Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL4215329 5ht4r_human Human No 10.0 EC50 = 0.1 nM Bind
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
398 6 1 5 3.3 CC(C)c1cc2cccc(C(=O)NCC3CCN(CC4CCOCC4)CC3)n2n1
CHEMBL1258451 5ht4r_human Human No 9.8 EC50 = 0.2 nM 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 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)cc2OC)CC1
CHEMBL2152922 5ht4r_human Human Yes 9.7 EC50 = 0.2 nM 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
432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1
CHEMBL2152922 5ht4r_human Human Yes 9.6 EC50 = 0.3 nM Bind
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1
CHEMBL2152922 5ht4r_human Human Yes 9.6 EC50 = 0.3 nM 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
432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1
CHEMBL4206847 5ht4r_human Human No 9.5 EC50 = 0.3 nM Bind
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
372 8 1 5 2.9 COCCCN1CCC(CNC(=O)c2cccc3cc(C(C)C)nn23)CC1
CHEMBL4217381 5ht4r_human Human No 9.5 EC50 = 0.3 nM Bind
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
412 6 2 5 3.6 CC(C)c1cn2cccc(C(=O)NCC3CCN(CC4(O)CCCCC4)CC3)c2n1
CHEMBL2152922 5ht4r_human Human Yes 9.4 EC50 = 0.4 nM 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
432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1
CHEMBL2179583 5ht4r_human Human No 9.4 EC50 = 0.4 nM 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
448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL2059588 5ht4r_human Human No 9.4 EC50 = 0.4 nM 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
532 8 2 8 1.3 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)c2ccccc21
CHEMBL538635 5ht4r_human Human No 9.4 EC50 = 0.4 nM 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 8 2 8 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL538635 5ht4r_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
559 8 2 8 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL539713 5ht4r_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
549 12 2 6 4.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCC[C@@H]2C(N)=O)cc2ccccc21
CHEMBL2402900 5ht4r_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
465 9 3 6 1.4 CC(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN(C)S(C)(=O)=O)CC3)cccc2[nH]1
CHEMBL2179580 5ht4r_human Human No 9.4 EC50 = 0.4 nM 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
446 7 2 8 2.8 O[C@@H]1CC[C@@H](Oc2cccc3onc(OCC4CCN(CC5(O)CCOCC5)CC4)c23)C1
CHEMBL4211044 5ht4r_human Human No 9.4 EC50 = 0.4 nM Bind
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
414 6 2 6 2.4 CC(C)c1cn2cccc(C(=O)NCC3CCN(CC4(O)CCOCC4)CC3)c2n1
CHEMBL2152922 5ht4r_human Human Yes 9.3 EC50 = 0.5 nM 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
432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1
CHEMBL3741376 5ht4r_human Human No 9.3 EC50 = 0.5 nM 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
430 5 2 7 2.2 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2ccccc21
CHEMBL2402904 5ht4r_human Human Yes 9.3 EC50 = 0.5 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C
CHEMBL2152922 5ht4r_rat Rat Yes 9.2 EC50 = 0.6 nM 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
432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1
CHEMBL4208302 5ht4r_human Human No 9.2 EC50 = 0.6 nM Bind
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
398 6 1 5 3.3 CC(C)c1cn2cccc(C(=O)NCC3CCN(CC4CCOCC4)CC3)c2n1
CHEMBL4213334 5ht4r_human Human No 9.2 EC50 = 0.6 nM Bind
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
455 6 1 6 3.4 COC(=O)N1CCC(CN2CCC(CNC(=O)c3cccn4cc(C(C)C)nc34)CC2)CC1
CHEMBL2152922 5ht4r_rat Rat Yes 9.2 EC50 = 0.6 nM 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
432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1
CHEMBL2087337 5ht4r_human Human No 9.2 EC50 = 0.6 nM 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
504 8 2 7 1.6 O[C@@H](CN(S(=O)(=O)C)C)CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)c1cc2ccccc2n(c1=O)C(C)C
CHEMBL2059583 5ht4r_human Human No 9.2 EC50 = 0.6 nM 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 10 3 8 2.0 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCC(CNS(C)(=O)=O)CC2)c2ccccc21
CHEMBL540981 5ht4r_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
627 14 2 7 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCC(CNS(C)(=O)=O)CC2)cc2ccccc21
CHEMBL553404 5ht4r_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
615 16 1 7 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN(C)CCCN(C)S(C)(=O)=O)cc2ccccc21
CHEMBL558163 5ht4r_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
581 12 2 5 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21
CHEMBL2402891 5ht4r_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
520 9 3 7 1.1 CC(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1
CHEMBL2402892 5ht4r_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
518 9 3 7 0.8 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]c(C5CC5)nc34)CC2)CC1
CHEMBL2152922 5ht4r_rat Rat Yes 9.2 EC50 = 0.7 nM 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
432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1
CHEMBL4216003 5ht4r_human Human No 9.2 EC50 = 0.7 nM Bind
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
372 6 2 5 2.7 CC(C)c1cn2cccc(C(=O)NCC3CCN(CC(C)(C)O)CC3)c2n1
CHEMBL2059582 5ht4r_human Human No 9.1 EC50 = 0.8 nM 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
509 12 1 6 5.0 COC[C@@H]1CCCN1CCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2
CHEMBL2059585 5ht4r_human Human No 9.1 EC50 = 0.8 nM 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
532 8 2 8 1.3 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCN(S(C)(=O)=O)CC2)c2ccccc21
CHEMBL2059587 5ht4r_human Human No 9.1 EC50 = 0.8 nM 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
532 8 2 8 1.3 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@H](O)CN2CCN(S(C)(=O)=O)CC2)c2ccccc21
CHEMBL551013 5ht4r_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
520 11 1 5 5.7 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCCCC2)cc2ccccc21
CHEMBL552484 5ht4r_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
567 15 3 5 6.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN(C)CCc2c[nH]c3ccccc23)CC1
CHEMBL553405 5ht4r_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
559 8 2 8 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL555222 5ht4r_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 8 1 6 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCN(c3ccccc3)CC2)cc2ccccc21
CHEMBL2402894 5ht4r_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
542 9 3 7 1.1 CC(F)(F)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1
CHEMBL2402897 5ht4r_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
490 8 2 6 1.7 CC(C)c1nc2c(C(=O)NCC3CCN(CCN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1
CHEMBL2179582 5ht4r_human Human Yes 9.1 EC50 = 0.8 nM 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 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL2179584 5ht4r_human Human No 9.1 EC50 = 0.8 nM 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 4.7 CCCCN1CCC(COc2noc3cccc(OC4CCC4)c23)CC1
CHEMBL2179582 5ht4r_human Human Yes 9.1 EC50 = 0.9 nM 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
433 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL2179583 5ht4r_human Human No 9.1 EC50 = 0.9 nM 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
448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL2179583 5ht4r_rat Rat No 9.1 EC50 = 0.9 nM 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
448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL2179583 5ht4r_rat Rat No 9.0 EC50 = 1.0 nM 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
448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL2179589 5ht4r_human Human No 9.0 EC50 = 1.0 nM 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
418 8 1 7 3.5 CC(C)COc1cccc2onc(OCC3CCN(CC4(O)CCOCC4)CC3)c12
CHEMBL2179583 5ht4r_human Human No 9.0 EC50 = 1.0 nM 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
448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL76370 5ht4r_human Human Yes 9.0 EC50 = 1 nM 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 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N
CHEMBL555210 5ht4r_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
623 15 2 5 7.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21
CHEMBL555223 5ht4r_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
571 10 2 7 3.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCC(CNS(C)(=O)=O)CC2)cc2ccccc21
CHEMBL558719 5ht4r_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
492 9 1 5 5.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2CCCCC2)cc2ccccc21
CHEMBL2402890 5ht4r_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
506 9 3 7 0.5 CCc1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1
CHEMBL2402903 5ht4r_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
475 7 2 5 2.8 CC(C)c1nc2c(C(=O)NCC3CCN(CC4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1
CHEMBL2179586 5ht4r_human Human No 9.0 EC50 = 1.1 nM 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
372 9 0 5 4.9 CCCCN1CCC(COc2noc3cccc(OCC4CCC4)c23)CC1
CHEMBL2179582 5ht4r_rat Rat Yes 8.9 EC50 = 1.2 nM 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 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL2179583 5ht4r_human Human No 8.9 EC50 = 1.2 nM 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
448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL2179585 5ht4r_human Human No 8.9 EC50 = 1.2 nM 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
372 8 0 5 5.0 CCCCN1CCC(COc2noc3cccc(OC4CCCC4)c23)CC1
CHEMBL2179587 5ht4r_human Human No 8.9 EC50 = 1.2 nM 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 4.8 CCCCN1CCC(COc2noc3cccc(OCC(C)C)c23)CC1
CHEMBL2179582 5ht4r_human Human Yes 8.9 EC50 = 1.2 nM 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 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL538706 5ht4r_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
534 12 1 5 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2CCCCC2)cc2ccccc21
CHEMBL541223 5ht4r_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
539 9 2 5 5.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN(C)CCc2c[nH]c3ccccc23)cc2ccccc21
CHEMBL541968 5ht4r_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
559 8 2 8 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@H](O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL553685 5ht4r_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
571 10 1 7 3.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL561278 5ht4r_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
525 12 3 5 5.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN(C)CCc2c[nH]c3ccccc23)CC1
CHEMBL3741376 5ht4r_human Human No 8.9 EC50 = 1.3 nM Bind
Agonist activity at 5-HT4D receptor (unknown origin)Agonist activity at 5-HT4D receptor (unknown origin)
430 5 2 7 2.2 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2ccccc21
CHEMBL2179582 5ht4r_human Human Yes 8.9 EC50 = 1.3 nM 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 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL2152922 5ht4r_human Human Yes 8.9 EC50 = 1.3 nM 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
432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1
CHEMBL4580044 5ht4r_human Human No 8.9 EC50 = 1.4 nM Funct
Partial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assayPartial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assay
432 8 2 6 4.5 COc1ccc(CN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1O
CHEMBL201621 5ht4r_rat Rat No 8.8 EC50 = 1.5 nM Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
324 4 1 5 2.6 COc1cc(N)c(Cl)cc1C(=O)OC[C@@H]1CCN2CCC[C@@H]12
CHEMBL2402904 5ht4r_human Human Yes 8.8 EC50 = 1.5 nM 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
455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C
CHEMBL2152922 5ht4r_human Human Yes 8.8 EC50 = 1.5 nM Bind
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
432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1
CHEMBL4202791 5ht4r_human Human No 8.8 EC50 = 1.5 nM Bind
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
372 8 1 5 2.9 COCCCN1CCC(CNC(=O)c2cccn3cc(C(C)C)nc23)CC1
CHEMBL2179582 5ht4r_rat Rat Yes 8.8 EC50 = 1.5 nM 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 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL2059584 5ht4r_human Human No 8.8 EC50 = 1.6 nM 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
586 13 2 7 4.2 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCC(CNS(C)(=O)=O)CC2)c2ccccc21
CHEMBL549449 5ht4r_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
543 8 1 7 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL2401750 5ht4r_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
439 6 2 4 3.4 CC(=O)N1CCC(CN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1
CHEMBL2402895 5ht4r_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
554 9 3 7 1.6 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]c(-c5ccccc5)nc34)CC2)CC1
CHEMBL2402898 5ht4r_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
470 7 2 6 2.5 COC(=O)N1CCN(CCN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1
CHEMBL2402902 5ht4r_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
429 8 3 5 2.0 CC(=O)N(C)CC(O)CN1CCC(CNC(=O)c2cccc3[nH]c(C(C)C)nc23)CC1
CHEMBL2179583 5ht4r_rat Rat No 8.8 EC50 = 1.6 nM 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
448 5 2 7 2.3 CC(C)n1c(=O)n(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL2179590 5ht4r_human Human No 8.8 EC50 = 1.7 nM 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 8 2 8 2.6 CC(C)(O)COc1cccc2onc(OCC3CCN(CC4(O)CCOCC4)CC3)c12
CHEMBL315071 5ht4r_rat Rat No 8.7 EC50 = 1.9 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
366 6 1 5 3.5 CCCCN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCC3)CC1
CHEMBL2179581 5ht4r_human Human No 8.7 EC50 = 1.9 nM 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
446 7 1 8 3.0 OC1(CN2CCC(COc3noc4cccc(OC5CCOCC5)c34)CC2)CCOCC1
CHEMBL2059577 5ht4r_human Human No 8.7 EC50 = 2.0 nM 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
453 7 2 6 3.2 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN2CCCCC2)c2ccccc21
CHEMBL561398 5ht4r_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
464 7 1 5 4.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCCCC2)cc2ccccc21
CHEMBL76370 5ht4r_human Human Yes 8.7 EC50 = 2.0 nM 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 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N
CHEMBL538635 5ht4r_human Human No 8.7 EC50 = 2.0 nM 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
559 8 2 8 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL2402901 5ht4r_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
445 8 3 6 2.2 COC(=O)N(C)CC(O)CN1CCC(CNC(=O)c2cccc3[nH]c(C(C)C)nc23)CC1
CHEMBL538635 5ht4r_human Human No 8.7 EC50 = 2.0 nM 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
559 8 2 8 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL157880 5ht4r_cavpo Guinea pig No 8.0 EC50 = 10 nM 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
328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1
CHEMBL84398 5ht4r_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
336 7 1 4 3.8 C=CCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1
CHEMBL1258338 5ht4r_human Human No 8.0 EC50 = 10 nM 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
440 7 1 6 3.9 CCCCN1CCC(COC(=O)c2cc(Br)c(NC)c3c2OCCO3)CC1
CHEMBL39 5ht4r_cavpo Guinea pig Yes 8.0 EC50 = 10 nM 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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL2059590 5ht4r_cavpo Guinea pig No 8.0 EC50 = 10 nM 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
466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1
CHEMBL558259 5ht4r_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
450 6 1 5 3.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCCCC2)cc2ccccc21
CHEMBL559050 5ht4r_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
559 12 1 7 2.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN(C)CCCN(C)S(C)(=O)=O)cc2ccccc21
CHEMBL2059590 5ht4r_human Human No 8.0 EC50 = 10 nM 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
466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1
CHEMBL3741608 5ht4r_human Human No 8.0 EC50 = 10 nM 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
398 6 1 5 3.3 CC(C)c1nc(C(=O)NCC2CCN(CC3CCOCC3)CC2)c2ccccn12
CHEMBL2402887 5ht4r_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
478 8 3 7 -0.1 CS(=O)(=O)N1CCN(CC(O)CN2CCC(CNC(=O)c3cccc4[nH]cnc34)CC2)CC1
CHEMBL2059590 5ht4r_human Human No 8.0 EC50 = 10 nM 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 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1
CHEMBL2087333 5ht4r_human Human No 8.0 EC50 = 10 nM 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 2 7 2.4 COC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2
CHEMBL2087335 5ht4r_human Human No 8.0 EC50 = 10 nM 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
504 8 2 7 1.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)S(C)(=O)=O)cc2ccccc21
CHEMBL2181171 5ht4r_human Human No 8.0 EC50 = 10 nM 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 4.3 CCCN1CCC(COc2nc3ccccc3c3ncccc23)CC1
CHEMBL62023 5ht4r_rat Rat Yes 8.0 EC50 = 10 nM 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 5 2.0 CCn1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21
CHEMBL4210983 5ht4r_human Human No 8.0 EC50 = 10.4 nM Bind
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
382 5 1 5 2.5 CC(C)c1nc(C(=O)NCC2C3CN(C4CCOCC4)CC23)n2ccccc12
CHEMBL39 5ht4r_human Human Yes 7.0 EC50 = 100 nM Funct
Activity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assayActivity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL3759944 5ht4r_rat Rat No 7.0 EC50 = 100 nM Bind
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
494 6 2 6 3.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)C(C)(C)C)CC2)C[C@H]1OC
CHEMBL551535 5ht4r_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 4 2.3 CC(C)n1c(=O)c(C(=O)NCC2CCNCC2)cc2ccccc21
CHEMBL556438 5ht4r_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
309 3 3 4 1.9 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C[C@@H]2CC[C@H](C1)N2
CHEMBL563445 5ht4r_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
394 6 2 5 2.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2CCCCC2)CC1
CHEMBL1729 5ht4r_cavpo Guinea pig Yes 7.0 EC50 = 100 nM Bind
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
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL560739 5ht4r_cavpo Guinea pig Yes 7.0 EC50 = 100 nM Bind
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
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL50852 5ht4r_cavpo Guinea pig No 7.0 EC50 = 100 nM 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.
341 5 2 5 3.4 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCCCC1
CHEMBL549998 5ht4r_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
475 12 3 6 3.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCS(=O)(=O)O)CC1
CHEMBL74656 5ht4r_rat Rat Yes 7.0 EC50 = 102.3 nM Bind
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
465 9 2 6 3.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCOc2ccc(F)cc2)C[C@H]1OC
CHEMBL3758945 5ht4r_rat Rat No 6.0 EC50 = 1047.1 nM Bind
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
452 7 2 6 2.2 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCCCC2)C[C@H]1OC
CHEMBL3739689 5ht4r_human Human No 6.0 EC50 = 1061 nM 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
382 5 1 5 2.5 CC(C)c1nc(C(=O)NC2C3CN(CC4CCOCC4)CC32)c2ccccn12
CHEMBL4208394 5ht4r_human Human No 6.0 EC50 = 1090 nM Bind
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
406 8 1 5 3.6 COCCCN1CCC(CNC(=O)c2cccn3c(Cl)c(C(C)C)nc23)CC1
CHEMBL3739862 5ht4r_human Human No 8.0 EC50 = 11 nM 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
384 5 1 5 3.1 CC(C)c1nc(C(=O)NCC2CCN(C3CCOCC3)CC2)c2ccccn12
CHEMBL92100 5ht4r_rat Rat No 8.0 EC50 = 11.1 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
322 2 1 5 2.1 Nc1c(Cl)cc(C(=O)O[C@@H]2CN3CCC2CC3)c2c1CCO2
CHEMBL3417009 5ht4r_human Human No 8.0 EC50 = 11.3 nM Bind
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
392 7 1 4 5.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl
CHEMBL34224 5ht4r_cavpo Guinea pig Yes 7.0 EC50 = 110 nM 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
298 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OC1CCN(C)CC1
CHEMBL41769 5ht4r_cavpo Guinea pig No 7.0 EC50 = 110 nM 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 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2
CHEMBL41769 5ht4r_cavpo Guinea pig No 7.0 EC50 = 110 nM 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 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2
CHEMBL15585 5ht4r_human Human No 6.0 EC50 = 1122.0 nM Bind
Tested for 5-hydroxytryptamine 4 binding affinity against zacoprideTested for 5-hydroxytryptamine 4 binding affinity against zacopride
351 3 2 4 3.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2C(C)CCCC2C1
CHEMBL301039 5ht4r_human Human No 6.0 EC50 = 1122.0 nM Bind
Tested for 5-hydroxytryptamine 4 binding affinity against zacoprideTested for 5-hydroxytryptamine 4 binding affinity against zacopride
323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C
CHEMBL157631 5ht4r_cavpo Guinea pig No 7.0 EC50 = 113 nM 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
314 5 1 6 1.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCOCC1
CHEMBL4208144 5ht4r_human Human No 6.9 EC50 = 114 nM Bind
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
396 6 1 5 2.8 CC(C)c1cn2cccc(C(=O)NCC3C4CN(CC5CCOCC5)CC34)c2n1
CHEMBL39 5ht4r_human Human Yes 7.9 EC50 = 12 nM 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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL28499 5ht4r_rat Rat Yes 7.9 EC50 = 12.6 nM Funct
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
355 1 1 4 2.8 Nc1c(Cl)cc2c3c(cccc13)C(=O)N([C@@H]1CN3CCC1CC3)C2=O
CHEMBL79637 5ht4r_human Human No 7.9 EC50 = 12.6 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
338 7 1 4 4.0 CCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1
CHEMBL114112 5ht4r_human Human Yes 7.9 EC50 = 12.6 nM 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 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N
CHEMBL2087337 5ht4r_cavpo Guinea pig No 7.9 EC50 = 12.6 nM 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
504 8 2 7 1.6 O[C@@H](CN(S(=O)(=O)C)C)CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)c1cc2ccccc2n(c1=O)C(C)C
CHEMBL2059586 5ht4r_human Human No 7.9 EC50 = 12.6 nM 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
558 11 1 7 3.5 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCN(S(C)(=O)=O)CC2)c2ccccc21
CHEMBL556235 5ht4r_human Human No 7.9 EC50 = 12.6 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 4 2.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)cc2ccccc21
CHEMBL558924 5ht4r_human Human No 7.9 EC50 = 12.6 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
515 10 2 7 1.9 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2CCN(S(C)(=O)=O)CC2)CC1
CHEMBL559746 5ht4r_human Human No 7.9 EC50 = 12.6 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
489 9 2 6 3.4 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCS(=O)(=O)O)cc2ccccc21
CHEMBL2087325 5ht4r_human Human No 7.9 EC50 = 12.6 nM 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
468 7 2 6 2.1 CC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2
CHEMBL2087328 5ht4r_human Human No 7.9 EC50 = 12.6 nM 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 4 6 1.6 CNC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2
CHEMBL76370 5ht4r_cavpo Guinea pig Yes 7.9 EC50 = 12.6 nM Bind
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 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N
CHEMBL59834 5ht4r_rat Rat Yes 7.9 EC50 = 12.6 nM 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 5 2.6 CC(C)n1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21
CHEMBL571799 5ht4r_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
531 8 3 7 3.8 COc1cccc([C@]2(O)CCCC[C@H]2CN2CC[C@@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@@H](OC)C2)c1
CHEMBL310451 5ht4r_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
325 6 2 4 2.5 COc1cc(N)c(Cl)cc1C(=O)NCCCN1CCCCC1
CHEMBL82833 5ht4r_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
296 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCNCC1
CHEMBL15585 5ht4r_human Human No 6.9 EC50 = 125.9 nM Bind
Tested for 5-hydroxytryptamine 4 binding affinity against renzaprideTested for 5-hydroxytryptamine 4 binding affinity against renzapride
351 3 2 4 3.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2C(C)CCCC2C1
CHEMBL301039 5ht4r_human Human No 6.9 EC50 = 125.9 nM Bind
Tested for 5-hydroxytryptamine 4 binding affinity against renzaprideTested for 5-hydroxytryptamine 4 binding affinity against renzapride
323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C
CHEMBL1181946 5ht4r_rat Rat No 6.9 EC50 = 129 nM Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
338 4 2 3 2.3 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CC[N@@+]2(C)CCC[C@@H]12
CHEMBL199866 5ht4r_rat Rat No 6.9 EC50 = 129 nM Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
338 4 2 3 2.3 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CC[N@@+]2(C)CCC[C@@H]12
CHEMBL156348 5ht4r_cavpo Guinea pig No 7.9 EC50 = 13 nM 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
369 6 2 6 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(C)=O)CC1
CHEMBL3741224 5ht4r_human Human No 7.9 EC50 = 13.2 nM 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
366 6 1 4 3.2 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC4CCC4)C[C@H]23)c2ccccn12
CHEMBL4215943 5ht4r_human Human No 7.9 EC50 = 13.6 nM Bind
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
370 8 1 5 2.4 COCCCN1CC2C(CNC(=O)c3nc(C(C)C)c4ccccn34)C2C1
CHEMBL4203277 5ht4r_human Human No 7.9 EC50 = 13.8 nM Bind
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
370 8 1 5 2.4 COCCCN1CC2C(CNC(=O)c3cccn4cc(C(C)C)nc34)C2C1
CHEMBL3742086 5ht4r_human Human No 6.9 EC50 = 132 nM 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 3.4 CC(C)c1nc(C(=O)NC2CCN(CC(C)(C)F)CC2)c2ccccn12
CHEMBL3740278 5ht4r_human Human No 5.9 EC50 = 1358 nM 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
416 6 1 5 3.4 CC(C)c1nc(C(=O)NCC2(F)CCN(CC3CCOCC3)CC2)c2ccccn12
CHEMBL1183709 5ht4r_rat Rat No 5.9 EC50 = 1360 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2
CHEMBL314198 5ht4r_rat Rat No 5.9 EC50 = 1360 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2
CHEMBL347235 5ht4r_cavpo Guinea pig No 7.9 EC50 = 14 nM 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
328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(O)CC1
CHEMBL325494 5ht4r_human Human No 7.9 EC50 = 14 nM Bind
Compound was tested for 5-hydroxytryptamine 4 binding affinityCompound was tested for 5-hydroxytryptamine 4 binding affinity
349 4 2 4 2.6 Nc1c(Cl)cc(C(=O)NCCC23CCCN2CCC3)c2c1CCO2
CHEMBL1258223 5ht4r_human Human No 7.9 EC50 = 14.1 nM 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
396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1
CHEMBL3740708 5ht4r_human Human No 6.8 EC50 = 144 nM 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
400 5 2 6 2.2 CC(C)c1nc(C(=O)NC2CCN(CC3(O)CCOCC3)CC2)c2ccccn12
CHEMBL3742190 5ht4r_human Human No 6.8 EC50 = 144 nM 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 5 2.3 COCCN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1
CHEMBL156349 5ht4r_cavpo Guinea pig No 7.8 EC50 = 15 nM 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
326 5 1 5 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(C)C1
CHEMBL3741826 5ht4r_human Human No 7.8 EC50 = 15.5 nM 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 4 3.5 CC(C)c1nc(C(=O)NC2CCN(CC3CCC3)CC2)c2ccccn12
CHEMBL76370 5ht4r_human Human Yes 7.8 EC50 = 15.9 nM Bind
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 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N
CHEMBL82360 5ht4r_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
324 6 1 4 3.6 CCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1
CHEMBL1258450 5ht4r_human Human No 7.8 EC50 = 15.9 nM 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 7 1 7 3.0 CCCCN1CCC(COC(=O)c2cc(C#N)c(NC)c3c2OCCO3)CC1
CHEMBL551820 5ht4r_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 5 2.2 CC(C)n1c(=O)n(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21
CHEMBL552693 5ht4r_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
369 8 3 5 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCO)CC1
CHEMBL555447 5ht4r_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
411 11 3 5 3.5 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCO)CC1
CHEMBL556595 5ht4r_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
483 9 3 5 3.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN(C)CCc2c[nH]c3ccccc23)CC1
CHEMBL560876 5ht4r_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 11 2 5 4.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCO)cc2ccccc21
CHEMBL560940 5ht4r_human Human Yes 7.8 EC50 = 15.9 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 5 1.9 CC(C)n1c(=O)n(C(=O)NCC2CCNCC2)c2ccccc21
CHEMBL288199 5ht4r_cavpo Guinea pig No 6.8 EC50 = 153 nM 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 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2
CHEMBL288199 5ht4r_cavpo Guinea pig No 6.8 EC50 = 153 nM 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 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2
CHEMBL3759348 5ht4r_rat Rat No 5.8 EC50 = 1548.8 nM Bind
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 7 2 6 2.4 CCC(=O)N1CCCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)C1
CHEMBL551614 5ht4r_human Human No 6.8 EC50 = 158.5 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 4 2.1 CC(C)n1c(=O)c(C(=O)NC2CCNCC2)cc2ccccc21
CHEMBL560597 5ht4r_human Human No 5.8 EC50 = 1584.9 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
391 6 3 6 1.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCS(=O)(=O)O)CC1
CHEMBL34291 5ht4r_rat Rat Yes 7.8 EC50 = 16.5 nM Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl
CHEMBL67554 5ht4r_rat Rat No 5.8 EC50 = 1658 nM 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
349 5 2 4 2.4 COc1cc(N)c(Cl)cc1C(=O)NCCC12CC3CN(CC3C1)C2
CHEMBL27846 5ht4r_cavpo Guinea pig No 6.8 EC50 = 166 nM 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
309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2
CHEMBL155631 5ht4r_cavpo Guinea pig No 7.8 EC50 = 17 nM 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
307 5 1 4 2.1 COc1cc(N)c(Cl)cc1C(=O)OCC[n+]1ccccc1
CHEMBL3291085 5ht4r_human Human Yes 7.8 EC50 = 17 nM Bind
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21
CHEMBL3306918 5ht4r_human Human Yes 7.8 EC50 = 17 nM Bind
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21
CHEMBL4213441 5ht4r_human Human No 7.8 EC50 = 17 nM Bind
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
370 6 2 5 2.1 CC(C)c1cn2cccc(C(=O)NCC3C4CN(CC(C)(C)O)CC34)c2n1
CHEMBL3291085 5ht4r_human Human Yes 7.8 EC50 = 17 nM 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
377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21
CHEMBL3306918 5ht4r_human Human Yes 7.8 EC50 = 17 nM 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
377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21
CHEMBL39 5ht4r_rat Rat Yes 7.8 EC50 = 17.1 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL490852 5ht4r_human Human No 7.8 EC50 = 18 nM 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
479 8 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)Cc2ccccc2Cl)CC1
CHEMBL3739931 5ht4r_human Human No 7.8 EC50 = 18 nM 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 4 2.9 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(C4CCC4)C[C@H]23)c2ccccn12
CHEMBL3741595 5ht4r_human Human No 7.8 EC50 = 18 nM 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 3.1 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC(C)(C)F)C[C@H]23)c2ccccn12
CHEMBL3740844 5ht4r_human Human No 7.7 EC50 = 18.3 nM 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 4 2.8 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(C(C)C)C[C@H]23)c2ccccn12
CHEMBL91147 5ht4r_rat Rat No 7.7 EC50 = 18.6 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
321 2 2 4 1.7 Nc1c(Cl)cc(C(=O)N[C@@H]2CN3CCC2CC3)c2c1CCO2
CHEMBL160705 5ht4r_cavpo Guinea pig No 6.8 EC50 = 180 nM 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
272 5 1 5 1.6 COc1cc(N)c(Cl)cc1C(=O)OCCN(C)C
CHEMBL156554 5ht4r_cavpo Guinea pig No 7.7 EC50 = 19 nM 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
355 6 2 6 1.3 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(N)=O)CC1
CHEMBL327798 5ht4r_rat Rat No 7.7 EC50 = 19.3 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
337 5 2 4 2.5 Nc1c(Cl)cc(C(=O)NCCCN2CCCCC2)c2c1CCO2
CHEMBL3741918 5ht4r_human Human No 7.7 EC50 = 19.8 nM 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
398 8 1 5 3.0 COCC(C)(C)CN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1
CHEMBL286136 5ht4r_human Human Yes 7.7 EC50 = 20.0 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl
CHEMBL34291 5ht4r_human Human Yes 7.7 EC50 = 20.0 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl
CHEMBL1258339 5ht4r_human Human No 7.7 EC50 = 20.0 nM 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 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(I)c(NC)c3c2OCCO3)CC1
CHEMBL74656 5ht4r_human Human Yes 7.7 EC50 = 20.0 nM 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
465 9 2 6 3.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCOc2ccc(F)cc2)C[C@H]1OC
CHEMBL550122 5ht4r_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
531 12 2 6 4.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCS(=O)(=O)O)cc2ccccc21
CHEMBL550530 5ht4r_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
473 7 2 7 0.7 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2CCN(S(C)(=O)=O)CC2)CC1
CHEMBL2087327 5ht4r_human Human No 7.7 EC50 = 20.0 nM 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 3 6 1.7 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)C(N)=O)cc2ccccc21
CHEMBL2087331 5ht4r_human Human No 7.7 EC50 = 20.0 nM 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
497 7 2 6 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CN(C)C(=O)N(C)C)cc2ccccc21
CHEMBL86 5ht4r_rat Rat Yes 5.7 EC50 = 1920 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC
CHEMBL4202922 5ht4r_human Human No 5.7 EC50 = 1941 nM Bind
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
373 8 1 6 2.3 COCCCN1CCC(CNC(=O)c2cccn3nc(C(C)C)nc23)CC1
CHEMBL4206020 5ht4r_human Human No 5.7 EC50 = 1941 nM Bind
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
373 8 1 6 2.3 COCCCN1CCC(CNC(=O)c2cccc3nc(C(C)C)nn23)CC1
CHEMBL201019 5ht4r_rat Rat No 6.7 EC50 = 195 nM Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
337 5 2 4 2.5 CCOc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN2CCC[C@@H]12
CHEMBL89259 5ht4r_rat Rat Yes 6.7 EC50 = 195 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
321 2 2 4 1.7 Nc1c(Cl)cc(C(=O)N[C@H]2CN3CCC2CC3)c2c1CCO2
CHEMBL3741703 5ht4r_human Human No 6.7 EC50 = 196 nM 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
402 5 1 5 3.2 CC(C)c1nc(C(=O)NC2CCN(CC3(F)CCOCC3)CC2)c2ccccn12
CHEMBL61130 5ht4r_human Human No 6.7 EC50 = 199.5 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 4 2.1 CC(C)n1nc(C(=O)NC2CCNCC2)c2ccccc21
CHEMBL311325 5ht4r_rat Rat No 5.7 EC50 = 1995.3 nM 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
352 9 1 4 4.6 CCCOc1cc(N)c(Cl)cc1C(=O)CCCCN1CCCCC1
CHEMBL85251 5ht4r_human Human Yes 8.7 EC50 = 2 nM 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 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL88973 5ht4r_rat Rat No 8.7 EC50 = 2.0 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
324 4 1 5 2.5 Nc1c(Cl)cc(C(=O)OCCN2CCCCC2)c2c1CCO2
CHEMBL2179582 5ht4r_rat Rat Yes 8.7 EC50 = 2.2 nM 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 4 2 5 2.4 CC1(C)C(=O)N(C(=O)NCC2CCN(CC3(O)CCOCC3)CC2)c2cc(F)ccc21
CHEMBL286136 5ht4r_human Human Yes 8.6 EC50 = 2.5 nM 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
312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl
CHEMBL83899 5ht4r_human Human Yes 8.6 EC50 = 2.5 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
417 9 2 6 2.2 COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CCNS(=O)(=O)C)Cl
CHEMBL2059578 5ht4r_human Human No 8.6 EC50 = 2.5 nM 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
479 10 1 5 5.4 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCN2CCCCC2)c2ccccc21
CHEMBL2059581 5ht4r_human Human No 8.6 EC50 = 2.5 nM 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
483 9 2 7 2.8 COC[C@@H]1CCCN1CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2
CHEMBL2059590 5ht4r_human Human No 8.6 EC50 = 2.5 nM 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 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1
CHEMBL540980 5ht4r_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
537 8 1 7 3.5 CCOC(=O)N1CCN(CCCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cc4ccccc4n(C(C)C)c2=O)C3)CC1
CHEMBL549650 5ht4r_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
466 7 1 6 3.0 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCOCC2)cc2ccccc21
CHEMBL555693 5ht4r_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
599 12 1 7 3.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL559322 5ht4r_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
522 11 1 6 4.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCOCC2)cc2ccccc21
CHEMBL76370 5ht4r_human Human Yes 8.6 EC50 = 2.5 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N
CHEMBL76370 5ht4r_human Human Yes 8.6 EC50 = 2.5 nM 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 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N
CHEMBL2402904 5ht4r_cavpo Guinea pig Yes 8.6 EC50 = 2.5 nM Bind
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
455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C
CHEMBL4526049 5ht4r_human Human No 8.6 EC50 = 2.8 nM Funct
Partial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assayPartial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assay
418 7 3 6 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccc(O)c(O)c2)CC1
CHEMBL3740472 5ht4r_human Human No 7.7 EC50 = 20 nM 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 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1
CHEMBL3740472 5ht4r_human Human No 7.7 EC50 = 20 nM 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 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1
CHEMBL3740472 5ht4r_rat Rat No 7.7 EC50 = 20 nM 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 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1
CHEMBL3740612 5ht4r_human Human No 7.7 EC50 = 20.7 nM 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
382 5 1 5 2.5 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(C4CCOCC4)C[C@H]23)c2ccccn12
CHEMBL48379 5ht4r_cavpo Guinea pig No 6.7 EC50 = 200 nM 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.
313 5 2 5 2.6 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCC1
CHEMBL28992 5ht4r_rat Rat Yes 6.7 EC50 = 203 nM 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
309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2
CHEMBL4205936 5ht4r_human Human Yes 7.7 EC50 = 21 nM Bind
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
409 5 0 7 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)n2n1
CHEMBL67555 5ht4r_rat Rat No 6.7 EC50 = 217 nM 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
335 4 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NCC12CC3CN(CC3C1)C2
CHEMBL33732 5ht4r_cavpo Guinea pig No 7.7 EC50 = 22 nM 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
312 4 1 5 2.6 CCN1CCC(OC(=O)c2cc(Cl)c(N)cc2OC)CC1
CHEMBL3740472 5ht4r_human Human No 7.7 EC50 = 22 nM 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 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1
CHEMBL3740472 5ht4r_human Human No 7.7 EC50 = 22 nM Bind
Inhibition of 5-HT4 receptor (unknown origin)Inhibition of 5-HT4 receptor (unknown origin)
370 8 1 5 2.4 COCCCN1C[C@H]2[C@H](CNC(=O)c3nc(C(C)C)n4ccccc34)[C@H]2C1
CHEMBL3742300 5ht4r_human Human No 5.7 EC50 = 2247 nM 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 5 2.4 CC(C)c1nc(C(=O)NCC2CN(C3CCC3)CCO2)c2ccccn12
CHEMBL34291 5ht4r_rat Rat Yes 7.6 EC50 = 23 nM 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
323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl
CHEMBL34291 5ht4r_rat Rat Yes 7.6 EC50 = 23.7 nM Funct
Efficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosaeEfficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosae
323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl
CHEMBL3740732 5ht4r_human Human No 7.6 EC50 = 25 nM 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 5 2.7 CC(C)c1nc(C(=O)NC2CCN(CC3CCOC3)CC2)c2ccccn12
CHEMBL557053 5ht4r_human Human No 7.6 EC50 = 25.1 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
353 7 2 4 3.3 CCCCCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1
CHEMBL559317 5ht4r_human Human No 7.6 EC50 = 25.1 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
554 9 1 6 4.8 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCN2C(=O)c3ccccc3C2=O)cc2ccccc21
CHEMBL563261 5ht4r_human Human No 7.6 EC50 = 25.1 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
425 8 2 5 3.5 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCO)cc2ccccc21
CHEMBL2087336 5ht4r_human Human No 7.6 EC50 = 25.1 nM 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
504 8 2 7 1.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@H](O)CN(C)S(C)(=O)=O)cc2ccccc21
CHEMBL2181188 5ht4r_human Human No 6.6 EC50 = 251 nM 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
368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1
CHEMBL420969 5ht4r_human Human Yes 6.6 EC50 = 251.2 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
311 5 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCCCC1
CHEMBL3758199 5ht4r_rat Rat No 6.6 EC50 = 251.2 nM Bind
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 7 2.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2ccnc2)C[C@H]1OC
CHEMBL2402888 5ht4r_human Human No 6.6 EC50 = 251.2 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
490 7 3 7 0.2 CS(=O)(=O)N1CCN(CC(O)CN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cccc4[nH]cnc24)C3)CC1
CHEMBL551743 5ht4r_human Human No 5.6 EC50 = 2511.9 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 2.2 COc1ccc2[nH]cc(C(=O)N[C@@H]3C[C@@H]4CC[C@H](C3)N4)c2c1
CHEMBL117287 5ht4r_human Human Yes 7.6 EC50 = 26 nM Bind
Agonist activity at 5-HT4E receptor (unknown origin)Agonist activity at 5-HT4E receptor (unknown origin)
367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N
CHEMBL117287 5ht4r_rat Rat Yes 7.6 EC50 = 26 nM 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
367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N
CHEMBL18041 5ht4r_cavpo Guinea pig Yes 6.6 EC50 = 260 nM 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
309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl
CHEMBL295155 5ht4r_rat Rat No 6.6 EC50 = 262 nM 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
335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2
CHEMBL295155 5ht4r_cavpo Guinea pig No 6.6 EC50 = 262 nM Bind
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
335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2
CHEMBL33676 5ht4r_cavpo Guinea pig No 7.6 EC50 = 27 nM 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
324 3 1 5 2.7 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC(C1)N2C
CHEMBL33676 5ht4r_cavpo Guinea pig No 7.6 EC50 = 27 nM 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
324 3 1 5 2.7 COc1cc(N)c(Cl)cc1C(=O)OC1CC2CCC(C1)N2C
CHEMBL156579 5ht4r_cavpo Guinea pig No 7.5 EC50 = 29 nM 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 5 1 5 2.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC=CCC1
CHEMBL1748 5ht4r_human Human Yes 6.5 EC50 = 290 nM Funct
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
313 4 3 5 1.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCNCC1OC
CHEMBL4217842 5ht4r_human Human No 6.5 EC50 = 291 nM Bind
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
416 5 1 5 3.2 CC(C)c1nn2c(C(=O)NCC3C4CN(C5CCOCC5)CC34)cccc2c1Cl
CHEMBL158238 5ht4r_cavpo Guinea pig No 8.5 EC50 = 3 nM 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
326 5 1 5 2.8 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C)CC1
CHEMBL538956 5ht4r_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
593 12 1 7 5.0 CCOC(=O)N1CCN(CCCCCCCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2cc4ccccc4n(C(C)C)c2=O)C3)CC1
CHEMBL556326 5ht4r_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
613 13 1 7 4.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL559548 5ht4r_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 12 2 6 4.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2C(=O)c3ccccc3C2=O)CC1
CHEMBL562636 5ht4r_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
478 12 2 5 5.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2CCCCC2)CC1
CHEMBL2402893 5ht4r_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
534 8 3 7 1.2 CC(C)(C)c1nc2c(C(=O)NCC3CCN(CC(O)CN4CCN(S(C)(=O)=O)CC4)CC3)cccc2[nH]1
CHEMBL2402899 5ht4r_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
454 7 2 5 2.3 CC(=O)N1CCN(CCN2CCC(CNC(=O)c3cccc4[nH]c(C(C)C)nc34)CC2)CC1
CHEMBL3739521 5ht4r_human Human No 8.5 EC50 = 3.4 nM 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 4 3.1 CC(C)c1nc(C(=O)NC2CCN(C(C)C)CC2)c2ccccn12
CHEMBL3740908 5ht4r_human Human No 8.4 EC50 = 3.9 nM 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 2.6 CC(C)c1nc(C(=O)NC2CCN(CCF)CC2)c2ccccn12
CHEMBL538635 5ht4r_human Human No 8.4 EC50 = 4.0 nM Bind
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
559 8 2 8 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL85251 5ht4r_human Human Yes 8.4 EC50 = 4.0 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL2059589 5ht4r_human Human No 8.4 EC50 = 4.0 nM 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
502 7 1 7 1.9 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCN(S(C)(=O)=O)CC2)c2ccccc21
CHEMBL558855 5ht4r_human Human No 8.4 EC50 = 4.0 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 8 2 6 2.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCN2CCC[C@@H]2C(N)=O)cc2ccccc21
CHEMBL83954 5ht4r_cavpo Guinea pig Yes 7.5 EC50 = 30 nM 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
326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl
CHEMBL49072 5ht4r_cavpo Guinea pig No 6.5 EC50 = 300 nM 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.
315 7 2 5 2.8 CCN(CC)CCOC(=O)Nc1cc(Cl)c(N)cc1OC
CHEMBL3739647 5ht4r_human Human No 7.5 EC50 = 31 nM 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
396 6 1 5 2.8 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC4CCOCC4)C[C@H]23)c2ccccn12
CHEMBL27966 5ht4r_rat Rat No 7.5 EC50 = 31.6 nM Funct
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
343 1 1 4 2.8 CN1CCC(N2C(=O)c3cccc4c(N)c(Cl)cc(c34)C2=O)CC1
CHEMBL552218 5ht4r_human Human No 7.5 EC50 = 31.6 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 4 3.3 CCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2
CHEMBL552420 5ht4r_human Human No 7.5 EC50 = 31.6 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 5 2.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCO)cc2ccccc21
CHEMBL2087329 5ht4r_human Human No 7.5 EC50 = 31.6 nM 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
483 7 3 6 1.9 CNC(=O)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2
CHEMBL3740030 5ht4r_human Human No 6.5 EC50 = 315.7 nM 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
388 8 2 6 2.1 COCCCN1CCC(O)(CNC(=O)c2nc(C(C)C)n3ccccc23)CC1
CHEMBL309655 5ht4r_human Human No 6.5 EC50 = 316.2 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
310 6 1 4 3.4 COc1cc(N)c(Cl)cc1C(=O)CCCN1CCCCC1
CHEMBL553658 5ht4r_human Human No 6.5 EC50 = 316.2 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 5 1.7 CC(C)n1c(=O)n(C(=O)NC2CCNCC2)c2ccccc21
CHEMBL37333 5ht4r_rat Rat No 6.5 EC50 = 323 nM Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
323 4 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN2CCC[C@H]12
CHEMBL303877 5ht4r_rat Rat No 5.5 EC50 = 3335 nM 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
363 4 2 4 2.1 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC1C2CC3CC1CN3C2
CHEMBL3741377 5ht4r_human Human No 7.5 EC50 = 34 nM 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 5 2.1 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC(C)(C)O)C[C@H]23)c2ccccn12
CHEMBL4203778 5ht4r_human Human No 7.5 EC50 = 34.2 nM Bind
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
340 5 1 4 2.8 CC(C)c1cn2cccc(C(=O)NCC3C4CN(C(C)C)CC34)c2n1
CHEMBL88867 5ht4r_rat Rat No 7.5 EC50 = 35.4 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
323 4 2 4 2.1 Nc1c(Cl)cc(C(=O)NCCN2CCCCC2)c2c1CCO2
CHEMBL4215651 5ht4r_human Human No 7.4 EC50 = 36 nM Bind
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
382 5 1 5 2.5 CC(C)c1cn2cccc(C(=O)NCC3C4CN(C5CCOCC5)CC34)c2n1
CHEMBL4557961 5ht4r_human Human No 6.4 EC50 = 360 nM Bind
Inhibition of 5-HT4 receptor (unknown origin)Inhibition of 5-HT4 receptor (unknown origin)
330 2 1 3 1.9 CCN1C(=O)N(C(=O)NC2CC3CCC(C2)N3C)C2C=CC=CC21
CHEMBL325603 5ht4r_mouse Mouse No 6.4 EC50 = 360 nM Bind
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 5 2.4 CCn1c(=O)n(C(=O)NC2CC3CCCC(C2)N3C)c2ccccc21
CHEMBL201414 5ht4r_rat Rat No 6.4 EC50 = 374.2 nM Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
342 3 1 5 2.4 CC(C)n1c(=O)n(C(=O)NC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21
CHEMBL3759259 5ht4r_rat Rat No 6.4 EC50 = 380.2 nM Bind
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 7 2 6 2.4 CCC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1
CHEMBL66768 5ht4r_rat Rat No 6.4 EC50 = 382 nM 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
321 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN3C2
CHEMBL315443 5ht4r_rat Rat No 6.4 EC50 = 385 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
322 2 1 5 2.1 Nc1c(Cl)cc(C(=O)O[C@H]2CN3CCC2CC3)c2c1CCO2
CHEMBL2448137 5ht4r_rat Rat No 5.4 EC50 = 3870 nM 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
321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1C2CC3CN(C2)CC31
CHEMBL3739826 5ht4r_human Human No 7.4 EC50 = 39 nM 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
384 5 2 5 3.0 CC(C)c1nc(C(=O)NC2CC3CCC(C2)N3CC(C)(C)O)c2ccccn12
CHEMBL80015 5ht4r_human Human No 7.4 EC50 = 39.8 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
310 5 1 4 3.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(C)CC1
CHEMBL83841 5ht4r_human Human No 7.4 EC50 = 39.8 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
324 7 1 4 3.8 COc1cc(N)c(Cl)cc1C(=O)CCCCN1CCCCC1
CHEMBL550064 5ht4r_human Human No 7.4 EC50 = 39.8 nM 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 4 2.6 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21
CHEMBL550064 5ht4r_human Human No 7.4 EC50 = 39.8 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 4 2.6 CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3)c2ccccc21
CHEMBL551940 5ht4r_human Human No 7.4 EC50 = 39.8 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 10 2 4 4.5 CCCCCCCCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1
CHEMBL551941 5ht4r_human Human No 7.4 EC50 = 39.8 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
409 7 1 4 4.5 CCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2
CHEMBL558261 5ht4r_human Human No 7.4 EC50 = 39.8 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
557 13 2 7 3.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCCCCN2CCN(S(C)(=O)=O)CC2)CC1
CHEMBL562400 5ht4r_human Human No 7.4 EC50 = 39.8 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 10 1 4 5.7 CCCCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2
CHEMBL83841 5ht4r_rat Rat No 7.4 EC50 = 39.8 nM 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
324 7 1 4 3.8 COc1cc(N)c(Cl)cc1C(=O)CCCCN1CCCCC1
CHEMBL539652 5ht4r_human Human Yes 6.4 EC50 = 398.1 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
297 4 3 4 1.7 COc1cc(N)c(Cl)cc1C(=O)NCC1CCNCC1
CHEMBL541969 5ht4r_human Human Yes 6.4 EC50 = 398.1 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
283 3 3 4 1.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCNCC1
CHEMBL551678 5ht4r_human Human No 6.4 EC50 = 398.1 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
433 9 3 6 2.2 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCS(=O)(=O)O)CC1
CHEMBL286136 5ht4r_cavpo Guinea pig Yes 8.4 EC50 = 4 nM 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
312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl
CHEMBL286136 5ht4r_cavpo Guinea pig Yes 8.4 EC50 = 4 nM 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
312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl
CHEMBL157880 5ht4r_cavpo Guinea pig No 8.4 EC50 = 4 nM 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
328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1
CHEMBL286136 5ht4r_cavpo Guinea pig Yes 8.4 EC50 = 4 nM Bind
Agonist activity at 5-HT4 receptor in guinea pig ileum assessed as increase in response to electrical stimulationAgonist activity at 5-HT4 receptor in guinea pig ileum assessed as increase in response to electrical stimulation
312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl
CHEMBL452353 5ht4r_human Human No 8.4 EC50 = 4 nM 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
621 11 3 9 3.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCCN2C(=O)c3cccc4c(N)ccc(c34)C2=O)CC1
CHEMBL348311 5ht4r_cavpo Guinea pig No 8.4 EC50 = 4.4 nM 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
326 5 1 5 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCCCC1
CHEMBL91771 5ht4r_rat Rat No 8.4 EC50 = 4.5 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
365 6 2 4 3.1 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)c3c2OCC3)CC1
CHEMBL121913 5ht4r_human Human No 8.4 EC50 = 4.5 nM Bind
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
391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1
CHEMBL4457426 5ht4r_human Human No 8.4 EC50 = 4.5 nM Funct
Partial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assayPartial agonist activity at human HA-tagged 5HT4 receptor expressed in COS7 cells assessed as induction of cAMP production measured after 10 mins by HTRF assay
515 11 3 7 4.2 COc1cc(/C=C/C(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)ccc1O
CHEMBL3741821 5ht4r_human Human No 8.3 EC50 = 4.8 nM 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 8 1 5 2.9 COCCCN1CCC(CNC(=O)c2nc(C(C)C)n3ccccc23)CC1
CHEMBL4203491 5ht4r_human Human No 8.3 EC50 = 4.9 nM Bind
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
455 6 1 6 3.4 COC(=O)N1CCC(CN2CCC(CNC(=O)c3nc(C(C)C)c4ccccn34)CC2)CC1
CHEMBL156965 5ht4r_cavpo Guinea pig No 7.4 EC50 = 40 nM 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
338 5 1 5 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1C2CCCC1CC2
CHEMBL156970 5ht4r_cavpo Guinea pig No 7.4 EC50 = 40 nM 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
298 5 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC1
CHEMBL3739611 5ht4r_human Human No 7.4 EC50 = 40 nM 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 5 2.4 CC(C)c1nc(C(=O)NC2CCN(CC(C)(C)O)CC2)c2ccccn12
CHEMBL3741776 5ht4r_human Human No 7.4 EC50 = 40 nM 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 5 2.7 COCCCN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1
CHEMBL324057 5ht4r_rat Rat No 7.4 EC50 = 40.3 nM 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 5 3.0 CC(C)n1c(=O)n(C(=O)NC2CC3CCCC(C2)N3C)c2ccccc21
CHEMBL4210381 5ht4r_human Human No 7.4 EC50 = 42 nM Bind
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
384 5 1 5 3.1 CC(C)c1nc(C(=O)NCC2CCN(C3CCOCC3)CC2)n2ccccc12
CHEMBL70205 5ht4r_rat Rat No 6.4 EC50 = 421 nM 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
335 4 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN3C2
CHEMBL59834 5ht4r_cavpo Guinea pig Yes 7.4 EC50 = 43 nM 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 5 2.6 CC(C)n1c(=O)n(C(=O)NC2CC3CCC(C2)N3C)c2ccccc21
CHEMBL32986 5ht4r_cavpo Guinea pig No 7.4 EC50 = 44 nM 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
312 4 1 5 2.6 CCN1CCCC(OC(=O)c2cc(Cl)c(N)cc2OC)C1
CHEMBL318154 5ht4r_rat Rat No 6.4 EC50 = 449 nM 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
337 4 2 4 2.5 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN2CCC[C@@]12C
CHEMBL3759860 5ht4r_rat Rat No 7.3 EC50 = 45.7 nM Bind
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
480 7 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)C(C)C)CC2)C[C@H]1OC
CHEMBL3741508 5ht4r_human Human No 6.3 EC50 = 467 nM 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 6 2.1 CC(C)c1nc(C(=O)NCC2CN(C3CCOCC3)CCO2)c2ccccn12
CHEMBL3739933 5ht4r_human Human No 7.3 EC50 = 47 nM 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 7 1 5 3.3 COCC(C)(C)CN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1
CHEMBL4207586 5ht4r_human Human No 7.3 EC50 = 48 nM Bind
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
342 5 1 4 3.3 CC(C)c1nc(C(=O)NCC2CCN(C(C)C)CC2)n2ccccc12
CHEMBL4207136 5ht4r_human Human No 6.3 EC50 = 484 nM Bind
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
409 5 0 7 4.1 CC(C)c1nc(-c2nnc(C3CCN(CC4CCOCC4)CC3)o2)n2ccccc12
CHEMBL3739470 5ht4r_human Human No 7.3 EC50 = 49 nM 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 4 3.1 CC(C)c1nc(C(=O)NC2CCN(CC3CC3)CC2)c2ccccn12
CHEMBL3741322 5ht4r_human Human No 7.3 EC50 = 49 nM 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 5 2.8 CC(C)c1nc(C(=O)NC2CCN(C3CCOCC3)CC2)c2ccccn12
CHEMBL39 5ht4r_cavpo Guinea pig Yes 8.3 EC50 = 5 nM 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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht4r_cavpo Guinea pig Yes 8.3 EC50 = 5 nM 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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL157880 5ht4r_cavpo Guinea pig No 8.3 EC50 = 5 nM 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
328 5 2 6 1.5 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(O)C1
CHEMBL2059579 5ht4r_human Human No 8.3 EC50 = 5.0 nM 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
441 8 2 6 3.0 CC(C)N(C)CC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2
CHEMBL2059580 5ht4r_human Human No 8.3 EC50 = 5.0 nM 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 11 1 5 5.2 CC(C)N(C)CCCCCCN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1nn(C(C)C)c3ccccc13)C2
CHEMBL557867 5ht4r_human Human No 8.3 EC50 = 5.0 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
498 9 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2C(=O)c3ccccc3C2=O)CC1
CHEMBL562902 5ht4r_human Human No 8.3 EC50 = 5.0 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
436 9 2 5 3.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCCCCN2CCCCC2)CC1
CHEMBL2087337 5ht4r_human Human No 8.3 EC50 = 5.0 nM 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
504 8 2 7 1.6 O[C@@H](CN(S(=O)(=O)C)C)CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)c1cc2ccccc2n(c1=O)C(C)C
CHEMBL2087326 5ht4r_human Human No 8.3 EC50 = 5.0 nM 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 4 6 1.3 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNC(N)=O)cc2ccccc21
CHEMBL117287 5ht4r_human Human Yes 8.3 EC50 = 5.2 nM 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 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N
CHEMBL117287 5ht4r_human Human Yes 8.3 EC50 = 5.2 nM Bind
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
367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N
CHEMBL156088 5ht4r_cavpo Guinea pig No 8.3 EC50 = 5.3 nM 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 5 1 4 2.7 COc1cc(N)c(Cl)cc1C(=O)OCC[N+]12CCC(CC1)CC2
CHEMBL86 5ht4r_cavpo Guinea pig Yes 8.2 EC50 = 5.7 nM 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 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC
CHEMBL3741548 5ht4r_human Human No 8.2 EC50 = 5.7 nM 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
384 7 2 5 2.4 CC(C)c1nc(C(=O)NC[C@H]2[C@@H]3CN(CC(C)(C)CO)C[C@H]23)c2ccccn12
CHEMBL1258671 5ht4r_human Human No 8.2 EC50 = 5.9 nM 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 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1
CHEMBL3740400 5ht4r_human Human No 7.3 EC50 = 50 nM 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 4 2.7 CCN1CCC(NC(=O)c2nc(C(C)C)n3ccccc23)CC1
CHEMBL556279 5ht4r_human Human No 7.3 EC50 = 50.1 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
596 12 1 6 5.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCCN2C(=O)c3ccccc3C2=O)cc2ccccc21
CHEMBL3740313 5ht4r_human Human No 6.3 EC50 = 500 nM 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 6 4.1 CC(C)c1nc(-c2nnc(C3CCN(C(C)C)CC3)o2)c2ccccn12
CHEMBL27846 5ht4r_rat Rat No 6.3 EC50 = 501.2 nM Funct
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2
CHEMBL539212 5ht4r_human Human Yes 6.3 EC50 = 501.2 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 5 3 5 0.6 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCNCC1
CHEMBL2448165 5ht4r_rat Rat No 7.3 EC50 = 51 nM Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C2CC3CN(C2)CC31
CHEMBL319673 5ht4r_rat Rat No 7.3 EC50 = 51 nM 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
321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CN(C2)CC31
CHEMBL558226 5ht4r_rat Rat No 7.3 EC50 = 51 nM 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
321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CN(C2)CC31
CHEMBL286136 5ht4r_human Human Yes 7.3 EC50 = 51 nM 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
312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl
CHEMBL2448165 5ht4r_rat Rat No 7.3 EC50 = 51.3 nM 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
321 3 2 4 1.6 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1C2CC3CN(C2)CC31
CHEMBL3739455 5ht4r_human Human No 6.3 EC50 = 520 nM 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
379 5 0 6 4.5 CC(C)c1nc(-c2nnc(C3CCN(CC4CCC4)CC3)o2)c2ccccn12
CHEMBL3741062 5ht4r_human Human No 7.3 EC50 = 53 nM 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
412 6 1 5 3.7 CC(C)c1nc(C(=O)NCC2(C)CCN(CC3CCOCC3)CC2)c2ccccn12
CHEMBL295155 5ht4r_rat Rat No 6.3 EC50 = 538 nM 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
335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2
CHEMBL295155 5ht4r_cavpo Guinea pig No 6.3 EC50 = 538 nM Bind
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
335 3 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN(C3)C2
CHEMBL4203494 5ht4r_human Human No 7.3 EC50 = 54 nM Bind
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
353 4 0 6 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(C(C)C)CC4)o3)n2n1
CHEMBL1729 5ht4r_rat Rat Yes 7.3 EC50 = 54.7 nM Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL560739 5ht4r_rat Rat Yes 7.3 EC50 = 54.7 nM Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL3085015 5ht4r_cavpo Guinea pig No 6.3 EC50 = 545 nM Bind
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
349 4 2 4 2.2 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN(C3)C2
CHEMBL1729 5ht4r_rat Rat Yes 7.3 EC50 = 55 nM 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
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL560739 5ht4r_rat Rat Yes 7.3 EC50 = 55 nM 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
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL28992 5ht4r_rat Rat Yes 7.3 EC50 = 55.9 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2
CHEMBL3739459 5ht4r_human Human No 7.3 EC50 = 56.7 nM 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
414 6 2 6 2.4 CC(C)c1nc(C(=O)NCC2(O)CCN(CC3CCOCC3)CC2)c2ccccn12
CHEMBL3291085 5ht4r_human Human Yes 7.2 EC50 = 58 nM 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
377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21
CHEMBL3306918 5ht4r_human Human Yes 7.2 EC50 = 58 nM 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
377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21
CHEMBL3291085 5ht4r_human Human Yes 7.2 EC50 = 58 nM Bind
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
377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21
CHEMBL3306918 5ht4r_human Human Yes 7.2 EC50 = 58 nM Bind
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
377 6 2 6 3.0 CC(C)n1c(=O)c(C(=O)NCCCN2CCCCC2)c(O)c2ccsc21
CHEMBL4212757 5ht4r_human Human No 6.2 EC50 = 598 nM Bind
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
409 5 0 7 4.1 CC(C)c1cn2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)c2n1
CHEMBL349809 5ht4r_cavpo Guinea pig No 8.2 EC50 = 6 nM 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
326 5 1 5 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCCC1C
CHEMBL4205936 5ht4r_human Human Yes 8.2 EC50 = 6 nM Bind
Agonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
409 5 0 7 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)n2n1
CHEMBL4215911 5ht4r_human Human No 8.2 EC50 = 6 nM Bind
Agonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant human 5-HT4D receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccc4cc(C(C)C)nn34)o2)CC1
CHEMBL4205936 5ht4r_rat Rat Yes 8.2 EC50 = 6 nM Bind
Agonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
409 5 0 7 4.1 CC(C)c1cc2cccc(-c3nnc(C4CCN(CC5CCOCC5)CC4)o3)n2n1
CHEMBL4215911 5ht4r_rat Rat No 8.2 EC50 = 6 nM Bind
Agonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assayAgonist activity at recombinant rat 5-HT4L receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay
383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccc4cc(C(C)C)nn34)o2)CC1
CHEMBL2179588 5ht4r_human Human No 8.2 EC50 = 6.3 nM 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
374 8 0 5 5.1 CCCCN1CCC(COc2noc3cccc(OCC(C)(C)C)c23)CC1
CHEMBL2059590 5ht4r_human Human No 8.2 EC50 = 6.3 nM Bind
5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)5-HT4C receptor-mediated exchange of GDP for europium labeled GTP (pEC50)
466 6 1 6 2.5 CC(=O)N1CCN(CCN2[C@H]3CC[C@@H]2C[C@H](NC(=O)c2nn(C(C)C)c4ccccc24)C3)CC1
CHEMBL39 5ht4r_rat Rat Yes 8.2 EC50 = 6.3 nM Funct
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL76370 5ht4r_cavpo Guinea pig Yes 8.2 EC50 = 6.3 nM 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 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N
CHEMBL76370 5ht4r_cavpo Guinea pig Yes 8.2 EC50 = 6.3 nM 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 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N
CHEMBL552075 5ht4r_human Human No 8.2 EC50 = 6.3 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
447 6 2 6 2.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCS(=O)(=O)O)cc2ccccc21
CHEMBL565146 5ht4r_human Human No 8.2 EC50 = 6.3 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
529 7 1 7 1.9 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCN(S(C)(=O)=O)CC2)cc2ccccc21
CHEMBL2087324 5ht4r_human Human No 8.2 EC50 = 6.3 nM 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
454 7 3 6 1.8 CC(=O)NCC(O)CN1[C@H]2CC[C@@H]1C[C@H](NC(=O)c1cc3ccccc3n(C(C)C)c1=O)C2
CHEMBL49266 5ht4r_cavpo Guinea pig No 7.2 EC50 = 60 nM 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.
341 5 2 5 3.2 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCC(C)CC1
CHEMBL3759928 5ht4r_rat Rat No 5.2 EC50 = 6025.6 nM Bind
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
542 9 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCC(Cc3ccccc3)CC2)C[C@H]1OC
CHEMBL4215911 5ht4r_human Human No 7.2 EC50 = 62 nM Bind
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
383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccc4cc(C(C)C)nn34)o2)CC1
CHEMBL28992 5ht4r_rat Rat Yes 7.2 EC50 = 63.1 nM Funct
5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae
309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2
CHEMBL314489 5ht4r_human Human No 7.2 EC50 = 63.1 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
380 10 1 4 5.2 CCCCCCN1CCC(CCC(=O)c2cc(Cl)c(N)cc2OC)CC1
CHEMBL562477 5ht4r_human Human No 7.2 EC50 = 63.1 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 5 3 5 1.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCO)CC1
CHEMBL2181189 5ht4r_human Human No 7.2 EC50 = 63.1 nM 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 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1
CHEMBL159825 5ht4r_rat Rat No 7.2 EC50 = 63.1 nM 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
309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCC1C2
CHEMBL563276 5ht4r_human Human No 6.2 EC50 = 631.0 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
456 6 2 6 2.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CCN2C(=O)c3ccccc3C2=O)CC1
CHEMBL2402889 5ht4r_human Human No 6.2 EC50 = 631.0 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
464 7 3 7 -0.3 CS(=O)(=O)N1CCN(CC(O)CN2CCC(NC(=O)c3cccc4[nH]cnc34)CC2)CC1
CHEMBL570780 5ht4r_human Human No 5.2 EC50 = 6309.6 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 1.9 COc1ccc2[nH]cc(C(=O)NCC3CCNCC3)c2c1
CHEMBL3740864 5ht4r_human Human No 6.2 EC50 = 633 nM 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
390 8 1 5 3.0 COCCCN1CCC(F)(CNC(=O)c2nc(C(C)C)n3ccccc23)CC1
CHEMBL4205387 5ht4r_human Human No 7.2 EC50 = 65 nM Bind
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
372 8 1 5 2.9 COCCCN1CCC(CNC(=O)c2nc(C(C)C)c3ccccn23)CC1
CHEMBL121913 5ht4r_human Human No 7.2 EC50 = 66 nM Bind
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
391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1
CHEMBL34291 5ht4r_rat Rat Yes 7.2 EC50 = 66 nM 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
323 4 2 4 2.1 COc1cc(N)c(cc1C(=O)NC[C@@H]1CCN2[C@H]1CCC2)Cl
CHEMBL70205 5ht4r_rat Rat No 6.2 EC50 = 660 nM 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
335 4 2 4 2.0 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN3C2
CHEMBL3758932 5ht4r_rat Rat No 6.2 EC50 = 676.1 nM Bind
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
420 8 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cccc2)C[C@H]1OC
CHEMBL488325 5ht4r_human Human No 7.2 EC50 = 68 nM 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
580 13 3 8 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCNS(=O)(=O)c2ccc(C)cc2)CC1
CHEMBL4218152 5ht4r_human Human No 6.2 EC50 = 687 nM Bind
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
383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3cccn4cc(C(C)C)nc34)o2)CC1
CHEMBL4210176 5ht4r_human Human No 8.1 EC50 = 7.3 nM Bind
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
370 8 1 5 2.4 COCCCN1CC2C(CNC(=O)c3cccc4cc(C(C)C)nn34)C2C1
CHEMBL91842 5ht4r_rat Rat No 8.1 EC50 = 7.4 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
338 5 1 5 2.9 Nc1c(Cl)cc(C(=O)OCCCN2CCCCC2)c2c1CCO2
CHEMBL158147 5ht4r_cavpo Guinea pig No 8.1 EC50 = 7.8 nM 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
352 5 1 5 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC2CCC(CC2)C1
CHEMBL539651 5ht4r_human Human No 8.1 EC50 = 7.9 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 6 6.1 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCCCCN2CCN(c3ccccc3)CC2)cc2ccccc21
CHEMBL550459 5ht4r_human Human No 8.1 EC50 = 7.9 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl 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 6 0.8 CC(C)n1c(=O)n(C(=O)NCCN2CCNCC2)c2ccccc21
CHEMBL2087334 5ht4r_human Human No 8.1 EC50 = 7.9 nM 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
490 8 3 7 1.2 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CC(O)CNS(C)(=O)=O)cc2ccccc21
CHEMBL3759601 5ht4r_rat Rat No 6.2 EC50 = 708.0 nM Bind
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 8 1.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cncn2)C[C@H]1OC
CHEMBL66768 5ht4r_rat Rat No 6.2 EC50 = 712 nM 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
321 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1C2CC3CC1CN3C2
CHEMBL4560185 5ht4r_human Human No 7.1 EC50 = 72 nM Bind
Inhibition of 5-HT4 receptor (unknown origin)Inhibition of 5-HT4 receptor (unknown origin)
344 2 1 3 2.3 CC(C)N1C(=O)N(C(=O)NC2CC3CCC(C2)N3C)C2C=CC=CC21
CHEMBL324057 5ht4r_mouse Mouse No 7.1 EC50 = 72 nM Bind
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 5 3.0 CC(C)n1c(=O)n(C(=O)NC2CC3CCCC(C2)N3C)c2ccccc21
CHEMBL3742145 5ht4r_human Human No 7.1 EC50 = 72.3 nM 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
388 6 3 6 1.8 CC(C)c1nc(C(=O)NCC2(O)CCN(CC(C)(C)O)CC2)c2ccccn12
CHEMBL15585 5ht4r_human Human No 7.1 EC50 = 72.4 nM Bind
Tested for 5-hydroxytryptamine 4 binding affinity against cisaprideTested for 5-hydroxytryptamine 4 binding affinity against cisapride
351 3 2 4 3.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2C(C)CCCC2C1
CHEMBL301039 5ht4r_human Human No 7.1 EC50 = 72.4 nM Bind
Tested for 5-hydroxytryptamine 4 binding affinity against cisaprideTested for 5-hydroxytryptamine 4 binding affinity against cisapride
323 3 2 4 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC(C1)N2C
CHEMBL3085015 5ht4r_cavpo Guinea pig No 7.1 EC50 = 73.6 nM Bind
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
349 4 2 4 2.2 COc1cc(N)c(Cl)cc1C(=O)NCC1C2CC3CC1CN(C3)C2
CHEMBL3739467 5ht4r_human Human No 6.1 EC50 = 736 nM 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 7 3.7 COCCCN1CCC(c2nnc(-c3nc(C(C)C)n4ccccc34)o2)CC1
CHEMBL4207406 5ht4r_human Human No 6.1 EC50 = 758 nM Bind
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
353 4 0 6 4.1 CC(C)c1nc(-c2nnc(C3CCN(C(C)C)CC3)o2)n2ccccc12
CHEMBL28992 5ht4r_cavpo Guinea pig Yes 7.1 EC50 = 77 nM 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
309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CN2CCC1CC2
CHEMBL4210213 5ht4r_human Human No 7.1 EC50 = 79 nM Bind
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
399 6 1 6 2.7 CC(C)c1nc2c(C(=O)NCC3CCN(CC4CCOCC4)CC3)cccn2n1
CHEMBL2181187 5ht4r_human Human No 7.1 EC50 = 79.4 nM 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 4.9 CCCN1CCC(COc2nc3c(OC)cccc3c3ccccc23)CC1
CHEMBL563799 5ht4r_human Human No 7.1 EC50 = 79.4 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
512 6 1 6 3.6 CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2C(=O)c3ccccc3C2=O)cc2ccccc21
CHEMBL570074 5ht4r_human Human Yes 7.1 EC50 = 79.4 nM Funct
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assayAgonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
311 4 2 4 2.1 CCN1CCC(NC(=O)c2cc(Cl)c(N)cc2OC)CC1
CHEMBL1729 5ht4r_human Human Yes 7.1 EC50 = 79.4 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL560739 5ht4r_human Human Yes 7.1 EC50 = 79.4 nM Funct
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulationAgonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL74656 5ht4r_human Human Yes 7.1 EC50 = 79.4 nM 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
465 9 2 6 3.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCOc2ccc(F)cc2)C[C@H]1OC
CHEMBL86 5ht4r_human Human Yes 6.1 EC50 = 794.3 nM Funct
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosaeAgonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC
CHEMBL86 5ht4r_rat Rat Yes 6.1 EC50 = 794.3 nM 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
299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC
CHEMBL4206608 5ht4r_human Human No 6.1 EC50 = 796 nM Bind
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
383 7 0 7 3.7 COCCCN1CCC(c2nnc(-c3nc(C(C)C)c4ccccn34)o2)CC1
CHEMBL4205273 5ht4r_human Human No 8.1 EC50 = 8.4 nM Bind
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
453 6 1 6 2.8 COC(=O)N1CCC(CN2CC3C(CNC(=O)c4cccc5cc(C(C)C)nn45)C3C2)CC1
CHEMBL4210063 5ht4r_human Human No 8.1 EC50 = 8.4 nM Bind
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
441 5 1 6 3.1 COC(=O)N1CCC(N2CCC(CNC(=O)c3cccn4cc(C(C)C)nc34)CC2)CC1
CHEMBL1185621 5ht4r_rat Rat No 8.1 EC50 = 8.5 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2
CHEMBL423504 5ht4r_rat Rat No 8.1 EC50 = 8.5 nM Funct
In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.In vitro relaxation of carbachol pre-contracted rat oesophageal TMM.
378 5 2 3 3.0 CCCC[N+]12CCC(CC1)[C@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2
CHEMBL2402904 5ht4r_cavpo Guinea pig Yes 8.1 EC50 = 8.6 nM Bind
Agonist activity at 5-HT4 receptor in guinea pig colonAgonist activity at 5-HT4 receptor in guinea pig colon
455 6 2 5 3.6 COC(=O)N1CCC(CC1)CN1CCC(CC1)CNC(=O)c1cccc2c1nc([nH]2)C(C)C
CHEMBL85251 5ht4r_rat Rat Yes 8.1 EC50 = 8.7 nM Bind
Agonist activity at 5-HT4 receptor in Sprague-Dawley rat oesophagus assessed as relaxation of carbachol precontracted oesophagusAgonist activity at 5-HT4 receptor in Sprague-Dawley rat oesophagus assessed as relaxation of carbachol precontracted oesophagus
352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL3740669 5ht4r_human Human No 8.1 EC50 = 8.7 nM 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
453 6 1 6 2.8 COC(=O)N1CCC(CN2C[C@H]3[C@H](CNC(=O)c4nc(C(C)C)n5ccccc45)[C@H]3C2)CC1
CHEMBL4212433 5ht4r_human Human No 8.1 EC50 = 8.7 nM Bind
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
396 6 1 5 2.8 CC(C)c1cc2cccc(C(=O)NCC3C4CN(CC5CCOCC5)CC34)n2n1
CHEMBL4203734 5ht4r_human Human No 8.1 EC50 = 8.8 nM Bind
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
398 6 1 5 3.3 CC(C)c1nc(C(=O)NCC2CCN(CC3CCOCC3)CC2)n2ccccc12
CHEMBL1258109 5ht4r_human Human No 8.1 EC50 = 8.9 nM 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 7 1 6 3.2 CCCCN1CCC(COC(=O)c2ccc(NC)c3c2OCCO3)CC1
CHEMBL3741199 5ht4r_human Human No 6.1 EC50 = 840 nM 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 6 4.2 CC(C)c1nc(-c2nnc(C3CCN(C4CCC4)CC3)o2)c2ccccn12
CHEMBL3740000 5ht4r_human Human No 6.1 EC50 = 857 nM 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 6 4.1 CC(C)c1nc(-c2nnc(C3CCN(CC4CC4)CC3)o2)c2ccccn12
CHEMBL3742080 5ht4r_human Human No 7.1 EC50 = 88 nM 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
426 5 2 6 2.7 CC(C)c1nc(C(=O)NC2CC3CCC(C2)N3CC2(O)CCOCC2)c2ccccn12
CHEMBL442869 5ht4r_human Human No 8.1 EC50 = 9 nM 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
982 28 6 14 5.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(NC(=O)CCCNCCCc2ccc(CCCNCCCC(=O)NC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)cc2)CC1
CHEMBL4218868 5ht4r_human Human No 8.1 EC50 = 9 nM Bind
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
342 5 1 4 3.3 CC(C)c1cn2cccc(C(=O)NCC3CCN(C(C)C)CC3)c2n1
CHEMBL1181147 5ht4r_rat Rat No 8.0 EC50 = 9.6 nM 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
380 6 2 3 3.5 CCCC[N+]12CCCC(C1)C(NC(=O)c1cc(Cl)c(N)cc1OC)CC2
CHEMBL156977 5ht4r_rat Rat No 8.0 EC50 = 9.6 nM 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
380 6 2 3 3.5 CCCC[N+]12CCCC(C1)C(NC(=O)c1cc(Cl)c(N)cc1OC)CC2
CHEMBL3741787 5ht4r_human Human No 8.0 EC50 = 9.7 nM 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
439 5 1 6 2.6 COC(=O)N1CCC(N2C[C@H]3[C@H](CNC(=O)c4nc(C(C)C)n5ccccc45)[C@H]3C2)CC1
CHEMBL350221 5ht4r_rat Rat Yes 8.0 EC50 = 9.8 nM 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 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O
CHEMBL3741733 5ht4r_human Human No 8.0 EC50 = 9.8 nM 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 4 3.5 CC(C)c1nc(C(=O)NCC2CCN(C3CCC3)CC2)c2ccccn12
CHEMBL585567 5ht4r_human Human No 7.1 EC50 = 90 nM Funct
Agonist activity at human recombinant 5-HT4 receptorAgonist activity at human recombinant 5-HT4 receptor
517 7 4 7 3.5 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(C[C@@H]2CCCC[C@@]2(O)c2cccc(O)c2)C[C@H]1OC
CHEMBL2448558 5ht4r_rat Rat Yes 7.0 EC50 = 98 nM Funct
Agonism at 5HT4 receptor in rat tunica muscularis mucosaAgonism at 5HT4 receptor in rat tunica muscularis mucosa
323 3 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN2CCC[C@@H]1C2
CHEMBL4215511 5ht4r_human Human No 7.0 EC50 = 98 nM Bind
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
342 5 1 4 3.3 CC(C)c1cc2cccc(C(=O)NCC3CCN(C(C)C)CC3)n2n1
CHEMBL159825 5ht4r_rat Rat No 7.0 EC50 = 98 nM 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
309 3 2 4 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN2CCC1C2
CHEMBL358119 5ht4r_cavpo Guinea pig No 10.6 IC50 = 0.0 nM Bind
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 6 0 5 4.1 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCO3)CC1
CHEMBL358119 5ht4r_cavpo Guinea pig No 10.6 IC50 = 0.0 nM Bind
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 6 0 5 4.1 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCO3)CC1
CHEMBL3967117 5ht4r_human Human No 10.4 IC50 = 0.0 nM Bind
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).
454 8 2 5 4.4 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2ccc3ccccc32)CC1
CHEMBL3950712 5ht4r_human Human Yes 10.2 IC50 = 0.1 nM Bind
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).
406 8 2 7 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2ccnn2)CC1
CHEMBL3934371 5ht4r_human Human No 10.1 IC50 = 0.1 nM Bind
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).
440 6 2 5 4.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2cn(C)c3ccccc23)CC1
CHEMBL68131 5ht4r_cavpo Guinea pig Yes 10.1 IC50 = 0.1 nM Bind
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
382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N
CHEMBL68131 5ht4r_cavpo Guinea pig Yes 10.1 IC50 = 0.1 nM Bind
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)
382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N
CHEMBL142490 5ht4r_cavpo Guinea pig No 10.0 IC50 = 0.1 nM Bind
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 7 1 4 3.8 CCCCN1CCC(COC(=O)c2c(OC)[nH]c3ccccc23)CC1
CHEMBL145075 5ht4r_cavpo Guinea pig No 10.0 IC50 = 0.1 nM Bind
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 6 0 5 3.7 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCO3)CC1
CHEMBL145075 5ht4r_cavpo Guinea pig No 10.0 IC50 = 0.1 nM Bind
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 6 0 5 3.7 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCO3)CC1
CHEMBL68131 5ht4r_cavpo Guinea pig Yes 10.0 IC50 = 0.1 nM 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)
382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N
CHEMBL3926377 5ht4r_human Human No 10.0 IC50 = 0.1 nM Bind
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).
434 10 2 7 2.8 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCCCn2ccnn2)CC1
CHEMBL3890747 5ht4r_human Human No 9.9 IC50 = 0.1 nM Bind
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).
405 6 2 4 3.7 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2ccc(F)cc2)CC1
CHEMBL143862 5ht4r_cavpo Guinea pig No 9.8 IC50 = 0.2 nM Bind
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
384 6 0 5 4.5 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCCO3)CC1
CHEMBL143862 5ht4r_cavpo Guinea pig No 9.8 IC50 = 0.2 nM Bind
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)
384 6 0 5 4.5 CCCCN1CCC(COC(=O)c2c3n(c4ccccc24)CCCCO3)CC1
CHEMBL3986866 5ht4r_human Human No 9.8 IC50 = 0.2 nM Bind
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).
407 8 2 8 1.4 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2cnnn2)CC1
CHEMBL3957180 5ht4r_human Human No 9.7 IC50 = 0.2 nM Bind
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).
406 8 2 7 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2nccn2)CC1
CHEMBL33884 5ht4r_human Human Yes 9.7 IC50 = 0.2 nM 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
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL3946162 5ht4r_human Human No 9.7 IC50 = 0.2 nM Bind
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).
406 8 2 7 2.1 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2cncn2)CC1
CHEMBL3928124 5ht4r_human Human No 9.6 IC50 = 0.2 nM Bind
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).
419 8 2 6 3.0 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(CCCn2ccnc2C)CC1
CHEMBL3982522 5ht4r_human Human No 9.6 IC50 = 0.3 nM Bind
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).
388 6 2 5 3.0 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2cccnc2)CC1
CHEMBL1729 5ht4r_human Human Yes 9.4 IC50 = 0.4 nM Bind
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).
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL560739 5ht4r_human Human Yes 9.4 IC50 = 0.4 nM Bind
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).
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL3920018 5ht4r_human Human No 9.4 IC50 = 0.4 nM Bind
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).
403 6 3 5 3.3 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2ccc(O)cc2)CC1
CHEMBL3915236 5ht4r_human Human No 9.4 IC50 = 0.4 nM Bind
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).
390 6 2 5 2.9 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2cccn2C)CC1
CHEMBL3910849 5ht4r_human Human No 9.3 IC50 = 0.5 nM Bind
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).
377 6 3 5 2.3 COc1cc(N)c(Cl)cc1C(=O)NCC1CCN(Cc2ncc[nH]2)CC1
CHEMBL143426 5ht4r_cavpo Guinea pig No 9.3 IC50 = 0.5 nM Bind
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 6 1 3 3.8 CCCCN1CCC(COC(=O)c2c[nH]c3ccccc23)CC1
CHEMBL143426 5ht4r_cavpo Guinea pig No 9.3 IC50 = 0.5 nM Bind
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 6 1 3 3.8 CCCCN1CCC(COC(=O)c2c[nH]c3ccccc23)CC1
CHEMBL35226 5ht4r_mouse Mouse No 9.3 IC50 = 0.6 nM Bind
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 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1
CHEMBL356359 5ht4r_human Human Yes 9.2 IC50 = 0.6 nM Bind
Binding affinity was determined against 5-hydroxytryptamine 3 receptorBinding affinity was determined against 5-hydroxytryptamine 3 receptor
369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2
CHEMBL334818 5ht4r_cavpo Guinea pig No 9.0 IC50 = 1 nM 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 1 5 3.6 CCCCN1CCC(COC(=O)c2cc(Cl)c(N)cc2OC)CC1
CHEMBL3220223 5ht4r_human Human No 8.9 IC50 = 1.4 nM Bind
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
467 7 1 8 3.4 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2-c2cnccn2)CC1
CHEMBL130809 5ht4r_cavpo Guinea pig No 8.0 IC50 = 10 nM 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)
353 7 2 4 3.2 CCCCN1CCC(CNC(=O)c2cc(Cl)c(N)cc2OC)CC1
CHEMBL123377 5ht4r_cavpo Guinea pig No 7.0 IC50 = 100 nM 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
389 6 1 6 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2)CC1
CHEMBL160237 5ht4r_cavpo Guinea pig No 7.0 IC50 = 100 nM 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
416 7 1 6 3.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(C(=O)c2ccccc2)CC1
CHEMBL56994 5ht4r_cavpo Guinea pig No 6.0 IC50 = 1000 nM Bind
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
323 3 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC1CN2C
CHEMBL57686 5ht4r_cavpo Guinea pig No 6.0 IC50 = 1000 nM Bind
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
323 3 2 4 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CC2CCC1N(C)C2
CHEMBL1550957 5ht4r_cavpo Guinea pig Yes 6.0 IC50 = 1000 nM Bind
Displacement of [3H]-GR113808 from guinea pig 5HT4 receptorDisplacement of [3H]-GR113808 from guinea pig 5HT4 receptor
212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1
CHEMBL99577 5ht4r_cavpo Guinea pig No 6.0 IC50 = 1000 nM Bind
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 5 0.1 CN1CCN(CCNC(=O)n2c(=O)[nH]c3ccccc32)CC1
CHEMBL49072 5ht4r_cavpo Guinea pig No 6.0 IC50 = 1000 nM 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.
315 7 2 5 2.8 CCN(CC)CCOC(=O)Nc1cc(Cl)c(N)cc1OC
CHEMBL4457426 5ht4r_human Human No 7.0 IC50 = 101 nM Bind
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
515 11 3 7 4.2 COc1cc(/C=C/C(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)ccc1O
CHEMBL10 5ht4r_cavpo Guinea pig Yes 5.0 IC50 = 10553 nM Bind
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 3 4.7 C[S+]([O-])c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL723 5ht4r_cavpo Guinea pig Yes 6.0 IC50 = 1088 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O
CHEMBL155917 5ht4r_cavpo Guinea pig Yes 8.0 IC50 = 11 nM 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
340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl
CHEMBL177573 5ht4r_cavpo Guinea pig No 8.0 IC50 = 11.2 nM Bind
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
465 10 3 6 3.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCCCN)CC2)CC1
CHEMBL3291078 5ht4r_human Human No 7.0 IC50 = 110 nM Bind
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 COc1cc2c3c(cccc3n1)C(=O)N(CCCN1CCCCC1)C2=O
CHEMBL3758523 5ht4r_human Human No 6.0 IC50 = 1121 nM Bind
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 9 0.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2ncnn2)C[C@H]1OC
CHEMBL60889 5ht4r_cavpo Guinea pig Yes 7.0 IC50 = 113 nM Bind
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
421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl
CHEMBL728 5ht4r_cavpo Guinea pig Yes 5.9 IC50 = 1164 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2
CHEMBL3758199 5ht4r_human Human No 5.9 IC50 = 1165 nM Bind
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
421 8 2 7 2.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2ccnc2)C[C@H]1OC
CHEMBL3759944 5ht4r_human Human No 6.9 IC50 = 118 nM Bind
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
494 6 2 6 3.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)C(C)(C)C)CC2)C[C@H]1OC
CHEMBL359744 5ht4r_cavpo Guinea pig Yes 4.9 IC50 = 12468 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1
CHEMBL53463 5ht4r_cavpo Guinea pig Yes 4.9 IC50 = 12468 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1
CHEMBL3759601 5ht4r_human Human No 5.9 IC50 = 1271 nM Bind
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 8 1.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cncn2)C[C@H]1OC
CHEMBL33884 5ht4r_cavpo Guinea pig Yes 7.9 IC50 = 13 nM 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
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL155917 5ht4r_cavpo Guinea pig Yes 7.9 IC50 = 13 nM 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
340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl
CHEMBL174935 5ht4r_cavpo Guinea pig No 7.9 IC50 = 13.4 nM Bind
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
437 8 3 6 2.2 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCN)CC2)CC1
CHEMBL3758641 5ht4r_human Human No 6.9 IC50 = 134 nM Bind
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
496 8 2 7 3.0 CCCOC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1
CHEMBL3759860 5ht4r_human Human No 6.9 IC50 = 134 nM Bind
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
480 7 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)C(C)C)CC2)C[C@H]1OC
CHEMBL806 5ht4r_cavpo Guinea pig Yes 4.9 IC50 = 13545 nM Bind
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 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1
CHEMBL368844 5ht4r_cavpo Guinea pig No 7.8 IC50 = 14.3 nM Bind
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
451 8 3 6 2.4 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CC(C)CN)CC2)CC1
CHEMBL426216 5ht4r_cavpo Guinea pig No 7.8 IC50 = 14.3 nM Bind
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
423 7 3 6 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCN)CC2)CC1
CHEMBL433984 5ht4r_cavpo Guinea pig No 7.8 IC50 = 14.4 nM Bind
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
453 8 4 7 1.2 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CC(O)CN)CC2)CC1
CHEMBL4580044 5ht4r_human Human No 7.8 IC50 = 14.5 nM Bind
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
432 8 2 6 4.5 COc1ccc(CN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1O
CHEMBL493677 5ht4r_human Human Yes 5.9 IC50 = 1400 nM Bind
Inhibition of 5HT4 receptorInhibition of 5HT4 receptor
388 5 1 2 4.8 CC(C)(C)CCN1CC[C@H](CNC(=O)c2cc(Cl)cc(Cl)c2)[C@H](F)C1
CHEMBL39 5ht4r_rat Rat Yes 6.8 IC50 = 147 nM Bind
Inhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptorInhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL1306 5ht4r_cavpo Guinea pig Yes 4.8 IC50 = 14780 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1
CHEMBL356546 5ht4r_cavpo Guinea pig No 7.8 IC50 = 15.9 nM Bind
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 4 3.3 CCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCO3)CC1
CHEMBL155682 5ht4r_cavpo Guinea pig No 6.8 IC50 = 150 nM 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
340 5 1 5 3.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC(C)(C)C1
CHEMBL3758674 5ht4r_human Human No 6.8 IC50 = 155 nM Bind
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
496 7 2 6 3.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=S)C(C)C)CC2)C[C@H]1OC
CHEMBL442 5ht4r_cavpo Guinea pig Yes 5.8 IC50 = 1584 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL127876 5ht4r_human Human No 6.8 IC50 = 162 nM Bind
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(Cl)c2)CC1
CHEMBL19215 5ht4r_cavpo Guinea pig Yes 5.8 IC50 = 1641 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C
CHEMBL421256 5ht4r_human Human No 7.8 IC50 = 17 nM Bind
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
407 6 1 6 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2F)CC1
CHEMBL3759546 5ht4r_human Human No 6.8 IC50 = 178 nM Bind
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
480 8 2 6 2.8 CCCC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1
CHEMBL339936 5ht4r_human Human No 7.8 IC50 = 18 nM Bind
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
419 7 1 7 2.9 COc1ccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1
CHEMBL299408 5ht4r_cavpo Guinea pig No 6.8 IC50 = 180 nM 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.
355 5 2 5 3.5 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CC(C)CC(C)C1
CHEMBL1748 5ht4r_human Human Yes 7.7 IC50 = 19 nM Bind
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
313 4 3 5 1.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCNCC1OC
CHEMBL3759969 5ht4r_human Human No 6.7 IC50 = 190 nM Bind
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
468 6 2 7 2.2 COC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1
CHEMBL3291079 5ht4r_human Human No 6.7 IC50 = 195 nM Bind
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
343 4 0 3 3.7 O=C1c2cc(Cl)nc3cccc(c23)CN1CCCN1CCCCC1
CHEMBL146386 5ht4r_cavpo Guinea pig Yes 6.7 IC50 = 199.5 nM Bind
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 3.4 CCCCN1CCC(CNC(=O)c2c[nH]c3ccccc23)CC1
CHEMBL286136 5ht4r_rat Rat Yes 8.6 IC50 = 2.4 nM Funct
5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae
312 5 1 5 2.6 COc1cc(N)c(cc1C(=O)OCCN1CCCCC1)Cl
CHEMBL174284 5ht4r_cavpo Guinea pig No 8.6 IC50 = 2.5 nM Bind
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
479 7 3 6 2.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(N)C(C)C)CC2)CC1
CHEMBL172802 5ht4r_cavpo Guinea pig No 8.6 IC50 = 2.6 nM Bind
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
479 8 3 6 2.5 CCCC(N)C(=O)N1CCC(CN2CCC(NC(=O)c3cc(Cl)c(N)cc3OC)CC2)CC1
CHEMBL368213 5ht4r_cavpo Guinea pig No 8.6 IC50 = 2.6 nM Bind
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
465 6 3 6 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(C)(C)N)CC2)CC1
CHEMBL2179674 5ht4r_human Human No 8.6 IC50 = 2.8 nM 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
443 7 1 5 4.8 Cn1cc2c(OCC3CCN(CCc4ccc(C(=O)O)cc4)CC3)nc3ccccc3c2c1
CHEMBL156970 5ht4r_cavpo Guinea pig No 6.7 IC50 = 200 nM 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
298 5 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCCC1
CHEMBL49266 5ht4r_cavpo Guinea pig No 6.7 IC50 = 200 nM 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.
341 5 2 5 3.2 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCC(C)CC1
CHEMBL3291075 5ht4r_human Human No 6.7 IC50 = 203 nM Bind
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 6 0 5 3.3 COc1cc(C(=O)OCCCN2CCCCC2)c2ccccc2n1
CHEMBL50852 5ht4r_cavpo Guinea pig No 6.7 IC50 = 207 nM 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.
341 5 2 5 3.4 COc1cc(N)c(Cl)cc1NC(=O)OCCN1CCCCCC1
CHEMBL367877 5ht4r_cavpo Guinea pig No 7.7 IC50 = 21.1 nM Bind
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
515 10 3 7 1.8 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCNS(C)(=O)=O)CC2)CC1
CHEMBL12089 5ht4r_cavpo Guinea pig Yes 5.7 IC50 = 2222 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2
CHEMBL295124 5ht4r_cavpo Guinea pig Yes 5.7 IC50 = 2222 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2
CHEMBL287045 5ht4r_cavpo Guinea pig Yes 6.6 IC50 = 251.2 nM 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)
300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC
CHEMBL439849 5ht4r_rat Rat Yes 6.6 IC50 = 252 nM Bind
Inhibition of rat hydroxytryptamine 4 receptorInhibition of rat hydroxytryptamine 4 receptor
441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2
CHEMBL1729 5ht4r_cavpo Guinea pig Yes 6.6 IC50 = 273 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL560739 5ht4r_cavpo Guinea pig Yes 6.6 IC50 = 273 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL125670 5ht4r_human Human No 6.5 IC50 = 296 nM Bind
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2Cl)CC1
CHEMBL334325 5ht4r_human Human No 8.5 IC50 = 3 nM Bind
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
419 7 1 7 2.9 COc1cccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)c1
CHEMBL39 5ht4r_rat Rat Yes 8.4 IC50 = 3.7 nM Funct
5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL173089 5ht4r_cavpo Guinea pig No 8.4 IC50 = 3.9 nM Bind
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
479 9 3 6 2.5 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CCCCN)CC2)CC1
CHEMBL172074 5ht4r_cavpo Guinea pig No 8.4 IC50 = 4.0 nM Bind
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
465 8 3 6 2.1 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CCCN)CC2)CC1
CHEMBL41769 5ht4r_cavpo Guinea pig No 7.5 IC50 = 30 nM 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
310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2
CHEMBL41769 5ht4r_cavpo Guinea pig No 7.5 IC50 = 30 nM 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
310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@H]1CN2CCC1CC2
CHEMBL351570 5ht4r_cavpo Guinea pig No 6.5 IC50 = 300 nM 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
342 5 1 6 2.2 COc1cc(N)c(Cl)cc1C(=O)OCCN1CC(C)OC(C)C1
CHEMBL56564 5ht4r_cavpo Guinea pig No 5.5 IC50 = 3162.3 nM 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 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2
CHEMBL39 5ht4r_human Human Yes 6.5 IC50 = 323 nM Bind
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL56564 5ht4r_cavpo Guinea pig No 6.5 IC50 = 324 nM Bind
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 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2
CHEMBL3759259 5ht4r_human Human No 6.5 IC50 = 329 nM Bind
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 7 2 6 2.4 CCC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1
CHEMBL3758398 5ht4r_human Human No 6.4 IC50 = 377 nM Bind
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 7 2 7 2.6 CCOC(=O)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1
CHEMBL1108 5ht4r_cavpo Guinea pig Yes 5.4 IC50 = 3789 nM Bind
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 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1
CHEMBL571799 5ht4r_human Human No 5.4 IC50 = 3900 nM Bind
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
531 8 3 7 3.8 COc1cccc([C@]2(O)CCCC[C@H]2CN2CC[C@@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@@H](OC)C2)c1
CHEMBL176672 5ht4r_cavpo Guinea pig No 7.4 IC50 = 40.6 nM Bind
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
453 8 4 7 1.2 COc1cc(N)c(Cl)cc1C(=O)NCC(O)CN1CCC(CN2CCC(N)CC2)CC1
CHEMBL366986 5ht4r_cavpo Guinea pig No 6.4 IC50 = 425.4 nM Bind
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
479 7 3 6 1.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(C(=O)C2CCN(C(=O)CCCN)CC2)CC1
CHEMBL267615 5ht4r_cavpo Guinea pig Yes 7.4 IC50 = 44 nM Bind
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC
CHEMBL288199 5ht4r_cavpo Guinea pig No 6.4 IC50 = 450 nM 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
310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2
CHEMBL288199 5ht4r_cavpo Guinea pig No 6.4 IC50 = 450 nM 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
310 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)O[C@@H]1CN2CCC1CC2
CHEMBL3291080 5ht4r_human Human No 6.3 IC50 = 453 nM Bind
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
357 4 0 4 3.4 O=C1c2cccc3nc(Cl)cc(c23)C(=O)N1CCCN1CCCCC1
CHEMBL570487 5ht4r_human Human No 5.3 IC50 = 4600 nM Bind
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
531 8 3 7 3.8 COc1cccc([C@]2(O)CCCC[C@H]2CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)c1
CHEMBL74656 5ht4r_human Human Yes 6.3 IC50 = 483 nM Bind
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
465 9 2 6 3.4 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCOc2ccc(F)cc2)C[C@H]1OC
CHEMBL83954 5ht4r_human Human Yes 7.3 IC50 = 49 nM Bind
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
326 6 1 5 3.0 COc1cc(N)c(cc1C(=O)OCCCN1CCCCC1)Cl
CHEMBL1255837 5ht4r_cavpo Guinea pig Yes 5.3 IC50 = 4912 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O
CHEMBL601773 5ht4r_cavpo Guinea pig Yes 5.3 IC50 = 4912 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O
CHEMBL3759348 5ht4r_human Human No 6.3 IC50 = 493 nM Bind
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 7 2 6 2.4 CCC(=O)N1CCCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)C1
CHEMBL172899 5ht4r_cavpo Guinea pig No 8.3 IC50 = 5.1 nM Bind
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
451 6 3 6 1.7 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(C)N)CC2)CC1
CHEMBL425329 5ht4r_cavpo Guinea pig No 8.3 IC50 = 5.1 nM Bind
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
465 7 3 6 2.0 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)C(C)CN)CC2)CC1
CHEMBL130118 5ht4r_cavpo Guinea pig No 7.3 IC50 = 50.1 nM 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 6 0 5 3.5 CCCCN1CCC(COC(=O)c2cccc3c2OCCCO3)CC1
CHEMBL572038 5ht4r_human Human No 5.3 IC50 = 5000 nM Bind
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
475 9 3 6 3.7 COc1cccc([C@@]2(O)CCCC[C@@H]2CN(C)CCNC(=O)c2cc(Cl)c(N)cc2OC)c1
CHEMBL3759759 5ht4r_human Human No 7.3 IC50 = 52 nM Bind
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 6 2 6 2.1 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)N(C)C)CC2)C[C@H]1OC
CHEMBL3758945 5ht4r_human Human No 6.3 IC50 = 560 nM Bind
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
452 7 2 6 2.2 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCCCC2)C[C@H]1OC
CHEMBL3758721 5ht4r_human Human No 5.2 IC50 = 5759 nM Bind
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
406 7 2 6 2.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCn2cccc2)C[C@H]1OC
CHEMBL3759362 5ht4r_human Human No 6.2 IC50 = 592 nM Bind
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
452 6 2 6 2.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(C)=O)CC2)C[C@H]1OC
CHEMBL3758397 5ht4r_human Human No 6.2 IC50 = 593 nM Bind
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 7 2 6 3.2 CCC(=S)N1CCC(CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1
CHEMBL130040 5ht4r_cavpo Guinea pig Yes 8.2 IC50 = 6.3 nM 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)
333 6 0 5 3.1 CCCCN1CCC(CC1)COC(=O)c1cccc2c1OCCO2
CHEMBL369037 5ht4r_cavpo Guinea pig No 8.2 IC50 = 6.5 nM Bind
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
451 9 3 6 2.6 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(CCCCN)CC2)CC1
CHEMBL34224 5ht4r_cavpo Guinea pig Yes 7.2 IC50 = 60 nM 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
298 3 1 5 2.2 COc1cc(N)c(Cl)cc1C(=O)OC1CCN(C)CC1
CHEMBL160705 5ht4r_cavpo Guinea pig No 6.2 IC50 = 600 nM 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
272 5 1 5 1.6 COc1cc(N)c(Cl)cc1C(=O)OCCN(C)C
CHEMBL569585 5ht4r_human Human No 5.2 IC50 = 6100 nM Bind
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
531 8 3 7 3.8 COc1cccc([C@@]2(O)CCCC[C@@H]2CN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)c1
CHEMBL364005 5ht4r_cavpo Guinea pig Yes 6.2 IC50 = 620 nM Bind
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C
CHEMBL132826 5ht4r_cavpo Guinea pig No 7.2 IC50 = 63.1 nM 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)
319 6 0 5 3.1 CCCCN1CCC(COC(=O)c2cccc3c2OCO3)CC1
CHEMBL121766 5ht4r_human Human No 7.2 IC50 = 64 nM Bind
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
419 7 1 7 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2OC)CC1
CHEMBL3758932 5ht4r_human Human No 6.2 IC50 = 648 nM Bind
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
420 8 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCCn2cccc2)C[C@H]1OC
CHEMBL3759928 5ht4r_human Human No 7.2 IC50 = 66 nM Bind
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
542 9 2 6 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCC(Cc3ccccc3)CC2)C[C@H]1OC
CHEMBL3758309 5ht4r_human Human No 7.2 IC50 = 68 nM Bind
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
480 7 2 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CCN(CC2CCN(C(=O)C(C)C)CC2)C[C@@H]1OC
CHEMBL4526049 5ht4r_human Human No 8.1 IC50 = 7.5 nM Bind
Displacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assayDisplacement of [3H]-GR 113808 from recombinant human brain 5HT4 receptor measured after 60 mins by radio ligand binding assay
418 7 3 6 4.2 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(Cc2ccc(O)c(O)c2)CC1
CHEMBL142621 5ht4r_cavpo Guinea pig No 8.1 IC50 = 7.9 nM Bind
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 6 1 4 4.1 CCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCCO3)CC1
CHEMBL124485 5ht4r_human Human No 6.2 IC50 = 715 nM Bind
Antagonist activity at 5TH4 receptor (unknown origin)Antagonist activity at 5TH4 receptor (unknown origin)
423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)cc2)CC1
CHEMBL3758976 5ht4r_human Human No 7.1 IC50 = 73 nM Bind
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 3 6 2.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)NC(C)C)CC2)C[C@H]1OC
CHEMBL707 5ht4r_cavpo Guinea pig Yes 6.1 IC50 = 764 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2
CHEMBL287045 5ht4r_cavpo Guinea pig Yes 7.1 IC50 = 77 nM Funct
5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum; Not evaluable5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum; Not evaluable
300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC
CHEMBL287045 5ht4r_cavpo Guinea pig Yes 7.1 IC50 = 77 nM 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
300 7 1 5 2.4 CCN(CCOC(=O)c1cc(Cl)c(cc1OC)N)CC
CHEMBL3758433 5ht4r_human Human No 7.1 IC50 = 78 nM Bind
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
494 8 2 6 3.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCN(C(=O)CC(C)C)CC2)C[C@H]1OC
CHEMBL422116 5ht4r_cavpo Guinea pig No 7.1 IC50 = 79.4 nM Bind
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
343 7 2 3 3.4 CCCCN1CCC(CNC(=O)c2c(OC)[nH]c3ccccc23)CC1
CHEMBL417 5ht4r_cavpo Guinea pig Yes 5.1 IC50 = 7935 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1
CHEMBL691 5ht4r_cavpo Guinea pig Yes 5.1 IC50 = 7953 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C
CHEMBL3759824 5ht4r_human Human No 6.1 IC50 = 805 nM Bind
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
480 8 2 6 2.8 CCC(=O)N1CCC(CCN2CC[C@H](NC(=O)c3cc(Cl)c(N)cc3OC)[C@H](OC)C2)CC1
CHEMBL334923 5ht4r_human Human No 6.1 IC50 = 871.0 nM Funct
Compound was tested for agonistic activity against 5-hydroxytryptamine 4 receptor on guinea colon at a concentration 0.1 uMCompound was tested for agonistic activity against 5-hydroxytryptamine 4 receptor on guinea colon at a concentration 0.1 uM
275 4 0 5 2.5 Cc1csc2c1-n1cccc1/C2=N/OCCN(C)C
CHEMBL60889 5ht4r_cavpo Guinea pig Yes 6.1 IC50 = 881.8 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl
CHEMBL172314 5ht4r_cavpo Guinea pig No 8.0 IC50 = 9.3 nM Bind
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
437 6 3 6 1.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CN)CC2)CC1
CHEMBL174524 5ht4r_cavpo Guinea pig No 8.0 IC50 = 9.5 nM Bind
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
451 7 3 6 1.7 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(CC2CCN(C(=O)CCN)CC2)CC1
CHEMBL2179707 5ht4r_human Human No 8.0 IC50 = 9.8 nM 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
448 8 2 5 4.0 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(C(=O)O)cc3)CC2)c2ccccc21
CHEMBL86 5ht4r_cavpo Guinea pig Yes 6.0 IC50 = 912 nM Bind
Concentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatumConcentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatum
299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC
CHEMBL3291077 5ht4r_human Human No 6.0 IC50 = 916 nM Bind
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
339 5 0 4 3.1 COc1cc2c3c(cccc3n1)CN(CCCN1CCCCC1)C2=O
CHEMBL3758578 5ht4r_human Human No 6.0 IC50 = 920 nM Bind
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
438 7 2 6 1.8 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCCC2)C[C@H]1OC
CHEMBL1732 5ht4r_cavpo Guinea pig Yes 6.0 IC50 = 940 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL3758410 5ht4r_human Human No 6.0 IC50 = 954 nM Bind
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
454 7 2 7 1.0 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(CCC(=O)N2CCOCC2)C[C@H]1OC
CHEMBL194305 5ht4r_cavpo Guinea pig Yes 5.0 IC50 = 9800 nM Bind
Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pigInhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig
242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1
CHEMBL585567 5ht4r_human Human No 5.0 IC50 = 9900 nM Bind
Displacement of [3H]GR-113808 from human recombinant 5-HT4 receptorDisplacement of [3H]GR-113808 from human recombinant 5-HT4 receptor
517 7 4 7 3.5 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(C[C@@H]2CCCC[C@@]2(O)c2cccc(O)c2)C[C@H]1OC
CHEMBL68131 5ht4r_cavpo Guinea pig Yes 10.7 Kd = 0.0 nM Bind
Binding affinity to 5HT4 receptor in guinea pig distal colonBinding affinity to 5HT4 receptor in guinea pig distal colon
382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N
CHEMBL114112 5ht4r_rat Rat Yes 9.5 Kd = 0.3 nM Bind
Binding affinity to 5HT4 receptor in rat striatal membranesBinding affinity to 5HT4 receptor in rat striatal membranes
474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N
CHEMBL3126112 5ht4r_rat Rat Yes 9.5 Kd = 0.3 nM Bind
Binding affinity to 5HT4 receptor in rat striatal membranesBinding affinity to 5HT4 receptor in rat striatal membranes
340 3 1 6 2.2 CN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCCO3)CC1
CHEMBL121913 5ht4r_human Human No 9.2 Kd = 0.7 nM Funct
,Antagonism of stimulation of 5-hydroxytryptamine receptor on the L-type calcium current (I Ca) in isolated human atrial myocytes,Antagonism of stimulation of 5-hydroxytryptamine receptor on the L-type calcium current (I Ca) in isolated human atrial myocytes
391 6 1 8 1.7 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1
CHEMBL201946 5ht4r_rat Rat No 8.9 Kd = 1.2 nM Funct
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
284 3 1 3 2.8 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1c[nH]c2ccccc12
CHEMBL371883 5ht4r_rat Rat No 7.0 Kd = 100 nM Funct
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
327 2 1 3 2.5 CC1(C)C(=O)N(C(=O)NC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21
CHEMBL33884 5ht4r_human Human Yes 7.8 Kd = 15.8 nM Bind
Binding affinity to human 5HT4 receptor expressed in HEK293 cells by saturation binding methodBinding affinity to human 5HT4 receptor expressed in HEK293 cells by saturation binding method
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL202481 5ht4r_rat Rat No 6.8 Kd = 177.8 nM Funct
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
319 3 0 5 2.6 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1cc(Cl)cn2ccnc12
CHEMBL383554 5ht4r_rat Rat No 6.8 Kd = 177.8 nM Funct
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
284 3 1 4 1.5 O=C(NC[C@@H]1CCN2CCC[C@@H]12)c1cccn2ccnc12
CHEMBL56564 5ht4r_cavpo Guinea pig No 5.7 Kd = 1995.3 nM Funct
Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.
284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2
CHEMBL383577 5ht4r_rat Rat No 8.6 Kd = 2.8 nM Funct
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
299 3 0 5 2.2 Cn1nc(C(=O)OC[C@@H]2CCN3CCC[C@@H]23)c2ccccc21
CHEMBL202149 5ht4r_rat Rat No 6.6 Kd = 275.4 nM Funct
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
312 4 1 4 2.1 CCc1nc(C(=O)NC[C@@H]2CCN3CCC[C@@H]23)c2ccccn12
CHEMBL202122 5ht4r_rat Rat No 8.5 Kd = 3.2 nM Funct
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
302 3 1 3 2.9 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1c[nH]c2ccc(F)cc12
CHEMBL201878 5ht4r_rat Rat No 8.5 Kd = 3.3 nM Funct
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
285 3 1 4 2.2 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1[nH]nc2ccccc12
CHEMBL143197 5ht4r_cavpo Guinea pig No 6.3 Kd = 501.2 nM Funct
Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 4 receptor in non-electrically stimulated guinea-pig ileum.
298 2 1 4 1.9 CN1C2CC(OC(=O)c3c[nH]c4ccccc34)CC1C1OC12
CHEMBL202434 5ht4r_rat Rat Yes 8.1 Kd = 7.4 nM Funct
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
318 3 1 4 2.2 O=C(NC[C@@H]1CCN2CCC[C@@H]12)c1cc(Cl)cn2ccnc12
CHEMBL425222 5ht4r_rat Rat No 7.2 Kd = 70.8 nM Funct
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
314 4 1 4 2.8 COc1ccc2[nH]cc(C(=O)OC[C@@H]3CCN4CCC[C@@H]34)c2c1
CHEMBL372776 5ht4r_rat Rat No 7.1 Kd = 81.3 nM Funct
Antagonism at 5HT4 receptor in rat tunica muscularis mucosaAntagonism at 5HT4 receptor in rat tunica muscularis mucosa
332 3 1 4 2.5 Cc1cnc2c(C(=O)NC[C@@H]3CCN4CCC[C@@H]34)cc(Cl)cn12
CHEMBL68131 5ht4r_cavpo Guinea pig Yes 10.9 Ki = 0.0 nM Bind
Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligandCompound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand
382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N
CHEMBL68131 5ht4r_human Human Yes 10.8 Ki = 0.0 nM Bind
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N
CHEMBL180835 5ht4r_human Human No 10.8 Ki = 0.0 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
534 9 1 7 2.2 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(C3CCCC3)CC2)CC1)c1cccc2c1OCCO2
CHEMBL181202 5ht4r_human Human No 10.6 Ki = 0.0 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
522 10 1 7 2.0 CCC(C)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1
CHEMBL361118 5ht4r_human Human No 10.6 Ki = 0.0 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
519 8 1 6 3.3 O=C(NCC1CCN(CCCS(=O)(=O)N2CCC3(CCCC3)CC2)CC1)c1cccc2c1OCCO2
CHEMBL181126 5ht4r_human Human No 10.5 Ki = 0.0 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
508 10 1 7 1.6 CCCN1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1
CHEMBL182999 5ht4r_human Human No 10.5 Ki = 0.0 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
508 9 1 7 1.6 CC(C)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1
CHEMBL367354 5ht4r_human Human No 10.5 Ki = 0.0 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
624 10 1 8 1.8 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(S(=O)(=O)c3ccc(F)cc3)CC2)CC1)c1cccc2c1OCCO2
CHEMBL33884 5ht4r_human Human Yes 10.4 Ki = 0.0 nM Bind
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL33884 5ht4r_human Human Yes 10.4 Ki = 0.0 nM Bind
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL2181170 5ht4r_human Human No 10.4 Ki = 0.0 nM Bind
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1
CHEMBL2181170 5ht4r_human Human No 10.4 Ki = 0.0 nM Bind
Binding affinity to human 5HT4RBinding affinity to human 5HT4R
353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1
CHEMBL2181170 5ht4r_human Human No 10.4 Ki = 0.0 nM Bind
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1
CHEMBL1632165 5ht4r_human Human No 10.4 Ki = 0.0 nM Bind
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
489 9 1 6 4.4 O=C(CCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1)OCc1ccccc1
CHEMBL2440460 5ht4r_human Human No 10.3 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
524 7 1 6 5.9 O=C(O)c1ccccc1-c1ccc(CN2CCC(COC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1
CHEMBL3040772 5ht4r_human Human No 10.3 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
524 7 1 6 5.9 O=C(O)c1ccccc1-c1ccc(CN2CCC(COC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1
CHEMBL3329805 5ht4r_human Human No 10.3 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
538 9 2 6 4.5 CC(C)CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1
CHEMBL180680 5ht4r_human Human No 10.3 Ki = 0.1 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
560 9 1 7 2.6 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(c3ccc(F)cc3)CC2)CC1)c1cccc2c1OCCO2
CHEMBL424790 5ht4r_human Human No 10.3 Ki = 0.1 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
494 9 1 7 1.3 CCN1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1
CHEMBL356359 5ht4r_human Human Yes 10.3 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2
CHEMBL1632163 5ht4r_human Human No 10.3 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
483 9 1 6 4.8 CC(C)(C)OC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1
CHEMBL2440457 5ht4r_human Human No 10.2 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
537 7 1 6 5.5 COC(=O)c1ccccc1-c1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1
CHEMBL180201 5ht4r_human Human No 10.2 Ki = 0.1 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
507 10 1 6 3.1 CCCC1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1
CHEMBL1632169 5ht4r_human Human No 10.2 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
541 11 1 8 4.5 CC(C)(C)C(=O)OCOC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1
CHEMBL3126108 5ht4r_rat Rat No 10.2 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma counting
386 6 1 6 2.9 Nc1c(Cl)cc(C(=O)OCC2CCN(CCCF)CC2)c2c1OCCO2
CHEMBL33884 5ht4r_human Human Yes 10.1 Ki = 0.1 nM Funct
Antagonistic activity at human 5HT4 receptor expressed in HEK293 cellsAntagonistic activity at human 5HT4 receptor expressed in HEK293 cells
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL33884 5ht4r_human Human Yes 10.1 Ki = 0.1 nM Bind
Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cellsBinding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL2177130 5ht4r_human Human No 10.1 Ki = 0.1 nM Bind
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
404 7 1 4 4.3 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccccc3)CC2)c2ccccc21
CHEMBL2220969 5ht4r_human Human No 10.1 Ki = 0.1 nM Bind
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
404 7 1 4 4.3 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccccc3)CC2)c2ccccc21
CHEMBL3329814 5ht4r_human Human No 10.1 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
388 6 2 7 1.6 O=C(OCC1CCN(CC(O)CO)CC1)c1c2n(c3ccccc13)CCCO2
CHEMBL360449 5ht4r_human Human No 10.1 Ki = 0.1 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
599 10 1 8 0.6 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(S(=O)(=O)N3CCCC3)CC2)CC1)c1cccc2c1OCCO2
CHEMBL3221572 5ht4r_rat Rat No 10.1 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysis
364 6 2 3 4.0 CCCCN1CCC(CNC(=S)c2cc(Cl)cc3[nH]cnc23)CC1
CHEMBL33884 5ht4r_human Human Yes 10.0 Ki = 0.1 nM Bind
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL69733 5ht4r_cavpo Guinea pig Yes 10.0 Ki = 0.1 nM Bind
Compound was evaluated for binding affinity against 5-hydroxytryptamine 4 receptor using radioligand binding assay using [3H]GR as radioligandCompound was evaluated for binding affinity against 5-hydroxytryptamine 4 receptor using radioligand binding assay using [3H]GR as radioligand
502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC
CHEMBL2179697 5ht4r_human Human Yes 10.0 Ki = 0.1 nM Bind
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
405 7 1 5 3.7 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccccn3)CC2)c2ccccc21
CHEMBL2220892 5ht4r_human Human Yes 10.0 Ki = 0.1 nM Bind
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
405 7 1 5 3.7 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccccn3)CC2)c2ccccc21
CHEMBL356359 5ht4r_human Human Yes 10.0 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2
CHEMBL356359 5ht4r_human Human Yes 10.0 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cellsDisplacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells
369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2
CHEMBL180830 5ht4r_human Human No 10.0 Ki = 0.1 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
560 9 1 8 1.7 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(C(=O)c3ccco3)CC2)CC1)c1cccc2c1OCCO2
CHEMBL360245 5ht4r_human Human No 10.0 Ki = 0.1 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
572 11 1 8 1.0 CCCS(=O)(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1
CHEMBL1632157 5ht4r_human Human No 10.0 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
427 8 1 6 3.2 CCOC(=O)CCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1
CHEMBL1632158 5ht4r_human Human No 10.0 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
441 9 1 6 3.6 COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1
CHEMBL329487 5ht4r_rat Rat No 10.0 Ki = 0.1 nM Bind
pKi against 5-hydroxytryptamine 4 receptor in rat striatum membranepKi against 5-hydroxytryptamine 4 receptor in rat striatum membrane
413 7 3 5 1.2 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1
CHEMBL33884 5ht4r_cavpo Guinea pig Yes 10.0 Ki = 0.1 nM Bind
Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligandBinding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL329487 5ht4r_rat Rat No 10.0 Ki = 0.1 nM Bind
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membraneBinding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
413 7 3 5 1.2 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1
CHEMBL3093186 5ht4r_human Human No 10.0 Ki = 0.1 nM Bind
Binding affinity to human 5HT4RBinding affinity to human 5HT4R
407 5 0 4 5.0 Fc1cccc2c1nc(OCC1CCN(CCC(F)(F)F)CC1)c1cccnc12
CHEMBL329487 5ht4r_rat Rat No 10.0 Ki = 0.1 nM Bind
In vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membraneIn vitro binding affinity to 5-hydroxytryptamine 4 receptor in rat striatum membrane
413 7 3 5 1.2 CS(=O)(=O)NCCN1CCC(CNC(=O)c2cc(Cl)cc3[nH]cnc23)CC1
CHEMBL2391994 5ht4r_human Human No 9.9 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
490 7 1 6 4.9 CC(C)(C(=O)O)c1ccc(CN2CCC(COC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1
CHEMBL178285 5ht4r_human Human No 9.9 Ki = 0.1 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
493 8 1 6 2.7 CC1(C)CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1
CHEMBL178669 5ht4r_human Human No 9.9 Ki = 0.1 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
508 8 1 7 0.8 CC(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1
CHEMBL179833 5ht4r_human Human No 9.9 Ki = 0.1 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
572 10 1 8 1.0 CC(C)S(=O)(=O)N1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1
CHEMBL315071 5ht4r_rat Rat No 9.9 Ki = 0.1 nM Bind
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
366 6 1 5 3.5 CCCCN1CCC(COC(=O)c2cc(Cl)c(N)c3c2OCC3)CC1
CHEMBL1632167 5ht4r_human Human No 9.9 Ki = 0.1 nM Bind
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
517 11 1 6 5.2 O=C(CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1)OCc1ccccc1
CHEMBL33884 5ht4r_rat Rat Yes 9.8 Ki = 0.2 nM Bind
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL33884 5ht4r_rat Rat Yes 9.8 Ki = 0.2 nM Bind
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL3221571 5ht4r_rat Rat No 9.8 Ki = 0.2 nM Bind
Displacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]GR113808 from 5-HT4 receptor in rat striatal membranes after 30 mins by liquid scintillation spectrometric analysis
330 6 2 3 3.3 CCCCN1CCC(CNC(=S)c2cccc3[nH]cnc23)CC1
CHEMBL2152922 5ht4r_human Human Yes 9.8 Ki = 0.2 nM Bind
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
432 7 1 8 2.6 OC1(CCOCC1)CN1CCC(CC1)COc1noc2c1c(ccc2)O[C@H]1COCC1
CHEMBL33884 5ht4r_human Human Yes 9.8 Ki = 0.2 nM Bind
Binding affinity at 5HT4 receptorBinding affinity at 5HT4 receptor
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL356359 5ht4r_human Human Yes 9.8 Ki = 0.2 nM Bind
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2
CHEMBL2179699 5ht4r_human Human No 9.8 Ki = 0.2 nM Bind
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
410 7 1 4 5.0 CC(C)n1nc(C(=O)NCC2CCN(CCC3CCCCC3)CC2)c2ccccc21
CHEMBL2221066 5ht4r_human Human No 9.8 Ki = 0.2 nM Bind
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
410 7 1 4 5.0 CC(C)n1nc(C(=O)NCC2CCN(CCC3CCCCC3)CC2)c2ccccc21
CHEMBL180697 5ht4r_human Human No 9.8 Ki = 0.2 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
466 8 2 7 0.5 O=C(NCC1CCN(CCCS(=O)(=O)N2CCNCC2)CC1)c1cccc2c1OCCO2
CHEMBL181415 5ht4r_human Human No 9.8 Ki = 0.2 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
557 10 1 8 1.8 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(Cc3cccnc3)CC2)CC1)c1cccc2c1OCCO2
CHEMBL201621 5ht4r_cavpo Guinea pig No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
324 4 1 5 2.6 COc1cc(N)c(Cl)cc1C(=O)OC[C@@H]1CCN2CCC[C@@H]12
CHEMBL201946 5ht4r_cavpo Guinea pig No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatumDisplacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum
284 3 1 3 2.8 O=C(OC[C@@H]1CCN2CCC[C@@H]12)c1c[nH]c2ccccc12
CHEMBL1632159 5ht4r_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
497 13 1 6 5.2 COC(=O)CCCCCCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1
CHEMBL2221193 5ht4r_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
419 7 2 5 3.9 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(N)cc3)CC2)c2ccccc21
CHEMBL3216126 5ht4r_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
419 7 2 5 3.9 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(N)cc3)CC2)c2ccccc21
CHEMBL3329803 5ht4r_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
496 7 2 6 3.4 CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3c4n(c5ccccc35)CCCO4)CC2)cc1
CHEMBL3329806 5ht4r_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
564 8 2 6 5.1 O=C(NCC1CCN(Cc2ccc(NS(=O)(=O)C3CCCCC3)cc2)CC1)c1c2n(c3ccccc13)CCCO2
CHEMBL3329807 5ht4r_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
459 7 2 6 2.5 CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)cc1
CHEMBL3329809 5ht4r_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
501 9 2 6 3.5 CC(C)CS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)cc1
CHEMBL181928 5ht4r_human Human No 9.7 Ki = 0.2 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
465 8 1 6 2.1 O=C(NCC1CCN(CCCS(=O)(=O)N2CCCCC2)CC1)c1cccc2c1OCCO2
CHEMBL3093187 5ht4r_human Human No 9.7 Ki = 0.2 nM Bind
Binding affinity to human 5HT4RBinding affinity to human 5HT4R
421 6 0 4 5.4 Fc1cccc2c1nc(OCC1CCN(CCCC(F)(F)F)CC1)c1cccnc12
CHEMBL3126109 5ht4r_rat Rat No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma countingDisplacement of [3H]GR113808 from 5HT4 receptor in Sprague-Dawley rat striatal membranes after 1 hr by gamma counting
372 5 1 6 2.5 Nc1c(Cl)cc(C(=O)OCC2CCN(CCF)CC2)c2c1OCCO2
CHEMBL114112 5ht4r_cavpo Guinea pig Yes 9.7 Ki = 0.2 nM Bind
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
474 6 1 6 3.3 CCCCN1CCC(CC1)COC(=O)c1cc(I)c(c2c1OCCO2)N
CHEMBL1258786 5ht4r_cavpo Guinea pig No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranesDisplacement of [3H]GR113808 from 5HT4 receptor in guinea pig striatal membranes
352 9 1 5 3.3 CCCCN1CCC(COC(=O)c2ccc(N)c(OCCF)c2)CC1
CHEMBL2181166 5ht4r_human Human No 9.6 Ki = 0.2 nM Bind
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12
CHEMBL1632162 5ht4r_human Human No 9.6 Ki = 0.2 nM Bind
Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting
455 7 1 6 4.0 CC(C)(C)OC(=O)CCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1
CHEMBL2179704 5ht4r_human Human No 9.6 Ki = 0.3 nM Bind
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
420 7 2 5 4.0 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(O)cc3)CC2)c2ccccc21
CHEMBL2221162 5ht4r_human Human No 9.6 Ki = 0.3 nM Bind
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cellsDisplacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
420 7 2 5 4.0 CC(C)n1nc(C(=O)NCC2CCN(CCc3ccc(O)cc3)CC2)c2ccccc21
CHEMBL33884 5ht4r_human Human Yes 9.6 Ki = 0.3 nM Bind
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C
CHEMBL3329808 5ht4r_human Human No 9.6 Ki = 0.3 nM Bind
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranesDisplacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
501 10 2 6 3.6 CCCCS(=O)(=O)Nc1ccc(CN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)cc1
CHEMBL356359 5ht4r_human Human Yes 9.6 Ki = 0.3 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2
CHEMBL180632 5ht4r_human Human Yes 9.6 Ki = 0.3 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
480 8 1 7 0.9 CN1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1
CHEMBL360531 5ht4r_human Human No 9.6 Ki = 0.3 nM Bind
Inhibitory constant for human cloned 5-HT4 receptorInhibitory constant for human cloned 5-HT4 receptor
543 9 1 8 1.8 O=C(NCC1CCN(CCCS(=O)(=O)N2CCN(c3ccccn3)CC2)CC1)c1cccc2c1OCCO2
CHEMBL50660 5ht4r_rat Rat No 9.6 Ki = 0.3 nM Bind
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
340 5 1 5 3.1 COc1cc(N)c(Cl)cc1C(=O)OCCN1C[C@@H](C)C[C@@H](C)C1
CHEMBL155917 5ht4r_rat Rat Yes 9.6 Ki = 0.3 nM Bind
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligandBinding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
340 5 1 5 3.1 COc1cc(N)c(cc1C(=O)OCCN1CC(C)CC(C1)C)Cl
CHEMBL2181168 5ht4r_human Human No 9.6 Ki = 0.3 nM Bind
Displacement of radioligand from human 5HT4R by Cerep protocol based assayDisplacement of radioligand from human 5HT4R by Cerep protocol based assay
461 5 0 4 4.9 CCCN1CCC(COc2nc3c(I)cccc3c3ncccc23)CC1