GPCRdb

Ligand source activities (1 row/activity)

ChEMBL ID	Receptor	Species	Purchasable	p-value (-log)	Activity Type	Activity Relation	Activity Value	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

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Ligand source activities (1 row/activity)