea pig No 6.3 EC50 = 538 Funct
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
336 3 2 4 2.0 COC1=CC(=C(C=C1C(=O)NC2C3CC4CC2CN(C4)C3)Cl)N
CHEMBL1358628 5ht4r_rat Rat Yes 7.3 EC50 = 54.7 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_rat Rat Yes 7.3 EC50 = 54.7 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_rat Rat Yes 7.3 EC50 = 54.7 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1358628 5ht4r_rat Rat Yes 7.3 EC50 = 54.7 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_rat Rat Yes 7.3 EC50 = 54.7 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_rat Rat Yes 7.3 EC50 = 54.7 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL3085015 5ht4r_cavpo Guinea pig No 6.3 EC50 = 545 Funct
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
350 4 2 4 3.0 COC1=CC(=C(C=C1C(=O)NCC2C3CC4CC2CN(C4)C3)Cl)N
CHEMBL3085015 5ht4r_cavpo Guinea pig No 6.3 EC50 = 545 Funct
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
350 4 2 4 3.0 COC1=CC(=C(C=C1C(=O)NCC2C3CC4CC2CN(C4)C3)Cl)N
CHEMBL1358628 5ht4r_rat Rat Yes 7.3 EC50 = 55 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_rat Rat Yes 7.3 EC50 = 55 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_rat Rat Yes 7.3 EC50 = 55 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL3739459 5ht4r_human Human No 7.3 EC50 = 56.7 Funct
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
415 6 2 5 2.9 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CC4CCOCC4)O
CHEMBL3739459 5ht4r_human Human No 7.3 EC50 = 56.7 Funct
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
415 6 2 5 2.9 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CC4CCOCC4)O
CHEMBL3306918 5ht4r_human Human Yes 7.2 EC50 = 58 Funct
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
378 6 2 5 3.5 CC(C)N1C2=C(C=CS2)C(=C(C1=O)C(=O)NCCCN3CCCCC3)O
CHEMBL3306918 5ht4r_human Human Yes 7.2 EC50 = 58 Funct
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
378 6 2 5 3.5 CC(C)N1C2=C(C=CS2)C(=C(C1=O)C(=O)NCCCN3CCCCC3)O
CHEMBL3306918 5ht4r_human Human Yes 7.2 EC50 = 58 Funct
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
378 6 2 5 3.5 CC(C)N1C2=C(C=CS2)C(=C(C1=O)C(=O)NCCCN3CCCCC3)O
CHEMBL349809 5ht4r_cavpo Guinea pig No 8.2 EC50 = 6 Funct
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
327 6 1 5 3.0 CC1CCCCN1CCOC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL2179588 5ht4r_human Human No 8.2 EC50 = 6.3 Funct
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
375 9 0 5 5.7 CCCCN1CCC(CC1)COC2=NOC3=C2C(=CC=C3)OCC(C)(C)C
CHEMBL2059590 5ht4r_human Human No 8.2 EC50 = 6.3 Funct
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
467 6 1 5 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)C(=O)C
CHEMBL76370 5ht4r_cavpo Guinea pig Yes 8.2 EC50 = 6.3 Funct
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
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL76370 5ht4r_cavpo Guinea pig Yes 8.2 EC50 = 6.3 Funct
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
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL552075 5ht4r_human Human No 8.2 EC50 = 6.3 Funct
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
448 6 2 6 -0.4 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCS(=O)(=O)O
CHEMBL565146 5ht4r_human Human No 8.2 EC50 = 6.3 Funct
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
530 7 1 7 2.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)S(=O)(=O)C
CHEMBL2087324 5ht4r_human Human No 8.2 EC50 = 6.3 Funct
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
455 7 3 5 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CNC(=O)C)O
CHEMBL2059590 5ht4r_human Human No 8.2 EC50 = 6.3 Funct
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
467 6 1 5 2.4 CC(C)N1C2=CC=CC=C2C(=N1)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)C(=O)C
CHEMBL76370 5ht4r_cavpo Guinea pig Yes 8.2 EC50 = 6.3 Funct
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
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL76370 5ht4r_cavpo Guinea pig Yes 8.2 EC50 = 6.3 Funct
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
301 8 3 4 2.1 CCCCCN=C(N)NNC=C1C=NC2=C1C=C(C=C2)OC
CHEMBL552075 5ht4r_human Human No 8.2 EC50 = 6.3 Funct
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
448 6 2 6 -0.4 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCS(=O)(=O)O
CHEMBL565146 5ht4r_human Human No 8.2 EC50 = 6.3 Funct
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
530 7 1 7 2.1 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCN5CCN(CC5)S(=O)(=O)C
CHEMBL2087324 5ht4r_human Human No 8.2 EC50 = 6.3 Funct
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
455 7 3 5 1.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CNC(=O)C)O
CHEMBL49266 5ht4r_cavpo Guinea pig No 7.2 EC50 = 60 Funct
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.
342 6 2 5 2.7 CC1CCN(CC1)CCOC(=O)NC2=C(C=C(C(=C2)Cl)N)OC
CHEMBL3759928 5ht4r_rat Rat No 5.2 EC50 = 6025.6 Funct
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
543 9 2 6 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCC(=O)N3CCC(CC3)CC4=CC=CC=C4
CHEMBL3759928 5ht4r_rat Rat No 5.2 EC50 = 6025.6 Funct
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
543 9 2 6 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCC(=O)N3CCC(CC3)CC4=CC=CC=C4
CHEMBL562477 5ht4r_human Human No 7.2 EC50 = 63.1 Funct
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
328 5 3 5 1.8 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCO)Cl)N
CHEMBL314489 5ht4r_human Human No 7.2 EC50 = 63.1 Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
381 10 1 4 4.9 CCCCCCN1CCC(CC1)CCC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL562477 5ht4r_human Human No 7.2 EC50 = 63.1 Funct
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
328 5 3 5 1.8 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCO)Cl)N
CHEMBL2181189 5ht4r_human Human No 7.2 EC50 = 63.1 Funct
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
352 5 0 4 5.5 CCCN1CCC(CC1)COC2=NC3=C(C=CC=C3F)C4=CC=CC=C42
CHEMBL159825 5ht4r_rat Rat No 7.2 EC50 = 63.1 Funct
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
310 3 2 4 1.7 COC1=CC(=C(C=C1C(=O)NC2CCN3CCC2C3)Cl)N
CHEMBL563276 5ht4r_human Human No 6.2 EC50 = 631.0 Funct
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
457 6 2 6 2.4 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCN3C(=O)C4=CC=CC=C4C3=O)Cl)N
CHEMBL563276 5ht4r_human Human No 6.2 EC50 = 631.0 Funct
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
457 6 2 6 2.4 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CCN3C(=O)C4=CC=CC=C4C3=O)Cl)N
CHEMBL2402889 5ht4r_human Human No 6.2 EC50 = 631.0 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
465 7 3 8 -0.2 CS(=O)(=O)N1CCN(CC1)CC(CN2CCC(CC2)NC(=O)C3=C4C(=CC=C3)NC=N4)O
CHEMBL570780 5ht4r_human Human No 5.2 EC50 = 6309.6 Funct
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
287 4 3 3 1.6 COC1=CC2=C(C=C1)NC=C2C(=O)NCC3CCNCC3
CHEMBL570780 5ht4r_human Human No 5.2 EC50 = 6309.6 Funct
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
287 4 3 3 1.6 COC1=CC2=C(C=C1)NC=C2C(=O)NCC3CCNCC3
CHEMBL3740864 5ht4r_human Human No 6.2 EC50 = 633 Funct
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
391 8 1 5 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CCCOC)F
CHEMBL3740864 5ht4r_human Human No 6.2 EC50 = 633 Funct
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
391 8 1 5 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CCCOC)F
CHEMBL121913 5ht4r_human Human No 7.2 EC50 = 66 Funct
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
392 7 1 8 1.9 COC1=CC(=C(C=C1C(=O)OCCN2CCN(CC2)C3=NC=CC=N3)Cl)N
CHEMBL34291 5ht4r_rat Rat Yes 7.2 EC50 = 66 Funct
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
324 4 2 4 2.1 COC1=CC(=C(C=C1C(=O)NCC2CCN3C2CCC3)Cl)N
CHEMBL70205 5ht4r_rat Rat No 6.2 EC50 = 660 Funct
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
336 4 2 4 2.8 COC1=CC(=C(C=C1C(=O)NCC2C3CC4CC2CN4C3)Cl)N
CHEMBL3758932 5ht4r_rat Rat No 6.2 EC50 = 676.1 Funct
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
421 8 2 5 2.0 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3C=CC=C3
CHEMBL3758932 5ht4r_rat Rat No 6.2 EC50 = 676.1 Funct
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
421 8 2 5 2.0 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3C=CC=C3
CHEMBL488325 5ht4r_human Human No 7.2 EC50 = 68 Funct
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
581 14 3 9 3.1 CC1=CC=C(C=C1)S(=O)(=O)NCCCC(=O)NCC2CCN(CC2)CCOC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL488325 5ht4r_human Human No 7.2 EC50 = 68 Funct
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
581 14 3 9 3.1 CC1=CC=C(C=C1)S(=O)(=O)NCCCC(=O)NCC2CCN(CC2)CCOC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL91842 5ht4r_rat Rat No 8.1 EC50 = 7.4 Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
339 6 1 5 3.0 C1CCN(CC1)CCCOC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
CHEMBL158147 5ht4r_cavpo Guinea pig No 8.1 EC50 = 7.8 Funct
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
353 6 1 5 3.2 COC1=CC(=C(C=C1C(=O)OCCN2CC3CCC(C2)CC3)Cl)N
CHEMBL550459 5ht4r_human Human No 8.1 EC50 = 7.9 Funct
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
331 4 2 4 1.3 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NCCN3CCNCC3
CHEMBL539651 5ht4r_human Human No 8.1 EC50 = 7.9 Funct
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
598 12 1 5 6.6 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCN(CC5)C6=CC=CC=C6
CHEMBL550459 5ht4r_human Human No 8.1 EC50 = 7.9 Funct
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
331 4 2 4 1.3 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NCCN3CCNCC3
CHEMBL539651 5ht4r_human Human No 8.1 EC50 = 7.9 Funct
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
598 12 1 5 6.6 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCCCCCCN5CCN(CC5)C6=CC=CC=C6
CHEMBL2087334 5ht4r_human Human No 8.1 EC50 = 7.9 Funct
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
491 8 3 7 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CNS(=O)(=O)C)O
CHEMBL2087334 5ht4r_human Human No 8.1 EC50 = 7.9 Funct
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
491 8 3 7 1.5 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CC(CNS(=O)(=O)C)O
CHEMBL3759601 5ht4r_rat Rat No 6.2 EC50 = 708.0 Funct
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
423 8 2 7 1.3 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3C=NC=N3
CHEMBL3759601 5ht4r_rat Rat No 6.2 EC50 = 708.0 Funct
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
423 8 2 7 1.3 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3C=NC=N3
CHEMBL324057 5ht4r_mouse Mouse No 7.1 EC50 = 72 Funct
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
356 2 1 3 2.9 CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NC3CC4CCCC(C3)N4C
CHEMBL3742145 5ht4r_human Human No 7.1 EC50 = 72.3 Funct
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
389 6 3 5 2.3 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CC(C)(C)O)O
CHEMBL3742145 5ht4r_human Human No 7.1 EC50 = 72.3 Funct
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
389 6 3 5 2.3 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3(CCN(CC3)CC(C)(C)O)O
CHEMBL15585 5ht4r_human Human No 7.1 EC50 = 72.4 Funct
Tested for 5-hydroxytryptamine 4 binding affinity against cisaprideTested for 5-hydroxytryptamine 4 binding affinity against cisapride
352 3 2 4 3.1 CC1CCCC2N1CCC(C2)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL301039 5ht4r_human Human No 7.1 EC50 = 72.4 Funct
Tested for 5-hydroxytryptamine 4 binding affinity against cisaprideTested for 5-hydroxytryptamine 4 binding affinity against cisapride
324 3 2 4 2.3 CN1C2CCC1CC(C2)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3085015 5ht4r_cavpo Guinea pig No 7.1 EC50 = 73.6 Funct
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
350 4 2 4 3.0 COC1=CC(=C(C=C1C(=O)NCC2C3CC4CC2CN(C4)C3)Cl)N
CHEMBL3739467 5ht4r_human Human No 6.1 EC50 = 736 Funct
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
383 7 0 6 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C3=NN=C(O3)C4CCN(CC4)CCCOC
CHEMBL3739467 5ht4r_human Human No 6.1 EC50 = 736 Funct
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
383 7 0 6 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C3=NN=C(O3)C4CCN(CC4)CCCOC
CHEMBL2181187 5ht4r_human Human No 7.1 EC50 = 79.4 Funct
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
364 6 0 4 5.4 CCCN1CCC(CC1)COC2=NC3=C(C=CC=C3OC)C4=CC=CC=C42
CHEMBL563799 5ht4r_human Human No 7.1 EC50 = 79.4 Funct
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
513 6 1 5 3.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCN5C(=O)C6=CC=CC=C6C5=O
CHEMBL570074 5ht4r_human Human No 7.1 EC50 = 79.4 Funct
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
312 4 2 4 2.8 CCN1CCC(CC1)NC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL1358628 5ht4r_human Human Yes 7.1 EC50 = 79.4 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_human Human Yes 7.1 EC50 = 79.4 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_human Human Yes 7.1 EC50 = 79.4 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL563799 5ht4r_human Human No 7.1 EC50 = 79.4 Funct
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
513 6 1 5 3.7 CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3CC4CCC(C3)N4CCN5C(=O)C6=CC=CC=C6C5=O
CHEMBL570074 5ht4r_human Human No 7.1 EC50 = 79.4 Funct
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
312 4 2 4 2.8 CCN1CCC(CC1)NC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL1358628 5ht4r_human Human Yes 7.1 EC50 = 79.4 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_human Human Yes 7.1 EC50 = 79.4 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_human Human Yes 7.1 EC50 = 79.4 Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1358628 5ht4r_human Human Yes 7.1 EC50 = 79.4 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_human Human Yes 7.1 EC50 = 79.4 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_human Human Yes 7.1 EC50 = 79.4 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL2402904 5ht4r_cavpo Guinea pig Yes 8.1 EC50 = 8.6 Funct
Agonist activity at 5-HT4 receptor in guinea pig colonAgonist activity at 5-HT4 receptor in guinea pig colon
456 7 2 5 3.4 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC4CCN(CC4)C(=O)OC
CHEMBL2402904 5ht4r_cavpo Guinea pig Yes 8.1 EC50 = 8.6 Funct
Agonist activity at 5-HT4 receptor in guinea pig colonAgonist activity at 5-HT4 receptor in guinea pig colon
456 7 2 5 3.4 CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC4CCN(CC4)C(=O)OC
CHEMBL3740669 5ht4r_human Human No 8.1 EC50 = 8.7 Funct
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
454 7 1 5 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC5CCN(CC5)C(=O)OC
CHEMBL3740669 5ht4r_human Human No 8.1 EC50 = 8.7 Funct
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
454 7 1 5 3.6 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)CC5CCN(CC5)C(=O)OC
CHEMBL1258109 5ht4r_human Human No 8.1 EC50 = 8.9 Funct
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
362 8 1 6 3.5 CCCCN1CCC(CC1)COC(=O)C2=C3C(=C(C=C2)NC)OCCO3
CHEMBL1258109 5ht4r_human Human No 8.1 EC50 = 8.9 Funct
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
362 8 1 6 3.5 CCCCN1CCC(CC1)COC(=O)C2=C3C(=C(C=C2)NC)OCCO3
CHEMBL3741199 5ht4r_human Human No 6.1 EC50 = 840 Funct
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
365 4 0 5 4.1 CC(C)C1=NC(=C2N1C=CC=C2)C3=NN=C(O3)C4CCN(CC4)C5CCC5
CHEMBL3741199 5ht4r_human Human No 6.1 EC50 = 840 Funct
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
365 4 0 5 4.1 CC(C)C1=NC(=C2N1C=CC=C2)C3=NN=C(O3)C4CCN(CC4)C5CCC5
CHEMBL3740000 5ht4r_human Human No 6.1 EC50 = 857 Funct
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
365 5 0 5 3.9 CC(C)C1=NC(=C2N1C=CC=C2)C3=NN=C(O3)C4CCN(CC4)CC5CC5
CHEMBL3740000 5ht4r_human Human No 6.1 EC50 = 857 Funct
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
365 5 0 5 3.9 CC(C)C1=NC(=C2N1C=CC=C2)C3=NN=C(O3)C4CCN(CC4)CC5CC5
CHEMBL3742080 5ht4r_human Human No 7.1 EC50 = 88 Funct
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
427 5 2 5 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CC4CCC(C3)N4CC5(CCOCC5)O
CHEMBL3742080 5ht4r_human Human No 7.1 EC50 = 88 Funct
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
427 5 2 5 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NC3CC4CCC(C3)N4CC5(CCOCC5)O
CHEMBL442869 5ht4r_human Human No 8.1 EC50 = 9 Funct
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
984 30 6 14 5.6 COC1=CC(=C(C=C1C(=O)OCCN2CCC(CC2)NC(=O)CCCNCCCC3=CC=C(C=C3)CCCNCCCC(=O)NC4CCN(CC4)CCOC(=O)C5=CC(=C(C=C5OC)N)Cl)Cl)N
CHEMBL442869 5ht4r_human Human No 8.1 EC50 = 9 Funct
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
984 30 6 14 5.6 COC1=CC(=C(C=C1C(=O)OCCN2CCC(CC2)NC(=O)CCCNCCCC3=CC=C(C=C3)CCCNCCCC(=O)NC4CCN(CC4)CCOC(=O)C5=CC(=C(C=C5OC)N)Cl)Cl)N
CHEMBL3741787 5ht4r_human Human No 8.0 EC50 = 9.7 Funct
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
440 6 1 5 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)C5CCN(CC5)C(=O)OC
CHEMBL3741787 5ht4r_human Human No 8.0 EC50 = 9.7 Funct
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
440 6 1 5 3.4 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3C4C3CN(C4)C5CCN(CC5)C(=O)OC
CHEMBL350221 5ht4r_rat Rat Yes 8.0 EC50 = 9.8 Funct
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
220 3 4 4 -1.2 C1=CC2=C(C=C1O)C(=CN2)CC(C(=O)O)N
CHEMBL3741733 5ht4r_human Human No 8.0 EC50 = 9.8 Funct
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
354 5 1 3 4.3 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CCN(CC3)C4CCC4
CHEMBL3741733 5ht4r_human Human No 8.0 EC50 = 9.8 Funct
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
354 5 1 3 4.3 CC(C)C1=NC(=C2N1C=CC=C2)C(=O)NCC3CCN(CC3)C4CCC4
CHEMBL585567 5ht4r_human Human No 7.1 EC50 = 90 Funct
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
518 7 4 7 3.2 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCCCC3(C4=CC(=CC=C4)O)O
CHEMBL585567 5ht4r_human Human No 7.1 EC50 = 90 Funct
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
518 7 4 7 3.2 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCCCC3(C4=CC(=CC=C4)O)O
CHEMBL2448558 5ht4r_rat Rat No 7.0 EC50 = 98 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
324 3 2 4 2.1 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N
CHEMBL2448558 5ht4r_rat Rat No 7.0 EC50 = 98 Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
324 3 2 4 2.1 COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N
CHEMBL159825 5ht4r_rat Rat No 7.0 EC50 = 98 Funct
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
310 3 2 4 1.7 COC1=CC(=C(C=C1C(=O)NC2CCN3CCC2C3)Cl)N
CHEMBL358119 5ht4r_cavpo Guinea pig No 10.6 IC50 = 0.0 Funct
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
370 7 0 4 4.3 CCCCN1CCC(CC1)COC(=O)C2=C3N(CCCO3)C4=CC=CC=C42
CHEMBL358119 5ht4r_cavpo Guinea pig No 10.6 IC50 = 0.0 Funct
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)
370 7 0 4 4.3 CCCCN1CCC(CC1)COC(=O)C2=C3N(CCCO3)C4=CC=CC=C42
CHEMBL68131 5ht4r_cavpo Guinea pig Yes 10.1 IC50 = 0.1 Funct
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
383 7 1 6 3.5 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)N)Cl
CHEMBL68131 5ht4r_cavpo Guinea pig Yes 10.1 IC50 = 0.1 Funct
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)
383 7 1 6 3.5 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)N)Cl
CHEMBL145075 5ht4r_cavpo Guinea pig No 10.0 IC50 = 0.1 Funct
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
356 7 0 4 3.9 CCCCN1CCC(CC1)COC(=O)C2=C3N(CCO3)C4=CC=CC=C42
CHEMBL142490 5ht4r_cavpo Guinea pig No 10.0 IC50 = 0.1 Funct
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
344 8 1 4 4.2 CCCCN1CCC(CC1)COC(=O)C2=C(NC3=CC=CC=C32)OC
CHEMBL145075 5ht4r_cavpo Guinea pig No 10.0 IC50 = 0.1 Funct
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)
356 7 0 4 3.9 CCCCN1CCC(CC1)COC(=O)C2=C3N(CCO3)C4=CC=CC=C42
CHEMBL68131 5ht4r_cavpo Guinea pig Yes 10.0 IC50 = 0.1 Funct
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)
383 7 1 6 3.5 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)N)Cl
CHEMBL143862 5ht4r_cavpo Guinea pig No 9.8 IC50 = 0.2 Funct
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
385 7 0 4 4.6 CCCCN1CCC(CC1)COC(=O)C2=C3N(CCCCO3)C4=CC=CC=C42
CHEMBL143862 5ht4r_cavpo Guinea pig No 9.8 IC50 = 0.2 Funct
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)
385 7 0 4 4.6 CCCCN1CCC(CC1)COC(=O)C2=C3N(CCCCO3)C4=CC=CC=C42
CHEMBL1358628 5ht4r_human Human Yes 9.4 IC50 = 0.4 Funct
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).
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_human Human Yes 9.4 IC50 = 0.4 Funct
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).
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_human Human Yes 9.4 IC50 = 0.4 Funct
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).
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL143426 5ht4r_cavpo Guinea pig No 9.3 IC50 = 0.5 Funct
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
314 7 1 3 4.7 CCCCN1CCC(CC1)COC(=O)C2=CNC3=CC=CC=C32
CHEMBL143426 5ht4r_cavpo Guinea pig No 9.3 IC50 = 0.5 Funct
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)
314 7 1 3 4.7 CCCCN1CCC(CC1)COC(=O)C2=CNC3=CC=CC=C32
CHEMBL35226 5ht4r_mouse Mouse No 9.3 IC50 = 0.6 Funct
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
339 5 1 4 4.5 CCCN1CCC(CC1)COC2=NC3=CC=CC=C3C4=C2CCCN4
CHEMBL356359 5ht4r_human Human Yes 9.2 IC50 = 0.6 Funct
Binding affinity was determined against 5-hydroxytryptamine 3 receptorBinding affinity was determined against 5-hydroxytryptamine 3 receptor
370 6 1 3 3.7 CCCCN1CCC(CC1)CNC(=O)C2=C3N(CCCO3)C4=CC=CC=C42
CHEMBL334818 5ht4r_cavpo Guinea pig No 9.0 IC50 = 1 Funct
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)
355 8 1 5 3.7 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL3220223 5ht4r_human Human No 8.9 IC50 = 1.4 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
468 8 1 8 2.8 COC1=CC(=C(C=C1C(=O)OCCN2CCN(CC2)C3=CC=CC=C3C4=NC=CN=C4)Cl)N
CHEMBL3220223 5ht4r_human Human No 8.9 IC50 = 1.4 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
468 8 1 8 2.8 COC1=CC(=C(C=C1C(=O)OCCN2CCN(CC2)C3=CC=CC=C3C4=NC=CN=C4)Cl)N
CHEMBL130809 5ht4r_cavpo Guinea pig No 8.0 IC50 = 10 Funct
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)
354 7 2 4 3.9 CCCCN1CCC(CC1)CNC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL123377 5ht4r_cavpo Guinea pig No 7.0 IC50 = 100 Funct
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
390 7 1 6 3.3 COC1=CC(=C(C=C1C(=O)OCCN2CCN(CC2)C3=CC=CC=C3)Cl)N
CHEMBL160237 5ht4r_cavpo Guinea pig No 7.0 IC50 = 100 Funct
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
417 8 1 6 3.6 COC1=CC(=C(C=C1C(=O)OCCN2CCC(CC2)C(=O)C3=CC=CC=C3)Cl)N
CHEMBL56994 5ht4r_cavpo Guinea pig No 6.0 IC50 = 1000 Funct
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
324 3 2 4 2.2 CN1CC2CCC1CC2NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL57686 5ht4r_cavpo Guinea pig No 6.0 IC50 = 1000 Funct
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
324 3 2 4 2.2 CN1CC2CCC1C(C2)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL1550957 5ht4r_cavpo Guinea pig Yes 6.0 IC50 = 1000 Funct
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptorDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor
212 1 2 1 2.2 CC1=C(C2=CC=CC=C2N1)C3=CCNCC3
CHEMBL99577 5ht4r_cavpo Guinea pig No 6.0 IC50 = 1000 Funct
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
303 3 2 4 0.8 CN1CCN(CC1)CCNC(=O)N2C3=CC=CC=C3NC2=O
CHEMBL49072 5ht4r_cavpo Guinea pig No 6.0 IC50 = 1000 Funct
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.
316 8 2 5 2.2 CCN(CC)CCOC(=O)NC1=C(C=C(C(=C1)Cl)N)OC
CHEMBL10 5ht4r_cavpo Guinea pig Yes 5.0 IC50 = 10553 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
377 4 1 5 3.2 CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F
CHEMBL10 5ht4r_cavpo Guinea pig Yes 5.0 IC50 = 10553 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
377 4 1 5 3.2 CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F
CHEMBL177573 5ht4r_cavpo Guinea pig No 8.0 IC50 = 11.2 Funct
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
466 10 3 6 2.6 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CC3CCN(CC3)CCCCCN)Cl)N
CHEMBL3291078 5ht4r_human Human No 7.0 IC50 = 110 Funct
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
353 5 0 5 2.7 COC1=NC2=CC=CC3=C2C(=C1)C(=O)N(C3=O)CCCN4CCCCC4
CHEMBL3291078 5ht4r_human Human No 7.0 IC50 = 110 Funct
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
353 5 0 5 2.7 COC1=NC2=CC=CC3=C2C(=C1)C(=O)N(C3=O)CCCN4CCCCC4
CHEMBL3758523 5ht4r_human Human No 6.0 IC50 = 1121 Funct
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
424 8 2 8 1.5 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3N=CN=N3
CHEMBL3758523 5ht4r_human Human No 6.0 IC50 = 1121 Funct
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
424 8 2 8 1.5 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3N=CN=N3
CHEMBL60889 5ht4r_cavpo Guinea pig Yes 7.0 IC50 = 113 Funct
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
422 7 2 6 2.8 CCOC1=CC(=C(C=C1C(=O)NCC2CN(CCO2)CC3=CC=C(C=C3)F)Cl)N
CHEMBL728 5ht4r_cavpo Guinea pig Yes 5.9 IC50 = 1164 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
374 4 0 4 4.9 CN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL3758199 5ht4r_human Human No 5.9 IC50 = 1165 Funct
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
422 8 2 6 1.3 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3C=CN=C3
CHEMBL3758199 5ht4r_human Human No 5.9 IC50 = 1165 Funct
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
422 8 2 6 1.3 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3C=CN=C3
CHEMBL3759944 5ht4r_human Human No 6.9 IC50 = 118 Funct
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
495 7 2 6 2.9 CC(C)(C)C(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759944 5ht4r_human Human No 6.9 IC50 = 118 Funct
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
495 7 2 6 2.9 CC(C)(C)C(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL53463 5ht4r_cavpo Guinea pig Yes 4.9 IC50 = 12468 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
544 5 6 12 1.3 CC1C(C(CC(O1)OC2CC(CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=O)CO)O)N)O
CHEMBL53463 5ht4r_cavpo Guinea pig Yes 4.9 IC50 = 12468 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
544 5 6 12 1.3 CC1C(C(CC(O1)OC2CC(CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=O)CO)O)N)O
CHEMBL3759601 5ht4r_human Human No 5.9 IC50 = 1271 Funct
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
423 8 2 7 1.3 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3C=NC=N3
CHEMBL3759601 5ht4r_human Human No 5.9 IC50 = 1271 Funct
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
423 8 2 7 1.3 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCN3C=NC=N3
CHEMBL174935 5ht4r_cavpo Guinea pig No 7.9 IC50 = 13.4 Funct
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
438 8 3 6 1.9 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CC3CCN(CC3)CCCN)Cl)N
CHEMBL3758641 5ht4r_human Human No 6.9 IC50 = 134 Funct
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
497 9 2 7 2.8 CCCOC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759860 5ht4r_human Human No 6.9 IC50 = 134 Funct
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
481 7 2 6 2.6 CC(C)C(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3758641 5ht4r_human Human No 6.9 IC50 = 134 Funct
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
497 9 2 7 2.8 CCCOC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759860 5ht4r_human Human No 6.9 IC50 = 134 Funct
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
481 7 2 6 2.6 CC(C)C(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL806 5ht4r_cavpo Guinea pig Yes 4.9 IC50 = 13545 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
276 2 1 6 3.3 CC(C)C(=O)NC1=CC(=C(C=C1)[N+](=O)[O-])C(F)(F)F
CHEMBL368844 5ht4r_cavpo Guinea pig No 7.9 IC50 = 14.3 Funct
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
452 8 3 6 2.3 CC(CN)CN1CCC(CC1)CN2CCC(CC2)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL426216 5ht4r_cavpo Guinea pig No 7.9 IC50 = 14.3 Funct
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
424 7 3 6 1.6 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CC3CCN(CC3)CCN)Cl)N
CHEMBL433984 5ht4r_cavpo Guinea pig No 7.8 IC50 = 14.4 Funct
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
454 8 4 7 0.9 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CC3CCN(CC3)CC(CN)O)Cl)N
CHEMBL493677 5ht4r_human Human Yes 5.9 IC50 = 1400 Funct
Inhibition of 5HT4 receptorInhibition of 5HT4 receptor
389 6 1 3 5.4 CC(C)(C)CCN1CCC(C(C1)F)CNC(=O)C2=CC(=CC(=C2)Cl)Cl
CHEMBL493677 5ht4r_human Human Yes 5.9 IC50 = 1400 Funct
Inhibition of 5HT4 receptorInhibition of 5HT4 receptor
389 6 1 3 5.4 CC(C)(C)CCN1CCC(C(C1)F)CNC(=O)C2=CC(=CC(=C2)Cl)Cl
CHEMBL1306 5ht4r_cavpo Guinea pig Yes 4.8 IC50 = 14780 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
532 8 0 7 4.8 CC(C)N1CCN(CC1)C2=CC=C(C=C2)OCC3COC(O3)(CN4C=NC=N4)C5=C(C=C(C=C5)Cl)Cl
CHEMBL1306 5ht4r_cavpo Guinea pig Yes 4.8 IC50 = 14780 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
532 8 0 7 4.8 CC(C)N1CCN(CC1)C2=CC=C(C=C2)OCC3COC(O3)(CN4C=NC=N4)C5=C(C=C(C=C5)Cl)Cl
CHEMBL356546 5ht4r_cavpo Guinea pig No 7.8 IC50 = 15.9 Funct
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
355 6 1 3 3.3 CCCCN1CCC(CC1)CNC(=O)C2=C3N(CCO3)C4=CC=CC=C42
CHEMBL155682 5ht4r_cavpo Guinea pig No 6.8 IC50 = 150 Funct
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
341 6 1 5 3.4 CC1(CCCN(C1)CCOC(=O)C2=CC(=C(C=C2OC)N)Cl)C
CHEMBL3758674 5ht4r_human Human No 6.8 IC50 = 155 Funct
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
497 7 2 6 3.2 CC(C)C(=S)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3758674 5ht4r_human Human No 6.8 IC50 = 155 Funct
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
497 7 2 6 3.2 CC(C)C(=S)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL127876 5ht4r_human Human No 6.8 IC50 = 162 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
424 7 1 6 4.0 COC1=CC(=C(C=C1C(=O)OCCN2CCN(CC2)C3=CC(=CC=C3)Cl)Cl)N
CHEMBL127876 5ht4r_human Human No 6.8 IC50 = 162 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
424 7 1 6 4.0 COC1=CC(=C(C=C1C(=O)OCCN2CCN(CC2)C3=CC(=CC=C3)Cl)Cl)N
CHEMBL421256 5ht4r_human Human No 7.8 IC50 = 17 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
408 7 1 7 3.4 COC1=CC(=C(C=C1C(=O)OCCN2CCN(CC2)C3=CC=CC=C3F)Cl)N
CHEMBL421256 5ht4r_human Human No 7.8 IC50 = 17 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
408 7 1 7 3.4 COC1=CC(=C(C=C1C(=O)OCCN2CCN(CC2)C3=CC=CC=C3F)Cl)N
CHEMBL3759546 5ht4r_human Human No 6.8 IC50 = 178 Funct
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
481 8 2 6 2.3 CCCC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759546 5ht4r_human Human No 6.8 IC50 = 178 Funct
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
481 8 2 6 2.3 CCCC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL339936 5ht4r_human Human No 7.8 IC50 = 18 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
420 8 1 7 3.3 COC1=CC=C(C=C1)N2CCN(CC2)CCOC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL339936 5ht4r_human Human No 7.8 IC50 = 18 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
420 8 1 7 3.3 COC1=CC=C(C=C1)N2CCN(CC2)CCOC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL299408 5ht4r_cavpo Guinea pig No 6.8 IC50 = 180 Funct
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.
356 6 2 5 3.2 CC1CC(CN(C1)CCOC(=O)NC2=C(C=C(C(=C2)Cl)N)OC)C
CHEMBL1748 5ht4r_human Human Yes 7.7 IC50 = 19 Funct
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
314 4 3 5 0.8 COC1CNCCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL1748 5ht4r_human Human Yes 7.7 IC50 = 19 Funct
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
314 4 3 5 0.8 COC1CNCCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL3759969 5ht4r_human Human No 6.7 IC50 = 190 Funct
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
469 7 2 7 1.9 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCN(CC3)C(=O)OC
CHEMBL3759969 5ht4r_human Human No 6.7 IC50 = 190 Funct
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
469 7 2 7 1.9 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCN(CC3)C(=O)OC
CHEMBL3291079 5ht4r_human Human No 6.7 IC50 = 195 Funct
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
344 4 0 3 3.4 C1CCN(CC1)CCCN2CC3=C4C(=CC=C3)N=C(C=C4C2=O)Cl
CHEMBL3291079 5ht4r_human Human No 6.7 IC50 = 195 Funct
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
344 4 0 3 3.4 C1CCN(CC1)CCCN2CC3=C4C(=CC=C3)N=C(C=C4C2=O)Cl
CHEMBL146386 5ht4r_cavpo Guinea pig No 6.7 IC50 = 199.5 Funct
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
313 6 2 2 3.8 CCCCN1CCC(CC1)CNC(=O)C2=CNC3=CC=CC=C32
CHEMBL174284 5ht4r_cavpo Guinea pig No 8.6 IC50 = 2.5 Funct
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
480 7 3 6 2.4 CC(C)C(C(=O)N1CCC(CC1)CN2CCC(CC2)NC(=O)C3=CC(=C(C=C3OC)N)Cl)N
CHEMBL172802 5ht4r_cavpo Guinea pig No 8.6 IC50 = 2.6 Funct
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
480 8 3 6 2.3 CCCC(C(=O)N1CCC(CC1)CN2CCC(CC2)NC(=O)C3=CC(=C(C=C3OC)N)Cl)N
CHEMBL368213 5ht4r_cavpo Guinea pig No 8.6 IC50 = 2.6 Funct
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
466 6 3 6 1.6 CC(C)(C(=O)N1CCC(CC1)CN2CCC(CC2)NC(=O)C3=CC(=C(C=C3OC)N)Cl)N
CHEMBL2179674 5ht4r_human Human No 8.6 IC50 = 2.8 Funct
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
444 7 1 5 2.5 CN1C=C2C3=CC=CC=C3N=C(C2=C1)OCC4CCN(CC4)CCC5=CC=C(C=C5)C(=O)O
CHEMBL156970 5ht4r_cavpo Guinea pig No 6.7 IC50 = 200 Funct
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
299 6 1 5 2.2 COC1=CC(=C(C=C1C(=O)OCCN2CCCC2)Cl)N
CHEMBL49266 5ht4r_cavpo Guinea pig No 6.7 IC50 = 200 Funct
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.
342 6 2 5 2.7 CC1CCN(CC1)CCOC(=O)NC2=C(C=C(C(=C2)Cl)N)OC
CHEMBL3291075 5ht4r_human Human No 6.7 IC50 = 203 Funct
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
328 7 0 5 3.6 COC1=NC2=CC=CC=C2C(=C1)C(=O)OCCCN3CCCCC3
CHEMBL3291075 5ht4r_human Human No 6.7 IC50 = 203 Funct
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
328 7 0 5 3.6 COC1=NC2=CC=CC=C2C(=C1)C(=O)OCCCN3CCCCC3
CHEMBL50852 5ht4r_cavpo Guinea pig No 6.7 IC50 = 207 Funct
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.
342 6 2 5 2.7 COC1=C(C=C(C(=C1)N)Cl)NC(=O)OCCN2CCCCCC2
CHEMBL367877 5ht4r_cavpo Guinea pig No 7.7 IC50 = 21.1 Funct
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
516 10 3 8 2.0 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CC3CCN(CC3)CCCNS(=O)(=O)C)Cl)N
CHEMBL287045 5ht4r_cavpo Guinea pig Yes 6.6 IC50 = 251.2 Funct
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)
301 8 1 5 3.2 CCN(CC)CCOC(=O)C1=CC(=C(C=C1OC)N)Cl
CHEMBL439849 5ht4r_rat Rat Yes 6.6 IC50 = 252 Funct
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
442 7 2 5 4.0 C1CN(CCN1CCCCC2=CNC3=C2C=C(C=C3)C#N)C4=CC5=C(C=C4)OC(=C5)C(=O)N
CHEMBL439849 5ht4r_rat Rat Yes 6.6 IC50 = 252 Funct
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
442 7 2 5 4.0 C1CN(CCN1CCCCC2=CNC3=C2C=C(C=C3)C#N)C4=CC5=C(C=C4)OC(=C5)C(=O)N
CHEMBL1358628 5ht4r_cavpo Guinea pig Yes 6.6 IC50 = 273 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_cavpo Guinea pig Yes 6.6 IC50 = 273 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_cavpo Guinea pig Yes 6.6 IC50 = 273 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1358628 5ht4r_cavpo Guinea pig Yes 6.6 IC50 = 273 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_cavpo Guinea pig Yes 6.6 IC50 = 273 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_cavpo Guinea pig Yes 6.6 IC50 = 273 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL125670 5ht4r_human Human No 6.5 IC50 = 296 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
424 7 1 6 4.0 COC1=CC(=C(C=C1C(=O)OCCN2CCN(CC2)C3=CC=CC=C3Cl)Cl)N
CHEMBL125670 5ht4r_human Human No 6.5 IC50 = 296 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
424 7 1 6 4.0 COC1=CC(=C(C=C1C(=O)OCCN2CCN(CC2)C3=CC=CC=C3Cl)Cl)N
CHEMBL334325 5ht4r_human Human No 8.5 IC50 = 3 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
420 8 1 7 3.3 COC1=CC=CC(=C1)N2CCN(CC2)CCOC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL334325 5ht4r_human Human No 8.5 IC50 = 3 Funct
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
420 8 1 7 3.3 COC1=CC=CC(=C1)N2CCN(CC2)CCOC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL173089 5ht4r_cavpo Guinea pig No 8.4 IC50 = 3.9 Funct
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
480 9 3 6 1.7 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CC3CCN(CC3)C(=O)CCCCN)Cl)N
CHEMBL172074 5ht4r_cavpo Guinea pig No 8.4 IC50 = 4.0 Funct
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
466 8 3 6 1.3 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CC3CCN(CC3)C(=O)CCCN)Cl)N
CHEMBL41769 5ht4r_cavpo Guinea pig No 7.5 IC50 = 30 Funct
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
311 4 1 5 2.3 COC1=CC(=C(C=C1C(=O)OC2CN3CCC2CC3)Cl)N
CHEMBL41769 5ht4r_cavpo Guinea pig No 7.5 IC50 = 30 Funct
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
311 4 1 5 2.3 COC1=CC(=C(C=C1C(=O)OC2CN3CCC2CC3)Cl)N
CHEMBL351570 5ht4r_cavpo Guinea pig No 6.5 IC50 = 300 Funct
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
343 6 1 6 2.2 CC1CN(CC(O1)C)CCOC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL56564 5ht4r_cavpo Guinea pig Yes 5.5 IC50 = 3162.3 Funct
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)
284 3 1 3 3.8 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43
CHEMBL56564 5ht4r_cavpo Guinea pig Yes 6.5 IC50 = 324 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
284 3 1 3 3.8 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43
CHEMBL3759259 5ht4r_human Human No 6.5 IC50 = 329 Funct
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
467 7 2 6 2.0 CCC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759259 5ht4r_human Human No 6.5 IC50 = 329 Funct
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
467 7 2 6 2.0 CCC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3758398 5ht4r_human Human No 6.4 IC50 = 377 Funct
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
483 8 2 7 2.3 CCOC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3758398 5ht4r_human Human No 6.4 IC50 = 377 Funct
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
483 8 2 7 2.3 CCOC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL1108 5ht4r_cavpo Guinea pig Yes 5.4 IC50 = 3789 Funct
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
379 6 1 4 3.5 C1CN(CC=C1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F
CHEMBL571799 5ht4r_human Human No 5.4 IC50 = 3900 Funct
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
532 8 3 7 3.6 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCCCC3(C4=CC(=CC=C4)OC)O
CHEMBL571799 5ht4r_human Human No 5.4 IC50 = 3900 Funct
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
532 8 3 7 3.6 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCCCC3(C4=CC(=CC=C4)OC)O
CHEMBL176672 5ht4r_cavpo Guinea pig No 7.4 IC50 = 40.6 Funct
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
454 8 4 7 0.9 COC1=CC(=C(C=C1C(=O)NCC(CN2CCC(CC2)CN3CCC(CC3)N)O)Cl)N
CHEMBL366986 5ht4r_cavpo Guinea pig No 6.4 IC50 = 425.4 Funct
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
480 7 3 6 0.5 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)C(=O)C3CCN(CC3)C(=O)CCCN)Cl)N
CHEMBL267615 5ht4r_cavpo Guinea pig Yes 7.4 IC50 = 44 Funct
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
246 5 1 2 3.2 CCC1=C(C2=C(N1)C=CC(=C2)OC)CCN(C)C
CHEMBL267615 5ht4r_cavpo Guinea pig Yes 7.4 IC50 = 44 Funct
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
246 5 1 2 3.2 CCC1=C(C2=C(N1)C=CC(=C2)OC)CCN(C)C
CHEMBL288199 5ht4r_cavpo Guinea pig No 6.4 IC50 = 450 Funct
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
311 4 1 5 2.3 COC1=CC(=C(C=C1C(=O)OC2CN3CCC2CC3)Cl)N
CHEMBL288199 5ht4r_cavpo Guinea pig No 6.4 IC50 = 450 Funct
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
311 4 1 5 2.3 COC1=CC(=C(C=C1C(=O)OC2CN3CCC2CC3)Cl)N
CHEMBL3291080 5ht4r_human Human No 6.3 IC50 = 453 Funct
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
358 4 0 4 3.4 C1CCN(CC1)CCCN2C(=O)C3=C4C(=CC=C3)N=C(C=C4C2=O)Cl
CHEMBL3291080 5ht4r_human Human No 6.3 IC50 = 453 Funct
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
358 4 0 4 3.4 C1CCN(CC1)CCCN2C(=O)C3=C4C(=CC=C3)N=C(C=C4C2=O)Cl
CHEMBL570487 5ht4r_human Human No 5.3 IC50 = 4600 Funct
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
532 8 3 7 3.6 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCCCC3(C4=CC(=CC=C4)OC)O
CHEMBL570487 5ht4r_human Human No 5.3 IC50 = 4600 Funct
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
532 8 3 7 3.6 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCCCC3(C4=CC(=CC=C4)OC)O
CHEMBL1358628 5ht4r_human Human Yes 6.3 IC50 = 483 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_human Human Yes 6.3 IC50 = 483 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_human Human Yes 6.3 IC50 = 483 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1358628 5ht4r_human Human Yes 6.3 IC50 = 483 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 5ht4r_human Human Yes 6.3 IC50 = 483 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 5ht4r_human Human Yes 6.3 IC50 = 483 Funct
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
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL3759348 5ht4r_human Human No 6.3 IC50 = 493 Funct
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
467 7 2 6 2.0 CCC(=O)N1CCCC(C1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759348 5ht4r_human Human No 6.3 IC50 = 493 Funct
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
467 7 2 6 2.0 CCC(=O)N1CCCC(C1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL172899 5ht4r_cavpo Guinea pig No 8.3 IC50 = 5.1 Funct
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
452 6 3 6 1.4 CC(C(=O)N1CCC(CC1)CN2CCC(CC2)NC(=O)C3=CC(=C(C=C3OC)N)Cl)N
CHEMBL425329 5ht4r_cavpo Guinea pig No 8.3 IC50 = 5.1 Funct
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
466 7 3 6 1.5 CC(CN)C(=O)N1CCC(CC1)CN2CCC(CC2)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL130118 5ht4r_cavpo Guinea pig No 7.3 IC50 = 50.1 Funct
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)
347 7 0 5 3.9 CCCCN1CCC(CC1)COC(=O)C2=C3C(=CC=C2)OCCCO3
CHEMBL572038 5ht4r_human Human No 5.3 IC50 = 5000 Funct
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
476 9 3 6 3.5 CN(CCNC(=O)C1=CC(=C(C=C1OC)N)Cl)CC2CCCCC2(C3=CC(=CC=C3)OC)O
CHEMBL572038 5ht4r_human Human No 5.3 IC50 = 5000 Funct
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
476 9 3 6 3.5 CN(CCNC(=O)C1=CC(=C(C=C1OC)N)Cl)CC2CCCCC2(C3=CC(=CC=C3)OC)O
CHEMBL3759759 5ht4r_human Human No 7.3 IC50 = 52 Funct
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
482 6 2 6 1.5 CN(C)C(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759759 5ht4r_human Human No 7.3 IC50 = 52 Funct
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
482 6 2 6 1.5 CN(C)C(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3758945 5ht4r_human Human No 6.3 IC50 = 560 Funct
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
453 7 2 6 1.5 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCC(=O)N3CCCCC3
CHEMBL3758945 5ht4r_human Human No 6.3 IC50 = 560 Funct
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
453 7 2 6 1.5 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCC(=O)N3CCCCC3
CHEMBL3758721 5ht4r_human Human No 5.2 IC50 = 5759 Funct
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
407 7 2 5 1.6 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCN3C=CC=C3
CHEMBL3758721 5ht4r_human Human No 5.2 IC50 = 5759 Funct
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
407 7 2 5 1.6 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCN3C=CC=C3
CHEMBL3759362 5ht4r_human Human No 6.2 IC50 = 592 Funct
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
453 6 2 6 1.5 CC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3759362 5ht4r_human Human No 6.2 IC50 = 592 Funct
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
453 6 2 6 1.5 CC(=O)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3758397 5ht4r_human Human No 6.2 IC50 = 593 Funct
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
483 7 2 6 2.6 CCC(=S)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL3758397 5ht4r_human Human No 6.2 IC50 = 593 Funct
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
483 7 2 6 2.6 CCC(=S)N1CCC(CC1)CN2CCC(C(C2)OC)NC(=O)C3=CC(=C(C=C3OC)N)Cl
CHEMBL369037 5ht4r_cavpo Guinea pig No 8.2 IC50 = 6.5 Funct
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
452 9 3 6 2.3 COC1=CC(=C(C=C1C(=O)NC2CCN(CC2)CC3CCN(CC3)CCCCN)Cl)N
CHEMBL34224 5ht4r_cavpo Guinea pig Yes 7.2 IC50 = 60 Funct
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
299 4 1 5 2.3 CN1CCC(CC1)OC(=O)C2=CC(=C(C=C2OC)N)Cl
CHEMBL160705 5ht4r_cavpo Guinea pig No 6.2 IC50 = 600 Funct
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
273 6 1 5 1.7 CN(C)CCOC(=O)C1=CC(=C(C=C1OC)N)Cl
CHEMBL569585 5ht4r_human Human No 5.2 IC50 = 6100 Funct
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
532 8 3 7 3.6 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCCCC3(C4=CC(=CC=C4)OC)O
CHEMBL569585 5ht4r_human Human No 5.2 IC50 = 6100 Funct
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
532 8 3 7 3.6 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CC3CCCCC3(C4=CC(=CC=C4)OC)O
CHEMBL364005 5ht4r_cavpo Guinea pig Yes 6.2 IC50 = 620 Funct
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
247 1 2 1 2.8 CC1=C(C2=C(N1)C=CC(=C2)Cl)C3=CCNCC3
CHEMBL364005 5ht4r_cavpo Guinea pig Yes 6.2 IC50 = 620 Funct
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
247 1 2 1 2.8 CC1=C(C2=C(N1)C=CC(=C2)Cl)C3=CCNCC3
CHEMBL132826 5ht4r_cavpo Guinea pig No 7.2 IC50 = 63.1 Funct
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-medi