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
CHEMBL4468523 v2r_rat Rat Yes 10.7 EC50 = 0.0 nM Funct
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
945 14 10 11 0.0 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1429 v2r_rat Rat Yes 10.5 EC50 = 0.0 nM Funct
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
None None None None
CHEMBL264448 v2r_rat Rat Yes 10.5 EC50 = 0.0 nM Funct
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
None None None None
CHEMBL373742 v2r_human Human Yes 10.3 EC50 = 0.1 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
None None None None
CHEMBL435323 v2r_human Human Yes 10.3 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL373742 v2r_human Human Yes 10.3 EC50 = 0.1 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None None
CHEMBL4539370 v2r_rat Rat Yes 10.3 EC50 = 0.1 nM Funct
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1044 17 10 12 0.3 CCN(CC)C(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL373742 v2r_human Human Yes 10.3 EC50 = 0.1 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None None
CHEMBL373742 v2r_human Human Yes 10.3 EC50 = 0.1 nM Funct
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
None None None None
CHEMBL4468523 v2r_human Human Yes 10.2 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
945 14 10 11 0.0 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4454891 v2r_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
957 15 12 13 -1.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4474518 v2r_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
975 15 11 12 -0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCSCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4454160 v2r_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
939 14 11 11 -0.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4462743 v2r_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
975 15 11 12 -0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4528032 v2r_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
957 15 12 13 -1.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4533159 v2r_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1034 16 11 13 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CSCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4579754 v2r_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1032 16 12 13 -1.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4536454 v2r_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1034 16 11 13 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CSCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4544907 v2r_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
963 14 10 12 -0.1 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4532363 v2r_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
975 15 11 12 -0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4472007 v2r_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1116 18 11 14 0.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCCc2cccs2)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4444891 v2r_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
885 13 9 12 -0.4 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCN)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4459424 v2r_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1016 16 11 12 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4539100 v2r_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1078 17 11 12 0.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1429 v2r_human Human Yes 9.7 EC50 = 0.2 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
None None None None
CHEMBL264448 v2r_human Human Yes 9.7 EC50 = 0.2 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
None None None None
CHEMBL1429 v2r_human Human Yes 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
None None None None
CHEMBL264448 v2r_human Human Yes 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
None None None None
CHEMBL4571464 v2r_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1060 17 12 13 -0.8 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4455496 v2r_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1048 17 11 13 -0.2 CCCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CSCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4473843 v2r_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1042 17 11 12 -0.1 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCC2CC2)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4446853 v2r_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4521807 v2r_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4574065 v2r_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
975 14 10 11 0.0 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4451555 v2r_human Human No 9.6 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1028 16 11 12 -0.3 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NC2CC2)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4531173 v2r_human Human No 9.6 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1060 17 12 13 -0.8 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4539370 v2r_human Human Yes 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1044 17 10 12 0.3 CCN(CC)C(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4543908 v2r_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1044 18 11 12 0.3 CCCCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4555263 v2r_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1060 17 12 13 -0.2 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4451692 v2r_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1002 15 11 12 -0.8 CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4557473 v2r_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1038 17 11 11 0.1 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4462616 v2r_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1026 16 12 12 -1.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4546884 v2r_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1016 16 11 12 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4557118 v2r_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1044 17 11 12 0.2 CC(C)CNC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4439313 v2r_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1128 18 11 13 0.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCCc2cccs2)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4438723 v2r_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
957 14 10 10 0.1 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4531053 v2r_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1096 17 11 13 0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4527761 v2r_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1034 16 11 13 -0.2 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4445168 v2r_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1030 17 11 12 -0.1 CCCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4435502 v2r_human Human No 9.5 EC50 = 0.4 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
987 15 11 11 -0.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4521602 v2r_human Human No 9.5 EC50 = 0.4 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
969 16 11 12 -0.7 CCc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3cccs3)NC2=O)cc1
CHEMBL4513567 v2r_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1028 16 11 12 -0.3 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4552500 v2r_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
955 15 11 12 -0.9 Cc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3cccs3)NC2=O)cc1
CHEMBL1819440 v2r_human Human Yes 9.4 EC50 = 0.4 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL4436571 v2r_human Human No 9.4 EC50 = 0.5 nM Funct
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
1030 16 11 12 -0.1 CC(C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL1819440 v2r_human Human Yes 9.4 EC50 = 0.5 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL363910 v2r_human Human Yes 9.2 EC50 = 0.7 nM Funct
Agonist activity at V2 receptor (unknown origin) by cAMP accumulation assayAgonist activity at V2 receptor (unknown origin) by cAMP accumulation assay
402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2
CHEMBL363910 v2r_human Human Yes 9.1 EC50 = 0.7 nM Funct
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2
CHEMBL594026 v2r_human Human No 9.0 EC50 = 1.0 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
503 5 2 4 4.4 C[C@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)C1
CHEMBL606464 v2r_human Human No 9.0 EC50 = 1.0 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
503 5 2 4 4.4 C[C@@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)C1
CHEMBL593325 v2r_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
537 5 2 4 4.7 C[C@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)C1
CHEMBL594488 v2r_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
537 5 2 4 4.7 C[C@@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)C1
CHEMBL1186825 v2r_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1
CHEMBL479918 v2r_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1
CHEMBL1819441 v2r_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1819441 v2r_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL201889 v2r_human Human No 8.8 EC50 = 1.7 nM Funct
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
449 2 1 5 5.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(C(F)(F)F)c2)n1
CHEMBL487164 v2r_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1
CHEMBL528996 v2r_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1
CHEMBL3353932 v2r_human Human No 8.7 EC50 = 1.8 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1005 19 11 14 -2.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CCC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL487164 v2r_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1
CHEMBL528996 v2r_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1
CHEMBL501078 v2r_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
568 7 1 4 4.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](OCc2ccccc2)C[C@H]1C(=O)N(C)C
CHEMBL507816 v2r_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
463 5 2 2 5.8 CCc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F
CHEMBL3353940 v2r_human Human No 7.0 EC50 = 100 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1035 23 11 14 -1.1 CCCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL3353943 v2r_human Human No 7.0 EC50 = 100 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1009 21 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354598 v2r_human Human No 7.0 EC50 = 100 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1038 21 11 13 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL460303 v2r_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
449 4 1 4 3.8 COC(=O)[C@@H]1CCCN1C(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C
CHEMBL516629 v2r_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
448 5 2 3 3.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N1CCCC1
CHEMBL181487 v2r_human Human No 7.0 EC50 = 100 nM Bind
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
643 6 1 6 5.6 CO[C@@H]1C[C@@H](C(=S)N2CCC(N3CCCC3)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1
CHEMBL3354587 v2r_human Human No 6.0 EC50 = 1000 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
988 22 10 12 -1.5 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL475129 v2r_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
464 4 1 4 3.2 Cc1cc(C(=O)N2CCCOc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C
CHEMBL1186831 v2r_human Human No 7.0 EC50 = 104 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1
CHEMBL480104 v2r_human Human No 7.0 EC50 = 104 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1
CHEMBL4127791 v2r_human Human No 5.0 EC50 = 10764 nM Funct
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
1095 17 11 14 -0.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2ccccc2CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353939 v2r_human Human No 8.0 EC50 = 11 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1019 19 11 14 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CCCC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354585 v2r_human Human No 7.0 EC50 = 110 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1004 22 11 13 -1.8 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL455696 v2r_human Human No 7.0 EC50 = 110 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
465 5 2 3 5.3 COc1cc(CNC(=O)Nc2c(F)cccc2F)ccc1C(=O)N1CCCCc2ccccc21
CHEMBL3301668 v2r_human Human Yes 6.0 EC50 = 1100 nM Funct
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
None None None CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C
CHEMBL3354577 v2r_human Human No 6.0 EC50 = 1100 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
975 21 10 13 -3.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCSC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1186826 v2r_human Human No 6.0 EC50 = 1100 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1
CHEMBL479919 v2r_human Human No 6.0 EC50 = 1100 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1
CHEMBL1817671 v2r_human Human No 6.0 EC50 = 1100 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O
CHEMBL362382 v2r_human Human No 6.0 EC50 = 1100 nM Bind
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
627 6 1 6 4.8 CO[C@@H]1C[C@@H](C(=O)N2CCC(N3CCCC3)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1
CHEMBL1817671 v2r_human Human No 6.0 EC50 = 1122.0 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O
CHEMBL1819548 v2r_human Human No 6.9 EC50 = 114.8 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819554 v2r_human Human No 5.9 EC50 = 1174.9 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL475333 v2r_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
499 4 1 4 3.8 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C
CHEMBL518349 v2r_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
451 5 2 4 4.1 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OC(C)(C)C
CHEMBL1819548 v2r_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354584 v2r_human Human No 5.9 EC50 = 1200 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
974 21 10 12 -1.9 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL1817690 v2r_human Human No 5.9 EC50 = 1200 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1035 19 11 16 -4.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)N(C)OC)NC1=O
CHEMBL1819553 v2r_human Human No 5.9 EC50 = 1200 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819554 v2r_human Human No 5.9 EC50 = 1200 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL443300 v2r_human Human No 5.9 EC50 = 1200 nM Bind
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
641 6 1 6 5.2 CO[C@@H]1C[C@@H](C(=O)N2CCC(N3CCCCC3)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1
CHEMBL1817690 v2r_human Human No 5.9 EC50 = 1230.3 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1035 19 11 16 -4.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)N(C)OC)NC1=O
CHEMBL1819553 v2r_human Human No 5.9 EC50 = 1230.3 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1837041 v2r_human Human No 7.9 EC50 = 13 nM Funct
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
458 3 0 7 3.0 CS(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1
CHEMBL455699 v2r_rat Rat No 7.9 EC50 = 13 nM Funct
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F
CHEMBL452853 v2r_human Human No 6.9 EC50 = 130 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
413 4 2 2 5.3 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccccc1
CHEMBL1817705 v2r_human Human No 6.9 EC50 = 130 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354578 v2r_human Human No 5.9 EC50 = 1300 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
975 21 10 13 -3.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL364994 v2r_human Human No 5.9 EC50 = 1300 nM Bind
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
587 5 1 6 3.8 CO[C@@H]1C[C@@H](C(=O)N2CCCN(C)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1
CHEMBL1817705 v2r_human Human No 6.9 EC50 = 131.8 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817706 v2r_human Human No 6.9 EC50 = 138.0 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL3354588 v2r_human Human No 6.9 EC50 = 140 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1023 20 11 13 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354595 v2r_human Human No 6.9 EC50 = 140 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1041 20 11 13 -1.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL454894 v2r_human Human No 6.9 EC50 = 140 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
430 4 3 3 4.0 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccc[nH]c1=O
CHEMBL460319 v2r_human Human No 6.9 EC50 = 140 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
423 6 2 4 3.3 CCOC(=O)CNC(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C
CHEMBL460320 v2r_human Human No 6.9 EC50 = 140 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
437 6 2 4 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OC(C)C
CHEMBL523596 v2r_human Human No 6.9 EC50 = 140 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
499 4 1 4 3.8 Cc1cc(C(=O)N2CCc3cccn3-c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C
CHEMBL1817706 v2r_human Human No 6.9 EC50 = 140 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL3354573 v2r_human Human No 5.9 EC50 = 1400 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1048 21 12 15 -2.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCC2CCCN2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354574 v2r_human Human No 5.9 EC50 = 1400 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1064 21 11 16 -3.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCN2CCOCC2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354596 v2r_human Human No 5.9 EC50 = 1400 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1025 20 10 12 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL472697 v2r_rat Rat No 7.8 EC50 = 15 nM Funct
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
506 6 1 4 3.8 CCO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1
CHEMBL3354580 v2r_human Human No 6.8 EC50 = 150 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
991 21 12 14 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL461725 v2r_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
462 5 2 3 3.8 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N1CCCCC1
CHEMBL518043 v2r_rat Rat Yes 6.8 EC50 = 150 nM Funct
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C
CHEMBL1819542 v2r_human Human Yes 6.8 EC50 = 154.9 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819542 v2r_human Human Yes 6.8 EC50 = 155 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL475684 v2r_human Human No 7.8 EC50 = 16 nM Funct
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnn4)c4ccccc43)c(Cl)c2)n1
CHEMBL3354597 v2r_human Human No 6.8 EC50 = 160 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1038 21 11 13 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354593 v2r_human Human No 5.8 EC50 = 1600 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1022 20 10 12 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817751 v2r_human Human No 5.8 EC50 = 1600 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
991 17 12 15 -4.8 CCNC(=O)C[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817702 v2r_human Human No 5.8 EC50 = 1600 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O
CHEMBL1817751 v2r_human Human No 5.8 EC50 = 1621.8 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
991 17 12 15 -4.8 CCNC(=O)C[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817691 v2r_human Human No 6.8 EC50 = 166.0 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1007 18 13 16 -4.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NO)NC1=O
CHEMBL1817702 v2r_human Human No 5.8 EC50 = 1659.6 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O
CHEMBL1819560 v2r_human Human No 5.8 EC50 = 1698.2 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1021 19 12 16 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NOC)NC1=O
CHEMBL3301668 v2r_human Human Yes 6.8 EC50 = 170 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
None None None CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C
CHEMBL3353951 v2r_human Human No 6.8 EC50 = 170 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccnc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817691 v2r_human Human No 6.8 EC50 = 170 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1007 18 13 16 -4.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NO)NC1=O
CHEMBL475128 v2r_human Human No 5.8 EC50 = 1700 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
498 4 1 3 4.3 Cc1cc(C(=O)N2CCCC(F)(F)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C
CHEMBL1819560 v2r_human Human No 5.8 EC50 = 1700 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1021 19 12 16 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NOC)NC1=O
CHEMBL3354582 v2r_human Human No 7.8 EC50 = 18 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
990 21 11 13 -2.2 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL3353950 v2r_human Human No 6.8 EC50 = 180 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccn2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353954 v2r_human Human No 6.8 EC50 = 180 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1056 21 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2ccccn2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL455695 v2r_human Human No 6.8 EC50 = 180 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
453 4 2 2 5.4 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)c(F)c1)Nc1c(F)cccc1F
CHEMBL460318 v2r_human Human No 6.8 EC50 = 180 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
395 5 3 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)O
CHEMBL4537162 v2r_human Human No 5.8 EC50 = 1800 nM Funct
Agonist activity at recombinant human V2 receptor expressed in CHOK1 cells assessed as increase in cAMP level measured after 30 mins by HTRF assayAgonist activity at recombinant human V2 receptor expressed in CHOK1 cells assessed as increase in cAMP level measured after 30 mins by HTRF assay
1724 62 18 24 -0.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)NCC(=O)N[C@@H](CSCC(=O)NCCOCCOCCC(=O)NCCOCCOCCC(=O)NCCCC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL184696 v2r_human Human No 5.8 EC50 = 1800 nM Bind
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
561 8 2 6 3.4 CO[C@@H]1C[C@@H](C(=O)NCCN(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1
CHEMBL185152 v2r_human Human No 5.8 EC50 = 1800 nM Bind
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
573 4 1 5 5.0 CN1CCCN(C(=S)[C@@H]2CCCN2C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)CC1
CHEMBL1817708 v2r_human Human No 6.7 EC50 = 186.2 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNCCC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL332447 v2r_human Human Yes 6.7 EC50 = 189 nM Funct
Agonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassayAgonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassay
453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C
CHEMBL4126100 v2r_human Human No 4.7 EC50 = 18919 nM Funct
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
1139 19 14 15 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2ccccc2CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817708 v2r_human Human No 6.7 EC50 = 190 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNCCC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL455699 v2r_human Human No 8.7 EC50 = 2.1 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F
CHEMBL462574 v2r_human Human No 8.6 EC50 = 2.3 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
478 4 2 4 2.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](O)C[C@H]1C(=O)N(C)C
CHEMBL594953 v2r_human Human No 8.6 EC50 = 2.4 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
534 5 2 5 4.4 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)n1
CHEMBL470326 v2r_human Human No 7.7 EC50 = 20 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
536 7 1 5 3.6 COC(OC)C1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1
CHEMBL1819549 v2r_human Human No 6.7 EC50 = 200 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccsc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL182627 v2r_human Human No 6.7 EC50 = 200 nM Bind
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
611 8 2 6 5.7 CO[C@@H]1C[C@@H](/C(S)=N/CCc2ccccn2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1
CHEMBL3354583 v2r_human Human No 5.7 EC50 = 2000 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
974 21 10 12 -1.9 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL1819549 v2r_human Human No 6.7 EC50 = 204.2 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccsc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819557 v2r_human Human No 6.7 EC50 = 208.9 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1005 18 12 15 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NC)NC1=O
CHEMBL395429 v2r_human Human Yes 6.7 EC50 = 210 nM Funct
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
None None None None
CHEMBL3354591 v2r_human Human No 6.7 EC50 = 210 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1038 20 11 13 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL462409 v2r_human Human No 6.7 EC50 = 210 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
394 5 3 3 2.3 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(N)=O
CHEMBL1819557 v2r_human Human No 6.7 EC50 = 210 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1005 18 12 15 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NC)NC1=O
CHEMBL3354586 v2r_human Human No 5.7 EC50 = 2100 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1004 22 11 13 -1.8 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL1837040 v2r_human Human No 6.7 EC50 = 215 nM Funct
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
422 2 0 6 3.6 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1
CHEMBL474120 v2r_human Human No 6.7 EC50 = 220 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
476 4 1 3 4.3 Cc1cc(C(=O)N2CCCC(C)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C
CHEMBL3354572 v2r_human Human No 6.6 EC50 = 230 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1035 20 11 15 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)CC2CCCO2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL474119 v2r_human Human No 6.6 EC50 = 230 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
478 4 2 4 3.2 Cc1cc(C(=O)N2CCCC(O)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C
CHEMBL362483 v2r_human Human No 6.6 EC50 = 230 nM Bind
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
603 5 1 6 4.6 CO[C@@H]1C[C@@H](C(=S)N2CCCN(C)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1
CHEMBL3763342 v2r_human Human Yes 5.6 EC50 = 2300 nM Funct
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
581 5 4 8 4.1 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCN(Cc2cc(O)cc(O)c2)CC1
CHEMBL518043 v2r_human Human Yes 7.6 EC50 = 24 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C
CHEMBL3354600 v2r_human Human No 6.6 EC50 = 250 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1029 20 11 14 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819547 v2r_human Human No 5.6 EC50 = 2500 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cscn2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819547 v2r_human Human No 5.6 EC50 = 2511.9 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cscn2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817707 v2r_human Human No 6.6 EC50 = 257.0 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1817707 v2r_human Human No 6.6 EC50 = 260 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL3352839 v2r_human Human No 5.6 EC50 = 2600 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
975 21 11 13 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817696 v2r_human Human No 5.6 EC50 = 2600 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
993 17 13 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NO)NC1=O
CHEMBL1819558 v2r_human Human No 5.6 EC50 = 2600 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1019 19 12 15 -4.0 CCNC(=O)CC[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817709 v2r_human Human Yes 5.6 EC50 = 2630.3 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None None
CHEMBL1817696 v2r_human Human No 5.6 EC50 = 2630.3 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
993 17 13 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NO)NC1=O
CHEMBL1819558 v2r_human Human No 5.6 EC50 = 2630.3 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1019 19 12 15 -4.0 CCNC(=O)CC[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1837037 v2r_human Human Yes 6.6 EC50 = 265 nM Funct
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
394 2 0 6 3.6 CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1
CHEMBL472900 v2r_human Human No 7.6 EC50 = 27 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
476 4 1 4 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CC(=O)C[C@H]1C(=O)N(C)C
CHEMBL460308 v2r_human Human No 6.6 EC50 = 270 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
484 7 3 3 4.1 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)NCc1ccccc1
CHEMBL1817709 v2r_human Human Yes 5.6 EC50 = 2700 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None None
CHEMBL1817704 v2r_human Human No 6.6 EC50 = 281.8 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL395429 v2r_human Human Yes 7.5 EC50 = 29 nM Funct
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
None None None None
CHEMBL1817704 v2r_human Human No 6.5 EC50 = 290 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1187728 v2r_human Human No 8.5 EC50 = 3.1 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1
CHEMBL516757 v2r_human Human No 8.5 EC50 = 3.1 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1
CHEMBL462212 v2r_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
478 4 1 3 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N(C)C
CHEMBL439044 v2r_human Human Yes 8.5 EC50 = 3.5 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
991 17 11 14 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353946 v2r_human Human No 7.5 EC50 = 30 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1055 20 11 14 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354601 v2r_human Human No 7.5 EC50 = 30 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1029 20 11 14 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL455717 v2r_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
431 4 2 2 5.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccccc1F
CHEMBL3354599 v2r_human Human No 5.5 EC50 = 3000 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1022 21 10 12 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819559 v2r_human Human No 5.5 EC50 = 3000 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1047 20 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NCC(C)C)NC1=O
CHEMBL1819559 v2r_human Human No 5.5 EC50 = 3020.0 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
1047 20 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NCC(C)C)NC1=O
CHEMBL1837038 v2r_human Human No 7.5 EC50 = 31 nM Funct
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
438 2 0 7 3.8 COC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1
CHEMBL3354594 v2r_human Human No 6.5 EC50 = 330 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1041 20 11 13 -1.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819550 v2r_human Human No 6.5 EC50 = 330 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819550 v2r_human Human No 6.5 EC50 = 331.1 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353944 v2r_human Human No 7.5 EC50 = 34 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1041 20 11 14 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353931 v2r_human Human No 7.5 EC50 = 35 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1007 21 11 14 -1.9 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL461519 v2r_human Human No 6.5 EC50 = 350 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
490 6 1 3 4.5 CCN(CC)C(=O)[C@@H]1CCCN1C(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C
CHEMBL3354589 v2r_human Human No 7.4 EC50 = 36 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1023 20 11 13 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL4128839 v2r_human Human No 5.4 EC50 = 3669 nM Funct
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
1081 17 11 14 -0.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2ccc(cc2)SC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL516788 v2r_human Human No 7.4 EC50 = 37 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
409 5 2 4 3.0 COC(=O)CNC(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C
CHEMBL1817752 v2r_human Human No 5.4 EC50 = 3700 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL24781 v2r_human Human Yes 4.4 EC50 = 37000 nM Bind
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C
CHEMBL1817752 v2r_human Human No 5.4 EC50 = 3715.4 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL3353952 v2r_human Human No 6.4 EC50 = 380 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccncc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL461520 v2r_human Human No 6.4 EC50 = 380 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C
CHEMBL1819556 v2r_human Human No 6.4 EC50 = 380 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)C2(CCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819556 v2r_human Human No 6.4 EC50 = 380.2 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)C2(CCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817761 v2r_human Human No 6.4 EC50 = 389.1 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL363910 v2r_human Human Yes 7.4 EC50 = 39.9 nM Bind
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2
CHEMBL462595 v2r_human Human No 6.4 EC50 = 390 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
491 4 1 4 5.0 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
CHEMBL1817761 v2r_human Human No 6.4 EC50 = 390 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL4129142 v2r_human Human No 5.4 EC50 = 3900 nM Funct
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
1095 17 11 14 -0.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2cccc(c2)CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL4205046 v2r_human Human No 8.4 EC50 = 4 nM Funct
Agonist activity at human V2 receptor expressed in human HeLa cells assessed as cAMP accumulation incubated for 10 mins by radioimmunoassayAgonist activity at human V2 receptor expressed in human HeLa cells assessed as cAMP accumulation incubated for 10 mins by radioimmunoassay
408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1
CHEMBL1819541 v2r_human Human No 8.4 EC50 = 4.1 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819541 v2r_human Human No 8.4 EC50 = 4.1 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL478902 v2r_human Human No 8.4 EC50 = 4.2 nM Funct
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
457 3 1 4 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)O)c4ccccc43)c(Cl)c2)n1
CHEMBL3353929 v2r_human Human No 8.4 EC50 = 4.2 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
991 19 11 14 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL472697 v2r_human Human No 8.4 EC50 = 4.3 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
506 6 1 4 3.8 CCO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1
CHEMBL515607 v2r_human Human No 8.3 EC50 = 4.7 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
492 5 1 4 3.4 CO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1
CHEMBL3353935 v2r_human Human No 7.4 EC50 = 40 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1017 19 11 14 -3.1 CCOc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3C[C@@H](O)C[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]([C@@H](C)CC)NC2=O)cc1
CHEMBL509960 v2r_human Human No 7.4 EC50 = 40 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
469 4 2 2 5.9 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1)Nc1c(F)cccc1F
CHEMBL4204210 v2r_human Human Yes 7.4 EC50 = 41 nM Funct
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
531 4 2 6 4.2 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N(C)C
CHEMBL462574 v2r_rat Rat No 7.4 EC50 = 41 nM Funct
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
478 4 2 4 2.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](O)C[C@H]1C(=O)N(C)C
CHEMBL3353936 v2r_human Human No 6.4 EC50 = 450 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1032 20 10 14 -2.5 CCOc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3C[C@@H](OC)C[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]([C@@H](C)CC)NC2=O)cc1
CHEMBL3353937 v2r_human Human No 6.4 EC50 = 450 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
947 19 11 13 -3.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL512349 v2r_human Human No 7.3 EC50 = 46 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
534 5 1 4 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](OC(C)(C)C)C[C@H]1C(=O)N(C)C
CHEMBL1819552 v2r_human Human No 6.3 EC50 = 467.7 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353955 v2r_human Human No 7.3 EC50 = 47 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1056 21 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2ccncc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL455718 v2r_human Human No 7.3 EC50 = 47 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
435 4 2 2 5.3 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1)Nc1c(F)cccc1F
CHEMBL1819552 v2r_human Human No 6.3 EC50 = 470 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL473917 v2r_human Human No 7.3 EC50 = 50 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
512 5 1 3 4.2 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CC(C(F)F)C[C@H]1C(=O)N(C)C
CHEMBL182852 v2r_rat Rat Yes 7.3 EC50 = 50 nM Funct
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
422 5 2 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N(C)C
CHEMBL3354579 v2r_human Human No 6.3 EC50 = 500 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
991 21 12 14 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354576 v2r_human Human No 7.3 EC50 = 52 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
991 21 11 14 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817750 v2r_human Human No 5.3 EC50 = 5248.1 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
977 16 12 15 -5.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NC)NC1=O
CHEMBL1817750 v2r_human Human No 5.3 EC50 = 5300 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
977 16 12 15 -5.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NC)NC1=O
CHEMBL3354592 v2r_human Human No 7.3 EC50 = 55 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1038 20 11 13 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353941 v2r_human Human No 7.2 EC50 = 57 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1033 19 11 14 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CCCCC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353956 v2r_human Human No 7.2 EC50 = 57 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1047 20 11 15 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL445393 v2r_human Human No 6.2 EC50 = 570 nM Bind
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
595 8 2 6 4.4 CO[C@@H]1C[C@@H](C(=O)NCCc2ccccn2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1
CHEMBL182852 v2r_human Human Yes 7.2 EC50 = 58 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
422 5 2 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N(C)C
CHEMBL478283 v2r_human Human No 8.2 EC50 = 6.3 nM Funct
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1
CHEMBL478283 v2r_human Human No 8.2 EC50 = 6.3 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1
CHEMBL1186989 v2r_human Human No 7.2 EC50 = 61.9 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1
CHEMBL485760 v2r_human Human No 7.2 EC50 = 61.9 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1
CHEMBL3354570 v2r_human Human No 7.2 EC50 = 62 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1031 20 11 15 -1.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccco2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1187505 v2r_human Human No 6.2 EC50 = 646 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1
CHEMBL505517 v2r_human Human No 6.2 EC50 = 646 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1
CHEMBL515607 v2r_rat Rat No 7.2 EC50 = 65 nM Funct
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
492 5 1 4 3.4 CO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1
CHEMBL3353953 v2r_human Human No 7.2 EC50 = 66 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1055 21 11 14 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL4204210 v2r_human Human Yes 6.2 EC50 = 660 nM Funct
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
531 4 2 6 4.2 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N(C)C
CHEMBL3353934 v2r_human Human No 6.2 EC50 = 670 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1033 19 10 14 -2.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2C[C@H](SC)C[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3301668 v2r_human Human Yes 5.2 EC50 = 6700 nM Funct
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
None None None CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C
CHEMBL3353945 v2r_human Human No 7.2 EC50 = 68 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1055 20 11 14 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL462590 v2r_human Human No 6.2 EC50 = 680 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
435 4 2 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)O
CHEMBL3353933 v2r_human Human No 6.2 EC50 = 690 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1017 19 10 14 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2C[C@H](OC)C[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL395429 v2r_human Human Yes 8.1 EC50 = 7.3 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
None None None None
CHEMBL603708 v2r_human Human No 8.1 EC50 = 7.6 nM Bind
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL3354575 v2r_human Human No 7.2 EC50 = 70 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
991 21 11 14 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819543 v2r_human Human No 7.1 EC50 = 72.4 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354590 v2r_human Human No 6.1 EC50 = 720 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1007 20 10 12 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817703 v2r_human Human No 6.1 EC50 = 720 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817703 v2r_human Human No 6.1 EC50 = 724.4 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354581 v2r_human Human No 7.1 EC50 = 73 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
990 21 11 13 -2.2 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL1819543 v2r_human Human No 7.1 EC50 = 73 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL516985 v2r_human Human No 6.1 EC50 = 730 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
485 7 2 4 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OCc1ccccc1
CHEMBL1819555 v2r_human Human No 6.1 EC50 = 758.6 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354602 v2r_human Human No 6.1 EC50 = 760 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1013 20 10 13 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819555 v2r_human Human No 6.1 EC50 = 760 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353938 v2r_human Human No 7.1 EC50 = 77 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1021 22 11 14 -1.5 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL3353949 v2r_human Human No 7.1 EC50 = 78 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1071 21 11 15 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(OC)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353942 v2r_human Human No 7.1 EC50 = 80 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1009 21 11 15 -3.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL395429 v2r_human Human Yes 6.1 EC50 = 810 nM Funct
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
None None None None
CHEMBL3353948 v2r_human Human No 7.1 EC50 = 82 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1059 20 11 14 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL454892 v2r_human Human No 7.1 EC50 = 82 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
463 4 2 2 5.9 Cc1cc(C(=O)N2CCCCc3ccccc32)cc(C)c1CNC(=O)Nc1c(F)cccc1F
CHEMBL462408 v2r_human Human No 6.1 EC50 = 820 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
471 6 2 4 4.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)Oc1ccccc1
CHEMBL3353947 v2r_human Human No 7.1 EC50 = 84 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1055 20 11 14 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(C)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL475733 v2r_human Human No 7.1 EC50 = 84 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
510 4 1 3 4.6 Cc1cc(C(=O)N2CCc3ccccc3-c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C
CHEMBL360648 v2r_human Human Yes 6.1 EC50 = 850 nM Bind
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1
CHEMBL360648 v2r_human Human Yes 6.1 EC50 = 850 nM Funct
Agonist activity at human V2 receptor expressed in CHO cells co-expressing CRE-luciferase incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human V2 receptor expressed in CHO cells co-expressing CRE-luciferase incubated for 5 hrs by luciferase reporter gene assay
600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1
CHEMBL360648 v2r_human Human Yes 6.1 EC50 = 850 nM Bind
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1
CHEMBL3354571 v2r_human Human No 7.1 EC50 = 86 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1061 21 11 15 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2cccs2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL365862 v2r_human Human No 6.1 EC50 = 890 nM Bind
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
553 4 1 5 4.7 Cc1cc(C(=O)N2CCCCc3sccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1
CHEMBL1819540 v2r_human Human No 8.0 EC50 = 9.1 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1819540 v2r_human Human No 8.0 EC50 = 9.2 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL3353930 v2r_human Human No 8.0 EC50 = 9.9 nM Bind
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1005 20 11 14 -2.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)CC2CC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL516627 v2r_human Human No 6.0 EC50 = 950 nM Funct
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
477 5 1 4 4.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)OC(C)C
CHEMBL1817756 v2r_human Human No 6.0 EC50 = 950 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817756 v2r_human Human No 6.0 EC50 = 955.0 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817770 v2r_human Human No 6.0 EC50 = 970 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817770 v2r_human Human No 6.0 EC50 = 977.2 nM Funct
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL102311 v2r_human Human No 9.7 IC50 = 0.2 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
466 4 1 3 6.3 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1
CHEMBL49429 v2r_rat Rat Yes 9.3 IC50 = 0.5 nM Bind
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL311931 v2r_human Human No 9.3 IC50 = 0.5 nM Bind
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
469 3 1 3 6.2 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1C
CHEMBL603708 v2r_human Human No 9.2 IC50 = 0.6 nM Funct
Antagonist activity at V2 receptor (unknown origin)Antagonist activity at V2 receptor (unknown origin)
446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL420031 v2r_human Human No 9.2 IC50 = 0.7 nM Bind
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
493 3 1 3 6.4 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1Cl
CHEMBL49322 v2r_human Human No 9.2 IC50 = 0.7 nM Bind
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
438 3 1 3 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cc1
CHEMBL434654 v2r_human Human No 9.0 IC50 = 1.0 nM Funct
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
462 5 1 3 6.0 Cc1ccccc1OCC(=O)Nc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(C)c1
CHEMBL165670 v2r_rat Rat No 9.0 IC50 = 1 nM Bind
Binding affinity towards V2 receptorBinding affinity towards V2 receptor
471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1
CHEMBL3924331 v2r_human Human No 9.0 IC50 = 1 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
575 10 3 8 2.9 NC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl
CHEMBL46295 v2r_rat Rat No 9.0 IC50 = 1 nM Bind
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
440 3 1 4 4.8 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1
CHEMBL310416 v2r_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
455 3 1 3 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1
CHEMBL49429 v2r_human Human Yes 9.0 IC50 = 1 nM Bind
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL413748 v2r_rat Rat No 9.0 IC50 = 1 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
636 9 1 6 6.6 CN1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1
CHEMBL368354 v2r_human Human No 9.0 IC50 = 1 nM Bind
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
622 10 1 6 7.1 CN1CCN(CCCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1
CHEMBL301788 v2r_rat Rat No 9.0 IC50 = 1.1 nM Bind
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
460 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccc(F)cc1Cl
CHEMBL347020 v2r_rat Rat No 8.9 IC50 = 1.2 nM Bind
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
486 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)c(Cl)c1)c1ccccc1-c1ccccc1
CHEMBL49429 v2r_human Human Yes 8.9 IC50 = 1.2 nM Bind
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL49429 v2r_human Human Yes 8.9 IC50 = 1.2 nM Bind
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL49429 v2r_human Human Yes 8.9 IC50 = 1.2 nM Bind
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL49429 v2r_human Human Yes 8.9 IC50 = 1.2 nM Bind
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL49429 v2r_human Human Yes 8.9 IC50 = 1.2 nM Bind
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL165340 v2r_human Human No 8.9 IC50 = 1.3 nM Bind
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
629 6 1 5 7.0 CN1CCN(Cc2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1
CHEMBL3965167 v2r_human Human No 8.9 IC50 = 1.4 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
496 7 2 7 3.2 O=c1n(Cc2nnc(Cc3ccccc3F)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL159359 v2r_rat Rat No 8.8 IC50 = 1.5 nM Bind
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1
CHEMBL3938717 v2r_human Human No 8.8 IC50 = 1.5 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
512 7 2 7 3.7 O=c1n(Cc2nnc(Cc3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL68085 v2r_human Human No 8.8 IC50 = 1.5 nM Bind
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL68085 v2r_rat Rat No 8.8 IC50 = 1.5 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL299532 v2r_rat Rat No 8.8 IC50 = 1.6 nM Bind
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
486 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1Br
CHEMBL350973 v2r_human Human No 8.8 IC50 = 1.7 nM Bind
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
524 4 2 4 6.9 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1)c1ccccc1-c1ccccc1
CHEMBL300963 v2r_rat Rat No 8.7 IC50 = 1.8 nM Bind
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
442 3 1 4 5.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1Cl
CHEMBL80029 v2r_human Human No 8.7 IC50 = 1.9 nM Bind
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
473 3 1 3 6.1 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1
CHEMBL81269 v2r_human Human No 8.7 IC50 = 1.9 nM Bind
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
505 4 1 4 6.3 COc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1NC(=O)c1ccc(Cl)cc1Cl
CHEMBL319636 v2r_human Human No 8.0 IC50 = 10 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
569 6 2 5 5.0 COC(=O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3C)cc1)c1ccccc1C2
CHEMBL3923775 v2r_human Human No 8.0 IC50 = 10 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
607 9 3 7 3.5 CC(=O)NC(C)(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1
CHEMBL105961 v2r_human Human No 8.0 IC50 = 10 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
505 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl
CHEMBL175212 v2r_rat Rat No 8.0 IC50 = 10 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
525 6 1 5 6.7 COc1cc(C(=O)N2CCCC(N(C)C)c3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1
CHEMBL176146 v2r_rat Rat No 8.0 IC50 = 10 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
550 7 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCCC3)c3sccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL177285 v2r_rat Rat No 8.0 IC50 = 10 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
579 7 1 6 5.8 CN1CCN(CCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1
CHEMBL368818 v2r_human Human No 8.0 IC50 = 10 nM Bind
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
650 9 1 6 7.0 CN1CCCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1
CHEMBL71305 v2r_rat Rat No 8.0 IC50 = 10.2 nM Bind
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F
CHEMBL334363 v2r_human Human No 7.0 IC50 = 100 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
528 6 1 3 7.8 O=C(Nc1ccc(C(=O)N2CCC(CC(F)F)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL249340 v2r_human Human No 7.0 IC50 = 100 nM Funct
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
518 4 2 3 6.1 O=C(O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2
CHEMBL3964983 v2r_human Human No 7.0 IC50 = 100 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
509 6 1 7 4.4 O=c1n(Cc2ccnc(-c3ccccc3Cl)n2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL317243 v2r_human Human No 7.0 IC50 = 100 nM Funct
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
612 8 2 4 6.6 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL337725 v2r_human Human No 7.0 IC50 = 100 nM Funct
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
508 6 2 4 6.5 O=C(Nc1ccc(C(=O)N2CCC(CCO)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL366816 v2r_rat Rat No 7.0 IC50 = 100 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
607 6 1 6 5.7 CN1CCCN(CC(=O)N2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1
CHEMBL369712 v2r_rat Rat No 7.0 IC50 = 100 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
433 4 1 4 5.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3sccc32)cc1
CHEMBL118805 v2r_rat Rat No 6.0 IC50 = 1000 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
441 4 0 3 5.3 Cc1ccccc1C(=O)N(C)c1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1
CHEMBL119730 v2r_rat Rat No 6.0 IC50 = 1000 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
370 4 1 2 4.5 O=C(Cc1ccccc1)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1
CHEMBL237987 v2r_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
426 5 3 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2C(=O)O)c(Cl)c1
CHEMBL238206 v2r_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
505 7 3 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2Cn2cccc2C(=O)O)c(Cl)c1
CHEMBL343538 v2r_human Human No 6.0 IC50 = 1000 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
320 2 0 2 4.3 O=C(c1ccc(N2CCCC2)cc1)N1CCCCc2ccccc21
CHEMBL128398 v2r_rat Rat No 5.0 IC50 = 10000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
510 6 1 5 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cn1ccnc1)C2
CHEMBL128680 v2r_rat Rat No 5.0 IC50 = 10000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
521 6 1 4 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1cccnc1)C2
CHEMBL129234 v2r_rat Rat No 5.0 IC50 = 10000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
508 7 1 4 3.8 CCCS(=O)(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C
CHEMBL131269 v2r_rat Rat No 5.0 IC50 = 10000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
521 6 1 4 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1ccncc1)C2
CHEMBL131613 v2r_rat Rat No 5.0 IC50 = 10000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
520 6 1 3 4.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@H](NC(=O)Cc1ccccc1)C2
CHEMBL337667 v2r_rat Rat No 5.0 IC50 = 10000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
535 6 2 5 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1ccncc1)C2
CHEMBL339151 v2r_rat Rat No 5.0 IC50 = 10000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
472 5 2 4 3.1 CC(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C
CHEMBL435613 v2r_rat Rat No 5.0 IC50 = 10000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
512 6 1 7 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cn1cnnn1)C2
CHEMBL274955 v2r_rat Rat No 4.0 IC50 = 100000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
430 4 2 4 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@](O)(CN)C2
CHEMBL2332718 v2r_human Human No 5.0 IC50 = 10200 nM Bind
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression competition binding assay
None None None NC[C@@H]1NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O
CHEMBL326225 v2r_human Human No 7.0 IC50 = 105 nM Funct
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
568 7 2 4 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN(C)C)CC3)Cc3ccccc32)cc1
CHEMBL400860 v2r_human Human No 6.0 IC50 = 1050 nM Funct
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
572 5 2 5 6.0 COc1cc(C(=O)N2CC[C@]3(C=C(C4=NCCN4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl
CHEMBL1755 v2r_human Human Yes 8.0 IC50 = 11 nM Funct
Antagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulationAntagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulation
498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1
CHEMBL249740 v2r_human Human No 8.0 IC50 = 11 nM Funct
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
626 6 3 6 4.4 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)NS(N)(=O)=O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl
CHEMBL317243 v2r_human Human No 8.0 IC50 = 11 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
612 8 2 4 6.6 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL421039 v2r_human Human No 8.0 IC50 = 11 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
585 7 3 4 6.0 O=C(NCCO)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL3950716 v2r_human Human No 8.0 IC50 = 11 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
554 8 1 7 5.5 COc1ccc(Cn2c(-c3ccc(Cl)cc3)nn(Cc3nnc(Cc4c(Cl)cccc4Cl)[nH]3)c2=O)cc1
CHEMBL3915616 v2r_human Human No 8.0 IC50 = 11 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
651 9 3 8 5.0 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(Cl)c1Cl
CHEMBL424183 v2r_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
485 4 2 2 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4c[nH]c5cccc3c45)cc2)cc1
CHEMBL392363 v2r_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
489 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C=C3CCC(=O)N3Cc3ccccc32)c(Cl)c1
CHEMBL1181319 v2r_human Human No 7.9 IC50 = 11.5 nM Bind
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
643 5 1 5 6.7 CN1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1
CHEMBL164387 v2r_human Human No 7.9 IC50 = 11.5 nM Bind
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
643 5 1 5 6.7 CN1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1
CHEMBL3890193 v2r_human Human No 7.0 IC50 = 110 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
473 7 0 6 5.2 C=CCn1c(-c2ccc(Cl)cc2)nn(Cc2cncn2Cc2c(Cl)cccc2Cl)c1=O
CHEMBL332060 v2r_rat Rat No 7.0 IC50 = 110 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
386 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCOc3ccccc32)cc1
CHEMBL249133 v2r_human Human No 7.0 IC50 = 110 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
528 5 2 4 5.8 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1CCC2(C=C(C(=O)O)CC2)Cc2ccccc21
CHEMBL338018 v2r_rat Rat No 7.0 IC50 = 110 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H]2CCCCN2C1=O
CHEMBL3920097 v2r_human Human No 6.0 IC50 = 1100 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
490 6 0 6 5.8 O=c1n(Cc2ncc(Cc3cccc(C(F)(F)F)c3)s2)nc(-c2ccc(Cl)cc2)n1C1CC1
CHEMBL2112248 v2r_rat Rat No 6.0 IC50 = 1100 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCC=NN2C1=O
CHEMBL278377 v2r_rat Rat No 6.0 IC50 = 1100 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
584 9 1 6 3.2 CN(C)CCCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL128258 v2r_rat Rat No 6.0 IC50 = 1100 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
592 7 2 6 2.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CCS(N)(=O)=O)C1=O)C2
CHEMBL339498 v2r_rat Rat No 6.0 IC50 = 1100 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
622 10 3 7 1.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)NC(=O)CN)C2
CHEMBL35226 v2r_pig Pig No 5.0 IC50 = 11000 nM Bind
Ability to displace [3H]AVP from Vasopressin V2 receptorAbility to displace [3H]AVP from Vasopressin V2 receptor
339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1
CHEMBL129733 v2r_rat Rat No 5.0 IC50 = 11000 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL338020 v2r_rat Rat No 5.0 IC50 = 11000 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC(C)C[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL132210 v2r_rat Rat No 5.0 IC50 = 11000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
554 5 2 4 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)NC1CN3CCC1CC3)C2
CHEMBL281361 v2r_rat Rat No 4.9 IC50 = 11600 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](NCc3ccccc3)C1=O)C2
CHEMBL64391 v2r_human Human Yes 4.9 IC50 = 11900 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O
CHEMBL131439 v2r_human Human No 7.9 IC50 = 12 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
572 7 2 5 6.4 O=C(Nc1ccc(C(=O)N2CCC(CCS(=O)(=O)O)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL3917760 v2r_human Human No 7.9 IC50 = 12 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
508 6 1 6 5.1 O=c1n(Cc2cncc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F
CHEMBL3981686 v2r_human Human No 7.9 IC50 = 12 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
556 8 2 9 3.3 O=C(O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl
CHEMBL420762 v2r_rat Rat Yes 7.9 IC50 = 12 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C
CHEMBL166135 v2r_human Human No 7.9 IC50 = 12 nM Bind
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
585 5 3 4 6.6 O=C(Nc1ccc(C(=O)N2CCCc3c(S(=O)(=O)O)[nH]c4cccc2c34)cc1Cl)c1ccccc1-c1ccccc1
CHEMBL399289 v2r_human Human No 6.9 IC50 = 120 nM Funct
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
548 5 2 4 6.1 COc1cc(C(=O)N2CCC3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl
CHEMBL350383 v2r_rat Rat No 6.9 IC50 = 120 nM Bind
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1
CHEMBL136065 v2r_human Human No 6.9 IC50 = 120 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
368 2 0 2 5.3 O=C(c1ccc(N2CCCCC2)cc1Cl)N1CCCCc2ccccc21
CHEMBL3965109 v2r_human Human No 5.9 IC50 = 1200 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
603 10 2 9 4.5 COCCn1c(-c2ccc(Cl)s2)nn(CC(=O)NCC(NC(=O)OC(C)(C)C)c2ccccc2C(F)(F)F)c1=O
CHEMBL118128 v2r_rat Rat No 5.9 IC50 = 1200 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
384 3 1 2 5.1 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1C
CHEMBL2370623 v2r_rat Rat No 5.9 IC50 = 1200 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCC=NN2C1=O
CHEMBL128388 v2r_rat Rat No 4.9 IC50 = 12000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
499 5 1 4 3.3 CNC1CCN([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL131239 v2r_rat Rat No 4.9 IC50 = 12000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
527 6 2 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CC1CCCNC1)C2
CHEMBL2111851 v2r_rat Rat No 4.9 IC50 = 12000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
565 8 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCS(C)(=O)=O)C2
CHEMBL237120 v2r_human Human No 5.9 IC50 = 1214 nM Bind
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
418 2 0 4 4.5 Cc1ccn(-c2ccc(C(=O)N3C=C4CCC(=O)N4Cc4ccccc43)c(Cl)c2)n1
CHEMBL64391 v2r_human Human Yes 4.9 IC50 = 12589.3 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O
CHEMBL4205046 v2r_human Human No 7.9 IC50 = 13 nM Funct
Antagonist activity at human V2 receptor expressed in human HeLa cells assessed as inhibition of AVP-induced cAMP accumulation incubated for 10 mins by radioimmunoassayAntagonist activity at human V2 receptor expressed in human HeLa cells assessed as inhibition of AVP-induced cAMP accumulation incubated for 10 mins by radioimmunoassay
408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1
CHEMBL3963751 v2r_human Human No 7.9 IC50 = 13 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
530 7 1 6 5.4 O=c1n(Cc2nnc(Cc3c(Cl)cccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1CCC(F)(F)F
CHEMBL3926829 v2r_human Human No 7.9 IC50 = 13 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
579 10 3 7 2.9 O=CNC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1
CHEMBL119638 v2r_rat Rat No 7.9 IC50 = 13 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccc(Cl)cc3Cl)cc2)c2ccccc21
CHEMBL324251 v2r_rat Rat No 7.9 IC50 = 13 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
470 6 2 4 4.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC(N)=O)c3ccccc32)cc1
CHEMBL165554 v2r_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
551 5 3 4 5.9 O=C(Nc1ccc(C(=O)N2CCCc3c(S(=O)(=O)O)[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1
CHEMBL304060 v2r_rat Rat No 7.9 IC50 = 13 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
453 4 1 4 5.7 CSc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL304956 v2r_rat Rat No 7.9 IC50 = 13 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
435 3 1 3 5.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)c1C
CHEMBL136109 v2r_human Human No 7.9 IC50 = 13 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
365 2 0 3 4.8 Cc1ccn(-c2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1
CHEMBL335592 v2r_human Human No 7.9 IC50 = 13 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
362 2 0 2 5.0 CN(C)c1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(Cl)c1
CHEMBL318392 v2r_human Human No 7.9 IC50 = 13 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
519 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(CC4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl
CHEMBL2112895 v2r_rat Rat No 6.9 IC50 = 130 nM Bind
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
637 11 3 8 1.9 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCNCC2)C3(C)C)CC1
CHEMBL350383 v2r_human Human No 6.9 IC50 = 130 nM Bind
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1
CHEMBL2112247 v2r_rat Rat No 5.9 IC50 = 1300 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL276990 v2r_rat Rat No 5.9 IC50 = 1300 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
499 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](N)C1=O)C2
CHEMBL417458 v2r_rat Rat No 5.9 IC50 = 1300 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
570 8 1 6 2.8 CN(C)CCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL128749 v2r_rat Rat No 5.9 IC50 = 1300 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
593 9 1 6 3.0 CN(C)C(CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C
CHEMBL128194 v2r_rat Rat No 4.9 IC50 = 13000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
515 7 2 5 2.8 CC(C(N)=O)[C@@H](N)C(=O)[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C
CHEMBL128879 v2r_rat Rat No 4.9 IC50 = 13000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
510 6 2 4 3.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@H](NC(=O)Cc1c[nH]cn1)C2
CHEMBL337842 v2r_rat Rat No 4.9 IC50 = 13000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
416 3 1 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)/C(=N\O)C2
CHEMBL338499 v2r_rat Rat No 4.9 IC50 = 13000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
542 8 2 4 4.9 CCC(C)(C)C(=O)NCC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C
CHEMBL340016 v2r_rat Rat No 4.9 IC50 = 13000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
530 8 1 5 4.0 CCOC(=O)CCC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C
CHEMBL331098 v2r_rat Rat No 7.9 IC50 = 14 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
427 4 1 3 5.3 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)cc2)c1
CHEMBL332685 v2r_rat Rat No 7.9 IC50 = 14 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
399 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3ccccc32)cc1
CHEMBL350408 v2r_human Human No 7.9 IC50 = 14 nM Bind
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
517 4 2 4 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3ccc(C(=O)O)n3Cc3ccccc32)c(Cl)c1
CHEMBL73286 v2r_rat Rat No 7.9 IC50 = 14 nM Bind
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL400266 v2r_human Human No 7.9 IC50 = 14 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL68948 v2r_rat Rat No 7.9 IC50 = 14 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cc(Cl)ccc1Cl
CHEMBL73286 v2r_rat Rat No 7.9 IC50 = 14 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL164226 v2r_human Human No 7.8 IC50 = 14.8 nM Bind
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
556 6 2 5 6.4 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1O)C2
CHEMBL249133 v2r_human Human No 6.9 IC50 = 140 nM Funct
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
528 5 2 4 5.8 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1CCC2(C=C(C(=O)O)CC2)Cc2ccccc21
CHEMBL119671 v2r_rat Rat No 6.9 IC50 = 140 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
487 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2CCCC(N3CCCCC3)c3ccccc32)cc1)c1ccccc1Cl
CHEMBL162588 v2r_human Human No 6.9 IC50 = 140 nM Bind
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
466 3 2 4 5.4 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1)c1ccc(F)cc1Cl
CHEMBL332090 v2r_rat Rat No 5.9 IC50 = 1400 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
370 3 1 2 4.8 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1
CHEMBL338294 v2r_rat Rat No 5.9 IC50 = 1400 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H]2CCCCN2C1=O
CHEMBL341289 v2r_rat Rat No 5.9 IC50 = 1400 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
565 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(Cc3c[nH]cn3)C1=O)C2
CHEMBL341507 v2r_rat Rat No 4.9 IC50 = 14000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
552 7 3 6 1.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CS(N)(=O)=O)C2
CHEMBL421248 v2r_rat Rat No 4.9 IC50 = 14000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
539 7 3 4 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)NCCc1c[nH]cn1)C2
CHEMBL128688 v2r_human Human No 7.8 IC50 = 15 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL4114132 v2r_human Human No 7.8 IC50 = 15 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
566 9 3 7 3.0 O=C(Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)N[C@@H](CO)Cc1cccc(C(F)(F)F)c1
CHEMBL165076 v2r_human Human No 7.8 IC50 = 15 nM Bind
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1Cl)c1ccccc1-c1ccccc1
CHEMBL302955 v2r_rat Rat No 7.8 IC50 = 15 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1c(Cl)cccc1Cl
CHEMBL319418 v2r_human Human No 7.8 IC50 = 15 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1
CHEMBL438523 v2r_human Human No 6.8 IC50 = 150 nM Funct
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
562 6 2 4 6.5 CCOc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl
CHEMBL340893 v2r_rat Rat No 6.8 IC50 = 150 nM Bind
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21
CHEMBL340893 v2r_rat Rat No 6.8 IC50 = 150 nM Bind
Binding affinity towards rat Vasopressin V2 receptorBinding affinity towards rat Vasopressin V2 receptor
354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21
CHEMBL3957738 v2r_human Human No 6.8 IC50 = 150 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
549 6 1 8 4.9 O=c1n(Cc2nnc(-c3ccccc3C(F)(F)F)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL119591 v2r_rat Rat No 6.8 IC50 = 150 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
441 4 2 3 4.9 CC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21
CHEMBL349506 v2r_human Human No 6.8 IC50 = 150 nM Bind
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2
CHEMBL340204 v2r_rat Rat No 6.8 IC50 = 150 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H]2CCCCN2C1=O
CHEMBL283994 v2r_rat Rat No 5.8 IC50 = 1500 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
500 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](O)C1=O)C2
CHEMBL338951 v2r_rat Rat No 5.8 IC50 = 1500 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
621 11 1 6 3.8 CCN(CC)C(CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C
CHEMBL341289 v2r_rat Rat No 5.8 IC50 = 1500 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
565 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(Cc3c[nH]cn3)C1=O)C2
CHEMBL371055 v2r_human Human No 4.8 IC50 = 15000 nM Bind
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
427 4 0 4 5.5 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(-c3cccs3)cc1)C2
CHEMBL131581 v2r_rat Rat No 4.8 IC50 = 15000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
538 7 2 4 4.5 CCC(C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C)c1c[nH]cn1
CHEMBL336992 v2r_rat Rat No 4.8 IC50 = 15000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
588 6 2 4 4.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1[nH]cnc1Br)C2
CHEMBL104 v2r_human Human Yes 4.8 IC50 = 15100 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1
CHEMBL1520590 v2r_human Human Yes 4.8 IC50 = 15200 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12
CHEMBL50 v2r_human Human Yes 4.8 IC50 = 15200 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12
CHEMBL594828 v2r_human Human Yes 5.8 IC50 = 1530 nM Funct
Antagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced calcium release by Aequorin based assayAntagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced calcium release by Aequorin based assay
419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1
CHEMBL1520590 v2r_human Human Yes 4.8 IC50 = 15848.9 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12
CHEMBL50 v2r_human Human Yes 4.8 IC50 = 15848.9 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12
CHEMBL104 v2r_human Human Yes 4.8 IC50 = 15848.9 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1
CHEMBL100447 v2r_human Human No 6.8 IC50 = 159 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
504 3 1 2 7.6 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1c(Cl)cccc1Cl
CHEMBL334777 v2r_human Human No 7.8 IC50 = 16 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
536 7 2 4 7.0 O=C(O)CC[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL321656 v2r_human Human No 7.8 IC50 = 16 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
626 9 2 4 7.0 CN(C)CCCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL3976964 v2r_human Human No 7.8 IC50 = 16 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
609 10 3 8 3.3 NC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F
CHEMBL310581 v2r_rat Rat No 7.8 IC50 = 16 nM Bind
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
471 4 1 4 5.6 COc1cc(Cl)ccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL136628 v2r_human Human No 7.8 IC50 = 16 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
388 2 0 2 5.6 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2cc(Cl)ccc21
CHEMBL49796 v2r_rat Rat No 6.8 IC50 = 160 nM Bind
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
453 4 1 6 4.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1[N+](=O)[O-]
CHEMBL2112893 v2r_rat Rat No 6.8 IC50 = 160 nM Bind
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
686 11 2 9 1.7 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCS(=O)(=O)CC2)C3(C)C)CC1
CHEMBL118244 v2r_rat Rat Yes 5.8 IC50 = 1600 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
406 4 1 3 4.5 O=C(c1ccc(NS(=O)(=O)c2ccccc2)cc1)N1CCCCc2ccccc21
CHEMBL338308 v2r_rat Rat No 5.8 IC50 = 1600 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCN)NC(=O)[C@H]2CCC=NN2C1=O
CHEMBL131538 v2r_rat Rat No 4.8 IC50 = 16000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
501 7 2 5 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](C(=O)[C@H](N)CC(N)=O)C2
CHEMBL339096 v2r_rat Rat No 4.8 IC50 = 16000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
499 4 1 5 2.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(=O)C1=O)C2
CHEMBL277022 v2r_rat Rat No 5.8 IC50 = 1620 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
571 7 1 7 2.4 COC(=O)CNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL333652 v2r_rat Rat No 6.8 IC50 = 170 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
399 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCN(C)Cc3ccccc32)cc1
CHEMBL349965 v2r_human Human No 6.8 IC50 = 170 nM Bind
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
527 4 1 4 7.1 CC(=O)n1cc2c3c(cccc31)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccc(C)cc3)cc1)CCC2
CHEMBL421039 v2r_human Human No 6.8 IC50 = 170 nM Funct
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
585 7 3 4 6.0 O=C(NCCO)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL3956553 v2r_human Human No 5.8 IC50 = 1700 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
473 6 1 5 5.1 O=c1n(Cc2ncc(Cc3cccc(C(F)(F)F)c3)[nH]2)nc(-c2ccc(Cl)cc2)n1C1CC1
CHEMBL334009 v2r_rat Rat No 5.8 IC50 = 1700 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
362 3 1 3 4.6 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccsc1
CHEMBL71283 v2r_rat Rat No 5.8 IC50 = 1700 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
434 3 1 3 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Oc3ccccc32)cc1
CHEMBL405289 v2r_rat Rat No 5.8 IC50 = 1700 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL265073 v2r_rat Rat No 5.8 IC50 = 1700 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
610 9 0 7 3.9 COC(=O)CCN(C(=O)Cc1cn(C)cn1)[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C
CHEMBL338984 v2r_rat Rat No 5.8 IC50 = 1700 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
524 5 0 5 3.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(CC#N)C1=O)C2
CHEMBL435019 v2r_rat Rat No 5.8 IC50 = 1700 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
484 4 0 4 3.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CCC1=O)C2
CHEMBL20230 v2r_rat Rat No 4.8 IC50 = 17000 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
510 6 2 4 3.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1c[nH]cn1)C2
CHEMBL338522 v2r_rat Rat Yes 4.8 IC50 = 17000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
510 6 2 4 3.6 O=C(Cc1cnc[nH]1)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCC2(CC1)CCc1c2cccc1)(C)C
CHEMBL419183 v2r_human Human No 7.8 IC50 = 18 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
599 7 3 4 6.1 O=C(O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL119793 v2r_rat Rat No 7.8 IC50 = 18 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1
CHEMBL334376 v2r_human Human No 7.8 IC50 = 18 nM Bind
Displacement of [3H]AVP from human Vasopressin V2 receptor expressed in HeLa cells after 2 hrs by liquid scintillation counterDisplacement of [3H]AVP from human Vasopressin V2 receptor expressed in HeLa cells after 2 hrs by liquid scintillation counter
314 1 1 2 4.2 Cc1cc(N)ccc1C(=O)N1CCCCc2cc(Cl)ccc21
CHEMBL250346 v2r_human Human No 7.8 IC50 = 18 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
528 5 2 3 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=C(CO)CC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL136177 v2r_human Human No 7.8 IC50 = 18 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
342 4 1 2 5.1 CCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1
CHEMBL343935 v2r_human Human No 7.8 IC50 = 18 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
328 2 0 2 4.4 CN(C)c1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1
CHEMBL332450 v2r_rat Rat No 6.8 IC50 = 180 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
385 3 2 2 5.3 O=C(Nc1ccccc1)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1
CHEMBL349062 v2r_human Human No 6.8 IC50 = 180 nM Bind
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
427 3 2 2 5.5 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1
CHEMBL100893 v2r_human Human No 6.8 IC50 = 180 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
470 3 1 2 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1Cl
CHEMBL344848 v2r_human Human Yes 6.8 IC50 = 180 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
266 1 1 2 3.3 Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1
CHEMBL400267 v2r_human Human No 5.8 IC50 = 1800 nM Funct
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
541 6 2 3 7.1 CNCC1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL119534 v2r_rat Rat No 5.8 IC50 = 1800 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
386 4 1 3 4.5 COc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1
CHEMBL128219 v2r_rat Rat No 5.8 IC50 = 1800 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
601 11 4 6 1.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)CCN)C2
CHEMBL338177 v2r_rat Rat No 4.8 IC50 = 18000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
555 6 3 4 4.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)NC1CCCCC1)C2
CHEMBL203513 v2r_human Human No 6.7 IC50 = 183 nM Bind
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
415 2 1 5 5.0 Cn1ccc(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Cl)c2)n1
CHEMBL159831 v2r_rat Rat No 7.7 IC50 = 19 nM Bind
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
478 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2CCCCc3sc(Cl)cc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL297293 v2r_human Human No 7.7 IC50 = 19 nM Bind
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
492 3 1 3 7.1 O=C(Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL334688 v2r_human Human No 7.7 IC50 = 19 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
356 4 0 2 5.2 CCN(CC)c1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1
CHEMBL318530 v2r_human Human No 7.7 IC50 = 19 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
517 3 1 3 6.4 Cc1cc(F)cc(C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(CC5)N4Cc4ccccc43)c(Cl)c2)c1
CHEMBL250346 v2r_human Human No 6.7 IC50 = 190 nM Funct
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
528 5 2 3 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=C(CO)CC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL118878 v2r_rat Rat No 6.7 IC50 = 190 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
428 4 2 4 4.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3N)cc2)c2ccccc21
CHEMBL166265 v2r_human Human No 6.7 IC50 = 190 nM Bind
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
427 3 2 2 5.5 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1
CHEMBL119551 v2r_rat Rat No 5.7 IC50 = 1900 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc(Cl)cc1
CHEMBL338576 v2r_rat Rat No 5.7 IC50 = 1900 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
645 10 2 6 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)N(CCc1c[nH]cn1)CCS(C)(=O)=O)C2
CHEMBL340388 v2r_rat Rat No 5.7 IC50 = 1900 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
593 8 0 6 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(CCCn3ccnc3)C1=O)C2
CHEMBL2112654 v2r_rat Rat No 4.7 IC50 = 19000 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL3949118 v2r_human Human No 8.7 IC50 = 2 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
568 8 2 7 5.2 O=C(O)c1cccc(Cn2c(-c3ccc(Cl)cc3)nn(Cc3nnc(Cc4c(Cl)cccc4Cl)[nH]3)c2=O)c1
CHEMBL3912406 v2r_human Human No 8.7 IC50 = 2 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
595 9 3 8 3.5 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(Cl)c1Cl
CHEMBL3964135 v2r_human Human No 8.7 IC50 = 2 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
561 9 3 8 2.9 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl
CHEMBL311230 v2r_human Human No 8.7 IC50 = 2 nM Bind
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
509 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(Cl)cc1Cl
CHEMBL312036 v2r_human Human No 8.7 IC50 = 2 nM Bind
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
469 4 1 4 5.4 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1Cc2cccn2Cc2ccccc21
CHEMBL350869 v2r_human Human No 8.7 IC50 = 2 nM Bind
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
657 7 1 5 7.8 CN(C)C1CCN(Cc2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1
CHEMBL369832 v2r_human Human No 8.7 IC50 = 2 nM Bind
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
622 9 1 6 7.1 CN1CCCN(CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1
CHEMBL81133 v2r_human Human No 8.7 IC50 = 2.1 nM Bind
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
453 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(C)c1
CHEMBL165200 v2r_human Human No 8.7 IC50 = 2.1 nM Bind
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
697 7 1 5 8.7 O=C(Nc1ccc(C(=O)N2Cc3ccc(CN4CCC(N5CCCCC5)CC4)n3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1
CHEMBL49429 v2r_rat Rat Yes 8.6 IC50 = 2.3 nM Bind
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL49429 v2r_rat Rat Yes 8.6 IC50 = 2.3 nM Bind
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL49429 v2r_rat Rat Yes 8.6 IC50 = 2.3 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL159823 v2r_rat Rat No 8.6 IC50 = 2.6 nM Bind
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
483 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL349237 v2r_human Human No 8.6 IC50 = 2.6 nM Bind
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
631 9 1 5 7.3 CN(C)CCN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1Cl)C2
CHEMBL159359 v2r_human Human No 8.6 IC50 = 2.7 nM Bind
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1
CHEMBL131727 v2r_human Human No 7.7 IC50 = 20 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V2 receptor at 0.2 uMAbility to displace [3H]arginine vasopressin in cloned human V2 receptor at 0.2 uM
560 7 1 7 6.2 O=C(Nc1ccc(C(=O)N2CCC(CCn3cnnn3)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL326225 v2r_human Human No 7.7 IC50 = 20 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
568 7 2 4 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN(C)C)CC3)Cc3ccccc32)cc1
CHEMBL119318 v2r_rat Rat No 7.7 IC50 = 20 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3cc(Cl)cc(Cl)c3)cc2)c2ccccc21
CHEMBL165670 v2r_human Human No 7.7 IC50 = 20 nM Bind
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1
CHEMBL321656 v2r_human Human No 7.7 IC50 = 20 nM Funct
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
626 9 2 4 7.0 CN(C)CCCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL368353 v2r_rat Rat No 7.7 IC50 = 20 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
704 10 1 6 8.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1OCCCC(=O)N1CCC(N2CCCCC2)CC1)c1ccccc1-c1ccccc1
CHEMBL368791 v2r_rat Rat No 7.7 IC50 = 20 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
495 5 1 4 6.7 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21
CHEMBL435331 v2r_rat Rat No 7.7 IC50 = 20 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
524 7 1 5 6.1 CN(C)CCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21
CHEMBL175212 v2r_human Human No 7.7 IC50 = 20 nM Bind
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
525 6 1 5 6.7 COc1cc(C(=O)N2CCCC(N(C)C)c3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1
CHEMBL430083 v2r_human Human No 7.7 IC50 = 20 nM Bind
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
664 10 1 6 7.4 CN(C)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1
CHEMBL121455 v2r_rat Rat No 6.7 IC50 = 200 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccc(Cl)c1
CHEMBL331164 v2r_rat Rat No 6.7 IC50 = 200 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
370 3 1 2 4.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1
CHEMBL175211 v2r_rat Rat No 6.7 IC50 = 200 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
435 4 2 2 5.9 O=C(Nc1ccc(C(=O)N2CCCCc3[nH]ccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL441498 v2r_rat Rat No 6.7 IC50 = 200 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
410 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1Cl
CHEMBL176146 v2r_human Human No 6.7 IC50 = 200 nM Bind
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
550 7 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCCC3)c3sccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL2332717 v2r_human Human No 5.7 IC50 = 2000 nM Bind
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression competition binding assay
None None None NC(=O)CC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CNC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL198931 v2r_human Human No 5.7 IC50 = 2000 nM Bind
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
378 2 0 2 5.7 Cc1ccccc1-c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL341289 v2r_rat Rat No 5.7 IC50 = 2000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
565 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(Cc3c[nH]cn3)C1=O)C2
CHEMBL131235 v2r_rat Rat No 4.7 IC50 = 20000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
522 6 2 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)/C=C/c1c[nH]cn1)C2
CHEMBL49392 v2r_rat Rat No 6.7 IC50 = 210 nM Bind
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
423 3 2 5 3.9 Nc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1
CHEMBL117566 v2r_rat Rat No 6.7 IC50 = 210 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
384 3 1 2 5.1 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c(C)c1
CHEMBL165183 v2r_human Human No 6.7 IC50 = 210 nM Bind
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
499 4 1 3 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4cn(C)c5cccc3c45)cc2)cc1
CHEMBL335040 v2r_human Human No 6.7 IC50 = 210 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1)N1CCCCc2cc(Cl)ccc21
CHEMBL119442 v2r_rat Rat No 5.7 IC50 = 2100 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
386 4 1 3 4.5 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1
CHEMBL128712 v2r_rat Rat No 5.7 IC50 = 2100 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
499 4 1 4 3.4 CC1NC(=O)N([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL130905 v2r_rat Rat No 5.7 IC50 = 2100 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
514 5 2 5 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CN)C1=O)C2
CHEMBL338383 v2r_rat Rat No 5.7 IC50 = 2100 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
485 4 1 4 3.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CNC1=O)C2
CHEMBL128422 v2r_rat Rat No 4.7 IC50 = 21000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
524 7 2 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CCc1c[nH]cn1)C2
CHEMBL4538696 v2r_human Human No 4.7 IC50 = 21450 nM Funct
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
461 8 0 7 3.7 COc1ccc(-n2c(COCCF)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1
CHEMBL3900528 v2r_human Human No 7.7 IC50 = 22 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
557 9 2 7 4.2 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(Cc2ccccc2F)c1=O)c1ccccc1Cl
CHEMBL118863 v2r_rat Rat No 7.7 IC50 = 22 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
455 6 1 3 6.1 CCCN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21
CHEMBL71305 v2r_rat Rat No 7.7 IC50 = 22 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F
CHEMBL139415 v2r_human Human No 7.7 IC50 = 22 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
356 5 1 2 5.5 CCCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1
CHEMBL351587 v2r_human Human No 6.7 IC50 = 220 nM Bind
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1
CHEMBL132389 v2r_rat Rat No 5.7 IC50 = 2200 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
543 8 3 5 3.4 CC(C)C[C@H](N)C(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C
CHEMBL119291 v2r_rat Rat Yes 4.7 IC50 = 22000 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
356 3 1 2 4.5 O=C(Nc1ccccc1C(=O)N1CCCc2ccccc21)c1ccccc1
CHEMBL318083 v2r_human Human No 7.6 IC50 = 23 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
582 8 2 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCCN(C)C)CC3)Cc3ccccc32)cc1
CHEMBL3915055 v2r_human Human No 7.6 IC50 = 23 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
548 6 1 7 5.5 O=c1n(Cc2cnc(-c3ccccc3C(F)(F)F)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL3943019 v2r_human Human No 7.6 IC50 = 23 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
514 6 1 7 5.1 O=c1n(Cc2ncc(-c3ccccc3Cl)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL3965602 v2r_human Human No 7.6 IC50 = 23 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
533 6 1 8 4.4 O=c1n(Cc2nc(-c3ccccc3C(F)(F)F)no2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL332447 v2r_rat Rat Yes 6.6 IC50 = 230 nM Bind
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C
CHEMBL160029 v2r_rat Rat No 6.6 IC50 = 230 nM Bind
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
434 3 1 5 4.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)C3CCCCC3)cc1)CC2
CHEMBL2112900 v2r_rat Rat No 6.6 IC50 = 230 nM Bind
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
636 11 2 7 3.5 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCCCC2)C3(C)C)CC1
CHEMBL127686 v2r_rat Rat No 5.6 IC50 = 2300 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None None
CHEMBL279281 v2r_rat Rat No 5.6 IC50 = 2300 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
557 7 2 6 2.6 C[C@@H](O)CNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL283524 v2r_rat Rat No 5.6 IC50 = 2300 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
500 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](O)C1=O)C2
CHEMBL276906 v2r_rat Rat No 4.6 IC50 = 23000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
548 7 2 4 4.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)c1ccccc1)C2
CHEMBL4585239 v2r_human Human No 4.6 IC50 = 23047 nM Funct
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
485 7 0 8 3.5 COc1ccc(-n2c(CO[C@H]3CCOC3)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1
CHEMBL351587 v2r_rat Rat No 7.6 IC50 = 24 nM Bind
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1
CHEMBL324488 v2r_rat Rat No 7.6 IC50 = 24 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
413 4 2 3 4.9 CNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21
CHEMBL49657 v2r_rat Rat No 6.6 IC50 = 240 nM Bind
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
444 3 1 4 4.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(F)ccc1F
CHEMBL2112901 v2r_rat Rat No 6.6 IC50 = 240 nM Bind
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
614 12 3 9 0.8 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)N(CO)CO)C3(C)C)CC1
CHEMBL2112902 v2r_rat Rat No 5.6 IC50 = 2400 nM Bind
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
565 8 2 6 2.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](N)CCS(C)(=O)=O)C2
CHEMBL2112666 v2r_rat Rat No 5.6 IC50 = 2400 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
565 8 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](N)CCS(C)(=O)=O)C2
CHEMBL405016 v2r_rat Rat No 5.6 IC50 = 2400 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
609 7 2 8 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(CC(=O)Nc3nn[nH]n3)C1=O)C2
CHEMBL373742 v2r_human Human Yes 6.6 IC50 = 242 nM Bind
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assay
None None None None
CHEMBL323802 v2r_rat Rat No 7.6 IC50 = 25 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
452 5 1 4 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC#N)c3ccccc32)cc1
CHEMBL308741 v2r_rat Rat No 7.6 IC50 = 25 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
432 3 1 2 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3ccccc3-c3ccccc32)cc1
CHEMBL119087 v2r_rat Rat No 6.6 IC50 = 250 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
424 3 1 2 5.8 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL372766 v2r_human Human No 5.6 IC50 = 2500 nM Bind
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
400 2 0 2 5.6 O=C(c1ccc(-c2cc(F)cc(F)c2)cc1)N1Cc2cccn2Cc2ccccc21
CHEMBL20002 v2r_rat Rat No 5.6 IC50 = 2500 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
542 5 0 6 3.2 CC(=O)OC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL337221 v2r_rat Rat No 5.6 IC50 = 2500 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
542 6 1 5 3.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(CC(=O)O)C1=O)C2
CHEMBL436189 v2r_rat Rat No 5.6 IC50 = 2500 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
701 12 4 8 1.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C(CCS(C)(=O)=O)NC(=O)Cc1c[nH]cn1)C2
CHEMBL104 v2r_human Human Yes 5.6 IC50 = 2511.9 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1
CHEMBL4564411 v2r_human Human No 4.6 IC50 = 25665 nM Funct
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3cccc(F)c3Cl)C2)n1-c1ccc(OC)nc1
CHEMBL319433 v2r_human Human No 7.6 IC50 = 26 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
489 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1F
CHEMBL130993 v2r_rat Rat No 5.6 IC50 = 2600 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
565 7 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)C1=CCC(=O)N=C1)C2
CHEMBL337212 v2r_rat Rat No 4.6 IC50 = 26000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
444 4 1 3 3.6 CC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C
CHEMBL594828 v2r_human Human Yes 5.6 IC50 = 2620 nM Funct
Antagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of LIT-001-induced response incubated for 30 mins by beta-arrestin recruitment assayAntagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of LIT-001-induced response incubated for 30 mins by beta-arrestin recruitment assay
419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1
CHEMBL3909196 v2r_human Human No 7.6 IC50 = 27 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
507 6 1 5 5.7 O=c1n(Cc2cccc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F
CHEMBL118270 v2r_rat Rat No 7.6 IC50 = 27 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
447 4 1 3 5.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3Cl)cc2)c2ccccc21
CHEMBL334225 v2r_rat Rat No 7.6 IC50 = 27 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
413 4 1 3 5.0 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3)cc2)c2ccccc21
CHEMBL2112897 v2r_rat Rat No 6.6 IC50 = 270 nM Bind
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
638 11 2 8 2.3 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCOCC2)C3(C)C)CC1
CHEMBL339132 v2r_rat Rat No 5.6 IC50 = 2700 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
499 4 0 4 3.4 CN1CC(=O)N([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL104 v2r_human Human Yes 5.6 IC50 = 2700 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1
CHEMBL316958 v2r_human Human No 6.6 IC50 = 274 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
504 3 1 2 7.6 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL3975038 v2r_human Human No 7.6 IC50 = 28 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
548 7 1 7 5.4 O=c1n(Cc2nnc(Cc3ccccc3C(F)(F)F)[nH]2)nc(-c2ccc(Cl)s2)n1Cc1ccccc1F
CHEMBL119806 v2r_rat Rat No 7.6 IC50 = 28 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
398 3 1 2 5.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCCc3ccccc32)cc1
CHEMBL106229 v2r_human Human No 7.6 IC50 = 28 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
385 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCNc3ccccc32)cc1
CHEMBL131477 v2r_rat Rat No 6.6 IC50 = 280 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
673 11 3 7 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)NC(=O)Cc1c[nH]cn1)C2
CHEMBL19658 v2r_rat Rat No 5.6 IC50 = 2800 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
499 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](N)C1=O)C2
CHEMBL118271 v2r_rat Rat No 7.5 IC50 = 29 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3ccccc32)cc1
CHEMBL118387 v2r_rat Rat No 7.5 IC50 = 29 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
404 3 1 2 5.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1Cl
CHEMBL118922 v2r_rat Rat No 7.5 IC50 = 29 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
427 5 2 3 5.3 CCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21
CHEMBL331173 v2r_rat Rat No 7.5 IC50 = 29 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
499 7 1 5 5.2 CCOC(=O)CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21
CHEMBL296814 v2r_rat Rat No 7.5 IC50 = 29 nM Bind
In vitro inhibition of [3H]AVP binding to rat V2 receptorIn vitro inhibition of [3H]AVP binding to rat V2 receptor
457 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cn1
CHEMBL101678 v2r_human Human No 7.5 IC50 = 29 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
512 4 1 2 7.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL71282 v2r_rat Rat No 7.5 IC50 = 29 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cccc(Cl)c1Cl
CHEMBL72945 v2r_rat Rat No 7.5 IC50 = 29 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
418 3 1 2 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3-c3ccccc32)cc1
CHEMBL49323 v2r_rat Rat No 6.5 IC50 = 290 nM Bind
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
525 7 0 5 5.1 Cc1ccc(F)cc1C(=O)N(CCCN(C)C)c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1
CHEMBL2112896 v2r_rat Rat No 6.5 IC50 = 290 nM Bind
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
582 10 1 7 2.1 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)N(C)C)C3(C)C)CC1
CHEMBL339497 v2r_rat Rat No 5.5 IC50 = 2900 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
616 9 2 6 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)c1c[nH]cn1)C2
CHEMBL203739 v2r_human Human No 6.5 IC50 = 296 nM Bind
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
459 2 1 5 5.2 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Br)c2)n1
CHEMBL3933782 v2r_human Human No 8.5 IC50 = 3 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
595 9 3 8 3.3 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F
CHEMBL297990 v2r_rat Rat No 8.5 IC50 = 3 nM Bind
In vitro inhibition of (P[3H]-AVP binding towards isolated rat kidney medullary Vasopre ssin V2 receptorIn vitro inhibition of (P[3H]-AVP binding towards isolated rat kidney medullary Vasopre ssin V2 receptor
422 3 1 4 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1
CHEMBL418890 v2r_rat Rat No 8.5 IC50 = 3 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL368818 v2r_rat Rat No 8.5 IC50 = 3 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
650 9 1 6 7.0 CN1CCCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1
CHEMBL430083 v2r_rat Rat No 8.5 IC50 = 3 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
664 10 1 6 7.4 CN(C)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1
CHEMBL418890 v2r_rat Rat No 8.5 IC50 = 3.1 nM Bind
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL418890 v2r_rat Rat No 8.5 IC50 = 3.1 nM Bind
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL159856 v2r_rat Rat No 8.5 IC50 = 3.2 nM Bind
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
486 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2CCCCc3sc(Cl)cc32)cc1)c1ccccc1-c1ccccc1
CHEMBL418890 v2r_human Human No 8.5 IC50 = 3.2 nM Bind
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL418890 v2r_human Human No 8.5 IC50 = 3.2 nM Bind
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL3955416 v2r_human Human No 8.5 IC50 = 3.3 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
497 6 1 7 4.2 O=c1n(Cc2cn(-c3ccccc3Cl)cn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL373742 v2r_pig Pig Yes 8.5 IC50 = 3.3 nM Bind
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
None None None None
CHEMBL350089 v2r_human Human No 8.5 IC50 = 3.4 nM Bind
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
442 3 1 3 6.1 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCCc3sccc32)c(Cl)c1
CHEMBL249741 v2r_rat Rat Yes 7.5 IC50 = 30 nM Funct
Antagonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl
CHEMBL321561 v2r_human Human No 7.5 IC50 = 30 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
595 4 1 3 8.2 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)c(Cl)c2)cc1
CHEMBL128688 v2r_human Human No 7.5 IC50 = 30 nM Funct
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL336825 v2r_human Human No 7.5 IC50 = 30 nM Funct
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
522 6 2 4 6.6 O=C(O)C[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL175182 v2r_rat Rat No 7.5 IC50 = 30 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
544 6 1 5 7.1 O=C(Nc1ccc(C(=O)N2CCCN(Cc3cccnc3)c3sccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL175930 v2r_rat Rat No 7.5 IC50 = 30 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
482 5 1 4 6.7 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCCc2sccc21
CHEMBL175930 v2r_human Human No 7.5 IC50 = 30 nM Bind
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
482 5 1 4 6.7 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCCc2sccc21
CHEMBL368353 v2r_human Human No 7.5 IC50 = 30 nM Bind
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
704 10 1 6 8.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1OCCCC(=O)N1CCC(N2CCCCC2)CC1)c1ccccc1-c1ccccc1
CHEMBL368791 v2r_human Human No 7.5 IC50 = 30 nM Bind
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
495 5 1 4 6.7 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21
CHEMBL3907257 v2r_human Human No 6.5 IC50 = 300 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
653 9 2 8 6.0 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)s2)n(Cc2ccccc2F)c1=O)c1ccccc1C(F)(F)F
CHEMBL333135 v2r_rat Rat No 6.5 IC50 = 300 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
386 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCOCc3ccccc32)cc1
CHEMBL424663 v2r_human Human No 6.5 IC50 = 300 nM Bind
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
378 2 0 2 5.7 Cc1ccc(-c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1
CHEMBL420762 v2r_rat Rat Yes 6.5 IC50 = 300 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C
CHEMBL175411 v2r_rat Rat No 6.5 IC50 = 300 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
436 4 1 3 6.2 O=C(Nc1ccc(C(=O)N2CCCCc3occc32)cc1)c1ccccc1-c1ccccc1
CHEMBL20757 v2r_rat Rat No 5.5 IC50 = 3000 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
557 7 2 6 2.6 C[C@H](CO)NC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL128652 v2r_rat Rat No 5.5 IC50 = 3000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
638 11 4 6 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](Cc1c[nH]cn1)NC(=O)CCC(N)=O)C2
CHEMBL130848 v2r_rat Rat No 5.5 IC50 = 3000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
558 9 4 6 1.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)[C@@H](N)CCC(N)=O)C2
CHEMBL132211 v2r_rat Rat No 5.5 IC50 = 3000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
544 8 2 5 2.3 CN(C)CC(=O)NCC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C
CHEMBL2112663 v2r_rat Rat No 5.5 IC50 = 3000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
581 8 3 7 1.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@](O)(CNC(=O)C(N)CS(C)(=O)=O)C2
CHEMBL337888 v2r_rat Rat No 5.5 IC50 = 3000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
532 8 2 6 2.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CC[N+](=O)[O-])C2
CHEMBL435009 v2r_rat Rat No 4.5 IC50 = 30000 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
486 6 2 4 3.5 CC(=O)NCC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C
CHEMBL20171 v2r_rat Rat No 5.5 IC50 = 3060 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
557 7 1 6 2.5 CN(CCO)C1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL318083 v2r_human Human No 7.5 IC50 = 31 nM Funct
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
582 8 2 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCCN(C)C)CC3)Cc3ccccc32)cc1
CHEMBL137500 v2r_human Human No 7.5 IC50 = 31 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
370 6 1 2 5.9 CCCCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1
CHEMBL2112894 v2r_rat Rat No 6.5 IC50 = 310 nM Bind
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
610 12 1 7 2.9 CCN(CC)[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1CC2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C
CHEMBL175813 v2r_rat Rat No 6.5 IC50 = 310 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
452 4 1 3 6.7 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL1790937 v2r_rat Rat No 5.5 IC50 = 3100 nM Bind
Ability to inhibit AVP stimulation of adenylate cyclase activity in the rat kidney medulla (AVP-V2) receptorAbility to inhibit AVP stimulation of adenylate cyclase activity in the rat kidney medulla (AVP-V2) receptor
None None None CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL3986461 v2r_human Human No 7.5 IC50 = 32 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
499 6 1 8 4.0 O=c1n(Cc2nnc(-c3ccccc3Cl)o2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL420880 v2r_rat Rat No 7.5 IC50 = 32 nM Bind
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
399 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N)c3ccccc32)cc1
CHEMBL342251 v2r_human Human No 6.5 IC50 = 320 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
316 2 0 2 4.5 O=C(c1ccc(-n2cccc2)cc1)N1CCCCc2ccccc21
CHEMBL128383 v2r_rat Rat No 5.5 IC50 = 3200 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
541 4 1 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C3CC(O)CN3C1=O)C2
CHEMBL4591825 v2r_human Human Yes 4.5 IC50 = 32604 nM Funct
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1
CHEMBL51645 v2r_rat Rat No 7.5 IC50 = 33 nM Bind
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
497 5 1 5 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3ccc(CN(C)C)n3Cc3ccccc32)cn1
CHEMBL303176 v2r_rat Rat No 7.5 IC50 = 33 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
421 3 1 3 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cccn3-c3ccccc32)cc1
CHEMBL332447 v2r_human Human Yes 6.5 IC50 = 330 nM Bind
Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determinedBinding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined
453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C
CHEMBL126765 v2r_rat Rat No 6.5 IC50 = 330 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCN)NC(=O)[C@H]2CCC=NN2C1=O
CHEMBL166261 v2r_human Human No 6.5 IC50 = 330 nM Funct
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)c(Cl)c1)c1ccccc1-c1ccccc1
CHEMBL339497 v2r_rat Rat No 5.5 IC50 = 3300 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
616 9 2 6 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)c1c[nH]cn1)C2
CHEMBL237772 v2r_human Human No 7.5 IC50 = 34 nM Bind
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
489 3 1 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3C=CC(=O)N3Cc3ccccc32)c(Cl)c1
CHEMBL249741 v2r_human Human Yes 7.5 IC50 = 34 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl
CHEMBL134525 v2r_human Human No 7.5 IC50 = 34 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
328 3 1 2 4.8 CCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1
CHEMBL162588 v2r_rat Rat No 6.5 IC50 = 340 nM Bind
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
466 3 2 4 5.4 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1)c1ccc(F)cc1Cl
CHEMBL419973 v2r_rat Rat No 5.5 IC50 = 3400 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
567 8 2 5 3.5 CN(C)[C@H](Cc1c[nH]cn1)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C
CHEMBL1788221 v2r_human Human No 6.5 IC50 = 341 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2
CHEMBL442743 v2r_rat Rat No 7.5 IC50 = 35 nM Bind
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
425 3 1 3 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1F
CHEMBL337098 v2r_human Human No 7.5 IC50 = 35 nM Bind
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
314 2 1 2 4.4 CNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1
CHEMBL2112898 v2r_rat Rat No 6.5 IC50 = 350 nM Bind
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
568 10 2 7 1.8 CN[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1CC2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C
CHEMBL419183 v2r_human Human No 6.5 IC50 = 350 nM Funct
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
599 7 3 4 6.1 O=C(O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL2391300 v2r_rat Rat No 6.5 IC50 = 350 nM Bind
Inhibition of rat kidney V2 receptorInhibition of rat kidney V2 receptor
568 10 2 7 1.8 CN[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C
CHEMBL3954357 v2r_human Human No 5.5 IC50 = 3500 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
581 11 2 9 2.5 COCCn1c(-c2ccc(Cl)s2)nn(CC(=O)NCC(NS(C)(=O)=O)c2ccccc2C(F)(F)F)c1=O
CHEMBL399888 v2r_human Human No 7.4 IC50 = 36 nM Funct
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL1788220 v2r_human Human No 7.4 IC50 = 36 nM Funct
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL351970 v2r_rat Rat No 7.4 IC50 = 36 nM Bind
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
500 3 2 4 6.0 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1)c1cc(Cl)ccc1F
CHEMBL341173 v2r_human Human No 7.4 IC50 = 36 nM Funct
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
522 6 2 4 6.6 O=C(O)C[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL400266 v2r_human Human No 6.4 IC50 = 360 nM Funct
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL130887 v2r_rat Rat No 5.4 IC50 = 3600 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
535 6 2 5 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1ccccn1)C2
CHEMBL1520590 v2r_human Human Yes 4.4 IC50 = 37800 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12
CHEMBL50 v2r_human Human Yes 4.4 IC50 = 37800 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12
CHEMBL349506 v2r_rat Rat No 7.4 IC50 = 38 nM Bind
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2
CHEMBL434654 v2r_rat Rat No 7.4 IC50 = 38 nM Bind
Binding affinity towards rat Vasopressin V2 receptor after peroral administration of the compoundBinding affinity towards rat Vasopressin V2 receptor after peroral administration of the compound
462 5 1 3 6.0 Cc1ccccc1OCC(=O)Nc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(C)c1
CHEMBL316849 v2r_human Human No 6.4 IC50 = 380 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
450 3 1 2 6.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCC4(C=CCCC4)Cc4ccccc43)cc2)c1
CHEMBL176264 v2r_rat Rat No 6.4 IC50 = 380 nM Bind
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
449 4 1 3 5.9 Cn1ccc2c1CCCCN2C(=O)c1ccc(NC(=O)c2ccccc2-c2ccccc2)cc1
CHEMBL339118 v2r_rat Rat No 5.4 IC50 = 3800 nM Bind
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL129983 v2r_rat Rat No 5.4 IC50 = 3800 nM Bind
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
538 4 1 5 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C3CCC(=N)N3C1=O)C2
CHEMBL104839 v2r_human Human No 7.4 IC50 = 39 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1
CHEMBL106938 v2r_human Human No 7.4 IC50 = 39 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
594 7 2 4 5.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCC4)CC3)Cc3ccccc32)cc1
CHEMBL125878 v2r_rat Rat No 6.4 IC50 = 390 nM Bind
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
453 5 1 3 5.4 CC(C)NC(=O)C[C@@H]1CCCN(C(=O)c2ccc(N3CCCC3)cc2Cl)c2ccccc21
CHEMBL381763 v2r_human Human No 6.4 IC50 = 390 nM Bind
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
415 2 1 5 5.1 Cc1ccnn1-c1ccc(C(=O)N2Cc3cccnc3Nc3ccccc32)c(Cl)c1
CHEMBL101935 v2r_human Human No 6.4 IC50 = 390 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
436 3 1 2 6.3 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1
CHEMBL381248 v2r_human Human No 6.4 IC50 = 390 nM Bind
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
364 2 0 2 5.4 O=C(c1ccc(-c2ccccc2)cc1)N1Cc2cccn2Cc2ccccc21
CHEMBL279022 v2r_rat Rat No 5.4 IC50 = 3930 nM Bind
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](NCc3ccccc3)C1=O)C2
CHEMBL2324200 v2r_human Human No 6.4 IC50 = 398.1 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21
CHEMBL1520590 v2r_human Human Yes 4.4 IC50 = 39810.7 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12
CHEMBL50 v2r_human Human Yes 4.4 IC50 = 39810.7 nM Bind
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arre